International Journal for Pharmaceutical Research Scholars (IJPRS)

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"International Journal for Pharmaceutical Research Scholars (IJPRS)" is an official scientific website for the online publication of research articles, review articles, case studies or short communications through various research scholars. IJPRS is published quarterly per year in January, April, July and October. IJPRS is committed to publish original research work done by pharmaceutical research scholars. This work contributes significantly to the society as well as in Pharmaceutical research field. The journal is mainly focusing on various subjects such as Pharmaceutics, Pharmaceutical Technology, Regulatory Affairs, Pharmacology, Pharmaceutical Chemistry, Quality Assurance, Pharmacognosy, Pharmaceutical Management and Natural Sciences.

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Universal Impact Factor : 2012 YEAR - 1.0285

Global Impact Factor : 2012 YEAR - 0.214, 2013 YEAR - 0.265

Scientific Journal Impact Factor : 2012 YEAR - 3.457

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Supervisors: DR. PORAS PATEL, DR. KUNAL PATEL, and MR. HARSH TRIVEDI
Phone: 7874572005
Address: Ahmedabad, Gujarat, India

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Mallappa Kumara Swamy

UPM - Universiti Putra Malaysia

Chitra Mandal

Veterinary World

PUNET KUMAR

UTTER PRADESH TECHNICAL UNIVERSITY

Sivananthan Manoharan

University of Malaya, Malaysia

Roshan Patel

Rabinarayan Acharya

Gujarat Ayurved University,Jamnagar

Chih-Cheng Lin

University of Southern Denmark

Editor CSRL

Carlos Alberto García Gonzalez

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VOLUME 1 ISSUE 1 by International Journal for Pharmaceutical Research Scholars (IJPRS)

Innovations in Transdermal Drug Delivery System- A Review

The number of medications and the ways in which they can be administered have expanded dramatical... more The number of medications and the ways in which they can be administered have expanded dramatically over the years. One such advance has been the development of transdermal delivery systems. The transdermal route of drug delivery has attracted researchers due to many biomedical advantages associated with it. However, excellent impervious nature of skin is the greatest challenge that has to be overcome for successfully delivery of the drug molecules to the systemic circulation via this route. Various types of transdermal approaches used to incorporate the active ingredients include use of prodrugs/lipophilic analogs, permeation enhancers, sub saturated systems and entrapment into vesicular systems. Innovations in technologies continue to occur at a positive rate, making the technology a fertile and vibrant. This article deals with the innovations in the field of TDDS to improve the release rate and other parameters and most suitable to the patient.

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Aquasomes : A Self Assembling Nano biopharmaceutical Carrier System for Bio - Active Molecules : A Review

Aquasomes are the self-assembling nanobiopharmaceutical carrier system, contains nanocrystalline ... more Aquasomes are the self-assembling nanobiopharmaceutical carrier system, contains nanocrystalline calcium phosphate or ceramic diamond, is covered by a glassy polyhydroxyl oligomeric film. Aquasomes are spherical (5â€“925nm) particles used for drug and antigen delivery. Aquasomes are called as â€œbodies of water" their water like properties protect and preserve fragile biological molecules. Its high degree of surface exposure is used in targeting of bio-active molecules to specific sites. Three types of core materials are mainly used for producing aquasomes: Tin oxide, Nanocrystalline carbon ceramics and Brushite. Calcium phosphate is the core of interest, due to its natural presence in the body. The brushite is unstable and converts to hydroxyapatite upon prolong storage and seems a better core for the preparation of aquasomes. It is widely used for the preparation of implants. Aquasomes exploited as a RBC substitutes, vaccines for delivery of viral antigen and as targeted system for intracellular gene therapy. Enzyme activity and sensitivity towards molecular conformation made aquasome as a novel carrier for enzymes like DNAses and pigment/dyes. This report reviews the principles of self assembly, the challenges of maintaining both the conformational integrity and biochemical activity of immobilized surface pairs.

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Study of Degradation Profile and Development of Stability Indicating Spectrophotometric Method for Ropinirole Hydrochloride under Acid/Base Hydrolytic and Oxidative Conditions

The degradation behavior of Ropinirole Hydrochloride (ROPI) was investigated under various stress... more The degradation behavior of Ropinirole Hydrochloride (ROPI) was investigated under various stress conditions of acid/base hydrolysis and oxidation using Spectrophotometry. Stability indicating spectrophotometric method was developed that could separate the drug from its degradation products formed under these stressed conditions. The UV spectral characteristics of the drug and degraded products were quite different and first order derivative UV spectrophotometric method was used to study the extent of degradation. ROPI was found to degrade extensively under experimental conditions. The method was validated with respect to linearity, precision, accuracy and specificity. The described method was found to be linear over the range of 5-50 µg mL-1 for ROPI. The mean recovery was found to be 99.03±1.11, %. The intermediate precision data were obtained under different experimental conditions and calculated value of the coefficient of variation (CV, %) was found to be less than critical value. The proposed method can be successfully useful to determine the degradation of drug during storage.

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Hypolipidemic Activity of Protocatechuic Acid in Atherogenic Diet Induced Hyperlipidemic Rats

Hyperlipidemia is an abnormally high level of fatty substances called lipids, largely cholesterol... more Hyperlipidemia is an abnormally high level of fatty substances called lipids, largely cholesterol and triglycerides, in the blood. The present study was designed to investigate the hypolipidemic effects of Protocatechuic acid in atherogenic diet induced hyperlipidemia. In atherogenic diet induced hyperlipidemic model, the rats receiving treatment of Protocatechuic acid at the dose of 25 and 50 mg/kg showed significant reduction in total cholesterol, triglyceride, total protein and elevation in high density lipoprotein cholesterol. Hence by considering the effects observed in this model, it has been suggested that Protocatechuic acid was found to possess significant hypolipidemic activity, this may be due to its effect on increasing the metabolism of the cholesterol by activating lipoprotein lipase or by increasing reverse cholesterol transport.

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A study of Nifedipine in the Treatment of Preterm Labor of South Indian Origin

The first line Treatment of preterm labour at CSI Kalyani hospital Chennai was hydration and bed ... more The first line Treatment of preterm labour at CSI Kalyani hospital Chennai was hydration and bed rest followed by tocolytics, the hospital followed a treatment protocol with nifedipine. A total of 48 patients with singleton pregnancies at a gestational age between 28-36 weeks were selected according to the protocol to receive nifedipine. The meta analysis showed similarities with respect to the age at preterm labor, status of gravid, suppression of preterm labor, prolongation of pregnancies, adverse events, neonatal outcomes by apgar scores. The results confirmed that nifedipine is a growing calcium channel blocker as a safe and potential drug in the treatment of preterm labor especially in situations where a woman needs a full course of corticosteroids for fetal lung maturation or transfer to hospital that can provide neonatal intensive care.

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Development and Validation of HPTLC Method For Simultaneous Analysis of Lopinavir and Ritonavir in Their Combined Tablet Dosage Form

Simultaneous quantification of Lopinavir and Ritonavir in tablet by HPTLC method was developed an... more Simultaneous quantification of Lopinavir and Ritonavir in tablet by HPTLC method was developed and validated. The chromatograms were developed using a mobile phase of Chloroform: 1, 4 - Dioxane (7:3 %v/v) on pre-coated plate of silica gel GF aluminum TLC plate and quantified by densitometric absorbance mode at 210 nm. The Rf value for lopinavir and ritonavir was 0.74 and 0.58 respectively. The linearity of the method was found to be within the concentration range of 160-960 ng/spot for Lopinavir and for Ritonavir, it was 40-240 ng/spot. The lower limits of detection and quantification were 9.56 ng/spot and 28.96 ng/spot for Lopinavir and 6.82 ng/spot and 20.66 ng/spot for Ritonavir. The method was also validated for precision, specificity and recovery. This developed method was used to analyze fixed-dose tablet (Lopimune, Cipla Ltd) sample of Lopinavir and Ritonavir.

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Microbubble : As A Therapeutic and Diagnostic Tool

Gas filled microbubbles are well known as ultrasound contrast agents for medical ultrasound imagi... more Gas filled microbubbles are well known as ultrasound contrast agents for medical ultrasound imaging and for non-invasive delivery of drugs and genes to different tissues. Microbubbles designate air or gas filled microspheres suspended in a liquid carrier phase which generally results from the introduction of air or gas. The liquid phase contains surfactants to control the surface properties as well as stability of the bubble. Microbubbles are manufactured from biocompatible materials, so they can be injected intravenously. Microbubbles have an average size (1-8 Âµm) less than that of RBCâ€™s i.e. they are capable of penetrating even into the smallest blood capillaries & releasing drugs or genes, incorporated on their surface, under the action of ultrasound. Ultrasound radiation are used which are non hazardous. Most of the physicians today prefer imaging with ultrasound in combination with microbubbles compared to other diagnostic techniques for low cost and rapidity. The ultrasonic field can be focused at the target tissues and organs; thus, selectivity of the treatment can be improved, reducing undesirable side effects. Recently, targeting ligands are attached to the surface of the microbubbles, which have been widely used in cardiovascular system, tumour diagnosis and therapy. This review focuses on the characteristics of microbubbles that give them therapeutic properties and some important aspects of ultrasound parameters that are known to influence microbubble-mediated drug delivery. In addition, current studies involve discussion of novel therapeutical application of microbubbles.

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Spectrophotometric methods for simultaneous estimation of Thiocolchicoside and Dexketoprofen Trometamol in pharmaceutical dosage form

Two simple spectrophotometric methods have been developed for simultaneous estimation of Thiocolc... more Two simple spectrophotometric methods have been developed for simultaneous estimation of Thiocolchicoside and Dexketoprofen trometemol from pharmaceutical dosage form. Method-I involved simultaneous equation method and Method-II is the Q-absorbance method. For simultaneous equation method, the absorbances of the standard solutions were taken at two wavelengths 368 nm (Î»-max of Thiocolchicoside) and 258 nm (Î»-max of dexketoprofen trometamol). For Q-absorbance method, the absorbances of the standard solutions were taken at two wavelengths 258 nm (Î»-max of dexketoprofen trometamol) and 281 nm (Isoabsorptive point), in methanol. Linearity range was found to be 2-24 Î¼g/ml for dexketoprofen trometamol and Thiocolchicoside in both methods based on the ratio of the two drugs in combined dosage form. The accuracy and precision of the methods were determined and validated statistically. Both methods showed good reproducibility and recovery with RSD less than 2. Proposed methods were found to be rapid, specific, precise and accurate and can be successfully applied for the routine analysis of dexketoprofen trometamol and Thiocolchicoside in pharmaceutical dosage form.

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Transdermal Patches: A Complete Review on Transdermal Drug Delivery System

Today about 70% of drugs are taken orally and are found not to be as effective as desired. To imp... more Today about 70% of drugs are taken orally and are found not to be as effective as desired. To improve such characters transdermal drug delivery system was emerged. Transdermal drug delivery system (TDDS) provides a means to sustain drug release as well as reduce the intensity of action and thus reduce the side effects associated with its oral therapy and differs from traditional topical drug delivery. Transdermal Drug Delivery System is the system in which the delivery of the active ingredients of the drug occurs by means of skin. Several important advantages of transdermal drug delivery are limitation of hepatic first pass metabolism, enhancement of therapeutic efficiency and maintenance of steady plasma level of the drug. Various types of transdermal patches are used to incorporate the active ingredients into the circulatory system via skin. This review article covers a brief outline of the principles of transdermal permeation, various components of transdermal patch, approaches of transdermal patch, evaluation of transdermal system, its application with its limitation.

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VOLUME 1 ISSUE 2 by International Journal for Pharmaceutical Research Scholars (IJPRS)

Temperature and pH Triggered Insitu Hydrogel of Doxycycline for the Treatment of Chlamydial Conjunctivitis

The present investigation describes the formulation and characterization of ophthalmic in situ hy... more The present investigation describes the formulation and characterization of ophthalmic in situ hydrogel for sustained delivery of doxycycline (DOX) that is frequently used to treat chlymydial conjunctivitis. Insitu hydrogel were prepared using thermo-reversible gelling polymer, Pluronic F 127 (PF127) and PH sensitive and viscosity enhancer polymer Carbopol 940 (CP940). Because of high concentration (20 to 25%w/v) of PF127 polymer required for insitu gelation causes irritation to the eye. So, to reduce this concentration, an attempt was made to combine the PF127 with CP940 showing a pH triggered sol-gel transition by pH of tear fluid. Different batches were prepared of varying concentrations of CP940 (0.1-0.3%) with PF127 (12%-18%) using DOX 2%w/v. Pluronic F68 (PF68) with 2% and 4% concentration were mixed to obtain a hydrogel with an appropriate gelation temperature. The formulations were optimized by the viscosity measurement and in vitro gelation study. Selected formulations were evaluated for in vitro drug release study using Franz diffusion cell and indicated sustain drug release over a period of 10 h. Stability testing at 80C and 400C and effect of sterilization and were on drug content, pH and clarity were also evaluated. The prepared formulation could reduce not only the concentration of individual polymers but also the side effects without compromising the in vitro gelling capacity. This formulation of Doxycycline insitu hydrogel represents potentially effective ophthalmic delivery system for the treatment of chlaymydial conjunctivitis.

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Development and Validation of A Stability-Indicating HPTLC Method For Analysis of Anti-asthmatic Drugs

The objective of the present work was to develop a stability-indicating HPTLC method for Monteluk... more The objective of the present work was to develop a stability-indicating HPTLC method for Montelukast sodium (MTKT) and Levocetirizine dihydrochloride (LCTZ) in the presence of its degradation products generated from forced decomposition studies. Both drugs were subjected to acid, base, peroxide, and photo degradation. Successful separation of the drugs from the degradation products formed on aluminum-backed silica gel 60 F254 with Ethyl acetate: Methanol: Ammonia (7.0:1.4:0.7 v/v/v) as the mobile phase. Densitometric analysis of was performed at 231nm in concentration range 100-1200 ng/spot with range of recovery 99.91 ± 0.91% for MTKT and 50-600 ng/spot with range of recovery 99.28 ± 0.51 % for LCTZ by the HPTLC method. Statistical analysis proved the method to be repeatable, specific, and accurate for estimation of MTKT and LCTZ. It can be used as a stability indicating method due to its effective separation of the drugs from its degradation products.

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A Review on Polymers Used In In-Situ Gel Drug Delivery Systems

In situ gel drug delivery systems are used in sol form before administration in the body, but onc... more In situ gel drug delivery systems are used in sol form before administration in the body, but once administered, undergo gelation in situ, to form a gel. The formation of gel depends on factors like temperature modulation, pH change, presence of ions and ultraviolet irradiation, electrical sensitivity, enzyme sensitive from which drug get released in a sustained and controlled manner. Typically, aqueous solutions of hydrogels used in biomedical applications are liquid at ambient temperature and gel at physiological temperature. The in situ gel forming polymeric formulations offer several advantages like sustained and prolonged action in comparison to conventional drug delivery systems. From a manufacturing point of view, the production of such devices is less complex and thus lowers the investment and manufacturing cost. This review stresses on the polymeric use of natural polymers and synthetic polymers.

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Design and Development of Transdermal Therapeutic system of Carvedilol using Combination of Natural and Synthetic Polymers

The present study was mainly focused on investigating the influence of concentration and combinat... more The present study was mainly focused on investigating the influence of concentration and combination of HPMC K4M, Carbopol 934P and Chitosan on physical characterization and drug release behavior of carvedilol transdermal films prepared by the solvent evaporation technique. The physicochemical compatibility of the drug and the polymers was studied by differential scanning calorimetry and infrared spectroscopy. The results suggested no physicochemical incompatibility between the drug and the polymers. The prepared films were evaluated for physicochemical characteristics like weight variation, thickness, folding endurance, tensile strength, percentage moisture uptake, water vapor transmission rate, percentage flatness and in vitro permeation study. In vitro permeation studies were performed by using Franz diffusion cells. The drug release profiles of selected formulations were subjected to kinetic treatment using zero order, first order, Higuchi and korsmeyer's peppas kinetic models. The results followed Higuchi kinetics (r2 = 0.951−0.995) and the mechanism of release was diffusion mediated. Based on physicochemical and in vitro permeation studies, transdermal film prepared by combination of HPMC K4M and Chitosan with ratio 3:1 selected as optimized formulation shows the drug release more than 24 hours with good flexibility and stability at 250C. The developed transdermal film increases the efficacy of carvedilol for the treatment of hypertension.

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Niosome as an Effective Drug Delivery : A Review

Niosomes are a novel drug delivery system, in which the medication is encapsulated in a vesicle. ... more Niosomes are a novel drug delivery system, in which the medication is encapsulated in a vesicle. The vesicle is composed of a bilayer of non-ionic surface active agents and hence the name given as "Niosomes". The niosomes are very small ranging usually in micron size. Their size lies in the nanometric scale. Although structurally similar to liposomes, they offer several advantages over them. Niosomes have recently been shown to greatly increase transdermal drug delivery and also can be used in targeted drug delivery, and thus increased study in these structures can provide new methods for drug delivery.

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Survey of Self-medication errors amongst students and faculty members of Educational Campus (Gujarat Technological University/Sardar Patel University) Of New V.V.Nagar

A total of 500 questionnaire were distributed in the college premises with respondent rate of 450... more A total of 500 questionnaire were distributed in the college premises with respondent rate of 450(90%).majority of respondents, 73% were aged between 18-23 years, while 269(59.5%) were female and 181(40.5%) were male. The survey was conducted in the colleges comprising of Ayurvedic, Biotechnology, Engineering and pharmacy. The survey comprised of 290 students (64.4%) including both undergraduate as well as postgraduate students. the rest were faculty members (26.6%) and administration incharge (8.8%). The most prevalent disorder was found to be GIT disturbances (80.1%) and headache (69.9%) on daily basis. The conditions for which self-medication was under taken included Cough and Cold (31.86%), followed by headache (22.98%) and fever (17.36%). Majority of the respondents (89.80%) purchased the drugs from private pharmacies. Side effects observed due to self-medication were found out to be GIT Disturbance(17.2%) followed by vomiting (16.4%) and drowsiness (15.4%).

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Niosomes in Targeted Drug Delivery : A Review

Over the past several years, treatment of infectious diseases and immunization has undergone a pa... more Over the past several years, treatment of infectious diseases and immunization has undergone a paradigm shift. Stemming from the nanobiotechnology research, not only a large number of disease-specific biologicals have been developed, but also enormous efforts have been made to effectively deliver these biologicals. Non-ionic surfactant vesicles (or niosomes) are now widely studied as alternates to liposomes. Different novel approaches used for delivering these drugs include liposomes, Microspheres, nanotechnology, micro emulsions, antibody-loaded drug delivery, magnetic Microcapsules, implantable pumps and niosomes. Niosomes and liposomes are equiactive In drug delivery potential and both increase drug efficacy as compared with that of free Drug. Niosomes are preferred over liposomes because the former exhibit high chemical Stability and economy. Niosomes are self assembled vesicles composed primarily of synthetic surfactants and cholesterol. They are analogous in structure to the more widely studied liposomes formed from biologically derived phospholipids. Niosomes represent an emerging class of novel vesicular systems. Niosome formation requires the presence of a particular class of amphiphile and aqueous solvent. In recent years a comprehensive research carried over niosome as a drug carrier. Various drugs are enlisted and tried in niosome surfactant vesicles. Niosome appears to be a Well preferred drug delivery system over liposome as niosome being stable and economic. Also niosomes have great drug delivery potential for targeted delivery of anti-cancer, Anti-infective agents. Drug delivery potential of niosome can enhance by using novel Concepts like proniosomes, discomes and aspasome. Niosomes also serve better aid in diagnostic imaging and as a vaccine adjuvant.

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Pharmacognostical and Analgesic Activity of Various Leaves Extracts of Achyranthus Aspera Linn

Aim of present study was to investigate the analgesic activity of the leaves extracts of Achyrant... more Aim of present study was to investigate the analgesic activity of the leaves extracts of Achyranthus aspera linn. The leaves of drug is converted in uniform particle size and extracted by using Petroleum ether (60-80oC), Benzene, Chloroform, Ethyl acetate, n-Butanol, and Ethanol solvents. Then TLC and column chromatography is performing for isolation of active principle. This active principle is further carryout analgesic activity by Tail flick method and Writhing test method with the help of Aspirin (150 mg/kg) as standard drug. In Tail Flick Method the Ethanol extract showed good significant increase in reaction time as compared to pretreatment reaction time, where as n-Butanol, Chloroform, and Pet- ether extract, showed significant increase in reaction time, when compared to pretreatment reaction time However, Benzene and Ethyl acetate extract showed less significant increase in pretreatment reaction time. In Writhing Test Method the Ethanol extract showed good significant decrease in abdominal writhes as compared to standard group, where as n-Butanol extract, Ethyl acetate extract, Chloroform extract, Benzene extract, showed significant decrease in abdominal writhes, However, Pet-ether extract and Benzene extract failed to decrease in abdominal writhes when compared to standard group.

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Intranasal Liposomes : An Approach for Drug Delivery to Brain

Targeting drug molecules to brain is one of the most challenging research areas in pharmaceutical... more Targeting drug molecules to brain is one of the most challenging research areas in pharmaceutical sciences. Drugs that are effective against diseases in the CNS and reach the brain via the blood compartment must pass the BBB. The blood-brain barrier (BBB) represents an insurmountable obstacle for a large number of drugs, including antibiotics, anti-neoplastic agents, and a variety of central nervous system (CNS)-active drugs. Therefore, various strategies have been proposed to improve the delivery of different drugs to this tissue which includes liposomes, colloidal drug carriers, micelles, chimeric peptide technology, intranasal and olfactory route of administration and nano technology. The discovery of liposome or lipid vesicle emerged from self forming enclosed lipid bi-layer upon hydration; liposome drug delivery systems have played a significant role in formulation of potent drug to improve therapeutics Liposomes have been investigated as carriers of various pharmacologically active agents such as antineoplastic, antimicrobial drugs, chelating agents, steroids, vaccines, and genetic materials. Liposomes provide an efficient drug delivery system because they can alter the pharmacokinetics and pharmacodynamics of the entrapped drugs. Liposomes have been widely used for brain delivery in vivo. Nowadays, the nasal route for systemic drug delivery has gained great interest. It provides several advantages over other routes of drug administrations, which includes rapid absorption, avoids intestinal and hepatic presystemic disposition and high potential for drug transfer to the CSF. Moreover, the nasal route is a potential alternative route for systemic availability of drugs restricted to intravenous administration, viz. peptide and protein drugs and vaccines. As well, intranasal route has also been successfully exploited for bypassing the blood brain barrier [BBB] and subsequently delivering drug molecules to central nervous system [CNS].

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A Quick View on Methods of Synthesis of Pyrimidines

Pyrimidine is a five membered heterocyclic ring which is a lead compound for designing potent bio... more Pyrimidine is a five membered heterocyclic ring which is a lead compound for designing potent bioactive agents. This heterocyclic moiety has versatile medicinal significance and has diverse biological activities such as antimicrobial, anticancer, antibacterial, antiprotozoal, antimicrobial, antiviral, antihypertensive, antihistaminic; CNS-active to metabolic adjuvants and many more thus Pyrimidines occupy a distinct and unique place in our life. The present work emphasizes on the various techniques and methods involved in synthesis of various pyrimidine moieties.

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Box-Behnken Design For Optimization of Formulation Variables of Tramadol HCl Sustained Release Matrix Tablets

The objective of this work was to develop sustained release tablets (Once in a day) of highly wat... more The objective of this work was to develop sustained release tablets (Once in a day) of highly water soluble Tramadol HCl using hydrophilic polymers (HPMC K100M, HPMC K15M, HPMC K 4M) as cost effective, non toxic easily available and suitable hydrophilic matrix system. Sustained release tablet of Tramadol HCl (dose 200mg) were produced by wet granulation method by PVP K30 5% solution. After the evaluation of physical characteristics of granules & tablets, The dissolution test was performed in 0.1 N HCl for 2 hr and remaining 22 hr performed in 6.8 pH buffer solution. We concluded that T1-T15 batches of Box-behnken design passed the pre-compressional and post-compressional parameters and increasing the polymer concentration, decreasing the drug release. Higher viscosity grade HPMC K100M is more drug retarding agent as compare to HPMC K15M & HPMC K4M. In combination of HPMC K4M, HPMC K15M & HPMC K100M, T7 batch having drug releasing up to 24 hrs as compare to others. Kinetics treatment of the box-behken design batches, concluded that zero order R2 value is near to 0.999 as compared to the first order R2 value. So, all batches follow the Zero order release mechanism. From the korsmeyer-peppas model, concluded that drug release mechanism is diffusion with dissolution or anomalous diffusion (Non-fickian). From the statastical analysis full model and reduced model was analyzed and got the significant effect of X3 polymer as compared to X1 & X2. X3 having more negative value than the X1 & X2 so concluded that the X3 polymer is effective to retardation of the drug release. T1-T15 batches are compared with marketed product (Tramazac OD tab.). T7 batch had more 73.58 similarity factor (f2) when Marketed formulation taken as a reference. So T7 batch is optimized batch. The optimized batch is passed the accelerated stability studies, No significant change in the dissolution profile.

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Innovations in Transdermal Drug Delivery System- A Review

Aquasomes : A Self Assembling Nano biopharmaceutical Carrier System for Bio - Active Molecules : A Review

Study of Degradation Profile and Development of Stability Indicating Spectrophotometric Method for Ropinirole Hydrochloride under Acid/Base Hydrolytic and Oxidative Conditions

Hypolipidemic Activity of Protocatechuic Acid in Atherogenic Diet Induced Hyperlipidemic Rats

A study of Nifedipine in the Treatment of Preterm Labor of South Indian Origin

Development and Validation of HPTLC Method For Simultaneous Analysis of Lopinavir and Ritonavir in Their Combined Tablet Dosage Form

Microbubble : As A Therapeutic and Diagnostic Tool

Spectrophotometric methods for simultaneous estimation of Thiocolchicoside and Dexketoprofen Trometamol in pharmaceutical dosage form

Transdermal Patches: A Complete Review on Transdermal Drug Delivery System

Temperature and pH Triggered Insitu Hydrogel of Doxycycline for the Treatment of Chlamydial Conjunctivitis

Development and Validation of A Stability-Indicating HPTLC Method For Analysis of Anti-asthmatic Drugs

A Review on Polymers Used In In-Situ Gel Drug Delivery Systems

Design and Development of Transdermal Therapeutic system of Carvedilol using Combination of Natural and Synthetic Polymers

Niosome as an Effective Drug Delivery : A Review

Survey of Self-medication errors amongst students and faculty members of Educational Campus (Gujarat Technological University/Sardar Patel University) Of New V.V.Nagar

Niosomes in Targeted Drug Delivery : A Review

Pharmacognostical and Analgesic Activity of Various Leaves Extracts of Achyranthus Aspera Linn

Intranasal Liposomes : An Approach for Drug Delivery to Brain

A Quick View on Methods of Synthesis of Pyrimidines

Box-Behnken Design For Optimization of Formulation Variables of Tramadol HCl Sustained Release Matrix Tablets

Derivative Spectrophotometric Method for Simultaneous Determination of Granisetron and Pantoprazole in Synthetic Mixture

The present work describes a First order Derivative Spectrophotometric method for simultaneous es... more The present work describes a First order Derivative Spectrophotometric method for simultaneous estimation of Granisetron and Pantoprazole in synthetic mixture. Method was performed on Elico's Double beam UV-Visible Spectrophotometer (SL-191) using methanol as a solvent. Absorbance were recorded at Zero Crossing Point (ZCP) of Granisetron (248 nm) and ZCP of Pantoprazole (291 nm) for all standard and sample solutions. The selected Spectrophotometric conditions were found to be effective for the determination of Granisetron and Pantoprazole from synthetic mixture in presence of common excipients without prior physical separation. Linearity was found over the range of 2-20 μg/ml for Granisetron and over 5-100 μg/ml for Pantoprazole. The values of Limit of Detection were found to be 0.40 μg/ml for Granisetron and 0.62 μg/ml for Pantoprazole. The values of Limit of Quantification were found to be 1.22 μg/ml for Granisetron and 1.89 μg/ml for Pantoprazole. The proposed method was found to be fast, simple, sensitive, accurate, precise, reproducible, robust and rugged and can be used for simultaneous analysis of these drugs in synthetic mixture.

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Formulation and Evaluation of Extended Release Tablet of Divalproex sodium

In the present work, an attempt was made to design an oral Extended release matrix tablet of Diva... more In the present work, an attempt was made to design an oral Extended release matrix tablet of Divalproex sodium and to optimize the drug release profile using 32 full factorial design. Tablets were prepared by direct compression method using HPMC K100M and Eudragit L100 as matrix forming polymers. Tablets were evaluated for various physicochemical parameters like Hardness, Thickness, Friability, Weight variation test, Content Uniformity and In vitro drug release. All the formulations complied with pharmacopoeial standards. A 32 full factorial design for 2 factors at 3 levels each was employed to systematically optimize drug release profile. HPMC K100M and Eudragit L100 were taken as the independent variables. The dependent variables selected were % of drug released in 3 hrs, % of drug released in 12 hrs. In vitro drug release study showed that batch F8 (HPMC K100M-15%, Eudragit L100-10%) was found to be optimized as it had almost identical dissolution profile with marketed product. The formulated tablets exhibited Non-fickian drug release kinetics approaching Zero-order as the value of release rate exponent (n) varied between 0.6024 and 0.7354, resulting in regulated and complete release until 24 hrs. The polymer HPMC K100M and Eudragit L100 had significant effect on the drug release from the tablets (P<0.05). Validation of optimization study performed using confirmatory run indicated very high degree of prognostic ability to 32 full factorial design. Stability study of optimized batch F8 was conducted at accelerated conditions for one month and it was found to be stable.

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Formulation and Evaluation of Microparticles for Controlled Delivery of Tramadol HCl

by International Journal for Pharmaceutical Research Scholars (IJPRS) and Shrujal Patel

Although Tramadol has less analgesic power than morphine, it presents fewer side effects and cons... more Although Tramadol has less analgesic power than morphine, it presents fewer side effects and consequently is currently considered as a drug of choice in the treatment of chronic pain. The aim of the present work was to study preparation of controlled drug delivery of Tramadol HCl via oral route. Drug was encapsulated within polymethacrylate copolymer i.e. Eudragit RS100 and Eudragit RL100, by solvent evaporation method using acetone/liquid paraffin system. FTIR and DSC of Tramadol HCl and it combination with Excipients shows no change in peak of absorbance and melting point. Microparticles of different drug-polymer concentrations 1:1, 1:2, 1:3 and 1:4 were prepared. Magnesium stearate was used as droplet stabilizer and lubricant in concentration of 0.3% (v/v). Selected formulations were characterized for their micromeritics property, % yield, drug loading, particle size, surface morphology and release behaviour. In-vitro dissolution tests were performed by using dissolution media with two different pH i.e. 1.2 pH for 2 hrs and 6.8 pH for 10 hrs. All the selected formulations exhibited a controlled release for almost 12 hrs. Among the entire prepared batches F25 shows good % drug loading (48.33%), high % yield (93%) and good controlled release (98%) within 12 hrs. The mean particle size of microspheres ranged from 252 ± 24.54 μm. Scanning electron microscopy of microspheres revealed a spherical and uniform appearance with smooth surface. Stability study was performed for batch F10 shows 96.78% drug release in 12 hrs. Release of TmH was best fitted to Higuchi model and Korsmeyer-Peppas model because it presented highest values of correlation coefficient (R2 = 0.9822).

Formulation and Characterization of Mouth Dissolving Tablet of Metoclopramide Hydrochloride

Metoclopramide hydrochloride is an anti-emetic, act by blocking D2 receptors in the Chemoreceptor... more Metoclopramide hydrochloride is an anti-emetic, act by blocking D2 receptors in the Chemoreceptor trigger zone (CTZ), and antagonize chemotherapy induced vomiting. In the present study an attempt has been made to prepare Mouth Dissolving Tablets (MDTs) of Metoclopramide HCl for use in specific population viz. pediatrics, geriatrics and patients experiencing difficulty in swallowing tablet. Mouth Dissolving Tablets containing Metoclopramide HCl were prepared by direct compression method using various superdisintegrants like Sodium Starch Glycolate (SSG), Crosscarmellose Sodium (CCS), Crospovidone (CP), LHPC-11 and Doshion P 544D in three different concentrations i.e. 5, 7.5, 10 mg. The slight bitter taste of the drug was masked using sweetener and flavour which also enhanced the mouth feel of tablet. The initial compatibility studies between the drug and excipients were carried out using DSC and FT-IR Spectra. The blend was examined for various pre-compression parameters like angle of repose, density, compressibility index, etc. The formulated tablets were evaluated for hardness, friability, in-vitro disintegration time, drug content, etc. The hardness of the tablets was in range of 3-5 kg/cm2. The percentage friability of the tablets was less than one. Weight variation test results showed that the tablets were deviating from the average weight within the permissible limits of ±7.5%. Drug content uniformity study results was found to be 99-100%. Batch F15 containing Doshion P 544D (10 mg) showed better disintegrating character along with the immediate release (100.09% within 6 minutes). There was no drastic change in result of tablets of an optimized batch at the end of one month accelerated stability study. It was concluded that the in-vitro drug release was influenced greatly by the concentration of superdisintegrants and Doshion P 544D was found to be better suited for the formulation of mouth dissolving tablets of Metoclopramide HCl compared to other superdisintegrants used in the study.

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Formulation and Evaluation of Asymmetric Membrane Capsule Osmotic Pump of Gliclazide

by International Journal for Pharmaceutical Research Scholars (IJPRS) and Sandip Teraiya

The aim of this study was to demonstrate that the asymmetric membrane capsule can be used to deli... more The aim of this study was to demonstrate that the asymmetric membrane capsule can be used to deliver a poorly water soluble drug with a pH sensitive solubility such as gliclazide. In order to obtain the desired delivery duration, the drug was solubilized with the use of a pH-controlling excipient. The capsule wall membrane was made by a phase inversion process, in which asymmetric membrane was formed on glass mold pins by dipping the mold pins into a coating solution containing a polymeric material followed by dipping into a quench solution. This study evaluates the influence of coating formulation that was cellulose acetate (CA), ethyl cellulose (EC), and plasticizer (glycerin and PEG 600). Results show capsule that made by CA with glycerol and PEG 600(F8), which appear in asymmetric structure and are able to release gliclazide(GLZ) in significant percentage. Results show that sodium bicarbonate and D-mannitol is able to promote the release of GLZ from polymeric capsules prepared with CA with asymmetrical membrane. The addition of solubilizer, sodium lauryl sulphate (SLS) could enhance the release of GLZ by micelle formation of GLZ. Based on these results, influence of core formulation variables, including D-mannitol, sodium bicarbonate and the added amount of SLS were examined on the release of GLZ. It was found that HPMC 15cp was suitable to be a thickening agent and both added amount of HPMC and SLS showed a comparable and profoundly positive effect. In vitro release studies for all the prepared formulations were done (n=3). Statistical test (Dunnett’s multiple comparison test) was applied for in vitro drug release at P>0.05. The best formulation closely corresponded to the marketed formulation by a similarity (f2) value of 78.36 and difference (f1) value of 4.49. The drug release was independent of pH but dependent on the osmotic pressure of the dissolution medium. The release kinetics followed the First order model and the mechanism of release was anomalous type.

Design and Evaluation of Piroxicam Microemulsion

The main objective of the present research work was to improve the oral bioavailability of BCS cl... more The main objective of the present research work was to improve the oral bioavailability of BCS class II drugs which are known to have low solubility but have high permeability. In the present study, Piroxicam has been chosen as a model drug which is having low oral bioavailability and associated with many dose related side effects. If the bioavailability of this drug is increased reduction of the dose and the dose related side effects can be controlled and this would lead to more affordable therapy. An oral microemulsion formulation for enhancing the bioavailability of Piroxicam was developed and evaluated. A microemulsion is one of the novel pharmaceutical interests for drug delivery, and is normally composed of oil, water, surfactants and co-surfactants. Microemulsions were prepared by titrating different ratio of oil to surfactant mixtures (surfactant + co-surfactant) with water and microemulsion zone was recorded in the Pseudo-ternary phase diagram. Stable mocroemulsions were obtained with Sesame oil as oil phase, Tween80 as surfactant, Glycerin as co-surfactant and distilled water as aqueous phase. The ratio of components (oil, surfactant, co-surfactant and water) was found to affect the pH, Conductivity, Clarity, Dilution shock, In vitro release and Intestinal permeability, Zeta potential and Particle Size. The higher permeability achieved with the microemulsion systems compared to the marketed product (Pirox-20) was encouraging. The developed microemulsion system improved the permeability by increasing the lipophillicity due to the oil phase and also by destabilizing the epithelial membrane due to the surfactants, and may be used as a vehicle for enhanced delivery of BCS class II drugs.

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Formulation and Evaluation of Gastro retentive Drug Delivery System for a Selective Anti-diabetic Drug

Convenience of administration and patient compliance are gaining significant importance in design... more Convenience of administration and patient compliance are gaining significant importance in design of dosage form. Sustained release gastroretentive dosage forms enable prolonged and continuous input of the drug to the upper parts of gastrointestinal tract and improve the bioavailability of medication that is characterized by narrow absorption window. Gastroretentive floating drug delivery systems (GFDDS) of metformin hydrochloride, an antidiabetic drug with an oral bioavailability of only 50% (because of its poor absorption from lower gastrointestinal tract) have been designed and evaluated. Xanthan gum and different grades of Hydroxy propyl methyl cellulose (HPMC) were used as strong gelling agent and sodium bicarbonate as gas generating agent to reduce floating lag time. Tablets were prepared by wet granulation method. Drug-excipients compatibility was studied by FTIR and Differential Scanning Calorimetry (DSC). Floating tablets were evaluated for pre-formulation parameters and for hardness, friability, weight variation, drug content, floating properties and in vitro release pattern. Formulation M3 showed minimum floating lag time and maximum floating time of 12 hours and gave slow and maximum drug release of Metformin HCl spread over 12 hours. The release of drug from the formulation followed zero order kinetics and was governed by non-Fickian diffusion mechanism. The optimized formulation was subjected to stability study.

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Formulation, Optimization and Evaluation of Orally Disintegrating Tablet of Non-Steroidal Anti-Inflammatory Drug

Piroxicam is a non steroidal anti-inflammatory drug with analgesic properties. The purpose of thi... more Piroxicam is a non steroidal anti-inflammatory drug with analgesic properties. The purpose of this study was to develop a taste masked orally disintegrating tablet of poorly soluble Piroxicam by direct compression technique with β-cyclodextrin (ß-CD) complexes using various superdisintegrants like sodium starch glycolate, crospovidone XL and croscarmellose sodium. Complex was characterized using infrared spectroscopy, differential scanning calorimetry, % drug release study, gustatory evaluation for taste masking. A 32 full factorial design was applied to systematically optimize the drug disintegration time. The concentration of Crospovidone (X1) and concentration of Croscarmellose (X2) were selected as independent variables. The Disintegration time (Y1) and Wetting time (Y2) were selected as dependent variables. The prepared tablets were evaluated for hardness, friability, disintegration time, wetting time and In-vitro drug release. FT-IR studies and physical compatibility study were conducted for drug, and drug excipient mixture for interactions if any. The different formulations showed disintegration time between 12 to 58 sec. The results indicated that concentration of Crospovidone (X1) and concentration of Croscarmellose (X2) significantly affected the Disintegration time (Y1) and Wetting time (Y2). Regression analysis and numerical optimization were performed to identify the best formulation. Formulation F10 prepared with croscarmellose (4.23%) & crospovidone (6.74%) was found to be the best formulation with disintegration time 16 sec, wetting time 21 sec and % drug release in 10 min 94.23%.

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Preparation and Evaluation Glutaraldehyde Cross Linked Chitosan Microspheres Containing Rivastigmine Tartrate

Rivastigmine tartrate is an anticholine esterase inhibitor that used in the treatment of Alzheime... more Rivastigmine tartrate is an anticholine esterase inhibitor that used in the treatment of Alzheimer's disease. In this study an attempt was made to encapsulate the Rivastigmine tartrate in Chitosan microspheres for controlled delivery of it. Chitosan microspheres were prepared by the emulsion cross linking method were Glutaraldehyde saturated toluene (GST) was used as a cross linker. Total four batches were prepared with different amount of Glutaraldehyde. It was found that GST had no significant effect on % yield, also increase in amount of GST decrease the particle size and increases the entrapment. GST had shown significant effect on the in vitro drug release and found that increase in amount of GST prolongs the drug release from 36 to 96 hrs. Chitosan microspheres shown to be follow the Higuchi model.

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Analytical Method Development and Validation of Esomeprazole and Levosulpiride in their Combined Capsule dosage form by RP-HPLC

A new simple, accurate, rapid and precise isocratic Reverse Phase High performance liquid chromat... more A new simple, accurate, rapid and precise isocratic Reverse Phase High performance liquid chromatographic (HPLC) method was developed and validated for the determination of Esomeprazole (ESO), and Levosulpiride (LEVO) in a capsule formulation. The Method employs Shimadzu HPLC system on Hypercil BDS C18 (25 cm × 4.6 mm i.e., 5 µm) and flow rate of 1 ml/min with a load of 20µl. Acetonitrile and Phosphate buffer was used as mobile phase in the composition of 50:50 at 3.5 PH. The Detection was carried out at 240 nm. Linearity ranges for Esomeprazole and Levosulpiride were 20-60 µg/ml, 37.5-225 µg/ml respectively. Retention Time of Levosulpiride and Esomeprazole were found to be 3.367 min, 4.320 min respectively. Percent Recovery study values of Esomeprazole and Levosulpiride were found to be within 98-102%. This newly developed method was successfully utilized for the Quantitative estimation of Esomeprazole and Levosulpiride in pharmaceutical dosage forms. This method was validated for accuracy, precision, linearity and Robustness as per ICH guidelines.

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Synthesis, Characterization and Biological Study of Novel Pyrrole Derivatives

A facile condensation of aromatic aldehydes with 2-(5-(phenoxymethyl)-2-thioxo-1,3,4-oxadiazol-3(... more A facile condensation of aromatic aldehydes with 2-(5-(phenoxymethyl)-2-thioxo-1,3,4-oxadiazol-3(2H)-yl)aceto hydrazide (1) was give the corresponding N’-aryl-2-(5-(phenoxymethyl)-2-thioxo-1,3,4-oxadiazol-3(2H)-yl)acetohydrazide (2a-e) in good yield. Cyclo condensation of compounds (2a-e) with maleic anhydride yields 2-aryl-5-oxo-1-(2-(5-(phenoxymethyl)-2-thioxo-1,3,4-oxadiazol-3(2H)-yl)acetamido)-2,5-dihydro-1H-pyrrole-3-carboxylic acid (3a-e). The structures of these compounds were established on the basis of analytical and spectral data. All the newly synthesized compounds were evaluated for their antibacterial and antifungal activities.

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Synthesis and Characterization of novel 6-[3,5-bis(trifluoromethyl)phenyl]-4-(substitutedphenyl)-1,4-dihydropyrimidin-2-ol

Synthesis of various pyrimidines 3(a-o) from (E)-1-(3,5-bis(trifluoromethyl)phenyl)-3-(substitute... more Synthesis of various pyrimidines 3(a-o) from (E)-1-(3,5-bis(trifluoromethyl)phenyl)-3-(substituted)phenylprop-2-en-1-one and Urea in presence of NaOH. The structures of the synthesized compounds were confirmed on the basis of spectral and elemental analysis. The synthesized compounds were screened for antimicrobial activity.

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Synthesis, characterization and anti-microbial activity of 3-{4-[3-chloro-2-(substitutedphenyl)-4-oxoazetidin-1yl] phenyl}-6-bromo-2-methylquinazoline-4-one

Heterocyclic Compounds have so far been synthesized mainly due to the wide range of biological ac... more Heterocyclic Compounds have so far been synthesized mainly due to the wide range of biological activities. Azetidine plays an important role in the biological field. From these reviews, we synthesized a new series of 3-{4-[3-chloro-2-(substituted phenyl)-4-oxoazetidin-1yl] phenyl}-6-bromo-2-methylquinazoline-4-one derived from the reflexes method of Schiff base in presence of triethyl amine with chloro acetyl chloride is developed. The title compounds were characterized by element analysis, IR, NMR and spectral data. All the compounds were tested for their antibacterial and antifungal activities by Cup Borer method.

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Study of Novel Pyrrole Derivatives

Substituted benzaldehydes on simplistic condensation with 2-(5-((naphthalen-1-yloxy) methyl)-2-th... more Substituted benzaldehydes on simplistic condensation with 2-(5-((naphthalen-1-yloxy) methyl)-2-thioxo-1,3,4-oxadiazol-3(2H)-yl)aceto hydrazide(1) was give the consequent N'-arylidene-2-(5-((naphthalen-1-yloxy)methyl)-2-thioxo-1,3,4-oxadiazol-3(2H)-yl) aceto hydrazide (2a-e) in fine yield. Cyclo condensation of compounds (2a-e) with maleic anhydride yields 2-aryl-5-oxo-1-(2-(5-(phenoxymethyl)-2-thioxo-1,3,4-oxadiazol-3(2H)-yl) acetamido)-2,5-dihydro-1H-pyrrole-3-carboxylic acid (3a-e). The structures of these compounds were established on the basis of analytical and spectral data. All the newly synthesized compounds were evaluated for their antibacterial and antifungal activities.

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Synthesis, Characterization and Biological Screening of novel N-[2-chloro-4-(trifluromethyl) phenyl]-4-(substituted phenyl)-3, 6-Dimethyl-2-oxo-1, 2, 3, 4-tetrahydropyrimidine-5-carboxamide

N-[2-chloro-4-(trifluromethyl)phenyl]-4-(substitutedphenyl)-3,6-Dimethyl-2-oxo-1,2,3,4-tetrahydro... more N-[2-chloro-4-(trifluromethyl)phenyl]-4-(substitutedphenyl)-3,6-Dimethyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide (4a-o) are synthesized. The synthesis of (4a-o) was achieved by acid catalysed cyclocondensation of N-(2-chloro-4-(trifluromethyl) phenyl)-3-oxobutanamide, N-methyl urea and benzaldehydes. The products were characterized by FT-IR, mass spectra, 1H NMR and elemental analyses. The newly synthesized compounds were subjected to various biological activities viz., antimicrobial.

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Analytical Method Development and Validation of RP-HPLC for Estimation of Roflumilast in Bulk drug and Tablet dosage Form

A new simple, specific, sensitive, rapid accurate and precise RP-HPLC method was developed for th... more A new simple, specific, sensitive, rapid accurate and precise RP-HPLC method was developed for the estimation of Roflumilast in bulk and pharmaceutical formulation. Roflumilast was chromatographed on zorbex XDB C18 column (150 mm × 4.6 mm, 5µm) in a mobile phase consisting of mixture of ammonium acetate buffer and a solvent mixture (Acetonitrile : Methanol : 80 : 20) in the ration of 40:60v/v. The mobile phase was pumped at a flow rate of 1.0 ml/min with detection at 245 nm. The detector response was linear in the concentration of 1-15µg/ml. the intra and inter day variation was found to be less than 1.0%. The mean recovery of the drug from the solution was 100.1%. Hence it can be applied for routine quality control analysis of Roflumilast in bulk and pharmaceutical formulation.

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Surface coating studies of polyurethane derived from [(alkyd)-(epoxy resin treated castor oil)] using isophorene diisocynate - II

Castor oil (C) was reacted with profitable epoxy resin (E) (diglycidylether of bisphenol-A, DGEBF... more Castor oil (C) was reacted with profitable epoxy resin (E) (diglycidylether of bisphenol-A, DGEBF) at a range of mole ratios. The consequential products (Castor oil- Epoxy resin) were nominated as CEs. Isocyanate terminated castor oil Polyurethane (ICOPU) was prepared by reaction of castor oil and various proportion of Isophoren diisocyanate. A commercial alkyd resin was blended with various proportions of CEs and ICOPU. A unique solvent system, which shows a one – phase clear solution and a clear coat of binder system, was used. All the blends were applied on mild steel panels and characterized for drying time, adhesion, flexibility, hardness, impact resistance and chemical resistance properties.

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Mouth Dissolving Film: A Review

Mouth Dissolvable films (MDFs) evolved over the past few years from the confection and oral care ... more Mouth Dissolvable films (MDFs) evolved over the past few years from the confection and oral care markets in the form of breath strips and became a novel and widely accepted form by consumers. MDF which disintegrates or dissolves within 1min when placed in the mouth without drinking water or chewing. Also, used for the taste masking of widely bitter tasted drugs which are most important for the pediatric patients. These drug delivery systems allow the medication to bypass the first pass metabolism thereby making the medication more bioavailable. Formulation of oral films involves the application of both aesthetic and performance characteristics such as plasticized hydrocolloids, active pharmaceutical ingredient, taste masking agent being laminated by solvent casting or hot melt extrusion. Solvent casting being the most preferred offers great uniformity of thickness and films have fine gloss and better physical properties. Oral strips are evaluated for various attributes such as thickness, Surface pH, folding endurance, disintegration, and dissolution study. This review describes the formulation methodology, evaluation parameter.

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Synthesis of novel 1,2,3,4-tetrahydro-N-(substitutedphenyl)-6-methyl-4-(4-(phenoxymethyl)phenyl)-2-thioxopyrimidine-5-carboxamide and study of their antimicrobial activity

During the last two decades, several pyrimidine derivatives have been developed as chemotherapeut... more During the last two decades, several pyrimidine derivatives have been developed as chemotherapeutic agents and have found wide clinical applications. We synthesize some pyrimidines by Biginelli condensation method. Novel 1,2,3,4-tetrahydro-N-(substitutedphenyl)-6-methyl-4-(4-(phenoxymethyl)phenyl)-2-thioxopyrimidine-5-carboxamide (AB116 to AB130) are synthesized and characterized by FT-IR, 1H NMR, Mass spectra, TLC and elemental analysis. The newly synthesized compounds were screened for antimicrobial activities(MIC) in vitro against two strains of gram –ve and two strains of gram +ve bacteria and three fungi by broth dilution method. Few of the compounds show excellent antimicrobial activity.

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An Efficient multi Component Synthesis Novel triazolopyrimidines

Synthesis and biological activity of new derivatives of triazolopyrimidines (4a-j) were achieved ... more Synthesis and biological activity of new derivatives of triazolopyrimidines (4a-j) were achieved from different acetoacetamides, new aldehyde and triazole using heating within 30 min with high yield. The triazolopyrimidines of the products were supported by FTIR, PMR and mass spectral data.

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Formulation and Evaluation of Aceclofenac Sustained Release Tablets Using Various Grades of Hpmc Polymer

The present work focuses on preparation of Aceclofenac sustained release tablets in order to redu... more The present work focuses on preparation of Aceclofenac sustained release tablets in order to reduce the dosing frequency, there by improve patient compliance and to produce uniform drug release for a prolonged period of time compared to the conventional Aceclofenac tablets. Six formulations were prepared by wet granulation method using HPMC K100M and HPMC K15M as release retardant polymers in the concentration of 5%, 6% and 7%. The prepared granules were evaluated for various pre-compression parameters like angle of repose, bulk density, tapped density, compressibility index and Hausner’s ratio. The FT-IR studies concluded that there was no drug-polymer interaction. The post compression parameters like appearance, thickness, hardness, weight variation, friability, drug content, in-vitro drug release and order of kinetics were studied. The drug release of best formulation F6 was found to be 62.1±0.378 % at the end of 10 hours. The overall results revealed that as the concentration of polymer was increased, the drug release decreased. Plots of log cumulative Percentage drug remaining Vs Time were found to be linear with all the formulations indicating that the drug release from these formulations was according to the first order kinetics. Stability studies of Formulation F6 revealed that the drug was stable even after stored at 25±2oC/60±5%RH and 40±2oC/75±5%RH for 45 days. From all the above observations, the formulation F6 was found to be a better one which satisfied all the criteria for sustained release tablets.

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A Stability-indicating liquid chromatographic method for the quantification of new anti-epileptic drug Lacosamide and its intermediates

A simple, selective, precise, and stability-indicating high-performance liquid chromatography (HP... more A simple, selective, precise, and stability-indicating high-performance liquid chromatography (HPLC) method has been established and validated for the determination of S (–) Enantiomer in Lacosamide drug substance. The chromatographic system used normal phase DAICEL Chiralcel OD-H column with UV-Vis detection at 210 nm. The mobile phase was a mixture of n–hexane–ethanol, 74:6 (%, v/v) and this mixture were transferred to isopropyl alcohol–trifluoroacetic acid in the ratio of 72:6:0.08 (%, v/v). The method is validated for its specificity, precision, accuracy, linearity and ruggedness. Regression analysis data for the calibration plots were indicative of good linear relationships between response and concentration over the range 0.0174µg mL–1 – 5.398 µg mL–1. The correlation coefficient, r2, was 0.9994 and 0.9988. The value of slop and intercept of the calibration plot was 79403 and -16673. The limit of detection and quantitation were 0.087 ± 7.18 µg mL–1 and 0.263 ± 3.68 µg mL–1. Statistical analysis proved the method is repeatable, selective, and accurate for estimation of S (–) Enantiomer in Lacosamide drug substance and its intermediates. Because the method could effectively separate the drug from their possible impurities like dibenzyl urea, benzyl acetamide, desmethyl, diacetyl and methylbenzyl serine, it can be used as a stability indicating method.

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Study of Novel Oligomeric azo dyes

Diazotization of p-anisidine and coupling with 3-amino-phenol-Formaldehyde (APF) resin give oligo... more Diazotization of p-anisidine and coupling with 3-amino-phenol-Formaldehyde (APF) resin give oligomaric azo dye TAPF, based on 3-amino-phenol-Formaldehyde (APF) polymer. The TAPF was then treated with 5-chloro methyl-8-quinolinol hydrochloride in the presence of a THF in alkaline medium (pH 9-10) at room temperature for 7 hrs. The resultant oligomaric ligand designated as azo polyphenol-formaldehyde-5-chloromethyl-8-quinolinol (AAPFQ) was characterized by elemental analysis, IR spectral studies, and thermogravimetry. The polymeric metal chelates of AAPFQ with Cu2+, Zn2+, Mn2+, Ni2+, Fe3+ and Co2+ metal ions were prepared and characterised by metal:ligand ratio, IR and reflectance studies, magnetic properties and thermogravimetry. The AAPFQ sample was also screened for its chelating and ion-exchanging properties. Batch equilibration method has been adopted for evolution of ion-exchange properties.

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Study of Novel polymeric ligand based on salicylic acid-formadehyde polymer

The reaction between Salicylic acid-formadehyde polymer and diazonium salt of p-anisidine yielded... more The reaction between Salicylic acid-formadehyde polymer and diazonium salt of p-anisidine yielded a novel ligand PASA. This ligand PASA treated with transition metal ions Cu+2, Zn+2, Co+2, Fe+3, Mn+2 and Ni+2 form its metal chelates. The PASA and its polymeric metal chelates were characterized by elemental analysis, spectral studies, thermogravimetry, diffuse reflectance spectral studies and magnetic susceptibilities. By Batch equilibration method chelation ion-exchanging properties of the polymers were studied. All the samples have also been monitored for microbicidal activity.

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Formulation, Evaluation and optimisation of Bilayer layer tablet of Repaglinide and Glipizide

Objective: The aim of the present research was to develop a bilayer floating drug delivery system... more Objective: The aim of the present research was to develop a bilayer floating drug delivery system. That contains two layers immediate release layer and sustain release layer. First immediate release layer quickly releases drugs and attains onset of action, subsequently floating sustained release layer floats over gastric fluid and releases the drug in sustained or controlled manner. Experimental Work: In bilayer tablet formulation, the floating sustained release layer was compressed and immediate release layer was added over it, then both layers were compressed. Tablets were characterized using the official methods. Immediate release layer contained Repaglinide, Sodium starch glycolate & Microcrystalline cellulose. In this study floating sustain release layer tablets were prepared using HPMC K4M alone, Na CMC alone & combination of HPMC K4M & Na CMC. Sodium bicarbonate & Citric acid were used as an effervescent agent. All formulations were prepared by using factorial design (32 & 23). All the above formulations were evaluated for in vitro drug release, buoyancy lag time (BLT), swelling ability, floating behavior. Results and Discussion: All formulations showed anomalous transport mechanism. This means diffusion as well as swelling controlled had played an essential role in drug release. Finally bilayer floating sustained release tablets was formulated by using optimized immediate release layer and optimized floating sustained release layer & evaluated as earlier. The optimized bilayer tablet formulation was subjected to stability study 40°C±2°C/75%RH±5%RH for 1 month according to ICH guidelines & evaluated. Conclusions: From the study it is concluded that the developed formulation has good appearance with good handling condition, therapeutically efficacious, stable. The developed Bilayer formulation is viable alternative to conventional Repaglinide and Glipizide tablet.

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FORMULATION AND EVALUATION OF TOPICAL HYDROGEL PATCH CONTAINING AMIDE TYPE LOCAL ANAESTHETIC AGENT

Hydrogel based drug delivery systems provides significant effect in designing sustained release t... more Hydrogel based drug delivery systems provides significant effect in designing sustained release topical dosage forms. Topical patch containing drug in hydrogel type polymer matrix provides not only targeted drug flux through the skin but also provides cooling effect on application site. Topical hydrogel patch containing lidocaine was prepared by using sodium poly acrylate as bioadhesive polymer. Effect of brij 30 and transcutol was also evaluated on topical flux of lidocaine base from hydrogel patch. Transcutol (10% w/w) provides sufficient drug release in contrast to brij 30(4%w/w) in prepared hydrogel patches. Maintenance of uniformity of weight is one of the critical task in preparation of hydrogel patch as polymers used are highly water absorbent. Excess amount of penetration enhancers leads to alter adhesive property of bioadhesive patch so formulation was optimized with Sodium polyacrylate (7%w/w) as the desired concentration for necessary bioadhesiveness and zinc oxide as cross linking agent.

A one-pot microwave irradiation synthesis of Pyrimido[1,2-a]benzimidazoles

Synthesis of a series of pyrimido[1,2-a]benzimidazoles (4a-j) was achieved from different acetoac... more Synthesis of a series of pyrimido[1,2-a]benzimidazoles (4a-j) was achieved from different acetoacetamides, 3,4-dimethoxybenzaldehyde and 2-Aminobenzimedazole using microwave irradiation within 50 minutes with high yield. The structures of the products were supported by FTIR, PMR and mass spectral data.

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Gas Powered Bioadhesive Tablets of Metformin Hydrochloride: In Vitro Evaluation

The low bioavailability and short half-life of Metformin HCl make the development of gas-powered ... more The low bioavailability and short half-life of Metformin HCl make the development of gas-powered mucoadhesive dosage forms desirable. However, drug absorption is limited to upper gastrointestinal tract thus requiring suitable drug delivery system providing complete release during stomach to jejunum transit. This study was undertaken to develop a Metformin HCl gas powered bioadhesive formulation in compliance with these requirements. The strategy proposed is based on directly compressed tablets consisting of a combination of Metformin HCl with different viscosity grades of HPMC (K4M, K15M, and K100M), Carbopol 934P, Xanthan gum and gas generating agent sodium bicarbonate with citric acid. Compatibility among the formulation components was assessed by FTIR. All the tablets were examined for post compressional analysis, drug release and bioadhesive strength. The result of the kinetics study obtained permits us to conclude that the fabricated tablets, in this case, deliver the drug through diffusional dominated mechanism.

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Drug Master File and Processing: An Overview

A Drug Master File is a confidential document used to provide detailed information about faciliti... more A Drug Master File is a confidential document used to provide detailed information about facilities, processes or articles used in the manufacturing process, packaging and storing of one or more human drug. The Drug Master File may be utilized either by the holder who establishes the file, or by one or more additional parties in support of their application. The Drug Master File filing allows a firm to protect its intellectual property from its partner while complying with regulatory requirements for disclosure of processing details. The review includes various types of Drug Master Files, the important aspects in filing and processing.

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Formulation and Evaluation of Okra Fruit Mucilage as a Binder in Paracetamol and Ibuprofen Tablet

The purpose of this study is to search for cheap and effective natural excipients that can be use... more The purpose of this study is to search for cheap and effective natural excipients that can be used as an effective alternative for the formulation of pharmaceutical dosage form. The mucilage from the Okra Fruit (Abelmoschus esculentus) was subjected to Preformulation study for evaluation of its safety and suitability for use as binding agent. The mucilage extracted is devoid of toxicity. Tablets of Lactose were prepared as a control and with 1-5% w/v concentrations of Abelmoschus esculentus mucilage and compared paracetamol, Ibuprofen tablet. The tablets were evaluated for weight variation, hardness,friability and disintegration time according to the USP. Studies indicate that the mucilage of Abelmoschus esculentus may be used as a pharmaceutical adjuvant and as a binding agent at 4 to 5% w/v, depending on its binding ability and the stability of the resulting tablets.

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Validated Stability Indicating RP-HPLC Method For The Determination of Silodosin in Pharmaceutical Dosage Form

A simple, rapid and economic stability indicating high performance liquid chromatography method w... more A simple, rapid and economic stability indicating high performance liquid chromatography method was developed for the determination of Silodosin in pharmaceutical dosage form. The chromatographic system comprised of a reverse phase Phenomenex C 18, 5µ Silica (250×4mm) column maintained at 25°C with mobile phase consisting of a mixture of methanol-water-acetonitrile-glacial acetic acid (60:27:10:3 % v/v) at pH 3.2 ± 0.1 with a flow rate of 1 ml/min, determined at 270 nm. The method was linear in the range of 10-100µg/ml. The results were validated according to ICH guidelines. The method could effectively separate the drug from its degradation products.

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Application of High Performance Liquid Chromatography to The Determination and Validation of Levodopa in Mucuna Pruriens L

The seeds of Mucuna pruriens L. were extracted with 40% ethyl-alcohol, 60% water with 1.5% glacia... more The seeds of Mucuna pruriens L. were extracted with 40% ethyl-alcohol, 60% water with 1.5% glacial acetic acid for the detection of levodopa and some physio-chemical parameters. A sensitive, precise and accurate high-performance liquid chromatographic (HPLC) method has been developed for the quantitative estimation of levodopa in Mucuna pruriens extract. The method utilises sample preparation step followed by separation on a Phenomenex C18, 250 x 4.6 mm, 5 Âµm particle size column, using 0.1 M KH2PO4 (pH 3.0 by ortho-phosphoric acid) as the mobile phase. Analysis of levodopa was carried out in the absorbance mode at 283 nm. The method was validated in terms of linearity, precision (inter and intraday), accuracy, limit of detection (LOD) and limit of quantification (LOQ). Linearity was observed in the range of 20-100 ppm with correlation coefficient of 0.9991. Detection limit was 5.6 ppm and quantification limit was 8.5 ppm. The repeatability of the method was found to be 0.49% and recovery values from 101.17 to 100.18% indicates best accuracy of the method. The results indicated that the extract obtained was 50% Levodopa content and 38% protein content. The proposed HPLC method was also found to be precise, specific, accurate and can be used for the identification and quantitative determination of levodopa in herbal extracts.

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Matrix Type Drug Delivery System: A Review

An appropriately designed controlled release drug delivery system can be a major advance towards ... more An appropriately designed controlled release drug delivery system can be a major advance towards solving problems concerning the targeting of a drug towards specific organ or a tissue and controlling the rate of drug delivery to the target tissue. Matrix tablet is an interesting option when developing as oral controlled release formulation. The Present study focus on oral controlled release dosage forms and types of various polymers used to formulate Matrix Tablets. The use of polymer in controlling the release of drug has become important in the formulation of pharmaceuticals.

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Development and Validation of UV Spectrophotometric Method for Simultaneous estimation of Cefixime and Linezolid in Combined Dosage Form

Cefixime(CEF) is a cephalosporin class of antibiotic drug and Linezolid(LIN) is a oxazolidinone c... more Cefixime(CEF) is a cephalosporin class of antibiotic drug and Linezolid(LIN) is a oxazolidinone class of antibiotic drug. This combination of drug is useful in many bacterial diseases. Accurate, precise, rapid and economical method was developed for the simultaneous estimation of Cefixime(CEF) and Linezolid(LIN) in tablet dosage form. Method is based on the simultaneous equations and wavelengths selected for analysis were 289.0nm (λmax of Cefixime) and 257.0 nm (λmax of Linezolid) respectively, in methanol. The linearity was obtained in the concentration range of 5-40μg/ml for Cefixime and 10-30μg/ml for Linezolid. The correlation coefficient of Cefixime and Linezolid were found to be 0.9998 and 0.9998 respectively. The proposed procedure was successfully applied for the simultaneous determination of both drugs in commercial tablet preparation. The results of the analysis have been validated statistically and by recovery studies have confirmed the accuracy of proposed method.

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A Novel Approach for Transdermal Drug Delivery As A Liposomes Their Progress and Limitations: A Review

The transdermal route of drug delivery has gained great interest of pharmaceutical research, as i... more The transdermal route of drug delivery has gained great interest of pharmaceutical research, as it circumvents number of problems associated with oral route of drug administration. The uniqueness of this type of drug carrier system lies in the fact that it can accommodate hydrophilic, lipophilic as well as amphiphilic drugs. These drugs find place in different places in the vesicle before they get delivered beneath the skin. Liposomes are micro particulate lipoidal vesicles which are under extensive investigation as drug carriers for improving the delivery of therapeutic agents. Due to new developments in liposome technology, several liposome based drug formulations are currently in clinical trial, and recently some of them have been approved for clinical use. Reformulation of drugs in liposomes has provided an opportunity to enhance the therapeutic indices of various agents mainly through alteration in their bio distribution. This review discusses the potential applications of liposomes in drug delivery with examples of formulations approved for clinical use, and the problems associated with further exploitation of this drug delivery system.

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DNA microarray technique

DNA Microarray is the emerging technique in Biotechnology. The many varieties of DNA microarray o... more DNA Microarray is the emerging technique in Biotechnology. The many varieties of DNA microarray or DNA chip devices and systems are described along with their methods for fabrication and their use. It also includes screening and diagnostic applications. The DNA microarray hybridization applications include the important areas of gene expression analysis and genotyping for point mutations, single nucleotide polymorphisms (SNPs), and short tandem repeats (STRs). In addition to the many molecular biological and genomic research uses, this review covers applications of microarray devices and systems for pharmacogenomic research and drug discovery, infectious and genetic disease and cancer diagnostics, and forensic and genetic identification purposes.

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Sustained Release Hydrophilic Matrix Tablet of Ibuprofen: Influence of Polymers on In-Vitro Release and Bioavailability

In the present study, an attempt has been made to evaluate the effect of hydrophilic polymers on ... more In the present study, an attempt has been made to evaluate the effect of hydrophilic polymers on the release profile of drug from matrix system. Ibuprofen, a non-steroidal anti-inflammatory drug (NSAIDs) was used as a model drug to evaluate its release characteristics from different matrices. Matrix tablets of Ibuprofen were prepared by direct compression process using different hydrophilic excipients (Methocel K4M, Methocel K100M, PolyoxWSR 1105 & Metolose 90 SH 100 SR).Before compression, the formulations were evaluated for angle of repose, % compressibility and Hausner’s ratio. Tablets were evaluated for hardness, friability, weight variation, uniformity of thickness & diameter, and drug content and results were found within acceptable limits. In-vitro drug release studies were carried out using USP XXII dissolution apparatus type II at 50 rpm with 900 ml 0.1N HCl & phosphate buffer solutions (PBS) of pH 7.4, maintained at 37±0.50C. The release kinetics was analyzed using the zero-order, first-order model equation, Higuchi’s square root equation, and the Korsmeyer-peppas model. In vitro release studies revealed that the release rate decreased with increases in polymer proportion. The matrix tablet containing 20% Methocel K100M & Polyox WSR 1105 (in ratio 1:1) (Formulation F6) were found to show good initial release (34.52% in an initial hour) and allowed sustained release up to 12 hours. Bioavailability parameters including Cmax, Tmax, AUC(0-t), for both tablet were compared. The sustained release tablet produces optimized Cmax and extended Tmax. Relative bioavailability of the test tablet was calculated as 124.14% for 12 hr. Mathematical analysis of the release kinetics indicated that the nature of drug release from the matrix tablets was dependent on polymer concentration and it was found to be diffusion coupled with erosion. Bioavailability parameters including Cmax, Tmax, AUC(0-t), for both tablet were compared. The sustained release tablet produces optimized Cmax and extended Tmax. Relative bioavailability of the test tablet was calculated as 124.14% for 12 hr. The developed controlled release matrix tablets of Ibuprofen, with sustained release characteristics, might be able to minimize the demerits of conventional therapy having Ibuprofen.

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Synthesis and Antimicrobial Activities of Some Pyrazoline Derivatives

An efficient synthesis of 3, 5-disubstituted-2-pyrazoline was carried out by the condensation of ... more An efficient synthesis of 3, 5-disubstituted-2-pyrazoline was carried out by the condensation of chalcones with hydrazine hydrate in ethanol in presence of piperidine. The newly synthesized compounds were characterized by 1H NMR spectroscopy, IR spectroscopy, MS, elemental analysis and screened for their antimicrobial activity against various strains of bacteria and fungi.

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Novel Approaches of Floating Drug Delivery System: A Review

Several approaches are currently utilized in the prolongation of the GRT, including floating drug... more Several approaches are currently utilized in the prolongation of the GRT, including floating drug delivery systems (FDDS), swelling and expanding systems, polymeric bioadhesive systems, high-density systems, modified-shape systems and other delayed gastric emptying devices. In this review, current & recent developments of Stomach Specific FDDS are discussed. Drugs with narrow absorption window in the gastrointestinal tract have poor absorption. Therefore, gastro retentive drug delivery systems (GRDDS) have been developed, which prolong the gastric emptying time. Several techniques such as floating drug delivery system, low-density systems, raft systems, mucoadhesive systems, high-density systems, superporous hydrogels and magnetic systems, have been employed. This review also summarizes the in vitro techniques, in vivo studies to evaluate the performance and application of floating systems, and applications of these systems. The purpose of writing this review on floating drug delivery systems (FDDS) was to compile the recent literature with special focus on the principal mechanism of floatation to achieve gastric retention.

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Anthelmintic Evaluation of Formulated Polyherbal Syrup

Helminthiasis is an infection of the human body with parasitic worm such as roundworms, earthworm... more Helminthiasis is an infection of the human body with parasitic worm such as roundworms, earthworms, hookworms, flukes, tapeworms and pinworms. The worms usually only involve the intestinal tract but sometimes they may invade other organs. The present study was done with the aim to evaluate the anthelmintic activity of formulated polyherbal syrup containing traditionally used herbs like Neolamarckia cadamba and Alstonia scholaris using adult earthworms Eisenia foetida against albendazole as standard reference and normal saline as control. The time to achieve paralysis of the worms was determined.

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Synthesis, Characterization, Antimicrobial and Antifungal Screening of Some Novel Benzene sulfonamide Derivatives

The present work reports the possible utility of the synthesis of some novel 4-(2-amino-3-cyano-4... more The present work reports the possible utility of the synthesis of some novel 4-(2-amino-3-cyano-4-(substituted-aryl)-5- oxo-5,6,7,8-tetrahydroquinolin-1(4H)-yl)benzene sulfonamide (1a–1u) starting with 4-(3-oxo-cyclohex- 1-enylamino)benzenesulfonamide and 4-(cyclohexenylamino) benzenesulfonamide in the synthesis of some novel 4-(quinolin-1-yl) benzenesulfonamide derivatives. The structures of the synthesized compounds were confirmed by IR, 1H NMR, 13C NMR and mass spectral data. Some of the newly synthesized compounds were evaluated for their in vitro antibacterial and antifungal activity.

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Synthesis and Characterization of 2-Phenyl-3-[(Phenyl Amino) Methyl-Amino)]-Quinazolin-4(3h)-One

The process of establishing a new drug is exceedingly complexioned involves the talents of people... more The process of establishing a new drug is exceedingly complexioned involves the talents of people from a variety of disciplines including Pharmaceutical chemistry, biochemistry, physiology, pharmacology, pharmaceutics and medicine. Heterocyclic chemistry is the branch of chemistry dealing with the synthesis, properties, and applications of heterocyclics. Heterocyclic chemistry comprises at least half of all organic chemistry research worldwide. In particular, heterocyclic structures form the basis of many pharmaceutical, agrochemical and veterinary products. Quinazolinone has been considered as a magic moiety possessing myriad spectrum of medicinal activities. Diversity of biological response profile has attracted considerable interest of several researchers across the globe to explore this skeleton for its assorted therapeutic significance. By using different synthetic methods new quinazolinone derivatives were synthesized and characterized by physic-chemical analysis. Quinazolinone is a lead nucleus for future developments to get effective compounds.

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Identification of Mutation of Pkd2 Gene For Autosomal Dominant Polycystic Kidney Disease in Selected Gujarat Population

Autosomal dominant polycystic kidney (ADPKD) is one of the most common hereditary disease with 1 ... more Autosomal dominant polycystic kidney (ADPKD) is one of the most common hereditary disease with 1 in 1000 in general population. ADPKD is characterised by formation of fluid filled cysts in both kidneys that leads to progressive renal failure. It is a heterogeneous disorder with mutations in two genes pkd1 and pkd2 gene. In Gujarat state ADPKD families the phenotype and genetic background has not previously been characterised. Therefore, in this study 4 subjects with ADPKD from Institute of Kidney Disease Research Centre, Ahmedabad, and Civil Hospital were identified and investigated for genomic study. The aim was to identify pkd2 gene mutation analysis for selected population. The mutation screening of pkd1 gene is difficult because of its size (around 14 kb) and it contains 46 exons. For the same study purpose we have used ABI 3730 SEQUENCER. The sequence data were compared and contrast within a group as well as with the available source of gene bank NCBI. The mutation cosegregating with ADPKD was identified in all 4 subjects for PKD2 gene. Of the four mutations 2 mutations were frameshift mutation, 1 was nonsense mutation and 1 was missense mutation. The maximum total score was matched with data and found to be few exceptions. Finally the mutation detection was done with help of codon code software with output of point mutation and heterozygous mutation. In selected patient out of 4 three sequencing samples were denoted a point mutation. So our findings reveal that the maximum patients showing were in heredited to polycystic kidney disease.

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Epoxy Aldehyde Schiff Bases : Synthesis and Antimicrobial Study

Some new Schiff bases have been synthesized from epoxy aldehyde and their characterization was do... more Some new Schiff bases have been synthesized from epoxy aldehyde and their characterization was done by IR, NMR and mass spectral data. The antibacterial activity of these compounds has also been studied against some Gram-positive and Gram-negative bacteria in DMF and DMSO solutions. It is observed that in DMF, P. mirabilis is the most resistant bacteria whereas in DMSO, S. aureus, K. Pneumoniae and S. typhimurium are the most resistant strains. Overall, nitro group is most effective substitution for inhibiting the studied bacteria.

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Design and Characterization of Cisplatin Magnetic Microspheres

The present study is aimed at the overall improvement in the efficacy, reduction in toxicity and ... more The present study is aimed at the overall improvement in the efficacy, reduction in toxicity and enhancement of therapeutic index of cisplatin. Magnetically responsive biodegradable microparticulate delivery system of cisplatin has been developed by phase separation emulsion polymerization technique by using bovine serum albumin. The formulations were evaluated with respect to particle size analysis, entrapment efficiency, magnetite content, in vitro magnetic responsiveness, in vitro drug release studies, in vivo drug targeting studies and stability studies. The formulated magnetic microspheres were found to be spherical with average particle size of 3-12 µm in diameter and incorporation efficiency up to 56.37%. Result of X-ray diffractometry confirmed the presence of magnetite in prepared cisplatin magnetic microspheres. The total percentage of Fe2O3 in the microspheres was found to be 42.53% to 55.48%. In vitro drug release after 24 hours was 89.60%, 82.22%, 78.41% and 76.35% for formulation F1, F2, F3 and F4 respectively. Results of in vitro magnetic responsiveness and in vivo tissue targeting proved that the retention of microspheres in presence of magnetic field was significantly high than those in the absence of the magnetic field. Stability studies revealed that 4º is the most suitable temperature for storage of cisplatin loaded magnetic microspheres. Overall, this study shows that the magnetic albumin microspheres can be retained at their target site in vivo, following the application of magnetic field, and are capable of releasing their drug content for an extended period of time.

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HPLC Method Development for Simultaneous Estimation of Telmisartan and Chlorthalidone in Tablet Dosage Form

A simple, precise and rapid high-performance liquid chromatography method is developed for the si... more A simple, precise and rapid high-performance liquid chromatography method is developed for the simultaneous quantitative determination of Telmisartan and Chlorthalidone from their combination drug product. It involves a Xterra 150 mm x 4.6 mm, 5μm, C-18 column. The separation is achieved on a simple isocratic method. The mobile phase contains a mixture of potassium dihydrogen phosphate buffer pH 2.5 (0.025M): acetonitrile in the ratio 60:40, v/v. The flow rate is 1.0 mL min−1 and the column is maintained at normal temperature. The detector wavelength is 235 nm. The retention times of Chlorthalidone and Telmisartan are 2.5 minutes and 4.4 minutes respectively. The total runtime for the separation of the two active compounds is 6.0 minutes. The described method is validated with respect to system suitability, specificity, linearity, precision and accuracy.

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Synthesis, Spectral Studies and Biological Activities of 1-Acetyl-5-(substitutedphenyl)-{3-[4-(2-phenyl-4-p-hydroxybenzylidene -5-oxo-imidazol-1-yl)]phenyl}-4,5-dihydropyrazol Derivatives

1-acetyl-5-(substitutedphenyl)-{3-[4-(2-phenyl-4-p-hydroxybenzylidene-5-oxo-imidazol-1-yl)]phenyl... more 1-acetyl-5-(substitutedphenyl)-{3-[4-(2-phenyl-4-p-hydroxybenzylidene-5-oxo-imidazol-1-yl)]phenyl}-4,5-dihydropyrazol have been prepared by the refluxation for three hours of 5-(substitutedphenyl)-[3-(4-{2-phenyl-4-(4-hydroxybenzylidene)-5-oxo-imidazol-1-yl})phenyl]-4,5-dihydropyrazol and Gly. aceticacid the intermediate A3 have been prepared by the refluxation for three hours of 4-(4-hydroxybenzylidene)-1-{4-[3-(substitutedphenyl)prop-2-enoyl]phenyl}-2-phenyl-imidazol-5-one with hydrazine hydrate in presence of ethanol the intermediate A2 synthesized by the condensation of 1-(4-acetylphenyl)-4-(4-hydroxybenzylidene)-2-phenyl-3,5-dihydro-imidazol-5-one with various aldehydes.

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