Pharmazie

The effect of six different preservatives on the production process and stability of resveratrol nanosuspensions was investigated. Nanosuspensions of the anti-oxidant resveratrol were prepared by high pressure homogenization (1,500 bar, 20 homogenization cycles). The preservatives used were: caprylyl glycol (0.75%), Euxyl PE 9010 (1.0%), Hydrolite-5 (2.0), Phenonip (0.75%), Rokonsal PB-5 (0.5%) and MultiEx Naturotics (2.0%). Preservation is essential for oral and dermal nanosuspensions, but can impair the stability. The effect of the preservatives on stability as a function of cycle numbers was determined by size measurements (photon correlation spectroscopy (PCS), laser diffraction (LD) and light microscopy). Zeta potential measurements were performed for determination of the Stern potential (measurements in water) and as stability criterion (measurements in original dispersion medium), to elucidate the mechanism of destabilization. The preservatives could be placed into three grou...

The present study aimed to produce verapamil hydrochloride-loaded solid lipid microparticles (SLM) by the w/o/w emulsion solvent evaporation technique, using diethyl ether as solvent phase, glyceryl monostearate as biodegradable polymer and Span 60 as surfactant. SLM of spherical shape were prepared by simple dilution of the emulsion with water. To increase the lipid load the process was conducted at 50 degrees C, and in order to reach sub-micron size, a high-shear homogenizer was used. The encapsulation efficiency of prepared SLM reached 74.29 +/- 0.76%. Particle size (98.55 +/- 1.42 microm), surface morphology (spherical) and drug loading efficiency (18.57 +/- 1.25% w/w) were investigated. And optimization of drug polymer ratio (3:1), nature and concentration of emulsion stabilizer in the external aqueous (0.1%), phase viscosity of external aqueous phase (0.5%), volume of external aqueous phase and stirring rate (1000 rpm) were detected. Analysis of microsphere content after proce...

This study presents the in vitro and in vivo testing of anti-inflammatory drug containing creams, hydrogels and organogels for dermal use. In vitro penetration studies were performed with products by measuring the diffused drug amount through synthetic membranes soaked in isopropyl myristate (IPM). Our developed preparations were investigated under in vitro conditions together with two marketed medicinal products used as reference preparations. In vivo studies were carried out on anaesthetized male Wistar rats; the carrageenan-induced paw oedema decreasing effect of twelve different formulations and the reference products were measured in comparison with a control group. All - previously in vitro screened - selected products reduced paw oedema in rats. Significant differences were found among the developed products both in vitro and in vivo. Correlation between the in vitro penetration studies and in vivo results were found in the case of o/w creams, organogels and hydrogels.

As an inheritor of the rich medico-pharmaceutical heritage in Asia Minor, Turkey constituted a critical junction of exchange and dissemination of pharmacy knowledge between East and West throughout history. This greatly contributed to the rapid development of pharmacy as an established profession. The 20th century saw scholarly examination of the field's history: the first book on the history of pharmacy appeared in Turkish (1911); a history of pharmacy course was offered for the first time in the pharmacy curriculum (1945); the first history of pharmacy museum was founded (1960); and national conferences on the history of pharmacy were launched (1990). In addition to providing information on the milestones of the history of pharmacy studies in Turkey in the last hundred years, this study aims to statistically evaluate the change in the number of history of pharmacy-related publications per decade as well as discuss the current situation of history of pharmacy education at Turki...

Ivy (Hedera helix L., Araliaceae), is an evergreen medicinal and ornamental plant. Depending on leaf polymorphism different shaped ivy leaves were extracted and subsequently analyzed by reversed-phase high performance liquid chromatography (RP-HPLC). Quantitative determination of its most prominent saponins hederacoside C (1) and alpha-hederin (2) from different ivy leaf extracts were detected, validated and optimized for quick profiling. The linearity of response, repeatability and reproducibility of the applied RP-HPLC method are reported.

Metronidazole (MTZ) is a nitroimidazole antibiotic used mainly for the treatment of infections caused by susceptible organisms, particularly anaerobic bacteria and protozoa. Distinct from its antibiotic, amoebicidal, and antiprotozoal effects, MTZ displays immunopharmacological behaviour. This review outlines multiple effects of MTZ on different aspects of immunity, including innate and acquired immunity, and also highlights the immunopharmacological behaviour of MTZ in terms of its relevance to inflammation, delayed type hypersensitivity (DTH) and graft versus host disease (GVHD).

Patienten werden heute immer häufiger als informierte Entscheider adressiert, die Risiken abwägen und verantworten sollen. Dieser Aufsatz analysiert die Adressierung von Handelnden als Entscheider als eine an Bedeutung zunehmende Strategie  der Risikoverarbeitung, die Individuen für Kontingentes (mit)verantwortlich macht. Zunächst wird die Eigenart von Risiken in der Medizin untersucht und das „probabilistische Risiko“ als spezifisch Risikoart konturiert, die oftmals nicht mit einer individuellen Bedrohung korrespondiert. Dann wird anhand der Fallbeispiele der Arzneimittelregulierung und der medizinisch-genetischen Beratung analysiert, wie diese probabilistischen Risiken sozial verarbeitet, also reguliert, verteilt, zugewiesen und verantwortet werden (sollen). Dabei zeigen sich typische Paradoxien, die mit der Aufforderung zur risikoabwägenden Entscheidung einhergehen: Trotz der Zunahme an Information vergrößert sich die persönliche Ungewissheit. Außerdem werden Patienten dazu aufgefordert, individuelle Entscheidungen auf einer statistische Rationalität zu gründen, die per definitionem von allem Individuellen und Konkreten absieht. Mit dieser exemplarischen Analyse untersucht der Aufsatz die sozialen Folgen der Tendenz individueller Responsibilisierung angesichts von probabilistischen Risiken.

In the present study chitosan based gel formulations containing Egg Yolk Oil (EYO) and Epidermal Growth Factor (EGF) were formulated successfully aiming at enhanced topical treatment of dermal burns the combination of traditional approaches with modern drug delivery systems. Physicochemical properties of the formulations were analyzed and efficacy of the formulations prepared were evaluated versus a commercial product; Silverdin® (1% silver sulfadiazine) in vivo on Wistar rats. Burns were generated on the back of the rats and at predetermined time intervals tissue samples were collected and evaluated histologically. The analyses showed that chitosan based gel formulations containing Egg Yolk Oil (E1) and chitosan based gel formulations containing EYO and EGF (M1) formulations seem to be better alternatives for Silverdin® with a significant difference (p < 0.05) considering healing ranks of tissue samples.

In the present article synthesis and evaluation for antibacterial and antifungal activity of a new series of 2,5-disubstituted-1,3,4-oxadiazole derivatives is described. 2,5-disubstituted-1,3,4-oxadiazole derivatives were synthesized by the reaction of quinolinyl hydrazone derivatives with dichloromethane. The compounds (6a-h) were characterized by IR, NMR, and mass spectroscopy. All the synthesized compounds were screened for their antimicrobial activity. The antimicrobial results reveal that among the synthesized compounds 6b and 6f showed excellent antibacterial and antifungal activity. The compounds 6c, 6d and 6e did not show antifungal activity against the Colletotrichum capsici.

Myo-inositol hexakisphosphate (InsP6, phytate) is a molecule to which diverse beneficial properties have been attributed. Some of these properties are related to its dermatological use as discolouring agent, on preventing calcinosis cutis or due to its important role on premature aging. Other studies also seem to demonstrate a capacity of InsP6 to inhibit skin cancer. In this paper, the effect of the vehicle of topical administration of phytate is studied, using four groups of male Wistar rats (n = 6) fed with an InsP6 defficient diet and treated with a hydrophyl gel or an O/W moisturizing cream with two different concentrations of InsP6. Due to the correlation between InsP6 absorption and its urinary excretion, these last values were used to evaluate this process. It was found that phytate was absorbed through the skin using both a gel or a cream, demonstrating that its absorption is independent on the matrix used for topical treatment. However, urinary InsP6 values were slightly h...

Solid dispersions of the poorly water soluble drug dexamethasone and newly synthesized chitosan derivatives (chitosan succinate, CS, and chitosan phthalate, CP) were prepared by spray drying. The resulting microspheres were evaluated in terms of their drug loading or encapsulation efficiency as well as drug release profile. Differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD) and infrared spectroscopy (IR) were used to evaluate the solid dispersion for possible interactions between drug and polymers. The pure drug was evaluated in the same manner for comparison purposes. High loading levels (>74%) were achieved using CP and CS as polymer matrices. Drug release rate was accelerated significantly upon the formation of the solid dispersions; the drug release rate was increased with increasing percentage of the chitosan derivatives in the microspheres. IR studies showed no chemical interaction while the X-ray studies showed a significant change in the crystallinit...

2,3,9,10-Tetramethoxy-12-oxo-12-H-indolo[2,1-a]isoquinolinium chloride 1 (compound X) and 13-(3,4-dimethoxyphenyl)-2,3,8,9-tetramethoxy-6a, 12a-diazadibenzo[a,g] fluorenylium chloride 2 (compound NF) are new papaverine oxidation products. A solution of compound 1 bleaches on addition of sodium hydroxide solution. A new entity, 2-(2-carboxy-4,5-dimethoxyphenyl)-6,7-dimethoxyisoquinolinium inner salt 3 (compound WP), is formed. The physico-chemical properties of compounds 1-3, such as solubility in water and lipophilicity, have been measured. The IC50 for compounds 1 and 3 was also assessed.

A simple, rapid and specific ion-pair HPLC method for the determination of (R,R)-glycopyrronium bromide and its related impurities is presented, and parameters affecting the chromatographic properties of these compounds are discussed. Optimal analyte separation was achieved on base deactivated Nucleosil at 40 degrees C, using phosphate buffer pH 2.30 with sodium-1-decanesulfonate (0.01 M)/methanol (35/65; v/v) as eluent for isocratic elution at a flow rate 1 ml x min(-1). The analytical assay was validated according to international guidelines. The methodis suitable for in-process control and as stability indicating assay.

An aqueous extract of Pterocarpus marsupium wood was screened for hypoglycemic activity on alloxan-induced diabetic rats. During both acute and sub-acute tests, the water extract, at an oral dose of 250 mg/kg, showed statistically significant hypoglycemic activity.

A comparison of different fractions of the fruit of Hyphaene thebaica (Doum) was performed in order to investigate their effects on serum cholesterol, triglycerides and lipoproteins: HDL (high density lipoprotein) cholesterol and Non-HDL cholesterol in normal rats. Female Sprague-Dawely rats were treated orally with different fractions of the Doum plant. We used atorvastatin and a natural extract of Monascus purpureus as references. The total cholesterol, HDL cholesterol, Non-HDL cholesterol and triglycerides were estimated. Three fractions of the Doum plant exhibited a highly significant decrease in serum cholesterol and Non-HDL cholesterol. One fraction exhibited a highly significant decrease in cholesterol level but with only a moderately significant effect in decreasing the Non-HDL level. Decreasing Non-HDL, especially LDL, cholesterol, can reduce the risk of atherosclerosis and subsequent cardiovascular diseases. The natural, safe and non-toxic Doum plant could be of great meri...

Terminalia arjuna bark extract is believed to exhibit cardio-protective effects. In the present study we investigated the possible involvement of thyroid hormones in the amelioration of cardiac and hepatic lipid peroxidation (LPO) by a bark extract of the plant in albino rats. While L-thyroxine (L-T4) treatment increased the level of thyroid hormones, heart/body weight ratio as well as cardiac and hepatic lipid peroxidation, simultaneous administration of 21.42 and 42.84 mg/kg of the plant extract decreased the level of thyroid hormones and also the cardiac LPO, suggesting the possible mediation of the drug action through an inhibition in thyroid function. These effects were comparable to a standard antithyroid drug, propyl thiouracil (PTU). When the drug was administered to euthyroid animals, serum concentrations of thyroid hormones were decreased, whereas the hepatic LPO increased indicating a drug induced toxicity in euthyroid subjects. Although a suboptimal dose of the drug was ...

Phenazopyridine hydrochloride (1) is an azo dye with local analgesic and anaesthetic effects on the urinary tract. Its photochemistry was studied in different reaction media including the drug adsorbed on silica gel. This resulted in photochemical cyclodehydrogenation, reductive photodegradation and rearrangement of the drug molecule. Four major products were isolated and identified on the basis of IR, NMR and mass spectral studies. The products are: pyrido[3,4-c]cinnoline-2,4-diamine (2), N3-phenylpyridine-2,3,4,6-tetraamine (3), pyridine-2,3,6-triamine (4), 2,6-diamino-1-(4-aminophenyl)pyridin-4(1H)-one (5).

The present research study deals with the evaluation of sixty four methanolic and aqueous extracts of thirty Yemeni plants used in traditional medicine for their in vitro antiproliferative activity against three human cancer cell lines in a microtiter plate assay based on cellular staining with crystal violet, for their antimicrobial activity against antibiotic susceptible three Gram-positive, three Gram-negative bacterial and one fungal stains and three multiresistant Staphylococcus strains by the agar diffusion method and the determination of MIC against three Gram-positive bacteria with the broth micro-dilution assay, as well as for their antioxidant activity using the DPPH radical scavenging method. Furthermore the chemical composition of the methanolic extracts was determined by using chromatographic methods. As a result of this work, 12 Yemeni herbs namely Centaurothamus maximus, Costus arabicus, Cupressus sempervirens, Dichrocephala integrifolia, Euphorbia schimperi, Gomphoca...

In this paper we developed a graphical method based on Haar (HA) and Mexican (MEX) one-dimensional continuous wavelet transforms and we applied it to a mixture of hydrochlorothiazide (HCT) and spironolactone (SP) in the presence of strongly overlapping signals. Keeping in mind to obtain an appropriately transformed spectrum, we tested several values of the scaling parameter a and the point number of the analysed spectrum in the concentration range of 2-22 microg/ml for both active compounds. The optimal values of the scale parameters and the corresponding frequencies were found to be a = 32 and 0.031 for HA and a = 30 and 0.008 for MEX corresponding to 400 points. HA and MEX methods based on a zero crossing technique were applied to the analysed signal and their regression lines at the selected points were obtained. The validation of the above methods was carried out by analysing different synthetic mixtures containing HCT and SP. MATLAB 6.5 software was used for one-dimensional wav...