Background : Inadequacies observed in the physicochemical properties of native starches suggest t... more Background : Inadequacies observed in the physicochemical properties of native starches suggest the need to co-process them with standard excipients in order to improve their material and packing properties. Objectives : This work was therefore aimed at characterizing starch obtained from local bread fruit tree, Artocarpus atilis (Moraceae) and assessing the effects of co-processing with sodium starch glycolate (SSG) and hydroxypropylmethylcellulose (HPMC). The effect of different co-processing methods was also investigated. Materials and Methods : Bread fruit starch (BF) was extracted and two methods of co-processing; physical mixing and kneading, were used to prepare starches with BF and either SSG or HPMC in the ratios 1:1, 1:2, 1:4 and 1:5. Flow properties and compressibility of the co-processed materials were evaluated using Hausner’s ratio, angle of repose and Carr’s compressibility index. Packing properties were determined by tapping experiment, while viscosity and solubility profiles were determined. Data were analysed with ANOVA and t-test at p≤0.05. Results : Improved flow and compressibility of BF starch were observed on co-processing with either excipient. The angle of repose of BF (63.330) decreased to 36.260 with SSG and to 58.250 with HPMC at the ratio of 1:2. There was a significant increase (p<0.05) in the swelling index (from 1.73 to 2.67) when BF was co-processed with SSG at ratio of 1:4. Co-processing with either HPMC or SSG enhanced volume reduction of BF starch, the highest volume reduction of 0.285 was obtained at the ratio of 1:1. Solubility of the product decreased with both SSG and HPMC at all ratios. Viscosity of BF starch increased when co-processed with HPMC at all ratios except 1:2. There was no significant change in viscosity when the starch was co-processed with SSG. Conclusion : Co-processing Breadfruit starch with either Sodium starch glycolate or HPMC yielded products with improved flow and compression properties; the properties of BF:SSG were better than BF:HPMC. The method used in the co-processing had no significant effect on the starch material properties. Keywords : Co-processing, Bread fruit starch, Compressibility, Material properties
Background: This study was undertaken with the objective of evaluating the pharmaceutical and che... more Background: This study was undertaken with the objective of evaluating the pharmaceutical and chemical equivalence of some commercially available loratadine tablets, and offers a possible explanation for the therapeutic failure of the drug products. Method: The equivalence of eight brands of loratadine hydrochloride tablets labelled A to H was assessed and compared with the Innovator brand labelled I. Visual observation and uniformity of weight tests were carried out on the tablets, mechanical properties were assessed using friability and crushing strength tests as parameters. Release properties of the tablets were assessed by disintegration and dissolution tests. Assay was based on non-aqueous titration procedure using crystal violet solution indicator. Result: All the brands studied were white in colour with different shapes and lustre, and complied with the official specification for uniformity of tablet weight. Friability tests showed that only brand G lost more than 1% of its initial weight, while brands A and E failed the crushing strength test. Brand C did not undergo complete disintegration within 15 minutes, while brands A, B, F and G had less than 70% of the active drug content still in solution after 45 minutes. Two of the brands had active drug content between officially specified range of 98.5% and 101.5% for loratadine tablets. Conclusion: There was a large variation in the pharmaceutical properties of the commercially available loratadine hydrochloride tablets that were selected for this study. Six of the brands evaluated exhibited poor pharmaceutical properties. Generally, only two of the brands were pharmaceutically equivalent with the innovator brand.
A 2(4) full factorial analysis was used to study the individual and interactive effects of binder... more A 2(4) full factorial analysis was used to study the individual and interactive effects of binder type, X1; binder concentration, X2; relative density, X3 and tabletting technique, X4, on disintegration time (DT), brittle fracture index (BFI), tensile strength (TS) and mucoadhesion time (MT) of ibuprofen tablets formulated by direct compression (DC) and wet granulation (WG), and containing Entandophragnia angolense gum (ENTA) as binder, in comparison with hydroxypropylcellulose. The result of the FTIR and UV peaks suggests the absence of any interaction between ENTA and ibuprofen. Interactions between the polymers and ibuprofen were determined using FTIR and UV determinations. The ranking of the individual effects on DT and BFI was X2 > X3 > X1 > X4, on TS; X3 > X2> X1 > X4 and on MT; X2> X > X4 > X3. The effects of changing the binder from hydroxypropylcellulose to ENTA led to an increase in DT and decrease in TS, BFI and MT. Changing X2 and X3 to higher values increased the DT and TS. The interaction between X1 and X2 had the highest influence on BEI and MT, while interaction between "X3 and X4", and "X2 and X3" had the highest influence on DT and TS, respectively. Ibuprofen tablets prepared by wet granulation method and containing Entandophragma angolense gum showed lower capping/lamination tendencies and better mucoadhesive drug release profiles.
Background:Crude seed oils consist essentially of naturally occurring mixtures of triacylglycerol... more Background:Crude seed oils consist essentially of naturally occurring mixtures of triacylglycerols (˃95%). They are purified to improve their overall quality. Oil purification facilitates elimination of impurities and toxicants.Objective: The objective of the study is to purify Garcinia kola seeds crude oil and to evaluate the purified oil for its emulsifying character.Materials and Methods:Crude seed oil of G. kola, obtained from the dried, powdered seed, was purified by passing the crude oil in n-hexane through silica gel and charcoal arranged in tandem. The crude and refined oils were evaluated by thin layer chromatography and infra-red spectroscopy. Emulsions of the refined oil at 30% and 20% concentrations were prepared and evaluated.Results: With the purification process, there was removal of dissolved polar solutes and pigments in the crude oil relative to the purified oil as revealed by the thin layer chromatographic profile and infra-red spectra. At 20% concentration of the refined oil, a lotion with viscosity of 25.67 ± 1.20 cP was formed while a creamy emulsion was produced with the refined oil at 30% concentration with viscosity of 46.00 ± 1.16 cP. This suggests the suitability of the purified oil as a base in the formulation of lotions and creams.Conclusion: The purified oil of G. kola possesses emulsifying property and could find applications in cosmetic and pharmaceutical industries.Keywords: Garcinia cola, seed oil, solid phase purification, emulsifying property
A novel hydrophilic polymer, Entandophragma angolense gum (ENTA), was characterized and incorpora... more A novel hydrophilic polymer, Entandophragma angolense gum (ENTA), was characterized and incorporated as excipient in Ibuprofen tablet matrices prepared by direct compression. Comparisons were made with formulations incorporating Gelatin or Hydroxypropylcellulose. The gum was analysed by X-ray Diffraction and drug-polymer interactions were assessed by Fourier-Transform Infrared (FTIR) spectrometric studies. Mechanical properties of matrices were assessed using crushing strength (CS) and friability (F). In vitro drug release studies were conducted for 24 hours at 37 oC in phosphate buffer pH 7.2 dissolution medium. The results were fitted into kinetic models to determine the drug release mechanism. There were no interactions between Ibuprofen and ENTA. Increased polymer content led to an increase in CS and a decrease in F values. The ranking of the CS was Hydroxypropylcellulose > ENTA > Gelatin, while the ranking was reversed for F. The ranking of the time for 25% drug release, at 80%w/w polymer concentration was ENTA > Hydroxypropylcellulose > Gelatin. The release kinetics determined using the Akaike criterion Index indicate Korsemeyer supercase II model at high concentrations of the gum. Incorporation of Entandophragma angolense gum enhanced the mechanical properties of Ibuprofen matrix tablets and also the controlled drug release. Rezumat Guma Entandophragma angolense (ENTA), un nou polimer hidrofil, a fost caracterizată și incorporată ca excipient in tablete matriceale cu Ibuprofen, preparate prin comprimare directă. Au fost făcute comparații cu formulări ce au incorporat gelatina sau hidroxipropilceluloza. Guma Entandophragma angolense a fost analizată prin difracție cu raze X și interacțiunile medicament-polimer au fost evaluate prin studii spectrometrice cu transformata Fourier in infraroșu (FTIR). Proprietăţile mecanice ale matricelor au fost evaluate cu ajutorul testelor de rezistență (CS) și friabilitate (F). Au fost efectuate studii in vitro de eliberare a substanţei active timp de 24 ore la 37 °C in tampon fosfat pH 7,2 ca mediu de dizolvare . Rezultatele au fost fitate in modele cinetice pentru a determina mecanismul de eliberare al medicamentului. Nu au existat interacțiuni intre Ibuprofen și ENTA. Conținutul crescut de polimer a condus la creșterea CS in ordinea hidroxipropilceluloză > ENTA > gelatină și scăderea valorilor F. Cinetica de eliberare determinată folosind criteriul Akaike Index indică modelul Korsemeyer supercase II, la concentrații ridicate de gumă. Incorporarea gumei Entandophragma angolense consolidează proprietățile mecanice ale comprimatelor matriceale cu Ibuprofen și eliberarea controlată a medicamentului din forma farmaceutică.
Aim: The purpose of this study was to develop microparticles of theophylline employing Cedrela gu... more Aim: The purpose of this study was to develop microparticles of theophylline employing Cedrela gum, a novel natural gums, as a polymer by spray drying method. Materials and Methods: The process parameters were different spray drying temperatures of 110o, 130o and 150oC. The microparticles were evaluated for characteristics like particle size, incorporation efficiency, thermal analysis, X-ray diffraction (XRD) analysis and in vitro drug release. Results: The microparticles were spherical with distorted surface morphology. The particle size ranged from 35.6 to 58.0 μm depending on the spray drying temperature. Differential scanning calorimetry (DSC) studies revealed that theophiline was molecularly dispersed at all operating temperatures. The release of drug from the microparticles was immediate with no lag time with complete release obtained from the microparticles prepared at the highest temperature. Conclusion: Cedrela gum could serve as a carrier for solid dispersion of drugs such as Theophilline by means of spray drying at a temperature as low as 110oC. Microspheres obtained at this temperature were smaller, more free flowing and less susceptible to agglomeration.
Background Antimicrobial resistance and the environmental threat posed by some synthetic antimicr... more Background Antimicrobial resistance and the environmental threat posed by some synthetic antimicrobial agents necessitate more research into development of novel pharmaceutical products that are environmentally friendly. Also, the use of plant derived excipients is growing and opening up new avenue to solve current drug delivery issues in the pharmaceutical industry. Main body This review summarizes studies related to the antimicrobial property of Mangifera indica extracts, possible mechanisms of antimicrobial action and antimicrobial formulations from the plant and overview of researches relating to the use of M. indica as a pharmaceutical excipient. Electronic searches were conducted on databases such as Pub Med, Wiley Online Library (WOL) and Google Scholar with focus on published articles relating to M. indica. Inclusion and exclusion criteria include publications relating to antimicrobial properties of M. indica extracts, its antimicrobial formulations and its use as a pharmace...
Pharmaceutical excipients of natural origin have numerous advantages which include biocompatibili... more Pharmaceutical excipients of natural origin have numerous advantages which include biocompatibility, non toxicity and biodegradability. Selection of a suitable film-forming polymer is important in the formulation of oral fast dissolving films. This work aims to investigate a natural gum from Enterolobium cyclocarpum tree, as a film forming polymer in chlorpheniramine oral film formulations; comparing it with hydroxylpropylmethyl cellulose (HPMC). Enterolobium gum was modified, using acetic anhydride (acetylation) and ethylene glycol. Physicochemical properties of native and modified gums were determined. Oral dissolving films were prepared from blends of HPMC and either native, acetylated or ethylene glycol modified gum, using the solvent evaporation technique. Films were evaluated for weight variation, thickness, folding endurance, in-vitro disintegration and release properties. FT-IR revealed no adverse chemical interaction. High moisture content was shown by the swelling index de...
Background : Inadequacies observed in the physicochemical properties of native starches suggest t... more Background : Inadequacies observed in the physicochemical properties of native starches suggest the need to co-process them with standard excipients in order to improve their material and packing properties. Objectives : This work was therefore aimed at characterizing starch obtained from local bread fruit tree, Artocarpus atilis (Moraceae) and assessing the effects of co-processing with sodium starch glycolate (SSG) and hydroxypropylmethylcellulose (HPMC). The effect of different co-processing methods was also investigated. Materials and Methods : Bread fruit starch (BF) was extracted and two methods of co-processing; physical mixing and kneading, were used to prepare starches with BF and either SSG or HPMC in the ratios 1:1, 1:2, 1:4 and 1:5. Flow properties and compressibility of the co-processed materials were evaluated using Hausner’s ratio, angle of repose and Carr’s compressibility index. Packing properties were determined by tapping experiment, while viscosity and solubility profiles were determined. Data were analysed with ANOVA and t-test at p≤0.05. Results : Improved flow and compressibility of BF starch were observed on co-processing with either excipient. The angle of repose of BF (63.330) decreased to 36.260 with SSG and to 58.250 with HPMC at the ratio of 1:2. There was a significant increase (p<0.05) in the swelling index (from 1.73 to 2.67) when BF was co-processed with SSG at ratio of 1:4. Co-processing with either HPMC or SSG enhanced volume reduction of BF starch, the highest volume reduction of 0.285 was obtained at the ratio of 1:1. Solubility of the product decreased with both SSG and HPMC at all ratios. Viscosity of BF starch increased when co-processed with HPMC at all ratios except 1:2. There was no significant change in viscosity when the starch was co-processed with SSG. Conclusion : Co-processing Breadfruit starch with either Sodium starch glycolate or HPMC yielded products with improved flow and compression properties; the properties of BF:SSG were better than BF:HPMC. The method used in the co-processing had no significant effect on the starch material properties. Keywords : Co-processing, Bread fruit starch, Compressibility, Material properties
Background: This study was undertaken with the objective of evaluating the pharmaceutical and che... more Background: This study was undertaken with the objective of evaluating the pharmaceutical and chemical equivalence of some commercially available loratadine tablets, and offers a possible explanation for the therapeutic failure of the drug products. Method: The equivalence of eight brands of loratadine hydrochloride tablets labelled A to H was assessed and compared with the Innovator brand labelled I. Visual observation and uniformity of weight tests were carried out on the tablets, mechanical properties were assessed using friability and crushing strength tests as parameters. Release properties of the tablets were assessed by disintegration and dissolution tests. Assay was based on non-aqueous titration procedure using crystal violet solution indicator. Result: All the brands studied were white in colour with different shapes and lustre, and complied with the official specification for uniformity of tablet weight. Friability tests showed that only brand G lost more than 1% of its initial weight, while brands A and E failed the crushing strength test. Brand C did not undergo complete disintegration within 15 minutes, while brands A, B, F and G had less than 70% of the active drug content still in solution after 45 minutes. Two of the brands had active drug content between officially specified range of 98.5% and 101.5% for loratadine tablets. Conclusion: There was a large variation in the pharmaceutical properties of the commercially available loratadine hydrochloride tablets that were selected for this study. Six of the brands evaluated exhibited poor pharmaceutical properties. Generally, only two of the brands were pharmaceutically equivalent with the innovator brand.
A 2(4) full factorial analysis was used to study the individual and interactive effects of binder... more A 2(4) full factorial analysis was used to study the individual and interactive effects of binder type, X1; binder concentration, X2; relative density, X3 and tabletting technique, X4, on disintegration time (DT), brittle fracture index (BFI), tensile strength (TS) and mucoadhesion time (MT) of ibuprofen tablets formulated by direct compression (DC) and wet granulation (WG), and containing Entandophragnia angolense gum (ENTA) as binder, in comparison with hydroxypropylcellulose. The result of the FTIR and UV peaks suggests the absence of any interaction between ENTA and ibuprofen. Interactions between the polymers and ibuprofen were determined using FTIR and UV determinations. The ranking of the individual effects on DT and BFI was X2 > X3 > X1 > X4, on TS; X3 > X2> X1 > X4 and on MT; X2> X > X4 > X3. The effects of changing the binder from hydroxypropylcellulose to ENTA led to an increase in DT and decrease in TS, BFI and MT. Changing X2 and X3 to higher values increased the DT and TS. The interaction between X1 and X2 had the highest influence on BEI and MT, while interaction between "X3 and X4", and "X2 and X3" had the highest influence on DT and TS, respectively. Ibuprofen tablets prepared by wet granulation method and containing Entandophragma angolense gum showed lower capping/lamination tendencies and better mucoadhesive drug release profiles.
Background:Crude seed oils consist essentially of naturally occurring mixtures of triacylglycerol... more Background:Crude seed oils consist essentially of naturally occurring mixtures of triacylglycerols (˃95%). They are purified to improve their overall quality. Oil purification facilitates elimination of impurities and toxicants.Objective: The objective of the study is to purify Garcinia kola seeds crude oil and to evaluate the purified oil for its emulsifying character.Materials and Methods:Crude seed oil of G. kola, obtained from the dried, powdered seed, was purified by passing the crude oil in n-hexane through silica gel and charcoal arranged in tandem. The crude and refined oils were evaluated by thin layer chromatography and infra-red spectroscopy. Emulsions of the refined oil at 30% and 20% concentrations were prepared and evaluated.Results: With the purification process, there was removal of dissolved polar solutes and pigments in the crude oil relative to the purified oil as revealed by the thin layer chromatographic profile and infra-red spectra. At 20% concentration of the refined oil, a lotion with viscosity of 25.67 ± 1.20 cP was formed while a creamy emulsion was produced with the refined oil at 30% concentration with viscosity of 46.00 ± 1.16 cP. This suggests the suitability of the purified oil as a base in the formulation of lotions and creams.Conclusion: The purified oil of G. kola possesses emulsifying property and could find applications in cosmetic and pharmaceutical industries.Keywords: Garcinia cola, seed oil, solid phase purification, emulsifying property
A novel hydrophilic polymer, Entandophragma angolense gum (ENTA), was characterized and incorpora... more A novel hydrophilic polymer, Entandophragma angolense gum (ENTA), was characterized and incorporated as excipient in Ibuprofen tablet matrices prepared by direct compression. Comparisons were made with formulations incorporating Gelatin or Hydroxypropylcellulose. The gum was analysed by X-ray Diffraction and drug-polymer interactions were assessed by Fourier-Transform Infrared (FTIR) spectrometric studies. Mechanical properties of matrices were assessed using crushing strength (CS) and friability (F). In vitro drug release studies were conducted for 24 hours at 37 oC in phosphate buffer pH 7.2 dissolution medium. The results were fitted into kinetic models to determine the drug release mechanism. There were no interactions between Ibuprofen and ENTA. Increased polymer content led to an increase in CS and a decrease in F values. The ranking of the CS was Hydroxypropylcellulose > ENTA > Gelatin, while the ranking was reversed for F. The ranking of the time for 25% drug release, at 80%w/w polymer concentration was ENTA > Hydroxypropylcellulose > Gelatin. The release kinetics determined using the Akaike criterion Index indicate Korsemeyer supercase II model at high concentrations of the gum. Incorporation of Entandophragma angolense gum enhanced the mechanical properties of Ibuprofen matrix tablets and also the controlled drug release. Rezumat Guma Entandophragma angolense (ENTA), un nou polimer hidrofil, a fost caracterizată și incorporată ca excipient in tablete matriceale cu Ibuprofen, preparate prin comprimare directă. Au fost făcute comparații cu formulări ce au incorporat gelatina sau hidroxipropilceluloza. Guma Entandophragma angolense a fost analizată prin difracție cu raze X și interacțiunile medicament-polimer au fost evaluate prin studii spectrometrice cu transformata Fourier in infraroșu (FTIR). Proprietăţile mecanice ale matricelor au fost evaluate cu ajutorul testelor de rezistență (CS) și friabilitate (F). Au fost efectuate studii in vitro de eliberare a substanţei active timp de 24 ore la 37 °C in tampon fosfat pH 7,2 ca mediu de dizolvare . Rezultatele au fost fitate in modele cinetice pentru a determina mecanismul de eliberare al medicamentului. Nu au existat interacțiuni intre Ibuprofen și ENTA. Conținutul crescut de polimer a condus la creșterea CS in ordinea hidroxipropilceluloză > ENTA > gelatină și scăderea valorilor F. Cinetica de eliberare determinată folosind criteriul Akaike Index indică modelul Korsemeyer supercase II, la concentrații ridicate de gumă. Incorporarea gumei Entandophragma angolense consolidează proprietățile mecanice ale comprimatelor matriceale cu Ibuprofen și eliberarea controlată a medicamentului din forma farmaceutică.
Aim: The purpose of this study was to develop microparticles of theophylline employing Cedrela gu... more Aim: The purpose of this study was to develop microparticles of theophylline employing Cedrela gum, a novel natural gums, as a polymer by spray drying method. Materials and Methods: The process parameters were different spray drying temperatures of 110o, 130o and 150oC. The microparticles were evaluated for characteristics like particle size, incorporation efficiency, thermal analysis, X-ray diffraction (XRD) analysis and in vitro drug release. Results: The microparticles were spherical with distorted surface morphology. The particle size ranged from 35.6 to 58.0 μm depending on the spray drying temperature. Differential scanning calorimetry (DSC) studies revealed that theophiline was molecularly dispersed at all operating temperatures. The release of drug from the microparticles was immediate with no lag time with complete release obtained from the microparticles prepared at the highest temperature. Conclusion: Cedrela gum could serve as a carrier for solid dispersion of drugs such as Theophilline by means of spray drying at a temperature as low as 110oC. Microspheres obtained at this temperature were smaller, more free flowing and less susceptible to agglomeration.
Background Antimicrobial resistance and the environmental threat posed by some synthetic antimicr... more Background Antimicrobial resistance and the environmental threat posed by some synthetic antimicrobial agents necessitate more research into development of novel pharmaceutical products that are environmentally friendly. Also, the use of plant derived excipients is growing and opening up new avenue to solve current drug delivery issues in the pharmaceutical industry. Main body This review summarizes studies related to the antimicrobial property of Mangifera indica extracts, possible mechanisms of antimicrobial action and antimicrobial formulations from the plant and overview of researches relating to the use of M. indica as a pharmaceutical excipient. Electronic searches were conducted on databases such as Pub Med, Wiley Online Library (WOL) and Google Scholar with focus on published articles relating to M. indica. Inclusion and exclusion criteria include publications relating to antimicrobial properties of M. indica extracts, its antimicrobial formulations and its use as a pharmace...
Pharmaceutical excipients of natural origin have numerous advantages which include biocompatibili... more Pharmaceutical excipients of natural origin have numerous advantages which include biocompatibility, non toxicity and biodegradability. Selection of a suitable film-forming polymer is important in the formulation of oral fast dissolving films. This work aims to investigate a natural gum from Enterolobium cyclocarpum tree, as a film forming polymer in chlorpheniramine oral film formulations; comparing it with hydroxylpropylmethyl cellulose (HPMC). Enterolobium gum was modified, using acetic anhydride (acetylation) and ethylene glycol. Physicochemical properties of native and modified gums were determined. Oral dissolving films were prepared from blends of HPMC and either native, acetylated or ethylene glycol modified gum, using the solvent evaporation technique. Films were evaluated for weight variation, thickness, folding endurance, in-vitro disintegration and release properties. FT-IR revealed no adverse chemical interaction. High moisture content was shown by the swelling index de...
Uploads
Papers by Michael Odeniyi