Objective: Delivery of the desired drug as mucoadhesive drug delivery systems has been subject of interest since 1980s. The various advantages associated with these systems made the buccal drug delivery as a novel route of drug administration. Buccal region offers an attractive route for the administration of systemic drug delivery. The objective of the study was to develop mucoadhesive buccal tablets of repaglinide. Methodology: The tablets were prepared by wet granulation method using a combination of mucoadhesive polymers like chitosan, hydroxyethyl cellulose, guar gum and carbopol 934P in different ratios. Results: Buccal tablets were evaluated by different methods for parameters such as thickness, hardness, weight uniformity, drug content uniformity, surface pH, ex vivo mucoadhesive strength, ex vivo residence time, in vitro drug release, ex vivo drug permeation. The tablets were evaluated for in vitro release in phosphate buffer of pH 6.8 for 12 h. In order to determine the mode of release, the data was subjected to zero order, first order, Higuchi and Korsmeyer-Peppas model. The mucoadhesive strength was evaluated by measuring the force required to detach the tablets from sheep buccal mucosal membrane. Carbopol 934P showed maximum mucoadhesion and required maximum force for detachment; the force required for detachment was directly proportional to its content. DSC and XRD study of the pure drug indicated that the drug is in the crystalline form. But in the formulations, peaks indicated that the drug is in the amorphous form. FTIR spectroscopic studies indicated that there is no drug-excipient interaction. Conclusion: The prepared formulations showed good mucoadhesive strength and ability to sustain the drug release over 12 h; hence, these are the versatile drug delivery systems for repaglinide.
{"title":"Formulation and Evaluation of Mucoadhesive Buccal Tablets of Repaglinide","authors":"M. Patel, C. C. Patil","doi":"10.5530/RJPS.2014.4.5","DOIUrl":"https://doi.org/10.5530/RJPS.2014.4.5","url":null,"abstract":"Objective: Delivery of the desired drug as mucoadhesive drug delivery systems has been subject of interest since 1980s. The various advantages associated with these systems made the buccal drug delivery as a novel route of drug administration. Buccal region offers an attractive route for the administration of systemic drug delivery. The objective of the study was to develop mucoadhesive buccal tablets of repaglinide. Methodology: The tablets were prepared by wet granulation method using a combination of mucoadhesive polymers like chitosan, hydroxyethyl cellulose, guar gum and carbopol 934P in different ratios. Results: Buccal tablets were evaluated by different methods for parameters such as thickness, hardness, weight uniformity, drug content uniformity, surface pH, ex vivo mucoadhesive strength, ex vivo residence time, in vitro drug release, ex vivo drug permeation. The tablets were evaluated for in vitro release in phosphate buffer of pH 6.8 for 12 h. In order to determine the mode of release, the data was subjected to zero order, first order, Higuchi and Korsmeyer-Peppas model. The mucoadhesive strength was evaluated by measuring the force required to detach the tablets from sheep buccal mucosal membrane. Carbopol 934P showed maximum mucoadhesion and required maximum force for detachment; the force required for detachment was directly proportional to its content. DSC and XRD study of the pure drug indicated that the drug is in the crystalline form. But in the formulations, peaks indicated that the drug is in the amorphous form. FTIR spectroscopic studies indicated that there is no drug-excipient interaction. Conclusion: The prepared formulations showed good mucoadhesive strength and ability to sustain the drug release over 12 h; hence, these are the versatile drug delivery systems for repaglinide.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"3 1","pages":"156-165"},"PeriodicalIF":0.0,"publicationDate":"2015-02-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88468569","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Purpose: This review article has been written with a purpose of providing extensive information regarding the theoretical considerations, mucoadhesive polymers and evaluation of mucoadhesive drug delivery system. It would be beneficial to the researchers working in this field. Approach: The anatomy and physiology of the mucosa is briefly discussed, followed by the elucidation of various theories of mucoadhesion. The properties of various mucoadhesive polymers have been discussed. The potential advantages and disadvantages have also been highlighted. Findings: The success and degree of mucoadhesion is influenced by various polymer-based properties such as the degree of cross-linking, chain length and the presence of various functional groupings. Conclusion: Mucoadhesive drug delivery system offer close contact with the absorption tissue, the mucous membrane, releasing the drug at the site of action leading to an increase in bioavailability and greater local and systemic effects.
{"title":"Review on Mucoadhesive Drug Delivery System: Novel Approaches in Modern Era","authors":"Arshad Khan, Rajat Mahamana, Emili Pal","doi":"10.5530/RJPS.2014.4.2","DOIUrl":"https://doi.org/10.5530/RJPS.2014.4.2","url":null,"abstract":"Purpose: This review article has been written with a purpose of providing extensive information regarding the theoretical considerations, mucoadhesive polymers and evaluation of mucoadhesive drug delivery system. It would be beneficial to the researchers working in this field. Approach: The anatomy and physiology of the mucosa is briefly discussed, followed by the elucidation of various theories of mucoadhesion. The properties of various mucoadhesive polymers have been discussed. The potential advantages and disadvantages have also been highlighted. Findings: The success and degree of mucoadhesion is influenced by various polymer-based properties such as the degree of cross-linking, chain length and the presence of various functional groupings. Conclusion: Mucoadhesive drug delivery system offer close contact with the absorption tissue, the mucous membrane, releasing the drug at the site of action leading to an increase in bioavailability and greater local and systemic effects.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"15 1","pages":"128-141"},"PeriodicalIF":0.0,"publicationDate":"2015-02-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75819418","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Objective: To develop a simple, specific, accurate, precise and stability-indicating RP-HPLC method for estimation of acamprosate calcium in tablet dosage form. Method: The optimized method uses a reverse phase column, Inertsil ODS 3V, 250 x 4.6 mm, 5 µm mobile phase of phosphate buffer (adjusted to pH 7.0 ± 0.05 with 0.1N potassium hydroxide or 0.1% orthophosphoric acid): methanol, 95:05 v/v, at a flow rate of 1 mL/min and a detection wavelength of 205 nm using a UV detector. The developed method resulted in acamprosate calcium eluting at 3.327 min. Results: Acamprosate calcium exhibited linearity in the range of 84-504 μg/ml. The intraday and interday precision is exemplified by relative standard deviation of 0.59% and 1.58% respectively. Percentage Mean recovery was found to be in the range of 98.71-99.24%, during accuracy studies. Degradation studies were performed under various conditions where purity threshold value was found to be greater than the angle value. The analytical method was validated according to International Conference on Harmonization guidelines. Conclusion: The developed method is simple, fast, sensitive, linear, accurate, rugged and precise and hence can be applied for routine quality control of acamprosate calcium in bulk and its pharmaceutical dosage forms.
{"title":"Development and validation of stability indicating RP-HPLC method for the estimation of acamprosate calcium in pure and pharmaceutical dosage forms","authors":"N. Mallikarjunarao, D. Sankar","doi":"10.5530/RJPS.2014.4.6","DOIUrl":"https://doi.org/10.5530/RJPS.2014.4.6","url":null,"abstract":"Objective: To develop a simple, specific, accurate, precise and stability-indicating RP-HPLC method for estimation of acamprosate calcium in tablet dosage form. Method: The optimized method uses a reverse phase column, Inertsil ODS 3V, 250 x 4.6 mm, 5 µm mobile phase of phosphate buffer (adjusted to pH 7.0 ± 0.05 with 0.1N potassium hydroxide or 0.1% orthophosphoric acid): methanol, 95:05 v/v, at a flow rate of 1 mL/min and a detection wavelength of 205 nm using a UV detector. The developed method resulted in acamprosate calcium eluting at 3.327 min. Results: Acamprosate calcium exhibited linearity in the range of 84-504 μg/ml. The intraday and interday precision is exemplified by relative standard deviation of 0.59% and 1.58% respectively. Percentage Mean recovery was found to be in the range of 98.71-99.24%, during accuracy studies. Degradation studies were performed under various conditions where purity threshold value was found to be greater than the angle value. The analytical method was validated according to International Conference on Harmonization guidelines. Conclusion: The developed method is simple, fast, sensitive, linear, accurate, rugged and precise and hence can be applied for routine quality control of acamprosate calcium in bulk and its pharmaceutical dosage forms.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"71 1-2 1","pages":"166-171"},"PeriodicalIF":0.0,"publicationDate":"2015-02-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78307546","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Biological Screening of some New N-Imino Substituted Thienopyrimidinones as Potential Antimicrobial Agents","authors":"S. Ramamurthy, E. Jayachandran","doi":"10.5530/rjps.2015.4.6","DOIUrl":"https://doi.org/10.5530/rjps.2015.4.6","url":null,"abstract":"","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"55 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77280434","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Purpose: This article gives a general review on self-micro emulsifying drug delivery system which is used for increasing dissolution rate, thereby, achieving better bioavailability. This technique of microemulsion can be applied for delivery of hydrophilic as well as lipophilic drugs. Approach: Out of number of approaches, microemulsion is a successful technique for the delivery of hydrophilic as well as lipophilic drug as drug carriers because of its improved drug solubilization capacity, long shelf life, ease of preparation and improvement of bioavailability. A vast review on theories of emulsification, methods of achieving micro emulsion, importance of phase diagram and applications of micro emulsions have been illustrated. Findings: The unique classes of optically clear, thermodynamically stable and usually low viscous solution are called micro emulsions. Size of microemulsion is less than 0.1 µm. Due to their unique properties such as ultralow interfacial tension, large interfacial area, thermodynamic stability and the ability to solubilize otherwise immiscible liquids, uses and applications of micro emulsions in pharmaceutical field have been numerous. Conclusion: This review covers a brief overview about various methods and applications of microemulsion technology as one of the successful dimension of novel drug delivery system.
{"title":"Microemulsion-a Versatile Dimension of Novel Drug Delivery System","authors":"P. Sudheer, K. Kar, C. Saha","doi":"10.5530/rjps.2015.1.3","DOIUrl":"https://doi.org/10.5530/rjps.2015.1.3","url":null,"abstract":"Purpose: This article gives a general review on self-micro emulsifying drug delivery system which is used for increasing dissolution rate, thereby, achieving better bioavailability. This technique of microemulsion can be applied for delivery of hydrophilic as well as lipophilic drugs. Approach: Out of number of approaches, microemulsion is a successful technique for the delivery of hydrophilic as well as lipophilic drug as drug carriers because of its improved drug solubilization capacity, long shelf life, ease of preparation and improvement of bioavailability. A vast review on theories of emulsification, methods of achieving micro emulsion, importance of phase diagram and applications of micro emulsions have been illustrated. Findings: The unique classes of optically clear, thermodynamically stable and usually low viscous solution are called micro emulsions. Size of microemulsion is less than 0.1 µm. Due to their unique properties such as ultralow interfacial tension, large interfacial area, thermodynamic stability and the ability to solubilize otherwise immiscible liquids, uses and applications of micro emulsions in pharmaceutical field have been numerous. Conclusion: This review covers a brief overview about various methods and applications of microemulsion technology as one of the successful dimension of novel drug delivery system.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"410 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84880644","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
S. Shirsand, G. Kumar, G. Keshavshetti, S. Sharanabasappa, P. V. Swamy
Objective: In the present investigation, an attempt is made to develop and characterize niosomal gel formulation of clotrimazole to increase retention time in the dermis layer through controlled release of the drug. Methodology: Clotrimazole niosomes were prepared by thin film hydration method using span 40 (as non-ionic surfactant) and cholesterol (as stable vesicle forming agent). The niosomal dispersion was evaluated for vesicle size, surface morphology, percent entrapment efficiency and in vitro drug release. Results: Among the five formulations prepared, the formulation CN3 (containing 100 mg drug, 200 mg surfactant) was found to be promising. Selected niosomal suspension (CN3) containing clotrimazole equivalent to 2 % w/w was incorporated into gel base composed of carbopol (1%), triethanolamine 0.3% and distilled water quantity sufficient. The gel was studied for it’s different parameters such as pH, in vitro drug release, anti-fungal activity and skin irritation effect. Conclusion: The studies suggest that encapsulating clotrimazole in nonionic surfactant vesicles would provide better patient compliance by achieving prolonged release of the drug to the dermis with improved efficacy.
{"title":"Formulation and Evaluation of Clotrimazole Niosomal Gel for Topical Application","authors":"S. Shirsand, G. Kumar, G. Keshavshetti, S. Sharanabasappa, P. V. Swamy","doi":"10.5530/rjps.2015.1.4","DOIUrl":"https://doi.org/10.5530/rjps.2015.1.4","url":null,"abstract":"Objective: In the present investigation, an attempt is made to develop and characterize niosomal gel formulation of clotrimazole to increase retention time in the dermis layer through controlled release of the drug. Methodology: Clotrimazole niosomes were prepared by thin film hydration method using span 40 (as non-ionic surfactant) and cholesterol (as stable vesicle forming agent). The niosomal dispersion was evaluated for vesicle size, surface morphology, percent entrapment efficiency and in vitro drug release. Results: Among the five formulations prepared, the formulation CN3 (containing 100 mg drug, 200 mg surfactant) was found to be promising. Selected niosomal suspension (CN3) containing clotrimazole equivalent to 2 % w/w was incorporated into gel base composed of carbopol (1%), triethanolamine 0.3% and distilled water quantity sufficient. The gel was studied for it’s different parameters such as pH, in vitro drug release, anti-fungal activity and skin irritation effect. Conclusion: The studies suggest that encapsulating clotrimazole in nonionic surfactant vesicles would provide better patient compliance by achieving prolonged release of the drug to the dermis with improved efficacy.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"12 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82434292","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Purpose: The objective of the present study was to formulate and evaluate buccal patches containing combination of lisinopril (LP) and hydrochlorothiazide (HCZ). Approach: Films were fabricated by solvent casting method, using combination of mucoadhesive polymers such as hydroxypropylmethyl cellulose (HPMC), hydroxypropyl cellulose (HPC), polyvinyl alcohol (PVA) and polyvinyl pyrolidone (PVP) and ethyl cellulose (EC) as backing layer. The patches were evaluated for physicochemical characteristics such as weight, thickness, surface pH, folding endurance, bioadhesive strength, swelling index, drug content, tensile strength, elongation at break, mucoadhesion time, in vitro and ex vivo drug permeation. Results: The IR spectra showed no interaction between drug and polymer. Physicochemical characteristics of all the samples were found to be satisfactory. Swelling of the films increased with increasing content of HPMC or HPC and PVP. Bioadhesive force, tensile strength, percentage elongation and mucoadhesion time increased with higher proportions of HPMC, HPC and PVA. In vitro drug release studies demonstrated slower release of both drugs in formulations with higher amount of HPMC, HPC and PVA. The in vitro drug release data of most formulations best fitted first order model, except for the formulations FA3 and FC. Ex vivo drug permeation studies of formulations through porcine buccal mucosa showed similar results as in vitro. Conclusion: Buccal delivery of this combination can resolve the drawbacks like incomplete absorption in the gut thereby possible improvement in bioavailability, apart from controlled release of the drugs.
{"title":"Design and Evaluation of Buccal Patch Containing Combination of Hydrochlorothiazide and Lisinopril","authors":"N. Patel, P. Prabhu, A. Dubey, J. Kamath","doi":"10.5530/rjps.2015.4.4","DOIUrl":"https://doi.org/10.5530/rjps.2015.4.4","url":null,"abstract":"Purpose: The objective of the present study was to formulate and evaluate buccal patches containing combination of lisinopril (LP) and hydrochlorothiazide (HCZ). Approach: Films were fabricated by solvent casting method, using combination of mucoadhesive polymers such as hydroxypropylmethyl cellulose (HPMC), hydroxypropyl cellulose (HPC), polyvinyl alcohol (PVA) and polyvinyl pyrolidone (PVP) and ethyl cellulose (EC) as backing layer. The patches were evaluated for physicochemical characteristics such as weight, thickness, surface pH, folding endurance, bioadhesive strength, swelling index, drug content, tensile strength, elongation at break, mucoadhesion time, in vitro and ex vivo drug permeation. Results: The IR spectra showed no interaction between drug and polymer. Physicochemical characteristics of all the samples were found to be satisfactory. Swelling of the films increased with increasing content of HPMC or HPC and PVP. Bioadhesive force, tensile strength, percentage elongation and mucoadhesion time increased with higher proportions of HPMC, HPC and PVA. In vitro drug release studies demonstrated slower release of both drugs in formulations with higher amount of HPMC, HPC and PVA. The in vitro drug release data of most formulations best fitted first order model, except for the formulations FA3 and FC. Ex vivo drug permeation studies of formulations through porcine buccal mucosa showed similar results as in vitro. Conclusion: Buccal delivery of this combination can resolve the drawbacks like incomplete absorption in the gut thereby possible improvement in bioavailability, apart from controlled release of the drugs.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"375 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76435030","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Address for correspondence Dr. B. C. Koti, Professor and Head, Department of Pharmacology, K. L. E. University’s College of Pharmacy, Vidyanagar, Hubballi-580031, Karnataka, INDIA. Ph no: 09945711281, E-mail: bc_koti@yahoo.com ABSTRACT Background: The leaves of Canthium parviflorum Lam. have been used in folklore medicine for the treatment of diabetes. Objective: To investigate the antidiabetic and antihyperlipidemic effect of ethanolic extract of plant Canthium parviflorum leaves in streptozotocin-induced diabetic rats. Materials and Methods: Extract was analyzed for the presence of various phytoconstituents like carbohydrates, proteins, amino acids, steroids, triterpenoids, glycosides, saponins, flavonoids, alkaloids, tannins and phenolic compounds. Streptozotocin (55mg/kg body weight, intraperitoneal) was administered to induce diabetes and hyperlipidemia in adult rats. Extract (100 and 200 mg/kg) and glibenclamide (5 mg/kg) as standard drug were administered orally for 21 days to evaluate antidiabetic and antihyperlipidemic activity. Blood glucose, Serum content of total cholesterol, triglycerides, High Density Lipoprotein, Low Density Lipoprotein, and insulin levels were estimated. Carbohydrate and lipid metabolizing enzymes like Glucose-6-phosphatase, Fructose1,6-diphosphatase, Phosphogluco isomerase, Aldolase, Glucose-6-phosphate dehydrogenase, amylase and lipase level were also measured. Histopathology of pancreas was studied. Results: Experimental data indicated that extract normalized the liver and pancreatic functions in streptozotocin induced diabetic rats. Conclusion: Extract possesses both antidiabetic and antihyperlipidemic activities in the streptozotocin induced diabetic rats. These findings support the conventional usage of Canthium Parviflorum leaves for the treatment of diabetes.
{"title":"Antidiabetic and Antihyperlipidemic Activity of Canthium parviflorum Extracts in Streptozotocin-Induced Diabetic Rats","authors":"Neelakanth M. Jeedi, B. Koti","doi":"10.5530/rjps.2015.4.8","DOIUrl":"https://doi.org/10.5530/rjps.2015.4.8","url":null,"abstract":"Address for correspondence Dr. B. C. Koti, Professor and Head, Department of Pharmacology, K. L. E. University’s College of Pharmacy, Vidyanagar, Hubballi-580031, Karnataka, INDIA. Ph no: 09945711281, E-mail: bc_koti@yahoo.com ABSTRACT Background: The leaves of Canthium parviflorum Lam. have been used in folklore medicine for the treatment of diabetes. Objective: To investigate the antidiabetic and antihyperlipidemic effect of ethanolic extract of plant Canthium parviflorum leaves in streptozotocin-induced diabetic rats. Materials and Methods: Extract was analyzed for the presence of various phytoconstituents like carbohydrates, proteins, amino acids, steroids, triterpenoids, glycosides, saponins, flavonoids, alkaloids, tannins and phenolic compounds. Streptozotocin (55mg/kg body weight, intraperitoneal) was administered to induce diabetes and hyperlipidemia in adult rats. Extract (100 and 200 mg/kg) and glibenclamide (5 mg/kg) as standard drug were administered orally for 21 days to evaluate antidiabetic and antihyperlipidemic activity. Blood glucose, Serum content of total cholesterol, triglycerides, High Density Lipoprotein, Low Density Lipoprotein, and insulin levels were estimated. Carbohydrate and lipid metabolizing enzymes like Glucose-6-phosphatase, Fructose1,6-diphosphatase, Phosphogluco isomerase, Aldolase, Glucose-6-phosphate dehydrogenase, amylase and lipase level were also measured. Histopathology of pancreas was studied. Results: Experimental data indicated that extract normalized the liver and pancreatic functions in streptozotocin induced diabetic rats. Conclusion: Extract possesses both antidiabetic and antihyperlipidemic activities in the streptozotocin induced diabetic rats. These findings support the conventional usage of Canthium Parviflorum leaves for the treatment of diabetes.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88586817","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
S. Joshi, U. A. More, Manoj S. Kulkarni, Kirankumar Nelaguddad, V. Kulkarni
Purpose: The purpose of the research was to synthesise novel pyrrole derivatives as antitubercular agents. Methodology: A series of various 5-(4-(1H-pyrrol-1-yl)phenyl)-1,3,4-oxadiazol-2-yl substituted benzothioate derivatives (5a-s) were synthesized. The newly synthesized compounds were characterized on the basis of IR, NMR and Mass spectra. The newly synthesized final compounds were evaluated for their in vitro antitubercular activity. Pharmacophore hypothesis and Surflex-Docking studies were carried out to understand the structure activity relationship. Findings: Preliminary results indicated that most of the compounds demonstrated moderate to good antitubercular activity. The effect of the nature of the substituent on the phenyl group; the effect of the hydrogen bond acceptors and the effect of the oxadiazole fragment on InhA and activities against Mycobacterium tuberculosis were assessed. The software generated results was in satisfactory agreement with the evaluated biological activity. Conclusion: These results can be exploited to develop potential leads and structure based drug design of novel InhA inhibitors.
{"title":"Combined Pharmacophore and Molecular Docking-based In silico Study of Some Pyrrolyl 1,3,4-oxadiazole benzothioate Derivatives","authors":"S. Joshi, U. A. More, Manoj S. Kulkarni, Kirankumar Nelaguddad, V. Kulkarni","doi":"10.5530/rjps.2015.2.6","DOIUrl":"https://doi.org/10.5530/rjps.2015.2.6","url":null,"abstract":"Purpose: The purpose of the research was to synthesise novel pyrrole derivatives as antitubercular agents. Methodology: A series of various 5-(4-(1H-pyrrol-1-yl)phenyl)-1,3,4-oxadiazol-2-yl substituted benzothioate derivatives (5a-s) were synthesized. The newly synthesized compounds were characterized on the basis of IR, NMR and Mass spectra. The newly synthesized final compounds were evaluated for their in vitro antitubercular activity. Pharmacophore hypothesis and Surflex-Docking studies were carried out to understand the structure activity relationship. Findings: Preliminary results indicated that most of the compounds demonstrated moderate to good antitubercular activity. The effect of the nature of the substituent on the phenyl group; the effect of the hydrogen bond acceptors and the effect of the oxadiazole fragment on InhA and activities against Mycobacterium tuberculosis were assessed. The software generated results was in satisfactory agreement with the evaluated biological activity. Conclusion: These results can be exploited to develop potential leads and structure based drug design of novel InhA inhibitors.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"231 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74507569","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Purpose: Targeted drug delivery systems are used to deliver drugs to specific areas in definite concentration. Ketoprofen, belongs to NSAID, has various side effects associated with oral administration and also has less rate of permeation through skin from topical formulations. With an intention to increase skin permeability of ketoprofen through the skin by the use of vesicular structures called niosomes this study was undertaken. Methodology: In this particular study, niosomes were prepared by thin film hydration technique and ether injection technique. A topical niosomal gel was prepared by incorporating niosomes into 2% carbopol gel. Findings: Formulations prepared by thin film hydration technique, using drug, tween 40 and cholesterol in a ratio of 1:1:1 resulted in better entrapment efficiency and vesicular size in comparison to ether injection method. Evaluation: The niosomal formulations were characterised for vesicle size distribution, SEM and zeta potential. The best formulation (F16) was selected on the basis of drug entrapment efficiency of 83.63 ± 0.11% and in vitro diffusion profile. Conclusion: A comparative ex-vivo permeation study of niosomal gel against marketed gel, 2.5% w/w gel on excised rat abdominal skin model indicateda two-fold increase in permeation in comparison to marketed gel and a three fold increase in permeation in comparison to 2.5% w/w ketoprofen gel formula.
{"title":"Formulation and Evaluation of Niosomal Drug Delivery System of Ketoprofen","authors":"K. Kar, P. Sudheer","doi":"10.5530/rjps.2015.4.7","DOIUrl":"https://doi.org/10.5530/rjps.2015.4.7","url":null,"abstract":"Purpose: Targeted drug delivery systems are used to deliver drugs to specific areas in definite concentration. Ketoprofen, belongs to NSAID, has various side effects associated with oral administration and also has less rate of permeation through skin from topical formulations. With an intention to increase skin permeability of ketoprofen through the skin by the use of vesicular structures called niosomes this study was undertaken. Methodology: In this particular study, niosomes were prepared by thin film hydration technique and ether injection technique. A topical niosomal gel was prepared by incorporating niosomes into 2% carbopol gel. Findings: Formulations prepared by thin film hydration technique, using drug, tween 40 and cholesterol in a ratio of 1:1:1 resulted in better entrapment efficiency and vesicular size in comparison to ether injection method. Evaluation: The niosomal formulations were characterised for vesicle size distribution, SEM and zeta potential. The best formulation (F16) was selected on the basis of drug entrapment efficiency of 83.63 ± 0.11% and in vitro diffusion profile. Conclusion: A comparative ex-vivo permeation study of niosomal gel against marketed gel, 2.5% w/w gel on excised rat abdominal skin model indicateda two-fold increase in permeation in comparison to marketed gel and a three fold increase in permeation in comparison to 2.5% w/w ketoprofen gel formula.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"43 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76407211","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
京公网安备 11010802042870号
京ICP备2023020795号-1
扫码关注我们
求助内容：
应助结果提醒方式：