Rajesh A Shastry, Smita D. Madagundi, Prasanna V Habbu, Basavaraj S. Patil, Shrinivas D. Joshi, V. H. Kulkarni
Purpose: The purpose of the research was to investigate the anticonvulsant activity of Asparagus racemosus (wild) (AR) by studying the effects on seizures by maximal electric shock, picrotoxin, and strychnine induced convulsive methods in mice. Methodology: The anticonvulsant effect of ethanolic extract of A. racemosus (ETAR) and methanolic extract of A. racemosus (MEAR) were evaluated. In maximal electric shock abolition of the hind leg tonic extensor component seizure were analyzed. In picrotoxin induced convulsion, time of onset of seizures and time of death were recorded; whereas in strychnine induced convulsion time of occurrence of tonic convulsions and death were noted. Findings: The ETAR (250 and 500 mg/kg, p.o) exhibited significant (P<0.001) effects against acute seizures induced by maximal electric shock (MES), chemical convulsants such as picrotoxin and strychnine as compared to MEAR (P<0.05) at the same dose compared statistically by ANOVA-Tukey’s comparison test. Conclusion: The data obtained suggest that the plant has anticonvulsant property. The ETAR exhibited prominent scavenging effect in in-vitro DPPH (2,2-diphenyl-1-picryl-hydrazyl) assay and hydroxyl radical scavenging activity as compared to MEAR thus preventing the oxidative free radicals. Flavonoid was isolated from MEAR extract, analyzed by spectral studies and was identified as quercetin. Further investigations are required to isolate other components responsible for anticonvulsant activity.
{"title":"Phytochemical Investigation and Antiepileptic Activity of Asparagus racemosus (Wild) Root Extracts in Rodents","authors":"Rajesh A Shastry, Smita D. Madagundi, Prasanna V Habbu, Basavaraj S. Patil, Shrinivas D. Joshi, V. H. Kulkarni","doi":"10.5530/rjps.2015.3.3","DOIUrl":"https://doi.org/10.5530/rjps.2015.3.3","url":null,"abstract":"Purpose: The purpose of the research was to investigate the anticonvulsant activity of Asparagus racemosus (wild) (AR) by studying the effects on seizures by maximal electric shock, picrotoxin, and strychnine induced convulsive methods in mice. Methodology: The anticonvulsant effect of ethanolic extract of A. racemosus (ETAR) and methanolic extract of A. racemosus (MEAR) were evaluated. In maximal electric shock abolition of the hind leg tonic extensor component seizure were analyzed. In picrotoxin induced convulsion, time of onset of seizures and time of death were recorded; whereas in strychnine induced convulsion time of occurrence of tonic convulsions and death were noted. Findings: The ETAR (250 and 500 mg/kg, p.o) exhibited significant (P<0.001) effects against acute seizures induced by maximal electric shock (MES), chemical convulsants such as picrotoxin and strychnine as compared to MEAR (P<0.05) at the same dose compared statistically by ANOVA-Tukey’s comparison test. Conclusion: The data obtained suggest that the plant has anticonvulsant property. The ETAR exhibited prominent scavenging effect in in-vitro DPPH (2,2-diphenyl-1-picryl-hydrazyl) assay and hydroxyl radical scavenging activity as compared to MEAR thus preventing the oxidative free radicals. Flavonoid was isolated from MEAR extract, analyzed by spectral studies and was identified as quercetin. Further investigations are required to isolate other components responsible for anticonvulsant activity.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"31 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77794315","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, Ashwini, Shailashri, G. Keshavshetti, Shivanand
Objectives: The aim of the present work was to prepare and evaluate fast dissolving tablets of metoclopramide hydrochloride with a view to enhance patient compliance and minimizes the side effects. Methodology: In this study, fast dissolving tablets of metoclopramide were formulated by direct compression method using mucilages of Musa paradisiaca Linn (banana fruit), Cucurbita pepo var. turbinata (cucurbita maxima pulp), Ceratonia siliqua Linn (locust bean seeds) as natural disintegrants and crospovidone as a synthetic superdisintegrant in different ratios with directly compressible mannitol (Pearlitol SD 200) as a diluent to enhance the mouth feel. The prepared formulations were evaluated for hardness, friability, drug content, in vitro dispersion time, wetting time, water absorption ratio, in vitro drug release studies, stability studies and excipients interaction studies. Results: Among all the formulations, the formulation (FBP3) containing 8%w/w mucilage of Musa paradisiaca Linn was the overall best formulation (t 50% 2 min) based on in vitro drug release studies. Stability studies on the formulations indicated that there are no significant changes in drug content and in vitro dispersion time (p<0.05). Conclusion: From the above studies, it can be concluded that fast dissolving tablets of metoclopramide can be prepared using different mucilages as a natural disintegrant for faster dispersion and disintegration in the mouth.
{"title":"Musa paradisiaca Linn Mucilage as a Disintegrant in Design of Fast Dissolving Tablets","authors":"S. Shirsand, Ashwini, Shailashri, G. Keshavshetti, Shivanand","doi":"10.5530/rjps.2015.2.3","DOIUrl":"https://doi.org/10.5530/rjps.2015.2.3","url":null,"abstract":"Objectives: The aim of the present work was to prepare and evaluate fast dissolving tablets of metoclopramide hydrochloride with a view to enhance patient compliance and minimizes the side effects. Methodology: In this study, fast dissolving tablets of metoclopramide were formulated by direct compression method using mucilages of Musa paradisiaca Linn (banana fruit), Cucurbita pepo var. turbinata (cucurbita maxima pulp), Ceratonia siliqua Linn (locust bean seeds) as natural disintegrants and crospovidone as a synthetic superdisintegrant in different ratios with directly compressible mannitol (Pearlitol SD 200) as a diluent to enhance the mouth feel. The prepared formulations were evaluated for hardness, friability, drug content, in vitro dispersion time, wetting time, water absorption ratio, in vitro drug release studies, stability studies and excipients interaction studies. Results: Among all the formulations, the formulation (FBP3) containing 8%w/w mucilage of Musa paradisiaca Linn was the overall best formulation (t 50% 2 min) based on in vitro drug release studies. Stability studies on the formulations indicated that there are no significant changes in drug content and in vitro dispersion time (p<0.05). Conclusion: From the above studies, it can be concluded that fast dissolving tablets of metoclopramide can be prepared using different mucilages as a natural disintegrant for faster dispersion and disintegration in the mouth.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"471 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76358130","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: In the present study, antitubercular activities and in silico physicochemical toxicities and bioactivity profile of some 3-chloro-6-arylpyridazines (3a-d) and 6-aryl-4,5-dihydropyridazine-3(2H)-thiones (4a-d) are studied. Approach: The compounds (3a-d) and (4a-d) were evaluated as antitubercular agents against Mycobacterium tuberculosis H37Rv by screening through in vitro Microplate Alamar Blue Assay (MABA) method. Findings: In silico physicochemical parameter revealed that the entire compounds follow Lipinski’s rule-of-5 to become a “drug like” molecule. ADME (absorption, distribution, metabolism and excretions) profile prediction has shown that all the compounds can be absorbed through human intestine (HIA + ), Caco-2 cell (Caco-2 + ) and can cross blood brain barrier (BBB + ), they all are non-substrate and non-inhibitor of p-glycoprotein. Compounds 4a-d are inhibitor of human microsomal enzyme like CYP 450 1A2, CYP 450 2C19 and CYP 450 3A4. Research limitations/implications: Compounds 4a-4d are better ligand for enzyme inhibition than 3a-d compounds. The MIC of compounds 4a-d and 3a is 6.25 µg/ml. They are potent than compound 3b-d with MIC 12.5 µg/ml. Originality: Toxicity prediction indicated that compounds 3a-3d and 4a-d are non-carcinogenic and non-mutagenic. Bioactivity prediction for compounds 3a-3d and 4a-d indicated better ligand as enzyme inhibitor in comparison to standard.
目的:研究几种3-氯-6-芳基吡嗪类化合物(3 -a -d)和6-芳基-4,5-二氢吡嗪-3(2H)-硫酮(4 -a -d)的抗结核活性、体内理化毒性和生物活性。方法:通过体外微孔板Alamar Blue Assay (MABA)法筛选化合物(3a-d)和(4a-d)，评价化合物(3a-d)对结核分枝杆菌H37Rv的抗结核作用。结果:硅理化参数显示，整个化合物遵循Lipinski的5法则成为“类药物”分子。ADME(吸收、分布、代谢和排泄)谱预测表明，所有化合物均可通过人体肠道(HIA +)、Caco-2细胞(Caco-2 +)吸收，并可穿过血脑屏障(BBB +)，均为p-糖蛋白的非底物和非抑制剂。化合物4a-d是人微粒体酶如CYP 450 1A2、CYP 450 2C19和CYP 450 3A4的抑制剂。研究局限性/启示:化合物4a-4d是比3a-d化合物更好的酶抑制配体。化合物4a-d和3a的MIC为6.25µg/ml。它们比MIC 12.5µg/ml的化合物3b-d更有效。原创性:毒性预测表明化合物3a-3d和4a-d不致癌、不致突变。化合物3a-3d和4a-d的生物活性预测表明，与标准配体相比，配体作为酶抑制剂的效果更好。
{"title":"In silico Physicochemical Bioactivities and Toxicities Prediction of 3-chloro-6-arylpyridazines and 6-aryl- 4,5-dihydropyridazine-3(2H)-thiones having Anti- tubercular Activity","authors":"M. Asif, M. Acharya, Lakshmayya, Anita Singh","doi":"10.5530/rjps.2015.2.7","DOIUrl":"https://doi.org/10.5530/rjps.2015.2.7","url":null,"abstract":"Purpose: In the present study, antitubercular activities and in silico physicochemical toxicities and bioactivity profile of some 3-chloro-6-arylpyridazines (3a-d) and 6-aryl-4,5-dihydropyridazine-3(2H)-thiones (4a-d) are studied. Approach: The compounds (3a-d) and (4a-d) were evaluated as antitubercular agents against Mycobacterium tuberculosis H37Rv by screening through in vitro Microplate Alamar Blue Assay (MABA) method. Findings: In silico physicochemical parameter revealed that the entire compounds follow Lipinski’s rule-of-5 to become a “drug like” molecule. ADME (absorption, distribution, metabolism and excretions) profile prediction has shown that all the compounds can be absorbed through human intestine (HIA + ), Caco-2 cell (Caco-2 + ) and can cross blood brain barrier (BBB + ), they all are non-substrate and non-inhibitor of p-glycoprotein. Compounds 4a-d are inhibitor of human microsomal enzyme like CYP 450 1A2, CYP 450 2C19 and CYP 450 3A4. Research limitations/implications: Compounds 4a-4d are better ligand for enzyme inhibition than 3a-d compounds. The MIC of compounds 4a-d and 3a is 6.25 µg/ml. They are potent than compound 3b-d with MIC 12.5 µg/ml. Originality: Toxicity prediction indicated that compounds 3a-3d and 4a-d are non-carcinogenic and non-mutagenic. Bioactivity prediction for compounds 3a-3d and 4a-d indicated better ligand as enzyme inhibitor in comparison to standard.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"4 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75207159","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}
We provide an overview of the field of bibliometrics, the quantitative analysis of publications, especially as it relates to science and medicine. Bibliometrics involves the analysis of citations, which can aid in measuring the impact of an article on a particular field of study; and of criteria related to assessing a journal’s importance within the field. While bibliometrics has many applications, its use in evaluating researchers has generated the most controversy. We explain and compare many of the standard metrics and the tools for generating them, and provide rankings for key Indian journals. Additionally, we discuss perceptions of metrics by supporters and detractors, some proposed alternatives, and the possible impact of technology and publishing trends on the future of bibliometrics.
{"title":"Bibliometrics: An Overview","authors":"J. M. Berger, Christine M. Baker","doi":"10.5530/RJPS.2014.3.2","DOIUrl":"https://doi.org/10.5530/RJPS.2014.3.2","url":null,"abstract":"We provide an overview of the field of bibliometrics, the quantitative analysis of publications, especially as it relates to science and medicine. Bibliometrics involves the analysis of citations, which can aid in measuring the impact of an article on a particular field of study; and of criteria related to assessing a journal’s importance within the field. While bibliometrics has many applications, its use in evaluating researchers has generated the most controversy. We explain and compare many of the standard metrics and the tools for generating them, and provide rankings for key Indian journals. Additionally, we discuss perceptions of metrics by supporters and detractors, some proposed alternatives, and the possible impact of technology and publishing trends on the future of bibliometrics.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"25 1","pages":"81-92"},"PeriodicalIF":0.0,"publicationDate":"2014-11-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82029749","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}
Anjan De, S. Chakraborty, A. Mukherjee, J. Chattopadhyay
The objective of preparing this article on gastroretentive floating drug delivery systems was to compile the recent literature with special focus on various gastroretentive approaches that have recently become leading methodologies in the field of site-specific orally administered controlled release drug delivery. Gastric emptying is a complex process and makes in vivo performance of the drug delivery systems uncertain. In order to understand various physiological difficulties to achieve gastric retention. In this article we have summarized important factors controlling gastric retention. Gastroretention would also facilitate local drug delivery to the stomach and proximal small intestine. So, gastroretention could help to provide greater availability of new as well as older generation products (5-FU) and consequently improved therapeutic activity with versatile clinical use and thus can provide required benefits to patients. In order to avoid various variability, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 hours. The floating or hydrodynamically controlled drug delivery systems are useful in such application. From the formulation and technological point of view, the floating drug delivery system is comparatively easy and logical approach. The present review addresses briefly about the gastroretentive floating drug delivery systems . It also summarizes methods of evaluation of various floating dosage forms and applications of these systems.
{"title":"Techniques of Gastroretentive Floating Drug Delivery Advancement A Review","authors":"Anjan De, S. Chakraborty, A. Mukherjee, J. Chattopadhyay","doi":"10.5530/RJPS.2014.3.3","DOIUrl":"https://doi.org/10.5530/RJPS.2014.3.3","url":null,"abstract":"The objective of preparing this article on gastroretentive floating drug delivery systems was to compile the recent literature with special focus on various gastroretentive approaches that have recently become leading methodologies in the field of site-specific orally administered controlled release drug delivery. Gastric emptying is a complex process and makes in vivo performance of the drug delivery systems uncertain. In order to understand various physiological difficulties to achieve gastric retention. In this article we have summarized important factors controlling gastric retention. Gastroretention would also facilitate local drug delivery to the stomach and proximal small intestine. So, gastroretention could help to provide greater availability of new as well as older generation products (5-FU) and consequently improved therapeutic activity with versatile clinical use and thus can provide required benefits to patients. In order to avoid various variability, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 hours. The floating or hydrodynamically controlled drug delivery systems are useful in such application. From the formulation and technological point of view, the floating drug delivery system is comparatively easy and logical approach. The present review addresses briefly about the gastroretentive floating drug delivery systems . It also summarizes methods of evaluation of various floating dosage forms and applications of these systems.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"11 1","pages":"93-102"},"PeriodicalIF":0.0,"publicationDate":"2014-11-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80741209","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: The main objective is to study the prescribing pattern of antibiotic in hospital pediatric in-patient. Method: An observational and retrospective study of two month’s duration was undertaken during April-May of 2014. A total number of 144 patients were taken for the study. Results: The mean age of patient on antibiotic was 3.71 ± 3.62. 209 antibiotics were prescribed to the patients and the average number of antibiotics per prescription was 1.45 ± 0.58. Fever (12.5%) and pneumonia (9.7%) were most frequently found diseases in infants, while other diseases constitute 47.9%. Cephalosporin group of antibiotics were most frequently (52%) prescribed antibiotics, followed by aminoglycoside group (17.3%), penicillins (12.5%), macrolides (8.3%) and quinolones (0.69%). Most of the antibiotics were administered parenterally for inpatients. Conclusion: Antibiotic prescribing in children is relatively high in Jazan region of Saudi Arabia. Prescription of broad-spectrum antibiotics though has increased demonstrably which may result in development of bacterial resistance; however development of guidelines for antibiotic prescription and use of appropriate drugs for the disease can result in minimizing the unfavorable use of antibiotics in children.
{"title":"Prescribing Pattern of Antibiotics in Pediatric Patients in the Jazan Region, Kingdom of Saudi Arabia","authors":"M. Alakhali, A. Mohammad","doi":"10.5530/RJPS.2014.3.6","DOIUrl":"https://doi.org/10.5530/RJPS.2014.3.6","url":null,"abstract":"Objective: The main objective is to study the prescribing pattern of antibiotic in hospital pediatric in-patient. Method: An observational and retrospective study of two month’s duration was undertaken during April-May of 2014. A total number of 144 patients were taken for the study. Results: The mean age of patient on antibiotic was 3.71 ± 3.62. 209 antibiotics were prescribed to the patients and the average number of antibiotics per prescription was 1.45 ± 0.58. Fever (12.5%) and pneumonia (9.7%) were most frequently found diseases in infants, while other diseases constitute 47.9%. Cephalosporin group of antibiotics were most frequently (52%) prescribed antibiotics, followed by aminoglycoside group (17.3%), penicillins (12.5%), macrolides (8.3%) and quinolones (0.69%). Most of the antibiotics were administered parenterally for inpatients. Conclusion: Antibiotic prescribing in children is relatively high in Jazan region of Saudi Arabia. Prescription of broad-spectrum antibiotics though has increased demonstrably which may result in development of bacterial resistance; however development of guidelines for antibiotic prescription and use of appropriate drugs for the disease can result in minimizing the unfavorable use of antibiotics in children.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"42 1","pages":"120-124"},"PeriodicalIF":0.0,"publicationDate":"2014-11-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78958232","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":"Pioneering efforts in drug discovery","authors":"Thakur","doi":"10.5530/rjps.2014.3.1","DOIUrl":"https://doi.org/10.5530/rjps.2014.3.1","url":null,"abstract":"","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"155 1","pages":"78-80"},"PeriodicalIF":0.0,"publicationDate":"2014-11-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83314324","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 present research work was to develop and evaluate In situ gels of Sparfloxacin . Method/approach: In situ gels were prepared by using HPMC and carbopol based on the concept of pH trigger gelation systems.Formulations were evaluated for gelling capacity, drug content, clarity, viscosity and In vitro release. Findings: FTIR studies showed that the drug and excipients were compatible. Experimental part showed that viscosity of sols was increased with increase in the concentration of polymers and the solutions showed pseudoplastic behaviour. Sol-to-gel transformation occurred in the presence of simulated tear fluid of pH 7.4. The drug content was found satisfactory. The In vitro release profile of Sparfloxacin from the S3 formulation have shown least drug release (72.34 %) in 8 hrs compared to formulation S2 that is 77.30%, the correlation coefficient ‘r’ indicated that the drug release followed diffusion controlled mechanism from the In situ gels. Sparfloxacin has In vitro activity against a wide range of gram-negative and gram-positive microorganisms.The antimicrobial studies against Streptococcus aureus were showed positive results. The formulations were therapeutically efficacious, sterile and provided sustained release of the drug over a period of time. Application/Value: These results demonstrate that the developed system is an alternative to conventional drug delivery system.
{"title":"Sustained Ocular Delivery of Sparfloxacin from pH Triggered In Situ Gelling System","authors":"K. Reddy, M. Ahmed","doi":"10.5530/RJPS.2014.3.4","DOIUrl":"https://doi.org/10.5530/RJPS.2014.3.4","url":null,"abstract":"Purpose: The present research work was to develop and evaluate In situ gels of Sparfloxacin . Method/approach: In situ gels were prepared by using HPMC and carbopol based on the concept of pH trigger gelation systems.Formulations were evaluated for gelling capacity, drug content, clarity, viscosity and In vitro release. Findings: FTIR studies showed that the drug and excipients were compatible. Experimental part showed that viscosity of sols was increased with increase in the concentration of polymers and the solutions showed pseudoplastic behaviour. Sol-to-gel transformation occurred in the presence of simulated tear fluid of pH 7.4. The drug content was found satisfactory. The In vitro release profile of Sparfloxacin from the S3 formulation have shown least drug release (72.34 %) in 8 hrs compared to formulation S2 that is 77.30%, the correlation coefficient ‘r’ indicated that the drug release followed diffusion controlled mechanism from the In situ gels. Sparfloxacin has In vitro activity against a wide range of gram-negative and gram-positive microorganisms.The antimicrobial studies against Streptococcus aureus were showed positive results. The formulations were therapeutically efficacious, sterile and provided sustained release of the drug over a period of time. Application/Value: These results demonstrate that the developed system is an alternative to conventional drug delivery system.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"10 1","pages":"103-109"},"PeriodicalIF":0.0,"publicationDate":"2014-11-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81066409","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}
Anjan De, S. Chakraborty, A. Mukherjee, J. Chattopadhyay
Purpose: 5-Fluorouracil (5-FU), a pyrimidine antimetabolite attains permeability but is low in solubility. Conventional intravenous administration of 5-FU is known to cause severe systemic toxic effects and thus restricts its versatile use in neoplastic diseases. Therefore, the present study was undertaken to develop stomach site specific 5-Fluorouracil (5-FU) loaded microcapsules in order to evaluate the effect of incorporated mineral oil on physiochemical properties of alginate and pectin microcapsules. Design/methodology: Mineral oil entrapped buoyant beads of 5-FU was prepared by the ionotropic gelation technique. During the preparation of various batches of beads, the ratio of mineral oil to water (v/v), the ratio of drug to polymer (w/w), were kept as variables at two levels; either high or low. Findings: Smooth, spherical beads with nominal weight variation were obtained. All batches of beads floated for 24 hours with a lag time of 41-84 sec. The release of drug followed for 9 h. Higuchi and other order kinetic modeling indicated a diffusion-controlled release of drug from the beads. The study also demonstrated the influence of mineral oil on drug entrapment (64.3 to 80.15%) and in vitro release. Higher level of oil increased drug entrapment efficiency but retarded drug release rate as compared to lower level of oil containing beads. Formulation D was found to be the optimized formulation. Practical implications: It is perceived that a saturation supply can provide a constant pool locally and up to the desired tissue sites such that the therapeutic effects can be attained in cancerous conditions. Social Implications: Oral bioavailability of 5-FU is only 28% and that limits its compliance and oral usage. This strategy for 5-FU delivery is a retentive formulation for a saturation supply of the drug. Value of paper: The optimized formulation showed 99.987% release of 5-FU in 9 h with 82.51% drug entrapment. The results were found statistically significant hence the developed formulation has enhanced therapeutic value and commercial potential.
{"title":"Development and Characterization of Oil Entrapped Stomach Site Specific 5-Fluorouracil Loaded Microcapsules","authors":"Anjan De, S. Chakraborty, A. Mukherjee, J. Chattopadhyay","doi":"10.5530/RJPS.2014.3.5","DOIUrl":"https://doi.org/10.5530/RJPS.2014.3.5","url":null,"abstract":"Purpose: 5-Fluorouracil (5-FU), a pyrimidine antimetabolite attains permeability but is low in solubility. Conventional intravenous administration of 5-FU is known to cause severe systemic toxic effects and thus restricts its versatile use in neoplastic diseases. Therefore, the present study was undertaken to develop stomach site specific 5-Fluorouracil (5-FU) loaded microcapsules in order to evaluate the effect of incorporated mineral oil on physiochemical properties of alginate and pectin microcapsules. Design/methodology: Mineral oil entrapped buoyant beads of 5-FU was prepared by the ionotropic gelation technique. During the preparation of various batches of beads, the ratio of mineral oil to water (v/v), the ratio of drug to polymer (w/w), were kept as variables at two levels; either high or low. Findings: Smooth, spherical beads with nominal weight variation were obtained. All batches of beads floated for 24 hours with a lag time of 41-84 sec. The release of drug followed for 9 h. Higuchi and other order kinetic modeling indicated a diffusion-controlled release of drug from the beads. The study also demonstrated the influence of mineral oil on drug entrapment (64.3 to 80.15%) and in vitro release. Higher level of oil increased drug entrapment efficiency but retarded drug release rate as compared to lower level of oil containing beads. Formulation D was found to be the optimized formulation. Practical implications: It is perceived that a saturation supply can provide a constant pool locally and up to the desired tissue sites such that the therapeutic effects can be attained in cancerous conditions. Social Implications: Oral bioavailability of 5-FU is only 28% and that limits its compliance and oral usage. This strategy for 5-FU delivery is a retentive formulation for a saturation supply of the drug. Value of paper: The optimized formulation showed 99.987% release of 5-FU in 9 h with 82.51% drug entrapment. The results were found statistically significant hence the developed formulation has enhanced therapeutic value and commercial potential.","PeriodicalId":21459,"journal":{"name":"RGUHS Journal of Pharmaceutical Sciences","volume":"25 1","pages":"110-119"},"PeriodicalIF":0.0,"publicationDate":"2014-11-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89869099","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}
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