Pub Date : 2010-10-12DOI: 10.5138/IJDD.2010.0975.0215.02038
Mukesh C. Sharma, D. Kohli, Smita Sharma
A new series of non peptide angiotensin (A-II) receptor antagonist has been prepared. This N-(biphenyl methyl) imidazoles e.g. Some new 4'-{5-amino-2-[2-substituted-phenylamino)-phenyl-methyl]-benzimidazol-1-ylmethyl}-biphenyl-2-carboxylic acid derivatives were synthesized by 2-( α -hydroxy benzyl) benzimidazole was converted to 2-(α-bromo benzyl) benzimidazole by reacting with HBr and Anhydrous ZnCl2 Schiff bases react with biphenyl carboxylic acid with different substituents amino group cyclocondensation with appropriate reagents. Differ from the previously reported and related compounds in that they produce a potent hypertensive effect. The compounds synthesized were identified by 1H NMR, 13C NMR, FAB Mass and FT-IR spectroscopic techniques. All compounds studied in this work were screened for their antihypertensive activity by tail cuff method and direct method measurement of blood pressure. Keywords: Benzimidazoles; Biphenyl Carboxylic acid; Angiotension-II.
{"title":"Synthesis and biological evaluation of some new benzimidazoles derivatives 4'-{5-amino-2-[2-substituted-phenylamino)-phenyl-methyl]-benzimidazol-1 ylmethyl}-biphenyl-2-carboxylic acid: Nonpeptide angiotensin II receptor antagonists","authors":"Mukesh C. Sharma, D. Kohli, Smita Sharma","doi":"10.5138/IJDD.2010.0975.0215.02038","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02038","url":null,"abstract":"A new series of non peptide angiotensin (A-II) receptor antagonist has been prepared. This N-(biphenyl methyl) imidazoles e.g. Some new 4'-{5-amino-2-[2-substituted-phenylamino)-phenyl-methyl]-benzimidazol-1-ylmethyl}-biphenyl-2-carboxylic acid derivatives were synthesized by 2-( α -hydroxy benzyl) benzimidazole was converted to 2-(α-bromo benzyl) benzimidazole by reacting with HBr and Anhydrous ZnCl2 Schiff bases react with biphenyl carboxylic acid with different substituents amino group cyclocondensation with appropriate reagents. Differ from the previously reported and related compounds in that they produce a potent hypertensive effect. The compounds synthesized were identified by 1H NMR, 13C NMR, FAB Mass and FT-IR spectroscopic techniques. All compounds studied in this work were screened for their antihypertensive activity by tail cuff method and direct method measurement of blood pressure. Keywords: Benzimidazoles; Biphenyl Carboxylic acid; Angiotension-II.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72774374","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}
Pub Date : 2010-10-12DOI: 10.5138/IJDD.2010.0975.0215.02030
GS Sharma, M. Srikanth, MU Uhumwangho, KS PhaniKumar, Ramana Murthy
The purpose of writing this review on pulsatile drug delivery systems (PDDS) is to compile the recent literatures with special focus on the different types and approaches involved in the development of the formulation. PDDS are gaining importance in the field of pharmaceutical technology as these systems deliver the right dose at specific time at a specific site. Some of the disease conditions wherein PDDS are promising include duodenal ulcer, cardiovascular diseases, arthritis, asthma, diabetes, neurological disorder, cancer, hypertension and hypercholesterolemia. PDDS can be classified into time controlled systems wherein the drug release is controlled primarily by the delivery system, stimuli induced PDDS in which release is controlled by the stimuli, such as the pH or enzymes present in the intestinal tract or enzymes present in the drug delivery system and externally regulated system where release is programmed by external stimuli like magnetism, ultrasound, electrical effect and irradiation. This review also summarizes some current PDDS already available in the market. These systems are useful to several problems encountered during the development of a pharmaceutical dosage form. Keywords: Pulsatile drug delivery systems; Circadian rhythm; Single unit, Multiple units, Pulsatile release pulsincap
{"title":"Recent trends in pulsatile drug delivery systems - A review","authors":"GS Sharma, M. Srikanth, MU Uhumwangho, KS PhaniKumar, Ramana Murthy","doi":"10.5138/IJDD.2010.0975.0215.02030","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02030","url":null,"abstract":"The purpose of writing this review on pulsatile drug delivery systems (PDDS) is to compile the recent literatures with special focus on the different types and approaches involved in the development of the formulation. PDDS are gaining importance in the field of pharmaceutical technology as these systems deliver the right dose at specific time at a specific site. Some of the disease conditions wherein PDDS are promising include duodenal ulcer, cardiovascular diseases, arthritis, asthma, diabetes, neurological disorder, cancer, hypertension and hypercholesterolemia. PDDS can be classified into time controlled systems wherein the drug release is controlled primarily by the delivery system, stimuli induced PDDS in which release is controlled by the stimuli, such as the pH or enzymes present in the intestinal tract or enzymes present in the drug delivery system and externally regulated system where release is programmed by external stimuli like magnetism, ultrasound, electrical effect and irradiation. This review also summarizes some current PDDS already available in the market. These systems are useful to several problems encountered during the development of a pharmaceutical dosage form. Keywords: Pulsatile drug delivery systems; Circadian rhythm; Single unit, Multiple units, Pulsatile release pulsincap","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79838663","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}
Pub Date : 2010-10-12DOI: 10.5138/IJDD.2010.0975.0215.02037
G. N. Kumar, S. Lakshmy, K. Srikumar
Homobrassinolide is a plant hormone implicated in plant growth and development. Its effect on animal metabolism was less known to date. We have investigated its effect on the marker enzymes such as alkaline phosphatase and creatine kinase in selected rat tissues-brain, heart, liver, kidney, skeletal muscle and testis. Homobrassinolide was administered (66 and 330ng/ Kg body weight) intradermally in male albino wistar strain rats and changes in alkaline phosphatase and creatine kinase activities were measured. An overall reduction in both the enzyme activities occurred within 2hr of administration with few exceptions. The reaction rate constants for the enzyme activities were in the order 10-7 mM/min for alkaline phosphatase and 10-3 mM/min for creatine kinase. Time course studies indicated a decrease in enzyme activities as a function of time. Elevated hemoglobin content correlated with rise in erythrocyte number. Blood glucose level decreased by a percentage of 15.7 and 21.7 compared to control with the administration of 10μg and 50μg homobrassinolide respectively. Serum cholesterol content showed 15% decrease and 25% increase compared to control following 10μg and 50μg homobrassinolide administration. We conclude that homobrassinolide inhibited both the enzymes in the tissues and produced erythrocytosis, leukocytosis and hypoglycemia, while cellular phosphorylation status remained principally affected by this oxysterol in rat. Even though the physiological and pathological significance of these observations is not clear, it is suggested that 28-HB enriched diets may not be appropriate for higher energy related work activities. Keywords: Alkaline phosphatase; Creatine kinase; Homobrassinolide; Oxysterol; Phosphorylation; Rate constant.
{"title":"Negative modulation of alkaline phosphatase and creatine kinase by homobrassinolide","authors":"G. N. Kumar, S. Lakshmy, K. Srikumar","doi":"10.5138/IJDD.2010.0975.0215.02037","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02037","url":null,"abstract":"Homobrassinolide is a plant hormone implicated in plant growth and development. Its effect on animal metabolism was less known to date. We have investigated its effect on the marker enzymes such as alkaline phosphatase and creatine kinase in selected rat tissues-brain, heart, liver, kidney, skeletal muscle and testis. Homobrassinolide was administered (66 and 330ng/ Kg body weight) intradermally in male albino wistar strain rats and changes in alkaline phosphatase and creatine kinase activities were measured. An overall reduction in both the enzyme activities occurred within 2hr of administration with few exceptions. The reaction rate constants for the enzyme activities were in the order 10-7 mM/min for alkaline phosphatase and 10-3 mM/min for creatine kinase. Time course studies indicated a decrease in enzyme activities as a function of time. Elevated hemoglobin content correlated with rise in erythrocyte number. Blood glucose level decreased by a percentage of 15.7 and 21.7 compared to control with the administration of 10μg and 50μg homobrassinolide respectively. Serum cholesterol content showed 15% decrease and 25% increase compared to control following 10μg and 50μg homobrassinolide administration. We conclude that homobrassinolide inhibited both the enzymes in the tissues and produced erythrocytosis, leukocytosis and hypoglycemia, while cellular phosphorylation status remained principally affected by this oxysterol in rat. Even though the physiological and pathological significance of these observations is not clear, it is suggested that 28-HB enriched diets may not be appropriate for higher energy related work activities. Keywords: Alkaline phosphatase; Creatine kinase; Homobrassinolide; Oxysterol; Phosphorylation; Rate constant.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75884443","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}
Pub Date : 2010-10-12DOI: 10.5138/IJDD.2010.0975.0215.02029
V. Mathur, Yamini Satrawala, M. Rajput, Piyush Kumar, P. Shrivastava, Akhilesh Vishvkarma
The use of solid lipid nanoparticles in medicine and more specifically drug delivery is set to spread rapidly. Currently many substances are under investigation for drug delivery and more specifically for cancer therapy technology is the latest trend in the cancer therapy. It helps the pharmacist to formulate the product with maximum therapeutic value and minimum or negligible range side effects. Cancer is a class of disorders characterized by abnormal growth of cells that proliferate in an uncontrolled way and a major disadvantage of anticancer drugs is their lack of selectivity for tumor tissue, which causes severe side effects and results in low cure rates. Thus, it is very hard to target the abnormal cells by the conventional method of the drug delivery system. In harmony with these approaches, this review’s basic approach is that the defining features of solid lipid nanoparticles are embedded in their breakthrough potential for patient care. This review article describes the possible way to exploit solid lipid nanoparticle technology to targeted drug therapy in cancer. We looked at the usefulness of solid lipid nanoparticles as a tool for cancer therapy. Keywords: Cancer therapy; Solid lipid nanoparticles; Quantum dots.
{"title":"Solid lipid nanoparticles in cancer therapy","authors":"V. Mathur, Yamini Satrawala, M. Rajput, Piyush Kumar, P. Shrivastava, Akhilesh Vishvkarma","doi":"10.5138/IJDD.2010.0975.0215.02029","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02029","url":null,"abstract":"The use of solid lipid nanoparticles in medicine and more specifically drug delivery is set to spread rapidly. Currently many substances are under investigation for drug delivery and more specifically for cancer therapy technology is the latest trend in the cancer therapy. It helps the pharmacist to formulate the product with maximum therapeutic value and minimum or negligible range side effects. Cancer is a class of disorders characterized by abnormal growth of cells that proliferate in an uncontrolled way and a major disadvantage of anticancer drugs is their lack of selectivity for tumor tissue, which causes severe side effects and results in low cure rates. Thus, it is very hard to target the abnormal cells by the conventional method of the drug delivery system. In harmony with these approaches, this review’s basic approach is that the defining features of solid lipid nanoparticles are embedded in their breakthrough potential for patient care. This review article describes the possible way to exploit solid lipid nanoparticle technology to targeted drug therapy in cancer. We looked at the usefulness of solid lipid nanoparticles as a tool for cancer therapy. Keywords: Cancer therapy; Solid lipid nanoparticles; Quantum dots.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77910497","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}
Pub Date : 2010-10-12DOI: 10.5138/IJDD.2010.0975.0215.02036
M. Rathore, V. Gupta
In last few years transporter targeted drug delivery has drawn attention of research to identify and explore various nutrient transport systems including amino acid transporters for better drug delivery. The aim of present research work is to investigate the transport characteristics of L-tryptophan (L-try) across goat cornea. Transport of L-try was investigated using a glass diffusion cell for effect of concentration, pH, presence of other amino acids or metabolic inhibitor or dipeptide and tripeptide. The amount of L-try transported increased as the pH of L-try aqueous solution increased from 5 to 9. Inhibition was observed in L-try transport in absence of sodium ions where L-try solution was made isotonic with dextrose. Amino acids like L-histidine, L-arginine, L-lysine (cationic), L-glutamic acid, L-aspartic acid (anionic), glycine and L-proline (neutral) inhibited the L-try transport as compared to control (L-try alone). In presence of sodium azide and Ouabain the inhibition in L-try transport across goat cornea was observed while no marked inhibition was observed on L-try transport across goat cornea in presence of aspartame and glutathione. The L-try transport was favored up to concentration 1% w/v and at higher pH in presence of sodium ions through excised goat cornea. Functional presence of a sodium dependent L-try transport system as inhibited by ouabain having affinity to cationic and neutral amino acid is evident on goat cornea. Keywords: Cornea; Amino acid; Tryptophan; Transport
{"title":"Functional characterization of L-tryptophan transport across mammalian cornea","authors":"M. Rathore, V. Gupta","doi":"10.5138/IJDD.2010.0975.0215.02036","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02036","url":null,"abstract":"In last few years transporter targeted drug delivery has drawn attention of research to identify and explore various nutrient transport systems including amino acid transporters for better drug delivery. The aim of present research work is to investigate the transport characteristics of L-tryptophan (L-try) across goat cornea. Transport of L-try was investigated using a glass diffusion cell for effect of concentration, pH, presence of other amino acids or metabolic inhibitor or dipeptide and tripeptide. The amount of L-try transported increased as the pH of L-try aqueous solution increased from 5 to 9. Inhibition was observed in L-try transport in absence of sodium ions where L-try solution was made isotonic with dextrose. Amino acids like L-histidine, L-arginine, L-lysine (cationic), L-glutamic acid, L-aspartic acid (anionic), glycine and L-proline (neutral) inhibited the L-try transport as compared to control (L-try alone). In presence of sodium azide and Ouabain the inhibition in L-try transport across goat cornea was observed while no marked inhibition was observed on L-try transport across goat cornea in presence of aspartame and glutathione. The L-try transport was favored up to concentration 1% w/v and at higher pH in presence of sodium ions through excised goat cornea. Functional presence of a sodium dependent L-try transport system as inhibited by ouabain having affinity to cationic and neutral amino acid is evident on goat cornea. Keywords: Cornea; Amino acid; Tryptophan; Transport","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80267641","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}
Pub Date : 2010-10-12DOI: 10.5138/IJDD.2010.0975.0215.02034
V. Parashar, D. Ahmad, S. Gupta, N. Upmanyu, Neha Parashar, V. Mudgal
The aim of present study is to develop biodegradable microspheres of Tinidazole. Bovine Serum Albumin was used for the preparation of microspheres. They were made in four batches. The emulsion cross-linking method was used for the preparation. The quantity of BSA varies for each formulation. Formulations were evaluated for particle size, Melting point, TLC, entrapment efficiency and in vitro release studies. Depending upon the drug to polymer ratio, the entrapment, loading were found to range between 48, 55, 75 and 78 (in %) respectively. Particle size of prepared microspheres was measured using a compound microscope. The surface topography and internal textures of the microspheres was observed by scanning electron microscopy. The microspheres were spherical, discrete and compact and size distribution was between 33.28 to 36.25 μm. In vitro studies were carried out at different pH for a period of 18 h and compared with marketed formulation. From all the batches it is concluded that when concentration of polymer increases microspheres shows more controlled and prolonged release. The drug release was between 66, 51, 48, 42 (in %). The drug release from 1:4 is most prolonged and constant. Both the IR spectra of drug and formulation were almost same. Combination multitone recorded due to N=O stretching and S=O in the IR region of 1500-1250 cm−1. Keywords: Biodegradable microspheres, BSA, Tinidazole, In vitro release.IntroductionMicrospheres
本研究的目的是研制可生物降解的替硝唑微球。用牛血清白蛋白制备微球。它们分四批生产。采用乳液交联法制备。每种配方的BSA含量不同。评价了制剂的粒径、熔点、薄层色谱、包封效率和体外释放研究。根据药物与聚合物的比例，包封和负载的范围分别为48%、55%、75%和78% (in %)。用复合显微镜测量制备的微球的粒径。用扫描电镜观察了微球的表面形貌和内部织构。微球呈球状、离散、致密，粒径分布在33.28 ~ 36.25 μm之间。在不同的pH下进行了18小时的体外研究，并与市售配方进行了比较。结果表明，随着聚合物浓度的增加，微球的释放具有更强的可控性和缓释性。释药量分别为66、51、48、42 (in %)。1:4的药物释放时间最长且最稳定。药物和制剂的红外光谱基本一致。在1500 ~ 1250 cm−1的红外区域，由于N=O拉伸和S=O记录了组合多音。关键词:可生物降解微球，牛血清白蛋白，替硝唑，体外释放IntroductionMicrospheres
{"title":"Formulation and evaluation of biodegradable microspheres of tinidazole","authors":"V. Parashar, D. Ahmad, S. Gupta, N. Upmanyu, Neha Parashar, V. Mudgal","doi":"10.5138/IJDD.2010.0975.0215.02034","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02034","url":null,"abstract":"The aim of present study is to develop biodegradable microspheres of Tinidazole. Bovine Serum Albumin was used for the preparation of microspheres. They were made in four batches. The emulsion cross-linking method was used for the preparation. The quantity of BSA varies for each formulation. Formulations were evaluated for particle size, Melting point, TLC, entrapment efficiency and in vitro release studies. Depending upon the drug to polymer ratio, the entrapment, loading were found to range between 48, 55, 75 and 78 (in %) respectively. Particle size of prepared microspheres was measured using a compound microscope. The surface topography and internal textures of the microspheres was observed by scanning electron microscopy. The microspheres were spherical, discrete and compact and size distribution was between 33.28 to 36.25 μm. In vitro studies were carried out at different pH for a period of 18 h and compared with marketed formulation. From all the batches it is concluded that when concentration of polymer increases microspheres shows more controlled and prolonged release. The drug release was between 66, 51, 48, 42 (in %). The drug release from 1:4 is most prolonged and constant. Both the IR spectra of drug and formulation were almost same. Combination multitone recorded due to N=O stretching and S=O in the IR region of 1500-1250 cm−1. Keywords: Biodegradable microspheres, BSA, Tinidazole, In vitro release.IntroductionMicrospheres","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86134370","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}
Pub Date : 2010-10-12DOI: 10.5138/IJDD.2010.0975.0215.02031
V. Shah, Meha Sharma, Vijaykumar K. Parmar, U. Upadhyay
The aim of the present study was to prepare gellan gum microspheres of Sildenafil citrate, for intranasal delivery to avoid the first pass metabolism. The microspheres were prepared using spray drying method. The microspheres were evaluated for characteristics like particle size, incorporation efficiency, swelling ability, zeta potential, in-vitro mucoadhesion, ex-vivo mucoadhesion, thermal analysis, XRD study and in-vitro drug release. Treatment of in-vitro data to different kinetic equations indicated diffusion controlled drug delivery from gellan gum microspheres. The results of DSC and XRD studies revealed the molecular amorphous dispersion of Sildenafil citrate into the gellan gum microspheres. Microspheres so prepared were discrete, bulky, free flowing and showed an average encapsulation efficiency ranging from 95-98%. The formulation exhibited a good mucoadhesive strength which was determined in in vitro conditions through falling film technique and was compared with ex vivo studies. The microspheres so prepared also exhibited a good swelling index which confirmed the strong mucoadhesive property of the formulation. Keywords: Gellan gum, Microsperes, Spray drying, Sildinafil citrate, Nasal delivery.
{"title":"Formulation of sildenafil citrate loaded nasal microsphers: An in vitro, ex vivo characterization","authors":"V. Shah, Meha Sharma, Vijaykumar K. Parmar, U. Upadhyay","doi":"10.5138/IJDD.2010.0975.0215.02031","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02031","url":null,"abstract":"The aim of the present study was to prepare gellan gum microspheres of Sildenafil citrate, for intranasal delivery to avoid the first pass metabolism. The microspheres were prepared using spray drying method. The microspheres were evaluated for characteristics like particle size, incorporation efficiency, swelling ability, zeta potential, in-vitro mucoadhesion, ex-vivo mucoadhesion, thermal analysis, XRD study and in-vitro drug release. Treatment of in-vitro data to different kinetic equations indicated diffusion controlled drug delivery from gellan gum microspheres. The results of DSC and XRD studies revealed the molecular amorphous dispersion of Sildenafil citrate into the gellan gum microspheres. Microspheres so prepared were discrete, bulky, free flowing and showed an average encapsulation efficiency ranging from 95-98%. The formulation exhibited a good mucoadhesive strength which was determined in in vitro conditions through falling film technique and was compared with ex vivo studies. The microspheres so prepared also exhibited a good swelling index which confirmed the strong mucoadhesive property of the formulation. Keywords: Gellan gum, Microsperes, Spray drying, Sildinafil citrate, Nasal delivery.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74259435","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}
Pub Date : 2010-10-12DOI: 10.5138/IJDD.2010.0975.0215.02033
Mukesh C. Sharma, D. Kohli, Smita Sharma
In this study we have synthesized some Benzimidazole derivatives (2-{6-Chloro-5-nitro-1-[2-(1H-tetrazol-5-yl) biphenyl-4-ylmethyl] 1H-benzoimidazol-2-yl}-phenyl)-(Substituted-benzylidene)-amine and screened for their antihypertensive activity. 4-chloro-o-Phenylenediamine was condensed with anthranilic acid in presence of Polyphosphoric acid and different aryl aldehydes compounds with biphenyl tetrazole ring. The presence of specific functional group were analysed by IR spectroscopy, The determination of structure for the synthesized compounds by NMR and Mass spectroscopy 13C NMR, 1H NMR, FAB Mass. All the synthesized compounds showed significant antihypertensive activity. Keywords: Benzimidazole; Antihypertensive; 4-chloro-o-Phenylenediamine; Biphenyl tetrazole; Blood pressure.
{"title":"Benzimidazoles derivatives with (2-{6-Chloro-5-nitro-1-[2-(1H-tetrazol-5-yl) biphenyl-4-ylmethyl] 1H-benzoimidazol-2-yl}-phenyl)-(substituted-benzylidene)-amine with potential angiotensin II receptor antagonists as antihypertensive activity","authors":"Mukesh C. Sharma, D. Kohli, Smita Sharma","doi":"10.5138/IJDD.2010.0975.0215.02033","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02033","url":null,"abstract":"In this study we have synthesized some Benzimidazole derivatives (2-{6-Chloro-5-nitro-1-[2-(1H-tetrazol-5-yl) biphenyl-4-ylmethyl] 1H-benzoimidazol-2-yl}-phenyl)-(Substituted-benzylidene)-amine and screened for their antihypertensive activity. 4-chloro-o-Phenylenediamine was condensed with anthranilic acid in presence of Polyphosphoric acid and different aryl aldehydes compounds with biphenyl tetrazole ring. The presence of specific functional group were analysed by IR spectroscopy, The determination of structure for the synthesized compounds by NMR and Mass spectroscopy 13C NMR, 1H NMR, FAB Mass. All the synthesized compounds showed significant antihypertensive activity. Keywords: Benzimidazole; Antihypertensive; 4-chloro-o-Phenylenediamine; Biphenyl tetrazole; Blood pressure.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90723092","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}
Pub Date : 2010-10-12DOI: 10.5138/IJDD.2010.0975.0215.02032
R. Das, Subhabrata Dutta Gupta, T. Pal
As the Vancomycin is itself a nephrotoxic antibiotics, so it is sometime recommended to the Slow-low Efficiency Dialysis (SLED) patients against highly resisted infection. In this case, the dose monitoring is strictly maintained after Intravenous injection. The collected blood was analyzed for its concentration in HPLC for 11 patients and the half life was evaluated to study Therapeutic drug monitoring. The T1/2 of evaluated vancomycin is 39.12+ 6.81 hrs. The mean of the systemic clearance is 16.91+6.99 and mean Vd is 0.57+ 0.147. Comparatively the reported study of Mean + SD of half-life, volume of distribution, and systemic clearance were 43.1 + 21.6 hours, 0.84 L/kg + 0.17 L/kg, and 24.3 mL/min + 8.39 mL/min respectively. Thus the t-test of the means was 0.5828, degree of freedom (df) was 20, standard error of difference was 6.829 and so, the two-tailed P value is 0.5665 i.e. P > 0.5. In ethnic Indian SLED patients, T1/2 of mean + SD of 39.12 + 6.81 hrs was compared to the Caucasian patients i.e, 43.1 + 21.6 hrs. And the t-test and P-value is 0.5828 & 0.5665 respectively. Thus it was concluded that the half-life of ethnic Indian patients is less in compare to Caucasians but this difference is not so significant. The half-life of ethnic 8 patients is less than 40 out of 11 patients. Keywords: Vancomycin assay; Slow-low efficiency dialysis; Pharmacokinetic analysis; Ethnic indians
{"title":"Prospective observational study of vancomycin injection in SLED patient of ethnic Indians","authors":"R. Das, Subhabrata Dutta Gupta, T. Pal","doi":"10.5138/IJDD.2010.0975.0215.02032","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02032","url":null,"abstract":"As the Vancomycin is itself a nephrotoxic antibiotics, so it is sometime recommended to the Slow-low Efficiency Dialysis (SLED) patients against highly resisted infection. In this case, the dose monitoring is strictly maintained after Intravenous injection. The collected blood was analyzed for its concentration in HPLC for 11 patients and the half life was evaluated to study Therapeutic drug monitoring. The T1/2 of evaluated vancomycin is 39.12+ 6.81 hrs. The mean of the systemic clearance is 16.91+6.99 and mean Vd is 0.57+ 0.147. Comparatively the reported study of Mean + SD of half-life, volume of distribution, and systemic clearance were 43.1 + 21.6 hours, 0.84 L/kg + 0.17 L/kg, and 24.3 mL/min + 8.39 mL/min respectively. Thus the t-test of the means was 0.5828, degree of freedom (df) was 20, standard error of difference was 6.829 and so, the two-tailed P value is 0.5665 i.e. P > 0.5. In ethnic Indian SLED patients, T1/2 of mean + SD of 39.12 + 6.81 hrs was compared to the Caucasian patients i.e, 43.1 + 21.6 hrs. And the t-test and P-value is 0.5828 & 0.5665 respectively. Thus it was concluded that the half-life of ethnic Indian patients is less in compare to Caucasians but this difference is not so significant. The half-life of ethnic 8 patients is less than 40 out of 11 patients. Keywords: Vancomycin assay; Slow-low efficiency dialysis; Pharmacokinetic analysis; Ethnic indians","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85344374","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}
Pub Date : 2010-10-12DOI: 10.5138/IJDD.2010.0975.0215.02035
Vikash Kumar, A. Tiwary, G. Kaur
The present study was designed to formulate colon release tablets of fluticasone by employing cross linked chitosan (CH) and carboxymethyl guar gum (CMG) interpolymer complexes (IPC). Matrix tablets were prepared by wet granulation method using IPC as binder and coating agent. The IPC were characterized by Fourier transform infrared spectroscopy (FTIR). The uncoated and coated tablets were tested for their suitability as colon specific drug delivery system by in vitro dissolution studies. The coated tablets were evaluated for their pharmacodynamic performance after oral administration to TNBS induced ulcerative colitic rats. FTIR studies demonstrated that the IPC was formed through an electrostatic interaction between –COO− groups of CMG and –NH3+ groups of CH. Tablets formulated with 50:50 CH:CMG as binder and coated with the respective ratio of IPC was capable of protecting the drug release in stomach and small intestine and delivering the drug in the colon. Histopathology of the rat colon after oral administration of these IPC film coated tablets revealed significantly greater (p<0.05) reduction in TNBS-induced ulcerative colitis The study confirmed that selective delivery of fluticasone to the colon can be achieved using cross-linked CH and CMG polysaccharides. Keywords: Chitosan; Colonic delivery; Carboxymethyl guar gum; Cross-linking; Guar gum; Fluticasone
{"title":"Investigations on chitosan-carboxymethyl guar gum complexes interpolymer complexes for colon delivery of fluticasone","authors":"Vikash Kumar, A. Tiwary, G. Kaur","doi":"10.5138/IJDD.2010.0975.0215.02035","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02035","url":null,"abstract":"The present study was designed to formulate colon release tablets of fluticasone by employing cross linked chitosan (CH) and carboxymethyl guar gum (CMG) interpolymer complexes (IPC). Matrix tablets were prepared by wet granulation method using IPC as binder and coating agent. The IPC were characterized by Fourier transform infrared spectroscopy (FTIR). The uncoated and coated tablets were tested for their suitability as colon specific drug delivery system by in vitro dissolution studies. The coated tablets were evaluated for their pharmacodynamic performance after oral administration to TNBS induced ulcerative colitic rats. FTIR studies demonstrated that the IPC was formed through an electrostatic interaction between –COO− groups of CMG and –NH3+ groups of CH. Tablets formulated with 50:50 CH:CMG as binder and coated with the respective ratio of IPC was capable of protecting the drug release in stomach and small intestine and delivering the drug in the colon. Histopathology of the rat colon after oral administration of these IPC film coated tablets revealed significantly greater (p<0.05) reduction in TNBS-induced ulcerative colitis The study confirmed that selective delivery of fluticasone to the colon can be achieved using cross-linked CH and CMG polysaccharides. Keywords: Chitosan; Colonic delivery; Carboxymethyl guar gum; Cross-linking; Guar gum; Fluticasone","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78313632","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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