Simvastatin, a BCS class II drug, is associated with poor aqueous solubility, first-pass metabolism and short half-life. In the present work, nanoparticles were prepared and evaluated. Optimization of formulation and ...Simvastatin, a BCS class II drug, is associated with poor aqueous solubility, first-pass metabolism and short half-life. In the present work, nanoparticles were prepared and evaluated. Optimization of formulation and process parameters was done through the use of independent and dependent variables. Preliminary studies were done to determine suitable range of the concentration of Eudragit polymer (10%–30%) and the ratio of drug to polymer (1:1 to 1:5) for the formation of nanoparticles by emulsification and a solvent evaporation technique. Results revealed that the mean size of nanoparticles was affected by stirring speed from 5000 RPM, 8000 RPM, and 12000 RPM. The results of increase in association efficiency and percent yield with increase in amount of drug from 100 mg, 150 mg, and 200 mg in selected range were observed. In-vitro release studies showed that two formulations possess highest initial burst and slow sustained drug release. There was 2.93-fold decrease in total cholesterol and 3.27-fold increases in triglyceride level during in-vivo study.展开更多
Tizanidine hydrochloride(THCl)is an antispasmodic agent which undergoes extensive first pass metabolism making it a possible candidate for buccal delivery.The aim of this study was to prepare a monolayered buccal patc...Tizanidine hydrochloride(THCl)is an antispasmodic agent which undergoes extensive first pass metabolism making it a possible candidate for buccal delivery.The aim of this study was to prepare a monolayered buccal patch containing THCl using the emulsification solvent evaporation method.Fourteen formulations were prepared using the polymers Eudragit■ RS 100 or EudragitB RL 100 and chitosan.Polymer solutions in acetone were combined with a THCl aqueous solution(in some cases containing chitosan)by homogenization at 9000 rpm for 2 min in the presence of triethyl citrate as plasticizer and cast in novel Teflon molds.Physicochemical properties such as film thickness,in vitro drug release and in vitro mucoadhesion were evaluated after which permeation across sheep buccal mucosa was examined in terms of flux and lag time.Formulations prepared using a Eudragit■polymer alone exhibited sa tisfactory physicomechanical properties but lacked a gradual in vitro drug release pattern.Incorporation of chitosan into formulations resulted in the formation of a porous structure which did exhibit gradual release of drug.In conclusion,THCl can be delivered by a buccal patch formulated as a blend of Eudragit■ and chitosan,the latter being necessary to achieve gradual drug release.展开更多
基金the Department of Science and Technology(DST-FIST)Letter no-SR/FST/COLLEGE/2018/418New Delhi for providing financial assistance.The authors AV acknowledge the Department of Science and Technology,New Delhi,India(DST/INSPIRE Fellowship/2019/IF190329 and DST/NM/NT/2018/20)for providing financial assistance for the successful completion of this work.
文摘Simvastatin, a BCS class II drug, is associated with poor aqueous solubility, first-pass metabolism and short half-life. In the present work, nanoparticles were prepared and evaluated. Optimization of formulation and process parameters was done through the use of independent and dependent variables. Preliminary studies were done to determine suitable range of the concentration of Eudragit polymer (10%–30%) and the ratio of drug to polymer (1:1 to 1:5) for the formation of nanoparticles by emulsification and a solvent evaporation technique. Results revealed that the mean size of nanoparticles was affected by stirring speed from 5000 RPM, 8000 RPM, and 12000 RPM. The results of increase in association efficiency and percent yield with increase in amount of drug from 100 mg, 150 mg, and 200 mg in selected range were observed. In-vitro release studies showed that two formulations possess highest initial burst and slow sustained drug release. There was 2.93-fold decrease in total cholesterol and 3.27-fold increases in triglyceride level during in-vivo study.
文摘Tizanidine hydrochloride(THCl)is an antispasmodic agent which undergoes extensive first pass metabolism making it a possible candidate for buccal delivery.The aim of this study was to prepare a monolayered buccal patch containing THCl using the emulsification solvent evaporation method.Fourteen formulations were prepared using the polymers Eudragit■ RS 100 or EudragitB RL 100 and chitosan.Polymer solutions in acetone were combined with a THCl aqueous solution(in some cases containing chitosan)by homogenization at 9000 rpm for 2 min in the presence of triethyl citrate as plasticizer and cast in novel Teflon molds.Physicochemical properties such as film thickness,in vitro drug release and in vitro mucoadhesion were evaluated after which permeation across sheep buccal mucosa was examined in terms of flux and lag time.Formulations prepared using a Eudragit■polymer alone exhibited sa tisfactory physicomechanical properties but lacked a gradual in vitro drug release pattern.Incorporation of chitosan into formulations resulted in the formation of a porous structure which did exhibit gradual release of drug.In conclusion,THCl can be delivered by a buccal patch formulated as a blend of Eudragit■ and chitosan,the latter being necessary to achieve gradual drug release.
