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首页> 外文期刊>Drug delivery. >Modulating drug release profiles by lipid semi solid matrix formulations for BCS class II drug - an in vitro and an in vivo study
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Modulating drug release profiles by lipid semi solid matrix formulations for BCS class II drug - an in vitro and an in vivo study

机译：BCS II类药物通过脂质半固体基质制剂调节药物释放曲线-体内和体外研究

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摘要

The main objective of the study was to alter the dissolution profile of a practically insoluble Biopharmaceutics Classification System class II drug, aceclofenac, by formulating into lipid semisolid matrix (SSM) formulations using liquid filling technology in hard gelatin capsules, for both immediate and sustained release. SSM formulations of aceclofenac were prepared by melt fusion technique, using Gelucires (44/14, 50/13, 33/01 and 43/01), polyethylene glycols (4000 and 6000) and Poloxamer 188 at different levels. Role of additives like docusate sodium, Tween 80, Aerosil 200 and polyvinylpyrrolidone K-30 in enhancement of drug release was investigated. The optimized immediate and sustained SSM capsules were characterized in terms of assay, in vitro drug release, moisture uptake and differential scanning calorimetry. More than 80% of the drug was released within 15 min in various dissolution media studied, from Gelucire 44/14-based immediate release formulations. Incorporation of docusate sodium and Tween 80 provided further enhancement in drug dissolution when compared to plain drug and marketed tablet. SSM formulations based on Gelucire blends of 50/13 and 43/01 and 44/14 and 43/01 sustained the release of the drug for a period of 24 h following zero-order kinetics. The in vivo study of the optimized immediate release and sustained release formulations revealed significant enhancement in anti inflammatory activity (p<0.01) in rats. From these findings, liquid fill technique in hard gelatin capsules using Gelucire and their blends might be an efficacious approach for designing immediate or sustained drug release profiles for poorly soluble drugs like aceclofenac.
机译：该研究的主要目的是通过在硬明胶胶囊中使用液体填充技术将脂质半固体基质（SSM）制剂配制成硬明胶胶囊，从而改变几乎不溶的生物药物分类系统II类药物醋氯芬酸的溶出度。 。醋氯芬酸的SSM制剂通过熔融融合技术制备，使用不同含量的Gelucires（44 / 14、50 / 13、33 / 01和43/01），聚乙二醇（4000和6000）和泊洛沙姆188。研究了多库酯钠，吐温80，Aerosil 200和聚乙烯吡咯烷酮K-30等添加剂在增强药物释放中的作用。根据测定，体外药物释放，水分吸收和差示扫描量热法对优化的即食和持续SSM胶囊进行了表征。超过80％的药物在15分钟内从基于Gelucire 44/14的速释制剂中在各种溶出介质中释放出来。与普通药物和市售片剂相比，多库酯钠和吐温80的结合进一步提高了药物的溶出度。基于50/13和43/01以及44/14和43/01的Gelucire共混物的SSM制剂在零级动力学后的24小时内持续释放药物。优化的立即释放和持续释放制剂的体内研究表明，大鼠抗炎活性显着增强（p <0.01）。从这些发现中，使用Gelucire及其掺合物在硬明胶胶囊中进行液体填充技术可能是一种有效的方法，用于为难溶性药物（如醋氯芬酸）设计即时或持续的药物释放曲线。

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