Dalvadi Hitesh, Patel Nikita, Parmar Komal
a Department of Pharmaceutics , ROFEL, Shri G M Bilakhia College of Pharmacy , Gujarat , India.
J Microencapsul. 2017 May;34(3):308-318. doi: 10.1080/02652048.2017.1324920. Epub 2017 May 17.
The aim of present investigation is to improve dissolution rate of poor soluble drug Zotepine by a self-microemulsifying drug delivery system (SMEDDS). Ternary phase diagram with oil (Oleic acid), surfactant (Tween 80) and co-surfactant (PEG 400) at apex were used to identify the efficient self-microemulsifying region. Box-Behnken design was implemented to study the influence of independent variables. Principal Component Analysis was used for scrutinising critical variables. The liquid SMEDDS were characterised for macroscopic evaluation, % Transmission, emulsification time and in vitro drug release studies. Optimised formulation OL1 was converted in to S-SMEDDS by using Aerosil 200 as an adsorbent in the ratio of 3:1. The S-SMEDDS was characterised by SEM, DSC, globule size (152.1 nm), zeta-potential (-28.1 mV), % transmission study (98.75%), in vitro release (86.57%) at 30 min. The optimised solid SMEDDS formulation showed faster drug release properties as compared to conventional tablet of Zotepine.
本研究的目的是通过自微乳化给药系统（SMEDDS）提高难溶性药物佐替平的溶出速率。使用以油（油酸）、表面活性剂（吐温80）和助表面活性剂（聚乙二醇400）为顶点的三元相图来确定有效的自微乳化区域。采用Box-Behnken设计研究自变量的影响。主成分分析用于审查关键变量。对液体SMEDDS进行宏观评价、透光率、乳化时间和体外药物释放研究等表征。通过使用比例为3:1的Aerosil 200作为吸附剂，将优化后的制剂OL1转化为固体自微乳化给药系统（S-SMEDDS）。通过扫描电子显微镜（SEM）、差示扫描量热法（DSC）、球粒大小（152.1纳米）、ζ电位（-28.1毫伏）、透光率研究（98.75%）、30分钟时的体外释放（86.57%）对S-SMEDDS进行表征。与佐替平传统片剂相比，优化后的固体自微乳化给药系统制剂显示出更快的药物释放特性。
