Jain Sunil K, Agrawal G P, Jain N K
SLT Institute of Pharmaceutical Sciences, Guru Ghasidas University, Bilaspur (C.G.) 495 009, India.
PDA J Pharm Sci Technol. 2008 Jul-Aug;62(4):292-9.
The purpose of the study is to prepare and evaluate an intragastric floating granular delivery system of orlistat using (i) calcium silicate as porous carrier; and (ii) hydroxypropyl methylcellulose K4M, ethyl cellulose, and Carbopol 940 as matrix-forming polymers. The effect of various formulation and process variables on the micro-meritic properties, in vitro floating behavior, percent drug content, and in vitro drug release was studied. The release mechanism of orlistat from these granules was evaluated on the basis of various theoretical equations. The optimized formulation demonstrated favorable in vitro floating and release characteristics. The release pattern of optimized, secondary-coated granules of orlistat in simulated gastrointestinal fluids corresponded best to the Peppas-Korsmeyer model and Higuchi matrix model. The results clearly indicated the controlled and sustained release of orlistat from its gastro-retentive floating granular delivery system.
本研究的目的是制备并评估一种奥利司他胃内漂浮颗粒给药系统,该系统使用(i)硅酸钙作为多孔载体;以及(ii)羟丙基甲基纤维素K4M、乙基纤维素和卡波姆940作为成膜聚合物。研究了各种制剂和工艺变量对微粉特性、体外漂浮行为、药物含量百分比和体外药物释放的影响。基于各种理论方程评估了奥利司他从这些颗粒中的释放机制。优化后的制剂表现出良好的体外漂浮和释放特性。奥利司他优化后的二次包衣颗粒在模拟胃肠液中的释放模式与Peppas-Korsmeyer模型和Higuchi基质模型最为吻合。结果清楚地表明了奥利司他从其胃滞留漂浮颗粒给药系统中的控释和缓释效果。