法莫替丁胃内滞留型漂浮多颗粒给药系统的优化研究

Optimization studies on floating multiparticulate gastroretentive drug delivery system of famotidine.

作者信息

Gupta Reshu, Pathak Kamla

机构信息

Department of Pharmaceutics, Rajiv Academy for Pharmacy, Mathura, India.

出版信息

Drug Dev Ind Pharm. 2008 Nov;34(11):1201-8. doi: 10.1080/03639040802005016.

DOI:10.1080/03639040802005016

PMID:18686085

Abstract

The objective of this study was to optimize floating microballoons of famotidine by the emulsion solvent diffusion technique using central composite design. Formulations F1-F15 were prepared using three independent variables (pH of medium, drug: Eudragit S100 ratio and ethanol : dichloromethane ratio) and evaluated for dependent variables (shape, percentage buoyancy, and encapsulation). The optimized formulation F9 was fractionated and a polymer combination of (Eudragit S100 : Eudragit L100-55, 9.5:0.5) resulted in microballoons that exhibited zero order release (94.73%) with 84.20% buoyancy at the end of the eighth hour when studied in the mesh-designed modified USP type II apparatus.

摘要

本研究的目的是采用中心复合设计的乳液溶剂扩散技术优化法莫替丁的漂浮微球。使用三个自变量（介质的pH值、药物与尤特奇S100的比例以及乙醇与二氯甲烷的比例）制备了F1-F15制剂，并对因变量（形状、浮力百分比和包封率）进行了评估。对优化后的制剂F9进行分级分离，（尤特奇S100:尤特奇L100-55，9.5:0.5）的聚合物组合产生的微球，在网孔设计的改良USP II型装置中进行研究时，在第八小时结束时呈现零级释放（94.73%），浮力为84.20%。