知识与财富的链接
目的制备以法莫替丁为模型药物的脉冲控释胶囊;探索制备脉冲微丸的方法。方法采用挤出滚圆法制备速释微丸。应用有机酸诱导机理制备脉冲微丸,于丸芯中加入有机酸,EudragitRS100为包衣材料,用正交设计优化处方。将两种微丸混合后制成脉冲控释微丸胶囊。结果脉冲控释胶囊的体外释放分为两步:速释微丸迅速溶出,胶囊的释放度30min达50%;脉冲微丸于5h左右开始溶出,累积释放度13h时达95%。脉冲微丸的时滞由丸芯中酸量及包衣膜厚度共同决定;而时滞后的释药速率则主要由前者控制。结论采用有机酸诱导机理可制备理想的脉冲微丸;与速释微丸混合即可制成释药两次的法莫替丁脉冲控释微丸胶囊。
Objective To prepare pulsed-release capsule(PRC) using famotidine(FM) as a model drug and to explore the way of preparing pulsed-release pellets(PRP). Methosd Normal pellets(NP)were prepared by extrusion-spheronization. PRP were "Organic acid-induced type drug delivery system"(OAITDDS), with organic acid in the core, Eudragit RS100 as the coating, using orthogonal test design to optimize the formulation. The two kinds of pellets were mixed to prepare FM PRC. Results The release of PRC had two steps in vitro. First, NP released drug quickly and the cumulative release quantity was nearly 50% within 30 min. Second, PRP release was initiated after a lag time of 5h and was completed within 13h. The lag time was dependent on the quantity of organic acid in the core and the coating level, while the release after the lag time was mainly dependent on the former. Conclusion PRP could be prepared by the principle of OAITDDS and with NP mixed together, FM PRC could be acquired.
