岩白菜素包合物渗透泵片体外释药机制研究

Studies on Mechanism of in Vitro Release from Bergenin Inclusion Compound Osmotic Pump Tablets

关键词:  岩白菜素  包合物  渗透泵片  释药机制

Key words:  bergenin  inclusion  osmotic pump tablets  release mechanism

摘要:

目的 探索岩白菜素β-环糊精(β-CD)包合物渗透泵片的体外释药机制。方法 通过考察可能影响药物释放的3个因素(包衣膜、片芯和释药孔)，探讨其主要的释药动力和零级释药机制。结果 水透膜的速率远小于片芯中药物的溶出速率及岩白菜素渗透泵片的释药速率；扩散与溶蚀机制对渗透泵片释药有影响。结论 岩白菜素包合物渗透泵片的释药受多种机制共同影响；片芯的渗透压主要由岩白菜素包合物产生；体外释药的限速步骤为水透膜速率，因此渗透泵系统呈现出零级释放。

Abstract:

OBJECTIVE To discover the in vitro release mechanism of bergenin β-cyclodextrin (β-CD) inclusion complex osmotic pump tablets. METHODS Three rate-limiting factors influencing drug release from dosage form(the semi-permeable membrane, tablet core and delivery orifice) were investigated to study the main pharmacodynamics of its driving and the zero order release mechanism. RESULTS The influx of water that passed the osmotic pump tablet was greatly less than the drug dissolution rate from tablet core and the bergenin release rate. Corrosion mechanism and diffusion mechanism have effect on drug release from osmotic pump tablets. CONCLUSION A variety of mechanisms have effect on drug release of the bergenin β-CD inclusion compound osmotic pump tablets, the main driving force of release is the membrane osmotic pressure difference inside and outside, the water influx through the membrane is the rate-limiting step, accordingly, the drug release had obvious characteristic of zero order release.