摘要
目的:制备布地奈德固体分散体增溶型单层渗透泵片(以下简称布地奈德渗透泵片),并进行其释药机制研究。方法:用超临界流体技术制备的布地奈德-聚氧乙烯N750固体分散体作为含药片芯,以提高难溶性药物的溶解度;通过单因素实验优化片芯处方和包衣膜处方,制备布地奈德渗透泵片;设计实验考察包衣膜内外渗透压差对制剂稳态释药速率的影响,阐述其释药机制。结果:药物溶解度、促渗透剂种类和用量、增塑剂用量均对布地奈德渗透泵片的体外释药行为有影响,优化处方的体外释药方程为:Q=7.6077t+0.7764,r=0.999 7;其释药行为主要受包衣膜内外溶液渗透压控制,扩散释药仅占整个药物释放的30.39%。结论:渗透泵机制在布地奈德渗透泵片释药过程中占主导地位,体外释药符合零级动力学过程。
To prepare budesonide solid dispersion solubilizing osmotic pump tablets （BUD OPT） and to elucidate its drug release mechanism. Method ： The budesonide-poly （ ethylene oxide） N750 solid dispersion by using supercritical fluids technology was utilized as drug core to enhance intrinsic solubility of drug. The single factor tests were adopted to optimize the drug core formula- tion and semipermeable membrane formulation and BUD OPT was designed successfully. The experiment of the effects of osmotic pres- sure difference in/out of the semipermeable membrane on homeostatic release rate was designed to illuminate the release mechanism of BUD OPT. Result： Drug solubility, the sort and amount of osmotic pressure promotor and amount of plasticizer have the effects on drug release of BUD OPT. The in vitro release equation of optimized formulation was as follows ： Q = 7. 6077t ＋ 0. 7764, r = 0. 999 7. The drug release was controlled mainly by the osmotic pressure in/out of coating membrane and the drug diffusion was only 30.39 % in overall drug release from BUD OPT. Conclusion： Osmotic pump mechanism is the key factor in the release procedure of BUD OPT and its in vitro drug release fittes well into zero-order model.
出处
《中国药师》
CAS
2009年第1期5-8,共4页
China Pharmacist
基金
辽宁省自然科学基金(项目编号:20052059)
关键词
布地奈德
固体分散体
渗透泵
释药机制
Budesonide
Solid dispersion
Osmotic pump
Release mechanism
