硝苯地平推拉式渗透泵片体外释放影响因素的研究

目的：本实验的目的是以难溶性药物硝苯地平为模型药物来研究推拉式渗透泵片剂中药物层和推动层的配方中聚合物聚氧乙烯的用量、氯化钠的用量、控释层包衣增重以及药物层和推动层的比例对药物释放的影响。方法：采用推拉式渗透泵设计,分别考察聚氧乙烯-N80在药物层中的不同用量、聚氧乙烯Coagulant在推动层中的不同用量以及氯化钠在推动层中不同用量的7个配方,7个配方片芯同时采用欧巴代CA包衣进行半透膜控释包衣,因片重大小不同,无法同时得到相同的包衣增重,所以结合实际包衣增重的数据,采用统计分析软件对包衣片在不同时间的药物释放数据进行建模分析。结果：统计结果表明欧巴代CA的包衣增重对药物释放有显著影响（P〈0.05）,随着包衣增重的增加,药物的释放变慢。聚氧乙烯N-80在药物层中的用量对药物释放也有显著影响（P〈0.05）,随着聚氧乙烯N-80在药物层中用量的增加,药物的释放变慢。而聚氧乙烯Coagulant和氯化钠在推动层的用量变化,在配方考察的比例范围内对药物的释放的影响不显著。对20小时的药物释放分析结果表明,药物层与推动层的比例对药物的后期释放有显著影响（P〈0.05）。药物层与推动层的比例越高,药物后期释放得越慢。

Study of Influence Factors on In-vitro Drug Release from Nifedipine Push-Pull Osmotic Pump System

Objective： To study the influence of polyethylene oxide level in drug layer and push layer, sodium chloride level in push layer and Opadry CA coating weight gain and the ratio of pull layer to push layer on drug release from push-pull osmotic pump system with nifedipine, a practically water insoluble model drug. Methods： Designed seven formulations with different polyethylene oxide N-80 level in drug layer, polyethylene oxide coagulant and sodium chloride level in push layer. Coated tablets with Opadry CA in a coating pan. Because of the difference in tablets weight, we could not get the same coating weight gain tablets. So we collected ac- tual weight gain data of every formulation and analyzed with other factors by statistics analysis software. Conclusion： The result showed that Opadry CA weight gain had significant influence on drug release（P〈0.05）. Drug release turned to slow while Opadry CA weight gain increasing. Polyethylene oxide N-80 in drug layer also had significant influence on drug release （P〈0.05）. Drug release became slow while PEO N-80 level increasing. Polyethylene oxide coagulant and sodium chloride had no influence on drug release in the range of researching. For the result of study on drug release at 20 hours, it showed that the ratio of pull layer and push layer had great influence on later stage of drug release （P〈0.05）. The higher pull layer and push layer ratio, the lower drug release on later stage.