黄连总碱―卡波姆复合物制备体外释药特性及其胃生物粘附性能评价.docVIP

黄连总碱―卡波姆复合物制备体外释药特性及其胃生物粘附性能评价 　　[摘要] 目的 探讨黄连总碱-卡波姆复合物的缓释特性及其胃生物粘附性能。 方法 以复合物收率和载药量为指标，采用单因素法分别探讨卡波姆品种、卡波姆浓度、黄连总碱浓度等因素对酸碱沉淀反应的影响。采用体外释放度测定法探讨黄连总碱-卡波姆复合物在pH值分别为1.2，5.0，6.8，7.0和7.4的介质中的释药动力学。采用大鼠胃内的留存量测定法初步探讨黄连总碱-卡波姆复合物在体内的胃生物粘附性。 结果 （1）黄连总碱-卡波姆复合物消除了黄连的强烈苦味，最佳的卡波姆品种为934P，卡波姆浓度为0.25%，黄连总碱浓度为1%。（2）黄连总碱-卡波姆复合物在人工胃液中具有较佳的缓释性能。但在纯水、pH 5.0、pH 6.8和pH 7.4四种介质中的释药非常缓慢。（3）黄连总碱-卡波姆复合物在胃内的滞留时间远远大于黄连总碱。 结论 黄连总碱-卡波姆复合物具有良好的缓释性能和胃生物粘附性能。 　　[关键词] 黄连；卡波姆；小檗碱 　　[中图分类号] R282.7 [文献标识码] A [文章编号] 2095-0616（2013）22-14-04 　　Evaluation of preparation， in vitro release characteristics and gastric bioadhesive properties of compound of total alkaloids of coptis and carbomer 　　LIU Taoshi ZHAO Xinhui DI Liuqing CAI Baochang 　　Nanjing University of Chinese Medicine，Nanjing 210023，China 　　[Abstract] Objective To explore the release characteristics and gastric bioadhesive properties of compound of total alkaloids of coptis and carbomer. Methods Making the yield and drug loading of compound as indexes， the varieties of carbomer and concentration of carbomer and total alkaloids of coptis which were effect on the acid precipitation reaction were respectively investigated by using the single factor method.The release kinetics of compound of total alkaloids of coptis and carbomer in the medium with pH 1.2，pH 5.0，pH 6.8，pH 7.0 or pH 7.4 were respectively investigated by using the determination of in vitro release rate. The vitro gastric bioadhesive properties of compound of total alkaloids of coptis and carbomer were preliminarily investigated by using the determination of rat gastric retained amount. Results （1）The compound of total alkaloids of coptis and carbomer eliminated the bitterness of coptis，the optimal varieties of carbomer was 934P，the optimal concentration of carbomer and total alkaloids of coptis were 0.25%，1% respectively.（2）The compound of total alkaloids of coptis and carbomer had better release characteristics in artificial gastric juice.But the drug release were very slowly in f