卡托普利缓释片处方及制备工艺的优化.doc

卡托普利缓释片处方及制备工艺的优化
作者:高迎春,文爱东,蒋永培,赵磊
【关键词】,卡托普利
关键词: 卡托普利;缓释制剂;体外释放度;制备
摘要:目的制备卡托普利缓释片剂. 方法以体外释放度为筛选指标,通过三因素多水平的随机试验设计,比较研究不同的缓释材料(羟丙基甲基纤维素,黄原胶,聚丙烯酸树脂II号,乙基纤维素,十八醇)与工艺路线(粉末直接压片,湿法制粒,熔融制粒)的优劣,并在此基础上对填充剂(淀粉,乳糖,硫酸钙)进行筛选. 结果最佳处方及制备工艺为:羟丙基甲基纤维素为缓释材料,粉末直接压片法为工艺路线,,聚丙烯酸树脂II号也具有较好的缓释作用. 结论用优化的处方,工艺制备的三批卡托普利缓释片体外释放良好,符合Higuchi方程,持续释药12h以上.

Keywords:captopril;sustained-release preparation;dissolu-tion;preparation

Abstract:AIM To prepare captopril sustained-release With dissolution as the screening guideline,matrix materials(HPMC,XG,EII,EC,OA)and technical routine(pression method,wet granula-tion method,melting granulation method)were selected to design two-factor-m
plete random these,the fillers(Starch,Lactose,CaSO4 )were sifted with the same The optimal formula-tion and technology were as follows:H
PMC as the matrix material,Lactose as the filler and pression as the technical these,EII was also a rather good sustained release matrix Three bates of Cap sustained release tablets prepared according to this optimal formulation and technology conform to Higuchi equation and the drug can be sustainedly released over12h in vitro.

0 引言

水溶性药物卡托普利(captopril,Cap)糖衣片或普通片,,需要日服3次,~~,峰浓度可达600μg・L-1 以上[1] ,而其治疗浓度为50μg&