卡托普利延迟起释型缓释片的研制  

Preparation of captopril delayed-onset,sustained release tablets

作　　者：骆快燕[1] 姚彤炜[1] 黄安琪[2] 

机构地区：[1]浙江大学药学院,浙江杭州310031 [2]杭州民生药业集团有限公司,浙江杭州310011

出　　处：《中国现代应用药学》2005年第3期224-228,共5页Chinese Journal of Modern Applied Pharmacy

摘　　要：目的制备适用于临睡前服用,间隔4～6h后于次日凌晨开始释放药物并持续释放较长一段时间的卡托普利延缓片。方法用干压包衣技术制备卡托普利延缓片,中心组合设计优化处方,人工神经网络预测释药时滞,在SAS上进行多元线性回归,并对优化结果进行验证,从而确定衣层处方。然后以卡托普利缓释片为对照制剂,以相似因子f2为筛选指标,确定片芯组成,从而确定最终处方。结果所优化的卡托普利延缓片体外释药时滞为5h,开始释放后与对照制剂有良好的相似性(f2=64.06),体外释放符合一级动力学规律。结论以干压包衣技术制得包芯片,由衣层控制延迟释放的释药时滞,由衣层和片芯共同控制药物缓慢释放。OBJECTIVE To prepare captopril delayed-onset,sustained release tablets that start releasing after a lag time 5h. METHODS Captopril delayed-onset,sustained release tablets were prepared with dry-coated technology.Central composite design was used to optimize the formulation, artificial neural networks was used to predict the lag time of release,and multiple regression was performed using statistic analysis software (SAS).The observed values of the lag time of captopril delayed-onset,sustained release tablets prepared under the optimum condition were compared with the predicted.The out shell composition was confirmed. The composition of core tablets was optimized using captopril sustained release tablets as reference preparation and the similarity factor(f_ 2 ) as the evaluation standard. Then the formulation of captopril dry-coated tablets was finally confirmed.RESULTS The lag time in vitro of captopril delayed-onset,sustained release tablets prepared under the optimum condition was 5h. The tablets had similar release behavior to reference products(f_ 2 =64.06) and the drug release pattern was accorded with the first order kinetics.CONCLUTION The lag time of this dry-coated tablets is only controlled by the composition of out shell. The sustained release after release starting is controlled by both out shell and core tablet.

关 键 词：卡托普利 延迟起释 缓释片 干压包衣技术 

分 类 号：R943.41[医药卫生—药剂学] R972.4[医药卫生—药学]