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.
出处
《中国现代应用药学》
CAS
CSCD
北大核心
2005年第3期224-228,共5页
Chinese Journal of Modern Applied Pharmacy
关键词
卡托普利
延迟起释
缓释片
干压包衣技术
captopril
delayed-onset
sustained release tablet
dry-coated technology
