卡托普利脉冲胶囊制备工艺优化

Optimization of Preparation Technology of Captopril Pulse Capsule

目的优化以卡托普利作为模型药物制备脉冲胶囊的工艺,并研究脉冲胶囊体外释药机制、体内药动学。方法分别制备非渗透性胶囊、含药片、蜡质溶蚀片、栓塞片,组装成卡托普利脉冲胶囊。采用单因素试验和星点设计优化制备工艺。以卡托普利普通片为对照进行家兔体内的药动学研究。结果卡托普利脉冲胶囊较卡托普利脉冲片的AUC和平均滞留时间(average residence time,MRT)均有显著性变化,MRT是普通片剂的2.39倍,滞后时间是普通片剂的10.66倍。结论根据Cmax和AUC数据(双单侧t检验及置信区间法)推断卡托普利脉冲胶囊与普通的片剂相比有明显的时滞。

OBJECTIVE To optimize the process of preparing pulse capsules with captopril as a model drug,and study the release mechanism in vitro and pharmacokinetics in vivo of pulse capsules.METHODS Impermeable capsules,tablets,wax dissolution tablets and embolic tablets were prepared and assembled into captopril pulse capsules.The preparation process was optimized by single factor test and star design.The pharmacokinetic study in rabbits was carried out with captopril ordinary tablets as a control.RESULTS The AUC and average residence time(MRT)of captopril pulse capsules were significantly different from those of captopril pulse tablets.MRT and time lag of captopril pulse capsules were 2.39 times and 10.66 times higher than those of common tablets respectively.CONCLUSION According to Cmax and AUC data(double one-sided t-test and confidence interval method),it is inferred that captopril pulse capsules had obvious time delay compared with ordinary tablets.