卡托普利脉冲微丸制备及大鼠体内药动学研究

 目的 研究卡托普利脉冲缓释微丸（简称Cap脉冲微丸）在Wistar大鼠体内的药动学。方法 制备卡托普利脉冲缓释微丸，采用RP-HPLC测定12只Wistar大鼠口服复方卡托普利脉冲缓释微丸胶囊及复方卡托普利片后在不同时间血浆中卡托普利的浓度，通过DAS2.1程序计算药动学参数。结果 大鼠体内时滞时间为4.75 h，与普通片剂相比，具有明显时滞，达峰时间明显延长（9.67 h），相对生物利用度（117.29±46.87）%。结论 卡托普利脉冲缓释微丸在体内外经明显的时滞后均能缓慢释放，可达到睡前服药，凌晨发挥药效的目的。

Preparation of Captopril Pulsed Pellets and Its Pharmacokinetics in Rats

OBJECTIVE Compared with the compound captopril tablets(compound Cap),to study the pharmacokinetics characteristics and bioavailability in twelve wista rats after oral administration of Cap pulsed pellets and compound CAP tablets by HPLC.METHODS To prepare captopril pulsed pellets(Cap pulsed pellets).The pharmacokinetic parameters were computed by software program DAS2.1.RESULTS In vivo the lag time for 4.75 h,compared with ordinary tablet,it has an obviously lag time,tmax was 9.67 h and the relative bioavailability was(117.29±46.87)%.CONCLUSION The release of CAP from CAP pulsed sustained-release pellets was shown to be sustained-release after an conspicuous lag time in vitro and in vivo.So the drug can be taken by the patient before sleeping and can achieve the purpose in the morning.