石杉碱甲磷脂原位凝胶的制备及其在大鼠体内的药动学研究

Preparation and pharmacokinetic study of Huperzine A phospholipid in situ-gel

目的制备石杉碱甲磷脂原位凝胶(PSE-H)并研究其在大鼠体内的药动学。方法采用直接载药法制备PSE-H,建立石杉碱甲(Hup A)血浆样品的分析方法,研究不同剂量制剂及制剂中Hup A油酸复合物的形成对PSE-H药动学特征的影响。结果 PSE-H在体内持续释放Hup A达15 d。将Hup A制备成油酸复合物可降低制剂中药物的突释作用;随着制剂重量的增加,缓释作用增强,突释作用降低。结论通过直接载药法制备PSE-H,方法简便可行,Hup A在体内持续释放达15 d,有望成为可生产的缓控释新剂型。

OBJECTIVE To prepare a phospholipid in situ - gel contained Huperzine A （ Hup A） （ PSE - H）. METHODS PSE - H was prepared by direct drug loading method. The analysis method of Hup A was established. The pharmacokinetics of PSE - H in different weight and PSE - H fornmlation containing Hup A oleic acid complex（ PSE - H - O） were studied. RESULTS PSE - H sustained the releasedof Hup A for 15 days in vivo. The Hup A oleic acid complex in 0.5 g of formulation decreased the initial burst effect in PSE - H. With the formulation weight increased, the sustained release effect was enhanced and the initial burst effect was decreased. CONCLUSION The direct drug loading preparation of PSE - H is simple and feasible. PSE - H can release Hup A in vivo for 15 d,which represents a new sustained release system for easy manufacture.