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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 huperzine-in-situ gel (PSE-H) and study its pharmacokinetics in rats. Methods The method of direct drug loading was used to prepare PSE-H. Hup A plasma samples were prepared for analysis of pharmacokinetics of Hup A oleate in different dosage formulations and preparations influences. Results PSE-H sustained release of Hup A in vivo for 15 days. The preparation of oleic acid complex by Hup A can reduce the burst effect of the drug in the preparation. With the increase of the weight of the preparation, the sustained-release effect is enhanced and the burst release effect is reduced. Conclusion The preparation of PSE-H by direct drug loading method is simple and feasible. Hup A sustained release in vivo for 15 days is expected to become a new controlled-release dosage form.