Giannola L I, De Caro V, Di Stefano V, Rizzo M C
Dipartimento di Chimica e Technologie Farmaceutiche, Università di Palermo, Italy.
Pharmazie. 1993 Dec;48(12):917-20.
Hexadecanol microspheres were investigated as a vehicle for the controlled release of valproic acid. Microsphere of the antiepileptic agent were prepared by the meltable dispersion method in water using wetting agents. To prevent hepatotoxicity, microspheres containing both the drug and vitamin E were also prepared. The method in simple, inexpensive, rapid and reproducible. The drug release was evaluated in vitro. Kinetic results were analyzed to distinguish between the first-order release model and the square root of time relationship. More than 99% of the isolated microspheres were particle size range 200-710 microns. The average drug content was 24%. Drug bioavailability was greatly affected as a result of microspheres formation.
研究了十六醇微球作为丙戊酸控释载体的情况。采用可熔分散法在水中使用湿润剂制备抗癫痫药物的微球。为防止肝毒性，还制备了同时含有药物和维生素E的微球。该方法简单、廉价、快速且可重复。体外评估了药物释放情况。分析动力学结果以区分一级释放模型和时间平方根关系。超过99%的分离微球粒径范围为200 - 710微米。平均药物含量为24%。微球形成导致药物生物利用度受到很大影响。
