美欧卡霉素胃内滞留漂浮型缓释片的制备及药代动力学研究

DEVELOPMENT AND PHARMACOKINETIC STUDY OF MIOCAMYCIN SUSTAINED-RELEASE TABLET REMAINING-FLOATING IN STOMACH

摘要: 本文根据流体动力学平衡药物控释系统的设计原理,制备了美欧卡霉素胃内滞留漂浮型缓释片(简称MOM-HBS)。该片剂由缓释、速释两种颗粒压制而成,其胃内滞留时间长达7h以上,明显长于普通片(3～4h)。体外溶出符合一级动力学过程(Kr=0.1619h^-1).体内血约浓度经时曲线平缓持久,达到良好的缓释效果。体内外实验数据有显著的相关性(P<0.001),相对生物利用度较日本产干糖浆有明显提高。

Abstract: A novel sustained-release tablet of miocamycin was developed based on the hydrodynamically balanced controlled drug delivery system (HBS). It was prepared to contain fast-release and sustained-release granules. The γ-scintiphotographic study after oral ingestion showed that MOM-HBS remained in human stomach for more than 7 hours, much longer than the conventional tablet (3～ 4 h). The in vitro release characteristics showed basically first- order kinetics (Kr= 0.1619 h^-1 ). The serum concentration- time course of MOM-HBS exhibited typical sustained- release characteristics.Moreover, The percentage of drug released in vitro versus the percentage of drug released in vivo of MOM-HBS indicated excellent linearity. Its relative bioavailability was increased greatly compared with MOM dry syrup produced in Japan.