[关键词]
[摘要]
目的 制备芒果苷(mangiferin,MGF)自微乳给药系统(SMEDDS),并对其进行药动学研究。方法 评价系统自微乳化速度,激光散射仪测定乳化后形成微乳粒径的大小及分布情况;以PBS 6.8缓冲液为释放介质,考察MGF-SMEDDS的体外释放行为;采用HPLC法测定大鼠血浆药物浓度,考察MGF-SMEDDS的体内吸收情况。结果 体系在1 min内可乳化完全,乳化后粒径在20 nm左右;MGF-SMEDDS在120 min的累积释放率可达80%以上;大鼠体内药动学研究结果表明,MGF-SMEDDS达峰时间为0.43 h,是MGF的1/7;最大血药浓度为0.93 mg/L,是MGF的2.16倍。结论 自微乳给药系统可以显著提高MGF的体外释放,改善其药动学性质。
[Key word]
[Abstract]
Objective To prepare the mangiferin (MGF) self-micro emulsifying drug delivery system (SMEDDS) and to study the pharmacokinetic behavior in rats. Methods The self-micro emulsifying rate was evaluated and the self-micro emulsifying efficiency was evaluated by the particle size and distribution of resultant micro emulsions. Using PBS 6.8 as releasing medium, the in vitro release of MGF-SMEDDS was investigated. The plasma concentration was determined by HPLC and the in vivo absorption of MGF-SMEDDS was also evaluated. Results The system was self-micro emulsified in 1 min and the particle size was about 20 nm. The accumulated release rate was more than 80% at 120 min, Tmax was 0.43 h and Cmax was 0.93 mg/L in SMEDDS group, which were 1/7 and 2.16 times of those in MGF group. Conclusion The SMEDDS could increase the drug dissolution in vitro significantly and improve the pharmacokinetic properties.
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[基金项目]
国家科技部“重大新药创制”科技重大专项(2012ZX09304007)