目的 制備芒果苷（mangiferin，MGF）自微乳給藥系統(tǒng)（SMEDDS），并對其進行藥動學研究。方法 評價系統(tǒng)自微乳化速度，激光散射儀測定乳化后形成微乳粒徑的大小及分布情況；以PBS 6.8緩沖液為釋放介質(zhì)，考察MGF-SMEDDS的體外釋放行為；采用HPLC法測定大鼠血漿藥物濃度，考察MGF-SMEDDS的體內(nèi)吸收情況。結(jié)果 體系在1 min內(nèi)可乳化完全，乳化后粒徑在20 nm左右；MGF-SMEDDS在120 min的累積釋放率可達80%以上；大鼠體內(nèi)藥動學研究結(jié)果表明，MGF-SMEDDS達峰時間為0.43 h，是MGF的1/7；最大血藥濃度為0.93 mg/L，是MGF的2.16倍。結(jié)論 自微乳給藥系統(tǒng)可以顯著提高MGF的體外釋放，改善其藥動學性質(zhì)。

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, T_max was 0.43 h and C_max 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.

國家科技部“重大新藥創(chuàng)制”科技重大專項（2012ZX09304007）