水飞蓟宾增溶作用的研究：胆酸钠/磷脂混合胶束对水难溶性药物水飞蓟宾的增溶作用。
Enhancement of oral bioavailability of the poorly water-soluble drug silybin by sodium cholate/phospholipid-mixed micelles.
机构信息
Department of Pharmaceutics, School of Pharmacy, Jiangsu University, Zhenjiang, China.
出版信息
Acta Pharmacol Sin. 2010 Jun;31(6):759-64. doi: 10.1038/aps.2010.55.
AIM
To evaluate a mixed micellar drug delivery system composed of sodium cholate and phospholipid for oral administration of silybin, a promising hepatoprotectants.
METHODS
The optimum formulation of sodium cholate/phospholipid-mixed micelles containing silybin was obtained based on the study of pseudo-ternary phase diagram. The dissolution of silybin-mixed micelles was investigated. The pharmacokinetic characteristics and bioavailability after oral administration of silybin-mixed micelles and silybin-N-methylglucamine were compared in dogs.
RESULTS
The mean particle size of prepared mixed micelles was 75.9+/-4.2 nm. The largest solubility of silybin was found to be 10.0+/-1.1 mg/mL in the optimum formulation of mixed micelles. The silybin-sodium cholate/phospholipid-mixed micelles showed a very slow release of silybin 17.5% (w/w) within 72 h in phosphate buffer (pH 7.4) and 15.6% (w/w) in HCl solution (pH 1.2). After oral administration to dogs, the relative bioavailability of mixed micelles versus silybin-N-methylglucamine in dogs was 252.0%.
CONCLUSION
Sodium cholate/phospholipid-mixed micelles are promising carriers in orally delivery of silybin, considering their capability of enhancing bioavailability and large-scale production.
目的
评估由胆酸钠和磷脂组成的混合胶束给药系统，用于口服水飞蓟宾，这是一种很有前途的肝保护剂。
方法
基于伪三元相图的研究，获得了含有水飞蓟宾的胆酸钠/磷脂混合胶束的最佳配方。考察了水飞蓟宾混合胶束的溶解情况。在犬体内比较了水飞蓟宾混合胶束和水飞蓟宾-N-甲基葡胺口服后的药代动力学特征和生物利用度。
结果
所制备的混合胶束的平均粒径为 75.9±4.2nm。在最佳混合胶束配方中，水飞蓟宾的最大溶解度为 10.0±1.1mg/mL。水飞蓟宾-胆酸钠/磷脂混合胶束在 pH7.4 的磷酸盐缓冲液中 72h 内缓慢释放 17.5%（w/w）的水飞蓟宾，在 pH1.2 的 HCl 溶液中缓慢释放 15.6%（w/w）的水飞蓟宾。犬口服给药后，混合胶束相对于犬体内水飞蓟宾-N-甲基葡胺的相对生物利用度为 252.0%。
结论
考虑到胆酸钠/磷脂混合胶束能够提高生物利用度和进行大规模生产，因此是一种很有前途的口服水飞蓟宾给药载体。
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