山茱萸中马钱苷在大鼠体内的药物动力学研究

Pharmacokinetic study on loganin from Comus officinalis Sieb.et Zucc.in rats

目的:建立测定大鼠血浆中马钱苷浓度的方法,研究并比较了口服马钱苷单体和山茱萸提取液后马钱苷在大鼠体内的药物动力学过程,考察了马钱苷单体口服后的绝对生物利用度。方法:利用 HPLC 法,色谱柱为反相 C_(18)柱(250 mm×4.6mm,5μm),流动相为甲醇-水(32∶68),流速为1 mL·min^(-1),检测波长236 nm。结果:线性范围15.25～7625 ng·mL^(-1),日内与日间 RSD<15%,回收率93.5%～109.3%。灌胃给药后马钱苷单体消除 t_(1/2)为93.6 min,绝对生物利用度为13.2%;山茱萸提取液中马钱苷消除 t_(1/2)为99.4 min,相对马钱苷单体口服给药的生物利用度为19.4%。结论:马钱苷单体口服生物利用度较低。本文方法灵敏度高,操作方便,适合于马钱苷的药动学研究。

Objective：To develop an HPLC method for determination of loganin in rat plasma,and to study the pharmacokinetics of loganin and loganin in the extract of Comus officinalis Sieb. et Zucc.,and to investigate absolute bioavailability of loganin given orally in rats. Method：The RP-C18 column（250 mm×4. 6mm,5μm）was used as the stationary phase with the mobile phase consisting of methanol - water （32： 68）. The flow rate was 1 mL·min^- 1, the UV detector was set at 236 nm. Results：The recovery of loganin in rat plasma was 93. 5% - 109. 3%. The calibration curve in plasma was linear over the range of 15. 25 -7625 ng · mL^-1 and the RSD values of intra - day and inter - day were less than 15%. The elimination t1/2of loganin was 93.6 rain and the absolute bioavailability was 13.2%. The elimination t1/2 of loganin in the extract from Comus officinalis was 99. 4 rain and the relative bioavailability was 19. 4%. Conclusion：Absolute bioavailability of loganin is low. The method is sensitive,simple and suitable for pharmacokinetic parameters study of loganin.