LC-MS/MS法测定木通皂苷D大鼠灌胃给药的生物利用度

LC-MS/MS DETERMINATION OF ORAL BIOAVAILABILITY OF AKEBIA SAPONIN D IN RAT

建立高效液相色谱-质谱联用法（LC-MS/MS）测定大鼠灌胃给药的生物利用度.大鼠随机分为2组,分别尾静脉和灌胃给予100mg·kg^-1木通皂苷D,于不同时间点眼眶取血,用LC-MS/MS法检测血浆中药物质量浓度,计算大鼠灌胃给药的生物利用度.结果表明：木通皂苷D线性范围为10-1 000ng·mL^-1,最低定量限为10ng·mL^-1.准确度与精密度试验结果显示方法日间、日内变异均小于15%,相对偏差为-2.8%-4.6%,低、中、高3个质量浓度提取回收率为95.3%-108.1%.静脉组和口服组的药时曲线下面积AUC0-INF分别为（231 725.98±46 527.21）和（383.63±54.62）ng·h·mL^-1,灌胃给药的绝对生物利用度为0.13%.表明木通皂苷D大鼠灌胃给药生物利用度很低.

A LC-MS/MS method was used to rats were randomly divided into two groups. Dose determine oral bioavailability of akebia saponin D in rat. SD of 100 mg·kg^-1 akebia saponin D was given by stomach tube or by caudal vein injection. Blood samples were collected at different time intervals after administration through orbit vein. Plasma drug concentration was detected by LC-MS/MS, oral bioavailability was then calculated. The LC-MS/MS assay calibration curve was linear over the range of 10-1 000 ng· mL^-1. Intra-and inter-day variations were both less than 15 %. Relative deviation was from -2.8%-4. 6 %. Recoveries of akebia saponin D were from 95.3%-108.1%. AUC0-INF in injection group and oral group were （231 725.98±46 527.21） and （383.63±54. 62） ng· h·mL^-1 respectively. Absolute bioavailability for intragastric administration was 0. 13 %. Bioavailability of akebia saponin D by intragastric administration was very low.