目的研究单次ig麦冬皂苷肠溶微球在大鼠体内的相对生物利用度,以期提供最为直接的制剂质量评价。方法建立HPLC-M S分析方法,以固相萃取技术(SPE)进行血样处理,测定单次ig麦冬皂苷肠溶微球(被测制剂)及混悬剂(参比制剂)后不同时间血浆中薯蓣皂苷元的质量浓度,绘制药-时曲线,计算药动学参数及相对生物利用度。结果Cm ax为(637.81±17.23)ng/mL,tm ax为(4.0±0.0)h,AUC0-72为7 840.01±412.03。结论麦冬皂苷肠溶微球与普通混悬剂在ig单次给药后,大鼠体内的吸收、分布、消除性质颇为相似,其药动学参数数据也较为一致,相对生物利用度为(91.10±3.44)%。

Objective To study the relative bioavailability after ig rats with Ophiopogon japonicus saponin enteric microsphere in single-dose so as to give directly preparation quality evaluation. Methods(Establishing the) analysis method of HPLC-MS and dealing with the blood sample by solid phase extraction. Determining the diosgenin concentration in plasma after ig Ophiopogon japonicas saponin enteric microsphere and the suspension as comparison in single-dose, and calculating pharmacokinetic parameters and relative bioavailability. Results C_(max), t_(max), and AUC_(0-72) were (637.81±17.23) ng/mL, (4.0±0.0) h, and 7 840.01±412.03, respectively. Conclusion The characteristics of absorption, distribution, and elimination are resembled in rats between two preparations by ig in single-dose. The pharmacokinetic parameters are also identical. The relative bioavailability is (91.10±3.44)%.