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目的:研究黄芪甲苷羟丙基-β-环糊精包合物在大鼠体内的相对生物利用度。方法:给大鼠口服单剂量黄芪甲苷羟丙基-β-环糊精包合物(受试制剂)和黄芪甲苷混悬液(参比制剂),用HPLC-MS法测定大鼠血浆中黄芪甲苷的浓度,并采用3P97程序计算药动学参数。结果:口服黄芪甲苷后大鼠血浆药物浓度-时间曲线符合二室模型。受试样品中黄芪甲苷的C_(max)为(250.29±25.19)ng·ml~(-1),t_(max)为(1.75±0.42)h,AUC_(0→∞)为(2 469.65±168.90)h·ng·ml~(-1),参比样品中黄芪甲苷的C_(max)为(57.83±8.02)ng·ml~(-1),t_(max)为(6.67±0.84)h,AUC_(0→∞)为(862.00±149.61)h·ng·ml~(-1)。黄芪甲苷羟丙基-β-环糊精包合物中黄芪甲苷的相对生物利用度为(293.6±28.9)%。结论:黄芪甲苷羟丙基-β-环糊精包合物的生物利用度较高。
Objective: To study the relative bioavailability of astragaloside-hydroxypropyl-β-cyclodextrin inclusion complex in rats. Methods: A single dose of astragaloside hydroxypropyl-β-cyclodextrin inclusion complex (test preparation) and astragaloside suspension (reference preparation) were orally administered to rats, and the plasma level of rat plasma In Astragaloside concentration, and use 3P97 program to calculate pharmacokinetic parameters. Results: The plasma concentration-time curve of rats after oral administration of Astragaloside Ⅳ agrees with the two-compartment model. The C_max of astragaloside in test sample was (250.29 ± 25.19) ng · ml -1, t max was (1.75 ± 0.42) h, AUC_ (0 → ∞) was (2 469.65) ± 168.90 h · ng · ml -1. The Cmax of reference sample was (57.83 ± 8.02) ng · ml -1 and the t max was (6.67 ± 0.84) ) h, AUC_ (0 → ∞) was (862.00 ± 149.61) h · ng · ml -1. The relative bioavailability of astragaloside in astragaloside hydroxypropyl-β-cyclodextrin inclusion complex was (293.6 ± 28.9)%. Conclusion: Astragaloside hydroxypropyl-β-cyclodextrin inclusion complex has high bioavailability.