水飞蓟素羟丙基-β-环糊精包合物在大鼠体内的生物利用度

Study on the bioavailability of HP-β-CD silymarin in rats

目的:研究水飞蓟素的羟丙基-β-环糊精包合物在大鼠体内的相对生物利用度。方法:给大鼠口服单剂量水飞蓟素羟丙基-β-环糊精包合物(受试样品)和水飞蓟宾胶囊剂(参比样品),用反相高效液相色谱法测定大鼠血浆中水飞蓟宾的浓度,并采用3P97程序进行统计学分析。结果:口服水飞蓟素后大鼠血浆药物浓度-时间曲线符合二室模型。受试样品中水飞蓟宾的Cm ax,tm ax,t1/2,AUC0-∞分别为(0.9±0.3)mg.L-1,(0.50±0.21)h,(12.6±3.7)h,(4.2±0.9)h.mg.L-1,参比样品中水飞蓟宾的Cm ax,tm ax,t1/2,AUC0-∞分别为(0.4±0.3)mg.L-1,(1.0±0.6)h,(31.2±15.0)h,(3.0±0.8)h.mg.L-1。受试样品中水飞蓟宾的相对生物利用度为(142.0±38.4)%。结论:与参比样品相比,受试样品的生物利用度较高。

OBJECTIVE To study the bioavailability of HP-β-CD silymarin in rats. METHODS HP-β-CD silymarin （test sample） and silibinin capsules（reference sample） were administrated to the rats in a single oral dose of 200 mg· kg^-1,The silibinin concentrations in rats＇plasma were determined by RP-HPLC and analysed with 3P97 program. RESULTS The concentration-time data of silibinin after oral administration were best fitted to two-compartraent model. The main pharmaeokinetie parameters were as folows： the Cmax,Tmax,t1/2,AUC0-∞ of the test sample were （0.9±0.3）mg·L^-1, （0.50±0.21）h, （12.6±3.7）b, （4.2±0.9）h·mg·L^-1; those of the reference one were （0.4±0.3）mg·L^-1, （1.0±0.6）h, （31.2±15.0）h, （3.0±0.8）b ·mg·L^-1, respectively. The relative bioavailability of silibinin of test sample was （ 142.0±38.4） %. CONCLUSION The test sample has a higher bioavailability than the reference one.