田蓟苷微乳在大鼠体内的药动学及生物利用度

目的:研究田蓟苷微乳在大鼠体内的药动学过程并考察生物利用度。方法:建立检测大鼠血浆中田蓟苷的HPLC方法,考察大鼠经灌胃和静脉途径给予田蓟苷单体及田蓟苷微乳后田蓟苷的药动学过程,DAS 2.0软件拟合药动学参数并计算生物利用度。结果:田蓟苷在0.027~43.200 μg·ml^-1范围内线性关系良好(r≥0.999),田蓟苷微乳在大鼠体内的药动学过程符合二室模型,当灌胃剂量由25 mg·kg^-1增至50 mg·kg^-1时,t_1/2β显著降低,而K、AUC_(0-t)和C_max显著增加;大鼠灌胃25 mg·kg^-1和50 mg·kg^-1田蓟苷微乳后田蓟苷的绝对生物利用度分别为3.4%和3.2%,相对于等剂量田蓟苷单体的相对生物利用度分别为147.2%和168.2%。结论:微乳给药系统作为田蓟苷的载体显著增加了田蓟苷的生物利用度。

Pharmacokinetics and bioavailability of tilianin microemulsion in rats

OBJECTIVE To study on pharmacokinetics and bioavailability of tilianin microemulsion in rats.METHODS Concentrations of tilianin in rat plasma after oral and intravenous administration of tilianin microemulsion were measured by HPLC method,pharmacokinetic parameters and bioavailability were calculated.RESULTS Calibration curve of tilianin was linear in range of 0.027-43.200 μg·ml^-1 (r≥0.999).Tilianin was best fitted with two-compartment model in rats after oral administration of tilianin microemulsion.As dose increased (25 mg·kg^-1 to 50 mg·kg^-1),t_1/2β of tilianin was significantly decreased,but AUC_(0-t),C_max and K values were much greater than those at high dose.Absolute bioavailability values of tilianin were 3.4% and 3.2% after oral administration of tilianin microemulsion at 25 mg·kg^-1 and 50 mg·kg^-1,respectively.Relative bioavailability values of tilianin microemulsion were 147.2% and 168.2% relative to tilianin at equal doses.CONCLUSION The prepared microemulsion can improve bioavailability of tilianin significantly.