灯盏花素在小鼠体内药物动力学研究

Pharmacokinetics of breviscapine in mice

目的:研究灯盏花素在小鼠体内的药物动力学和绝对生物利用度。方法:采用固相萃取 高效液相色谱(SPE HPLC)法,测定小鼠静脉注射灯盏花素5 0mg·kg-1和灌胃15 0mg·kg-1后血浆灯盏乙素浓度,3p97程序处理数据。结果:小鼠静注灯盏花素后灯盏乙素的血浓 时间变化符合三房室模型,AUC、C0 和T1 2 β分别为12 .97±3.5 5mg·L-1·h、132 .2 3±39.90mg·L-1和4 .0 4±1.2 9h。灌胃后药物吸收很快,但血浓低。采用非房室模型法计算AUC为1.97±0 .5 3mg·L-1·h ,T1 2Ke 为3.4 1±1.2 3h。绝对生物利用度为5 .0 5 %。结论:灯盏花素经静注在小鼠体内的药代动力学符合三室模型。灌胃给药吸收快,但吸收差,绝对生物利用度低,且药时曲线变化不规则。

AIM: To study the pharmacokinetics and absolute bioavailability of breviscapine in mice. METHODS: After iv injection (50 mg·kg -1) and ig administration (150 mg·kg -1) of breviscapine in mice, the plasma scutellarin concentration were detected by SPE-HPLC method. The pharmacokinetic parameters were calculated by 3p97 program. RESULTS: The plasma scutellarin concentration-time curve after iv injection of breviscapine was fitted with a three compartment model. AUC, C_0 and T_ 1/2β were 12.97 mg·h·L -1, 132.23 mg·L -1 and 4.04 h, respectively. After ig administration of breviscapine, the drug absorption was rapid, but the plasma concentration was very low. The parameters of AUC and T_ 1/2Ke calculated with non-compartment model were 1.966 mg·h·L -1 and 3.4 h, respectively. The absolute bioavailability was 5.05%. CONCLUSSION: The pharmacokinetics of breviscapine in mice after iv injection fitted with three-compartment model. After ig administration, the drug is absorbed rapidly but the absolute bioavailability is very low, and the changes of plasma concentration of scutellarin is not regulation.