复方茵芩制剂中黄芩苷的药代动力学研究

Pharmacokinetics of Compound Yin-chen Granule in mice

探讨复方茵芩制剂有效成分黄芩苷在小鼠体内的药物代谢动力学特征,按16.5 g.kg-1(相当于黄芩苷239.5 mg.kg-1)的剂量给小鼠口服复方茵芩制剂,用高效液相色谱法(HPLC)检测用药后0.25、0.5、1.0、2.0、3.0、4.0、5.0、6.0、8.0、12.0、14.0、16.0、20.0、24.0、36.0、48.0、72.0 h血浆中药物黄芩苷的质量浓度,研究在小鼠体内的药物代谢动力学.结果表明,复方茵芩制剂中黄芩苷在小鼠体内的药时数据符合开放性二室模型,动力学方程为:C=16.76 e-0.45t+3.10 e-0.03t-20.99 e-2.13t;主要药代动力学参数:T1/2α1.54 h,T1/2β5.25±2.96 h,T1/2 Ka0.34 h,AUC0→∞128.99 mg.L-1.h-1,CL/F0.19 L.h-1,Vd/F6.363 L.kg-1,Tpeak1.05 h,Cmax11.19μg.mL-1.

To investigate the pharmacokinetics of Compound Yin-chen Granule in mice, effective component baicalin was detected as a representative index. Pharmacokinetics orally administered at the dose of 16.5 g·kg^-1 Yin-chen compound preparation （239.5 mg · kg^-1 baicalin） was investigated in mice. Serum concentrations of effective component baicalin in 0.25, 0.5, 1.0, 2.0, 3.0, 4.0, 5.0, 6.0, 8.0, 12.0, 14.0, 16.0, 20.0, 24.0; 36.0, 48.0, 72.0 hours were measured using HPLC, and concentration-time data were analyzed with Pharmaceutical Kinetics Software. The results showed that the serum profiles of the drug＇s effective component baicalin was best described by a two compartment open model. The pharmacokinetics equation was C = 16.76 e^-0.45 ＋3.10 e^-0.03 -20.99 e^- 2.13 and the main parameters of pharmacokinetics were as follows ： T1/2α 1.5357 h, T1/2 β （ 5.25 ± 2.96 ） h, T1/2ka, 0.34 h,AUC0→∞ 128.99 mg · L^-1 · h^-1, CL/F0.194 L · h^-1, Vd/F6.363 L·kg^-1, Tpeak 1.054 h,Cmax 11.19 μg · mL^-1.