黄芩素与黄芩苷大鼠体内药动学比较研究

Comparison of Pharmacokinetics of Baicalein and Baicalin in Rats

目的对黄芩素与黄芩苷的大鼠体内药动学行为进行比较研究。方法采用高效液相-电化学色谱法,对等摩尔剂量灌胃给药黄芩素和黄芩苷后,大鼠体内黄芩苷的血药浓度进行测定。结果灌胃给药黄芩素740μmol.kg-1时,原型药完全被代谢,血浆中主要检测到代谢产物黄芩苷;分别灌胃给药等摩尔剂量的黄芩素和黄芩苷740μmol.kg-1后,大鼠血浆中黄芩苷的药-时曲线均呈现双峰现象,ρmax分别为14.63,10.92mg.L-1和8.51,4.87mg.L-1,AUC0～24h分别为149.63和63.68mg.h.L-1;黄芩素的相对生物利用度为235.9%。结论等摩尔剂量下黄芩素与黄芩苷的药动学行为具有显著差异,口服黄芩素比黄芩苷的达峰浓度高、生物利用度高。

OBJECTIVE To compare the pharmacokinetic behavior of baicalein and baicalin in rats.METHODS The concentration of baicalin in rat plasma was determined by a HPLC-ECD method after oral administration of baicalein and baicalin at the equivalent dose.RESULTS After oral administration of baicalein 740 μmol·kg^-1,the baicalein was metabolized entirely and the metabolite baicalin was detected mainly in rat plasma.The plasma drug concentration-time curves of baicalin both showed two peaks after oral administration of baicalein and baicalin at the equivalent dose 740 μmol·kg^-1 to rats,the ρmax values were 14.63,10.92 mg·L^-1 and 8.51,4.87 mg·L^-1,and the AUC0～24 h were 149.63 and 63.68 mg·h·L^-1,respectively.The relative bioavailability of baicalein was 235.9%.CONCLUSION There were marked differences in the pharmacokinetics between oral administration of baicalein and baicalin at the equivalent dose,and the ρmax values were higher and the bioavailability was better for oral administration of baicalein compared with that of baicalin.