用生苍术与用麸炒苍术的四妙丸中盐酸小檗碱大鼠体内药代动力学比较研究

Comparison on pharmacokinetic differences of berberine hydrochloride between Simiao Pill with crude Atractylodis Rhizoma and bran stir-baked Atractylodis Rhizom

目的以四妙丸中的君药黄柏中的主要有效成分盐酸小檗碱为指标,对分别以生苍术及麸炒苍术入药的四妙丸大鼠体内的药代动力学差异进行比较。方法以吴茱萸碱为内标物,采用高效液相色谱法,建立了盐酸小檗碱大鼠体内的血药浓度测定方法,并对分别以生苍术及麸炒苍术入药的四妙丸灌胃给药后盐酸小檗碱的血药浓度进行测定,采用DASS2.0数据处理。结果以生苍术入药的四妙丸中,盐酸小檗碱在大鼠体内的C_(max)为0.123 mg/L,T_(max)为1.05 h,MRT_(0-24)为8.69 h,AUC_(0-24)为0.778 mg/L·h;以麸炒苍术入药的四妙丸中盐酸小檗碱在大鼠体内的C_(max)为0.096 mg/L,T_(max)为1.03 h,MRT_(0-24)为9.04 h,AUC_(0-24)为0.728 mg/L·h。结论以生苍术或麸炒苍术入药的四妙丸中盐酸小檗碱在大鼠体内的药代动力学参数无显著差别。

Objective To study the pharmacokinetic differences of berberine hydrochloride between Simian Pills with crude Atractylodis Rhizoma and bran stir- baked Atractylodis Rhizoma. Methods Strychnine was taken as the marker,HPLC method was used to determine the berberine hydrochloride contents in the plasm of rats after oral administration Simiao pills（ crude Atractylodis Rhizoma） and Simiao pills（ bran stir- baked Atractylodis Rhizoma）. Results The main pharmacokinetic parameters（ Simiao pills with crude Atractylodis Rhizoma） consisted of 1. 05 h（ T_（max））,0. 123 mg/L（ C_（max））,8. 692 h（ MRT_（0-24））,0. 778（ AUC_（0-24））; The main pharmacokinetic parameters（ Simiao Pills with bran stir- baked Atractylodis Rhizoma） consisted of 1. 025h（ T_（max））,0. 096 mg/L（ C_（max））,9. 037 h（ MRT_（0-24））,0. 728（ AUC_（0-24））; Conclusion There is no obvious differences on the pharmacokinetic parameters of berberine hydrochloride in Simiao pills（ crude Atractylodis Rhizoma） and Simiao pills（ bran stir-baked Atractylodis Rhizoma.