黄连、木香药对提取物中盐酸小檗碱在大鼠血浆中的药动学研究

Pharmacokinetic Study on Berberine in the Extract of Rhizoma Coptidis-Radix Aucklandiae Drug-pair in Rats

关键词:  黄连  木香  盐酸小檗碱  药动学

Key words:  Rhizoma Coptidis  Radix Aucklandiae  berberine  pharmacokinetics

摘要:

目的 大鼠灌胃黄连-木香药对提取物后，测定盐酸小檗碱在大鼠血浆中的药动学参数，研究药对配伍后对盐酸小檗碱在大鼠血浆中的影响。方法 采用高效液相色谱法测定大鼠灌胃后血浆中盐酸小檗碱的含量，色谱柱：Diamonsil C18(150 mm×4.6 mm，5 μm)；流动相：乙腈-水(42∶58)，每100 mL含有0.34 g磷酸二氢钾，0.17 g十二烷基硫酸钠；流速：1.0 mL·min-1；检测波长：349 nm，柱温：35 ℃。结果 药对提取物药动学参数：MRT(0-24)(12.470±1.538)h，MRT(0→∞)(29.711±7.176)h，AUC(0→24) (17.797±7.956)mg·L-1·h-1，AUC(0→∞)(92.522±53.784)mg·L-1·h-1，Tmax 2 h，Cmax(1.360±0.042)mg·L-1。结论 黄连、木香药对配伍后，采用DAS2.0软件处理，房室模型拟合分析，药室模型符合一房室模型。

Abstract:

OBJECTIVE The pharmacokinetic parameters of berberine in rat plasma were studied after oral administration to the monomer of drug-pair of Rhizoma Coptidis-Radix Aucklandiae and explored the pharmacokinetics effect on berberine in rat plasma after oral administration to drug-pair. METHODS The HPLC method was used to determine the quantity of berberine in rat plasma. The Diamonsil C18(150 mm×4.6 mm，5 μm)column was used, the mobile phase consisted of acetonitrile and water (42∶58), including 0.34 g Potassium dihydrogen phosphate and 0.17 g Sodium dodecyl sulfate per 100 mL, the flow rate was 1.0 mL·min-1, the UV detector was operated at 349 nm and the column temperature was controlled at 35℃. RESULTS Pharmacokinetic parameters of the extract of drug-pair: MRT(0-24)(12.470±1.538)h，MRT(0→∞) (29.711±7.176)h，AUC(0→24) (17.797±7.956) mg·L-1·h-1，AUC(0→∞)(92.522±53.784) mg·L-1·h-1，Tmax 2 h，Cmax(1.360±0.042) mg·L-1. CONCLUSION Drug-pair of Rhizoma Coptidis-Radix Aucklandiae is one-compartment model.