关键词: 黄连解毒散, 超微粉, 小檗碱, 药代动力学, 生物利用度

Abstract: 【Objective】This paper aimed at studying the effect of ultromicro-pulverization method on pharmacokinetics of the berberine in Huanglian jiedusan 【Method】HPLC method was applied to determine of the concentration of plamsa berberine in rabbits which were given the ultra micro-powder and the common powder of Huanglian jiedusan by po 4mg·kg-1 respectively. The plasma concentration-time curve of berberine was dealt with PKS pharmacokinetics software, then pharmacokinetics characteristics were compared between the ultra micro- powder and the common powder of Huanglian jiedusan. 【Result】The results showed that the best pharmacokinetics model of berberine in two groups were all two-compartment open model. The main pharmacokinetic parameters of berberine in ultra micro- powder were as below：A =0.672 (μg/mL), α=0.641(1/h) , B=0.015(μg/mL), β=0.0241( 1/h) , Ka=0.911(1/h), t1/2a=1.08(h)，t1/2β=28.72(h)，AUC0→∞=0.895(μg·h /mL)，Vd =185.25(L/kg)，Tpeak=1.48(h), Cmax=0.0913(μg/mL)；The main pharmacokinetic parameters of berberine in common powder were as below：A=0.557(μg/mL) , α=0.520(1/h), B=0.0150(μg/mL), β=0.0367( 1/h) , Ka=0.617(1/h), t1/2a=1.33(h)，t1/2β=23.56(h), AUC0→∞=0.613(μg·h /mL), Vd/F=178.02(L/kg)，Tpeak=1.934(h)，Cmax=0.0565(μg/mL). Compared to common powder, ultra micro- powder has shorter Tpeak and increased Cmax and the relative bioavailability of berberine in the ultramicro-powder was improved by 46.00%. 【Conclusion】the ultromicro-pulverization method could promote the absorption and distribution of HLJDS in body and then improve the bioavailability of berberine in Huanglian jiedusan significantly.