探讨超微粉碎技术对黄连解毒散有效成分栀子苷的药代动力学影响。黄连解毒散分别制成超微粉和细粉，以4g/kg体质量的剂量分别灌服给家兔，采用HPLC测定家兔体内栀子苷的血药浓度，血药浓度-时间数据经药代动力学分析软件PKS处理，比较黄连解毒散超微粉及其细粉中栀子苷在家兔体内的药代动力学参数。结果显示，黄连解毒散超微粉及其细粉中栀子苷的药代动力学最佳房室模型均为一级一室开放模型。其主要药代动力学参数分别为：药物的吸收相半衰期T1/2ka为0.14，0.36h，药物的消除相半衰期T1/2ke为1.70，1.41h，达峰时间Tpeak为0.672，0.957h，达峰浓度Cmax为0.627，0.419μg/mL，血药浓度-时间曲线下面积（AUC）为1.899，1.356μg·h/mL，与细粉比较，黄连解毒散超微粉达峰时间提前0.285h；峰浓度提高49.64%；血药浓度-时间曲线下面积增加40.04%。结果表明，超微粉碎技术可显著提高黄连解毒散有效成分栀子苷的生物利用度。
To study the pharmacokinetics of geniposide as the effective ingredient of ultramicro pulverized powder of Huanglian Jiedusan (HLJDS) in rabbits in vitro, the plasma concentration of geniposide was determined by HPLC in two groups of rabbits after they were administered with ultramicro powder and ordinary powder of HLJDS at a single dose (4g/kg bw) by gastrogavage, respectively. The plasma concentration-time data of geniposide was analyzed with Pharmaceutical Kinetics Software (PKS). Pharmacokinetics characteristics in both groups were compared. The results show that the best pharmacokinetics model of geniposide in two groups is all one-compartment open models. The main pharmacokinetic parameters of geniposide are as follows: T1/2ka is 0.14h and 0.36h, T1/2ke is 1.70h and 1.41h, Tpeak is 0.672h and 0.957h, Cmax is 0.627μg/mL and 0.419μg/mL, AUC is 1.899(μg·h)/mL and 1.356(μg·h)/mL, respectively. Tpeak is elevated by 0.285h, Cmax is enlarged by 49.64%, and AUC is raised by 40.04%. It is indicated that the bioavailability of geniposide in HLJDS could be greatly improved by the technique of ultramicro pulverization.
