黄芩苷镁盐和黄芩苷的肠吸收动力学和药代动力学比较

Comparison of Intestinal Absorption Kinetics and Pharmacokinetics of Baicalin Magnesium Salt and Baicalin

目的：比较黄芩苷镁盐和黄芩苷的肠吸收动力学和药代动力学的异同。方法：采用高效液相色谱法（HPLC）测定样品中黄芩苷镁盐和黄芩苷的含量,计算黄芩苷镁盐的吸收速率常数（Ka）,每小时单位体积的肠吸收量（Abs）,表观渗透系数（Papp）等肠吸收动力学参数和药时曲线下面积（AUC0-t）等药动学参数,明确黄芩苷镁盐的肠吸收动力学和药动学特征。通过SPSS 19.0软件进行数据分析,探讨黄芩苷镁盐与黄芩苷在体和体内的吸收差异。结果：肠吸收动力学结果表明黄芩苷镁盐的Ka为黄芩苷的16.33倍,Abs为黄芩苷的1.78倍,Papp为黄芩苷的15.75倍,统计学差异明显（P〈0.05）。但药动学数据显示黄芩苷镁盐的药峰浓度（Cmax）,AUC0-t,达峰时间（Tmax）和血浆清除率（CLz）与黄芩苷比较均无统计学差异。结论：与黄芩苷比较,黄芩苷镁盐在大鼠肠道的吸收更好,且吸收迅速。黄芩苷镁盐灌胃给药后药动学特征与黄芩苷无显著性差异,原因是黄芩苷镁盐经体内胃酸的作用被还原成为了黄芩苷。

Objective： To compare the similarities and differences of intestinal absorption kinetics and pharmacokinetics between baicalin magnesium salt and baicalin.Method： HPLC was employed to determine the contents of baicalin magnesium salt and baicalin in samples,and the intestinal absorption kinetics parameters,such as absorption rate constant（Ka）,intestinal absorption per unit volume within one hour（Abs）,apparent permeability coefficient（Papp） and pharmacokinetics parameters such as the bioavailability（AUC0-t） were figured out.That was not only clarified the behaviors of baicalin magnesium salt,but also discussed the differences of the absorption of baicalin magnesium salt and baicalin in vivo and in suit by SPSS 19.0 statistical software.Result：The Ka,Abs and Pappof baicalin magnesium salt were 16.33,1.78,15.75 times than these of baicalin with significant difference（P〈0.05）.However,these pharmacokinetic data showed that AUC0-t of baicalin magnesium salt had no significant differences by comparing with baicalin,as well as parameters of Cmax,Tmax and CLz.Conclusion： The intestinal absorption of baicalin magnesium salt in whole intestine tract of rats is better and quicker than baicalin.Meanwhile,pharmacokinetic characteristics of baicalin magnesium salt after oral administration are not significantly different from these of baicalin,because it can be reduced into baicalin under the action of gastric acids in the body.