黄芩甙在兔脑水肿模型中血浆和脑脊液的药代动力学

Plasma and cerebrospinal fluid pharmacokinetics of baicalin in the rabbit model of brain edema

摘要:

目的测定黄芩甙在兔感染性脑水肿模型血浆和脑脊液中的药代动力学参数和脑脊液渗透性。方法采用高效液相色谱法（ＨＰＬＣ）同时测定血浆和脑脊液中黄芩甙浓度。结果血浆黄芩甙的浓度－时间曲线下的面积（ＡＵＣｐ）每小时３０．６３±９．２１μｇ／ｍｌ，半衰期（ｔ１／２ｐ）２．１９±０．４２ｈ，峰浓度（Ｃｍａｘｐ）５６±７．６μｇ／ｍｌ。黄芩甙在脑脊液浓度－时间曲线下的面积（ＡＵＣｃｓｆ）每小时１０．２９±５．６μｇ／ｍｌ，半衰期（ｔ１／２ｃｓｆ）２．３１±０．３７ｈ，峰浓度（Ｃｍａｘｃｓｆ）２．３５±１．２３μｇ／ｍｌ，达峰时间（ｔｍａｘｃｓｆ）２．３３±０．４ｈ，比血浆达峰时间明显滞后。脑脊液和血浆浓度－时间曲线下面积之比（ＡＵＣｃｓｆ／ＡＵＣｐ）达０．３２（＞０．２）。结论黄芩甙在兔感染性脑水肿模型脑脊液中具有较好的渗透性。

Abstract:

Objective To study the pharmacokinetics and cerebrospinal fluid penetration of baicalin in brain edema induced by pertussis bacilli in rabbits. Methods Baicalin concentrations of plasma and cerebrospinal fluid samples were determined by high-performance liquid chromatography. Results In plasma, area under the drug concentration-time curve (AUCp) was 30.63±9.21 μg/ml per hour, half-life (t 1/2p ) was 2.19±0.42 h, and time of maximum plasma concentration (Cmax p) was 56±7.6 μg/ml. In cerebrospinal fluid, AUCcsf was 10.29±5.6 μg/ml per hour, half-life (t 1/2csf ) was 2.31±0.37 h , maximum CSF concentration (Cmax csf) was 2.35±1.23 μg/ml, and time of maximum CSF concentration (tmax csf) was 2.33±0.4 h .The ratio of AUC in plasma and CSF (AUCcsf/AUCp) was 0.32 (>0.2). Conclusions There is a better CSF penetration of baicalin observed in infectious brain edema in rabbits.