冰片对原儿茶酸在家兔体内药动学的影响

目的:研究冰片对原儿茶酸在家兔体内药动学的影响.方法:建立测定家兔血浆中原儿茶酸的高效液相色谱方法.将12只健康新西兰家兔随机分为2组,分别灌胃原儿茶酸(原儿茶酸30 mg·kg~(-1))及原儿茶酸.冰片(原儿茶酸30 mg·kg~(-1)+冰片15 mg·kg~(-1)),采用RP-HPLC法测定家兔给药后不同时间血浆中原儿茶酸的浓度,DAS 2.0药动学软件拟合房室模型,计算药动学参数.结果:原儿茶酸在0.04～2.0 mg·L~(-1)线性良好(r=0.998 3).原儿茶酸与冰片配伍给药可使原儿茶酸的吸收半衰期(t_(1/2Ka))明显减小,药物达峰时间(T_(max))显著缩短,血药浓度曲线下面积(AUC(_0～∞)))增加,表观清除率(CL/F).降低,同时表观分布容积(V_1/F)也相应的减小.结论:冰片促进原儿茶酸在家兔体内的吸收,使其吸收量增加,排泄减缓,可提高原儿茶酸的生物利用度.

Effects of borneol on pharmacokinetics of protocatechuic acid in rabbitsYANG Jie, WANG Shixiang, LAN Wei, LIU Chunzhi, ZHENG Xiaohui*

Objective: To study the effect of borneol on the pharmacokinetics of protocatechuic acid (PA) in rabbits.  Method: A method for determinating PA in rabbit plasma by high performance liquid chromatography (HPLC) was established. The 12 healthy New Zealand rabbits were randomly divided into 2 groups. PA concentration in plasma samples of rabbits was determined by HPLC after oral administration of PA (30 mg·kg-1) and PA combined with borneol (protocatechuic acid 30 mg·kg-1+borneol 15 mg·kg-1). The data were processed by DAS 2.0 software to calculate the pharmacokinetic parametes.  Result: Chromatographic peaks were separated well by the HPLC method. Regression analysis of the data of PA concentration against its peak area showed a good straight line in the range of 0.04-2.0 mg·L-1 (r=0.998 3). In comparison with PA alone, the pharmacokinetics parameters of PA (t1/2Ka, Tmax, V1/F, CL/F) in the PA+borneol combination group were decreased, while the AUC(0-∞) was increased.  Conclusion: Borneol could significantly promote absorption, increase the dose absorption and slow elimination of PA in rabbits. Borneol could improve the bioavailability of PA.