保心微丸中肉桂酸大鼠体内的药代动力学研究

Pharmacokinetics of cinnamic acid of BAOXIN PILL in rat

目的 研究保心微丸中肉桂酸在大鼠体内的药代动力学。方法 采用高效液相色谱法测定肉桂酸血药浓度 ,色谱柱 :Hypersil ODS C1 8,15 0 mm× 4 .6m m ,5μm ,柱温 3 0℃。流动相 :甲醇 - 1%醋酸 ( 4 5∶ 5 5 ) :流速 :0 .5 m L /min;检测波长 2 73 nm;进样量 10 μL。结果与结论 :建立了用高效液相色谱法测定肉桂酸血药浓度的方法 ,肉桂酸的峰面积 ( Y)与浓度 ( X )之间的回归方程为 Y=4 973 .5 3 4 8+ 4 2 867.96678X ,相关系数 r=0 .9998。肉桂酸在血浆中的回收率为 97.5 % ,RSD为 1.3 3 %。检测限为 0 .15 ng,大鼠血浆中最低检测浓度为 75 ng/ m L。肉桂酸口服吸收在大鼠体内的药时过程为线性动力学过程 ,符合一级吸收一级消除的开放式室模型 ,t1 /2 ( Ka)为 7.12 min,tmax为 5 3 .2 9m in,Cmax为 0 .2 0 μg/ m L,t1 /2 ( Ke)为 3 4 0 .74 min。该药代动力学参数可能是保心微丸中肉桂酸及有关成分等多种成分在大鼠体内的综合体现。

Object To study the pharmacokinetics of cinnamic acid in BAOXIN PILL * in rat. Methods Plasma concentration of cinnamic acid was determined by HPLC under the following conditions: column: Hypersil ODS C 18 (150 mm×4.6 mm, 5 μm); column temperature 30 ℃; mobile phase methanol-1% acetic acid (45∶55); flow rate 0.5 mL/min; detection wavelength 273 nm; aliquot injected 10 μL. Results A method for the determination of plasma cinnamic acid concentration by HPLC was established. Regression equation of cinnamic acid peak area (Y) and plasma concentration (X) was found to be: Y= 4 973.534 8 +42 867.96 678 X; correlation factor r=0.999 8; rate of cinnamic acid recovery from plasma=97.50% and RSD=1.33%; detection limit=0.15 ng; minimal dectable concentration in rat plasma=75 ng/mL. Absorption pattern of cinnamic acid after ig does showed linearity, corresponding to a first order absorption and elimination of open chamber model. The t 1/2 (K a)=7.12 min; t max =53.29 min, C max =0.20 μg/mL, and t 1/2 (Ke)=340.74 min. Conclusion The pharmacokinetic parameters obtained in this study may be attributed to the combined action of cinnamic acid and other constituents in the compound preparation of BAOXIN PILL.