目的 探讨川芎、延胡索中主要活性成分在模型与正常大鼠体内药动学规律与差异。方法 SD大鼠分为对照组和子宫内膜异位症模型组, 每组8只, 各组均按川芎嗪50 mg/kg、阿魏酸30 mg/kg、延胡索乙素20 mg/kg ig给药, 采用高效液相色谱法测定各组大鼠血浆中川芎嗪、阿魏酸和延胡索乙素的质量浓度, DAS2.0程序计算药动学参数。结果 模型组川芎嗪药时曲线下面积(AUC_0~t)、达峰浓度(C_max)、达峰时间(t_max)、半衰期(t_1/2)和平均驻留时间(MRT_0~t)与对照组相比差异均不显著(P>0.05);模型组阿魏酸AUC_0~t、C_max、t_max都小于对照组, 但差异没有显著性(P>0.05), t_1/2、MRT_0~t显著小于对照组(P<0.05);模型组延胡索乙素AUC_0~t、C_max、t_max、MRT_0~t均显著大于对照组(P<0.05)。结论 川芎、延胡索主要活性成分在正常大鼠和模型大鼠的体内过程有所不同。阿魏酸在模型大鼠体内消除更快, 延胡索乙素在模型大鼠体内吸收浓度更高、消除更慢, 川芎嗪在正常及模型大鼠的体内过程无显著性差异。

Objective To study the in vivo pharmacokinetic law and difference of active compounds from Chuanxiong Rhizoma and Corydalis Rhizoma between control and model rats. Methods Sixteen Sprague-Dawley rats were randomly divided into two groups: control and model rats with endometriosis, eight rats in each group. All the rats were ig administrated of tetramethylpyrazine (50 mg/kg), ferulic acid (30 mg/kg), and tetrahydropalmatine (20 mg/kg). All the concentration of tetramethylpyrazine, ferulic acid, and tetrahydropalmatine in plasma was analyzed by RP-HPLC and the data were treated by DAS 2.0 program. Results The main pharmacokinetic parameters of tetramethylpyrazine in the model group, such as AUC_0~t, C_max, t_max, t_1/2, and MRT_0~t, were no significant difference compared with the control group (P > 0.05), and AUC_0~t, C_max, and t_max of ferulic acid in model group were less than those in the control group with no significant difference (P > 0.05); t_1/2 and MRT_0~t of ferulic acid in the model group were obviously less than those in control group (P<0.05); AUC_0~t, C_max, t_max, and MRT_0~t of tetrahydropalmatine in the model group were bigger than those in the control group with significant difference (P < 0.05). Conclusion There is difference of pharmacokinetics of the main active compounds from Chuanxiong Rhizoma and Corydalis Rhizoma between model and control rats. Ferulic acid is removed more quickly in model rats, tetrahydropalmatine is absorbed highly but removed slower, tetramethylpyrazine is no significant difference comparee with the control group.

重庆市重大科技攻关项目(CSTC2008AA5004);重庆市自然科学基金项目(CSTC2012jjA10012)