目的研究青木香及复方制剂冠心苏合胶囊中马兜铃酸A在小鼠体内的药动学特点及小鼠在ig给予含相同量马兜铃酸A的青木香和冠心苏合胶囊后,马兜铃酸A的吸收、分布规律的差异。方法采用RP-HPLC法测定血浆中马兜铃酸A的量。色谱条件色谱柱为DiamonsilTMC18柱(250mm×4.6mm,5μm),流动相为甲醇-水-冰醋酸(72∶27∶1),体积流量为1.0mL/min,检测波长为315nm,柱温为20℃。结果药动学实验结果显示小鼠分别ig给予青木香和冠心苏合胶囊(相当于2.5mg/kg马兜铃酸A)后,其体内的药动学房室模型均符合一室模型,青木香中马兜铃酸A主要药动学参数t1/2ka、t1/2ke,tmax、AUC、Cmax分别为5.103min、43.63min、17.89min、80.45(μg·min)/mL、0.9168μg/mL;冠心苏合胶囊中相应的参数分别为5.294min、43.50min、18.32min、33.08(μg·min)/mL、0.3818μg/mL。结论小鼠给予含马兜铃酸A相同剂量的青木香和冠心苏合胶囊后,冠心苏合胶囊中马兜铃酸A的Cmax明显低于青木香中的Cmax,说明复方配伍作用可减少马兜铃酸A的吸收。

objective To study the pharmaeokinetics of aristolochic acid A in Radix Aristolochiae andthe compound preparation of Guanxinsuhe Capsule in mice in vivo after single—dose oral administration andobserve the difference of aristolochic acid A absorption and distribution．Methods Aristolochic acid Aassay was performed by RP—HPLC on a Waters apparatus with a DiamonsilTM C18 column(250 mm×4．6mm，5Ⅲn)，a mobil phase{a mixture of methanol—water—acetic acid(72 I 27l 1)，flow rate：1．0 mL／min，detection wavelength：315 nm，and column temperature：20℃．Results Mice were given RadixAristolochiae and Guanxinsuhe Capsule by ig at the same level of 2．5 mg／kg of aristolochic acid A，respec— were suspended in 0．3％CMC—Na solution．Plasma concentrations were determined by RP—HPLC．After single—dose ig administration of Radix Aristolochiae or Guanxinsuhe Capsule to mice，themean plasma concentration—time courses of aristolochic acid A obtained fitted the one—compartment model．The main pharmacokinetic parameters of aristolochie acid A in Radix Aristolochiae，AUC，c。：are 5．103 rain，43．63 rain，1 7．89 min·80．45(pg·min)／mL，and 0．916 8／19／mL；the rela—tive pharmacokinetie parameters in Guanxinsuhe Capsule are 5．294 min，43．50 min，18．32 min，33．08(·min)／mL，and 0．381 8 vg／mL．Conclusion The of aristolochic acid A in Guanxinsuhe Capsuleis significantly less than that in Radix Aristolochiae，which indicates that the compound compability coulddecrease the absorption of aristolochiae acid A．

河北省科学技术研究计划项目(03276196D-2)