胃肠安丸中主要成分厚朴酚及和厚朴酚的药代动力学研究

Pharmacokinetics of magnolol and honokiol in Weichang'an pill

采用HPLC-MS/MS多反应监测(MRM)定量分析,以布洛芬为内标物在负离子模式条件下建立血样中厚朴酚及和厚朴酚药物浓度的测定方法,探讨不同剂量胃肠安丸口服给药后木脂素类成分的药代动力学过程,为进一步揭示胃肠安丸抗腹泻作用的物质基础提供理论依据。血浆样品中厚朴酚、和厚朴酚分别在5.25~1 344.00,10.08~2 580.00μg·L^(-1)线性关系良好;精密度、稳定性及提取回收率实验结果表明,该类成分血药浓度的测定方法稳定可靠。口服给药后所测成分血药浓度均随给药剂量的增加而增大,木脂素类成分Tmax为0.55~1.42 h,厚朴酚、和厚朴酚Cmax分别可达到996.36~2 330.96,189.87~1 469.43μg·L^(-1)。胃肠安丸口服给药后木脂素类成分入血吸收速度较快,为证明胃肠安丸口服给药后抗腹泻作用起效快、疗效持久提供实验依据。

To conduct multiple-reaction monitoring（ MRM） quantitative analysis with high-performance liquid chromatography coupled with mass spectrometry method,establish the quantification method of magnolol and honokiol in blood sample under negative ion mode with ibuprofen as internal standard,investigate the pharmacokinetic process of lignans constituents after oral administration of Weichang＇an pill（ WCA） at different doses,and provide theoretical basis to further reveal the material basis of WCA＇ s anti-diarrhea effect. In the plasma samples,the linear relationship was good over the concentration range of 5. 25 to 1 344. 00 μg·L-（-1）for magnolol and 10. 08 to 2 580. 00 μg·L-（-1）for honokiol. The results of precision,stability,and extraction recovery tests showed that the determination method of plasma concentration for such compositions was stable and reliable. Dose-dependence was shown for magnolol and honokiol in the plasma concentration-time profile. The results indicated that the time to reach the maximum plasma concentration（ T_（max））for lignanoids was 0. 55-（-1）. 42 h,when the maximum plasma concentration（ C_（max）） could reach 996. 36-2 330. 96,189. 87- 1 469. 43 μg·L-（-1）respectively for magnolol and honokiol. The lignanoids could be absorbed rapidly in the blood after oral administration of WAC pills,providing experimental basis to prove rapid and long-acting anti-diarrhea effect of WAC pills after oral administration.