目的 研究痰热清注射液不同组分配伍给药对3种活性标志物黄芩苷、熊去氧胆酸、鹅去氧胆酸在大鼠体内药动学的影响，探讨痰热清注射液配伍的合理性。方法 将36只SD大鼠随机分成6组，分别尾iv给予黄芩提取物、熊胆粉提取物、黄芩＋熊胆粉、黄芩＋山羊角提取物、黄芩＋熊胆粉＋山羊角、黄芩＋熊胆粉＋山羊角＋金银花提取物1次。LC-UV方法测定黄芩苷的血药浓度，LC-MS方法测定熊去氧胆酸和鹅去氧胆酸的血药浓度，WinNonlin 6.3软件计算药动学参数。结果 痰热清注射液不同配伍给药后，熊去氧胆酸和鹅去氧胆酸的药动学参数无显著差异，仅使黄芩苷的AUC发生改变，且其AUC值呈现黄芩<黄芩+山羊角<黄芩+熊胆粉+山羊角<黄芩+熊胆粉+山羊角+金银花的变化，但差异无统计学意义。熊去氧胆酸和鹅去氧胆酸的药动学参数基本未发生改变，表明不同配伍不改变熊去氧胆酸和鹅去氧胆酸的药动学行为。结论 痰热清注射液不同配伍可影响黄芩苷在大鼠体内的药动学行为，增加其暴露量，但不影响熊去氧胆酸和鹅去氧胆酸的药动学行为。

Objective To study the pharmacokinetic effect of three active markers, baicalin (BC), ursodeoxycholic acid (UDCA), and chenodeoxycholic acid (CDCA) in plasma of rats after iv administration of Tanreqing Injection (TI) in various compatibilities, which contained scutellaria extraction (SE), bear gall powder extraction (BE), Cornu caprae hircus extraction (CE) and Lonicerae Flos extraction (FE), including SE, BE, SE-BE (SE and BE), SE-CE (SE and CE), SE-BE-CE (SE, BE and CE), and SE-BE-CE-FE (SE, BE, CE, and FE):. To discuss the rationality of TI compatibility, the effects of TI in various compatibilities on the pharmacokinetics of BC, UDCA, and CDCA in plasma of rats were investigated. Methods Thirty-six experimental rats were randomly divided into six groups, and treated with SE, BE, SE-BE, SE-CE, SE-BE-CE, and SE-BE-CE-FE. After the simultaneous extraction of the three major bioactive components in plasma of rats, the concentration of BC was determined using LC-UV method, and UDCA as well as CDCA was determined using LC-MS method. The experimental data were analyzed by WinNonlin 6.3 software and the pharmacokinetic parameters of BC, UDCA, and CDCA in these recipes were evaluated. Results The pharmacokinetic parameters of UDCA and CDCA did not change after iv administration of TI in various compatibilities. However, the TI in various compatibilities increased the AUC of BC after iv administration. The change degrees were SE < SE-CE < SE-BE-CE < SE-BE-CE-FE but with no statistical significance. The pharmacokinetic parameters of UDCA and CDCA did not obviously change, which indicated that the different compatibilities did not change the pharmacokinetic behavior of UDCA and CDCA . Conclusion TI in various compatibelities could increase the exposure of BC following the iv administration, but could not affect the pharmacokinetic behaviors of UDCA and CDCA.

国家重点基础研究发展计划（“973”计划）（2011CB505300，2011CB505303）