目的：建立生脉注射液中人参皂苷Rb 1 在心绞痛患者体内的PK-PD结合模型。方法：10名稳定性心绞痛受试者静脉滴注生脉注射液，连续给药14天，于给药后不同时间点采集血浆样品，采用质谱法检测人参皂苷Rb 1 的血药浓度，绘制药-时曲线，进行非房室模型拟合并计算PK参数；以受试者的收缩压和舒张压作为药效指标，进行PK-PD模型的拟合，计算PK-PD结合模型参数。结果：10名受试者静脉滴注生脉注射液后，人参皂苷Rb 1 在心绞痛受试者体内的药动学过程符合一室模型，生脉注射液中人参皂苷Rb 1 的降压效应滞后于血药浓度，效应与效应室浓度呈良好的相关性，符合Inhibitory Effect Imax模型。结论：该研究成功建立了生脉注射液中人参皂苷Rb 1 在心绞痛患者体内的PK-PD结合模型，可有效地用于评价生脉注射液的药效物质基础。

This study was aimed to establish the pharmacokinetics-pharmacodynamics (PK-PD) model of ginsenosideRb 1 following the intravenous administration of Shengmai injection in subjects with stable angina pectoris. A total ofstable angina pectoris were selected and received Shengmai injection for 14 days. Plasma samples were collected at different time points. Plasma concentrations of ginsenoside Rb 1 were determined by liquid chromatography- mass spectrometry (LC/MS). The concentration-time curves (AUC) were drawn, and then the PK parameters were calculated.The systolic pressure and diastolic pressure were monitored, and the combined PK-PD model was established based on the theory of effect compartment. The results showed that PK of ginsenoside Rb 1 conformed to a mono-compartment model. The effect of Shengmai injection lagged behind the concentrations of ginsenoside Rb 1 in plasma. The effect exhibited good correlation with ginsenoside Rb 1 in effect compartment. The relationship between effect and plasma concentrations fits the Inhibitory Effect Imax model. It was concluded that the study successfully established the combined PK-PD model of ginsenoside Rb 1 in subjects with angina pectoris. The model can efficiently evaluate the effective substance of Shengmai injection.

科学技术部国家"十二五"重大新药创制项目（2012ZX09303-017）：中药新药临床评价研究技术平台，负责人：李国信；国家中医药管理局国家临床重点专科建设项目经费资助（2013年），负责人：李国信；国家中医药管理局临床中药学重点学科（2009年），负责人：李国信；辽宁中医药大学杏林学者青蓝工程（2013年），负责人：李国信。