目的：以舒血宁注射液为示范，探索中药进行0期临床药代动力学试验的可行性。方法：检测健康受试者在静脉滴注微剂量舒血宁注射液后的血药浓度；按照倍数分布关系，以单次给药爬坡的方式摸索血药浓度的最小检测剂量，计算药动学参数；以临床用药剂量为对照，考察药动学规律。结果：在舒血宁注射液微剂量组的药动学检测中，血药浓度低于检测下限；单次给药爬坡组在相当于临床给药剂量的1/25以上时，可以检测到血药浓度。结论：与临床给药剂量组相比，低剂量给药具有大致相同的药物代谢趋势，0期临床药代动力学试验。

This paper was aimed to explore the possibility for pharmacokinetics experiment of phase 0 clinical trial in traditional Chinese medicine (TCM). The plasma concentration of volunteers after being injected with micro- doseShuxuening Injection was tested. According to multiple distributions, the minimum detectable dose was explored by increasing single dose, in order to calculate the pharmacokinetics parameters and to find out the law in thepharmacokinetics experiment by comparing with the clinical dosage. The results showed that in the micro-dose group,concentrations cannot be detected. In the single-dose climbing group, the concentration was tested out above 1/25 ofclinical dosage. It was concluded that compared with the clinical group, low-dose has similar metabolic tendency ofdrugs. It is possible to conduct pharmacokinetics experiment of phase 0 clinical trial in TCM.

国家科技部“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，负责人：李国信；辽宁省科技厅科学技术计划项目（2015225015）：肺系重大疾病中医转化医学规范化研究，负责人：李国信。