目的 观察健康受试者单次和连续口服半枝莲总黄酮胶囊的耐受性和安全性，为Ⅱ期临床试验给药提供安全的剂量范围。方法 筛选36名受试者，随机分为单次给药组和连续给药组，单次给药组分别口服半枝莲总黄酮胶囊2、4、6、9粒，连续给药组分别每次口服2粒、3粒，tid，连续给药7 d。观察临床症状、体征，实验室指标（包括血常规、尿常规、便常规、肝肾功能、心电图等），记录可能出现的不良反应。结果 半枝莲总黄酮胶囊在单次6粒/次和连续3粒/次tid应用时，可能引起一过性腹泻的不良反应；上述剂量范围可能不会引起生命体征以及其他实验室指标的改变。结论 在观察剂量内，受试者对半枝莲总黄酮胶囊的耐受性和安全性较好。推荐Ⅱ期临床试验剂量为单次用药不超过9粒或连续给药不超过3粒/次，tid。

Objective To evaluate the tolerance and safety of total flavonoids of Scutellaria barbata capsule by single or multiple oral doses in healthy volunteers，and to assess the safety range of clinical use of drugs and given-drug project in phaseⅡclinical trial. Methods Thirty-six healthy volunteers were randomly divided into either single-dose or multiple-doses groups. In single-dose group, subjects received oral doses of 2, 4, 6 and 9 capsules; While in multiple-doses group, subjects received 2 or 3 capsules, thrice per day, for 7 d. The safety profiles and tolerability were evaluated by observing the symptoms, vital sign, and laboratory parameters including blood, urine routine, stool routine, liver and kidney function, ECG, and so on, at the same time, the adverse reactions which may occur were recorded. Results Slight diarrhea transient may occurr in volunteers with single dose of 6 capsules and multiple doses of 3 capsules, thrice per day. The above-mentioned dose range may not cause changes in vital signs and other laboratory parameters. Conclusion Total flavonoids of Scutellaria barbata capsule is safe and well-tolerated at the doses observed. Recommended phase II clinical trial dose is proved to be single dose of 9 capsules and successive dose of 3 capsules, thrice per day.

国家“十二五”重大新药创制科技重大专项课题（2011ZX09302-006-03）