目的 觀察健康受試者單次和連續(xù)口服半枝蓮總黃酮膠囊的耐受性和安全性，為Ⅱ期臨床試驗(yàn)給藥提供安全的劑量范圍。方法 篩選36名受試者，隨機(jī)分為單次給藥組和連續(xù)給藥組，單次給藥組分別口服半枝蓮總黃酮膠囊2、4、6、9粒，連續(xù)給藥組分別每次口服2粒、3粒，tid，連續(xù)給藥7 d。觀察臨床癥狀、體征，實(shí)驗(yàn)室指標(biāo)（包括血常規(guī)、尿常規(guī)、便常規(guī)、肝腎功能、心電圖等），記錄可能出現(xiàn)的不良反應(yīng)。結(jié)果 半枝蓮總黃酮膠囊在單次6粒/次和連續(xù)3粒/次tid應(yīng)用時(shí)，可能引起一過性腹瀉的不良反應(yīng)；上述劑量范圍可能不會(huì)引起生命體征以及其他實(shí)驗(yàn)室指標(biāo)的改變。結(jié)論 在觀察劑量?jī)?nèi)，受試者對(duì)半枝蓮總黃酮膠囊的耐受性和安全性較好。推薦Ⅱ期臨床試驗(yàn)劑量為單次用藥不超過9?；蜻B續(xù)給藥不超過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.

國家“十二五”重大新藥創(chuàng)制科技重大專項(xiàng)課題（2011ZX09302-006-03）