枸橼酸爱地那非片Ⅰ期临床耐受性研究

Phase Ⅰ human tolerability trial of aildenafil citrate tablet

目的：观察枸橼酸爱地那非片在健康人体的安全性和耐受性。方法：单次给药试验共入选28例健康男性志愿者，随机分为4个剂量组，由初始剂量30mg开始，在耐受性较好的情况下，逐渐增加至60，90，120mg。连续给药试验在单次给药试验结束后进行，共入选36例健康男性志愿者，随机分为3个剂量组，递增剂量分别为30，45，60mg，qd，连续3d。观察临床症状体征并严密观察记录试验期间发生的不良事件。结果：单次给药试验与研究药物有关的不良事件主要为视觉异常（发生率35．7％），面色潮红（发生率21．4％），头痛或头晕（发生率17．9％）等；连续给药试验与研究药物有关的不良事件为面色潮红（发生率7．4％），头痛或头晕（发生率7．4％）。试验中未发生严重不良事件，所有不良事件的程度均为轻度，均未经处理均自行消失。给药后生命体征、实验室检查和眼科检查均未见有临床意义的改变。结论：中国男性健康受试者单次口服30～120mg的枸橼酸爱地那非片和连续3d，30～60mg qd的枸橼酸爱地那非片安全耐受。

Objective： To assess the tolerability and safety of aildenafil citrate tablet in healthy Chinese male volunteers. Methods： Twenty-eight healthy Chinese male subjects were recruited to the single dose study. They were divided into 30, 60, 90 and 120 mg dose step with 30 mg as the first dose step; safety and tolerability findings at the previous dose level were the basis for the decision to proceed to the next higher dose level. Thirty-six healthy Chinese male subjects were enrolled to the multiple dose study, and the escalated dose level were 30, 45 and 60 mg·d^-1, once daily for continuous 3 days. The safety was assessed based on clinical symptoms and adverse events. Results： In the single dose study, the adverse events judged by the investigator to be related to aildenafil citrate tablet were abnormal vision （35.7%）, flushing （：21.4%）, headache or dizziness （17.9%）. In the multiple dose study, the adverse events related to aildenafil citrate tablet were flushing （7.4%） , headache or dizziness （7.4%）. There were no serious adverse events; all adverse events were mild in severity and resolved without any treatment. There were no clinically significant changes in vital signs, clinical laboratory tests and ophthalmological examination. Conclusion： Aildenafil citrate tablet is safe and well-tolerated in Chinese male healthy subjects after single doses of 30 - 120 mg and multiple doses of 30 -60 mg, qd for 3 days.