摘要
目的：观察奥兰替胃康片（枳实总黄酮苷提取物）在健康志愿者中的安全性和耐受性。方法：单次给药组38名健康志愿者分为7个剂量组,分别给予奥兰替胃康片100,300,600,1 000,1 600,2 400和3 000 mg（1片,n=4;3片,n=4;6片,n=6;10片,n=6;16片,n=6;24片,n=6;30片,n=6）。多次给药组12名健康志愿者分为2个剂量组,分别给予奥兰替胃康片200 mg（2片,n=6）或400 mg（4片,n=6）,tid,连续给药7 d。观察受试者的临床症状和体征、生命体征、实验室检查、心电图检查、腹部彩色B超及不良事件。结果：共32名健康志愿者完成了耐受性试验。单次、多次试验均未发生严重不良事件。单次给药试验和多次给药试验中,受试者均未出现有临床意义的体格检查、实验室检查、心电图检查异常。单次给药1 000mg组发生了5例不良事件,很可能与试验药物有关;1 600,2 400,3 000 mg组停止进行试验。多次给药试验中无不良事件发生。结论：奥兰替胃康片在100~600 mg范围内用药的安全性和耐受性良好。单次给药的最大耐受剂量为600 mg。多次给药每次200~400 mg,tid,连续7 d安全且耐受性好。推荐的II期临床试验的给药方案为每次400 mg,tid。
Objective： To assess the tolerance and safety of Weikang tablet（total flavonoid glycosides from aurantii fructus immaturus） in Chinese healthy volunteers.Methods： Thirty-eight healthy volunteers were enrolled,and took 7 single oral doses of 100,300,600,1 000,1 600,2 400 and 3 000 mg（1,3,6,10,16,24,30 tablets;n=4,4,6,6,6,6,6 subjects in each group,respectively）.Twelve healthy volunteers took oral multi-doses of 200 and 400 mg（2 and 4 tablets;n= 6 subjects in each group）,three times a day,for consecutive 7 days.The safety was evaluated based on clinical symptoms,vital signs,physical examinations,ECG,laboratory tests,abdominal CDFI and adverse events.Results： Three higher single-dose trials（1 600,2 400,3 000 mg） were canceled because more than half of subjects experienced adverse reactions in 1 000 mg dose group.Totally,32 healthy volunteers completed the tolerance test.No serious adverse events and clinically significant changes in vital signs,ECG,laboratory tests,and abdominal CDFI were found both in single-dose groups and multi-dose groups.In single-dose trial,diarrhea with abdominal discomfort occurred in 5 patients in 1 000 mg dose group,which were mild,transient,and recovered spontaneously following drug discontinuation.These were the adverse events related to the studied drug.There was no any adverse events after multi-doses administration of Weikang tablet.Conclusion： Weikang tablet is safe and well-tolerated in Chinese healthy subjects after administration of single-doses（100～600 mg） and multi-doses（200～400 mg,three times a day for consecutive 7 days）.The maximum tolerated dose of Weikang tablet is at 600 mg in the single-dose trial.The dose regimen of 400 mg,three times a day,is recommended for phase II study.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2011年第1期41-46,共6页
Chinese Journal of New Drugs
关键词
奥兰替胃康片
枳实总黄酮苷提取物
单次给药
多次给药
Ⅰ期临床试验
耐受性
Weikang tablet
total flavonoids glycoside from aurantii fructus immaturus
single-dose
multi-dose
phase I clinical trial
tolerance.
