异丁司特的临床安全性及体内药物浓度研究  

Study on the clinical safety and plasma concentration of ibudilast

作　　者：张伟[1] 戴丹萍[1] 金海英[1] 方雪期 

机构地区：[1]浙江宁波大学医学院附属医院药剂科,宁波315020 [2]浙江省宁波市药品检验所药剂科,宁波31500

出　　处：《海峡药学》2013年第4期277-279,共3页Strait Pharmaceutical Journal

摘　　要：目的通过对异丁司特安全性及体内药物浓度进行评价,为临床用药提供参考。方法 24位健康志愿者(男女各半)分成两组,每日口服40mg异丁司特或安慰剂首日单剂量20mg,从第三天开始每日2次,每次20mg,连续给药12d,期间对异丁司特血药浓度和临床不良反应进行了观察分析。结果异丁司特给药后约4h血药浓度达到峰值,平均稳态血浆浓度为60ng·mL-1。受试者对异丁司特耐受性良好,用药相关的不良反应主要包括多汗,头痛和恶心,无严重不良反应发生。结论异丁司特在较大剂量给药时安全性良好。OBJECTIVE To investigate the safety,tolerability and plasma concentration of ibudilast,which provide references for its clinical use.METHODS Healthy adult male（n=12） and female（n=12） volunteers were randomized 1∶ 2 to either oral placebo or ibudilast at 20-mg single administration followed by 12 days of 20 mg b.i.d.The ibudilast plasma concentration and clinical adverse reactions were analyzed during the trial.RESULTS Ibudilast reached peak plasma concentration approximately 4 hours after oral administration,with an average steady-state plasma concentration of 60ng·mL-1.Ibudilast was generally well tolerated in the subjects.Treatment-related adverse events included hyperhidrosis,headache and nausea,and no serious adverse events were observed.CONCLUSIONS Ibudilast potentially has a good safety profile for high-dose clinical applications.

关 键 词：异丁司特 不良反应 血药浓度 安全性 耐受性 

分 类 号：R969.4[医药卫生—药理学]