乙氧苯柳胺软膏的Ⅰ期临床试验  

Phase Ⅰ Clinical Trial of Etofesalamide Ointment in Healthy Volunteers

作　　者：李俊[1] 汤晓林[1] 金涌[1] 李常玉[1] 徐叔云[1] 

机构地区：[1]安徽医科大学临床药理研究所,合肥230032

出　　处：《中国临床药理学杂志》2001年第3期192-194,共3页The Chinese Journal of Clinical Pharmacology

摘　　要：目的：观察中国健康志愿者对乙氧苯柳胺软膏的临床耐受性和单次给药的药代动力学过程．方法：２２名健康志愿者，分别单次外用乙氧苯柳胺软膏（２．５％，５％，１０％，１５％）各０．２５ｇ，进行人体耐受性试验；８名健康试验者，分别涂乙氧苯柳胺软膏４ｇ（１５％）４ｃｍ × ４ｃｍ，采用高效液相电化学检测器，检测血药浓度，进行药代动力学研究．结果：人体耐受性试验结果表明，四组志愿者均无明显的皮肤反应，也无异常的自觉症状；乙氧苯柳胺的血药浓度时间曲线符合一级吸收的一房室模型，其主要药代动力学参数为： ｔ１／２ｋａ　０.６６ ± ０．１９ｈ， ｔ１／２ｋｅ４．９４±１．０９ｈ，ｔｐｅａｋ２．１４±０．２７ｈ，Ｃｍａｘ２１．１±３．３μｇ·Ｌ－１，ＡＵＣ２１６±３１μｇ·Ｌ－１·ｈ－１。结论：人体对乙氧苯柳胺软膏具有良好的耐受性。OBJECTIVE:To study the tolerance and the pharmacokinetics of Etofesalmideointment in Chinese healthy volunteers.METHODS: Single dose (0.25g)of Etofesalamde ointment(2.5%,5%,10% and 15%)was spread respectively on the skins in 22 healthy volunteers and in eight healthy male volunteers,single dose etofesalamide 4g(15%)was spread respectively on the skins(4cm× 4cm). The concentrations of etofesalamide in plasma were measured by HPLC with electrochemical detector. RESULTS: All dosages were well tolerated and no Prohibitive findings were discovered and the concentrationtime curve of etofesalamide conformed to a one-compartment model with first order rate absorption and the main parameters were as follows: t1/2,ka0.66±0.19h, t1/2ke4.94±1. 09h, tpeak2.14±0.27h, Cmax21.1±3.3μg.L-1, AUC216±31μg.L-1.h-1.CONCLUSION: The tolerance of etofesalamide ointment is good for all volunteers.

关 键 词：乙氧苯柳胺 软膏 药物耐受性 药代动力学 皮肤药 

分 类 号：R986[医药卫生—药品]