醋氯芬酸肠溶片在健康男性志愿者体内的药代动力学及生物等效性研究  

Pharmacokinetics and bioequivalance of aceclofenac enter-coated tablets in healthy male volunteers

作　　者：胡国新[1] 邱相君[1] 谢虹[2] 代宗顺[3] 王桂珍[2] 

机构地区：[1]温州医学院药理学教研室 [2]华中科技大学同济医学院环境卫生学教研室 [3]华中科技大学同济医学院临床药理学教研室

出　　处：《中国临床药理学与治疗学》2003年第3期329-332,共4页Chinese Journal of Clinical Pharmacology and Therapeutics

摘　　要：目的 :研究国产醋氯芬酸肠溶片在健康志愿者体内的药代动力学参数和生物等效性。方法 :2 0名健康男性志愿者随机交叉口服国产醋氯芬酸肠溶片 1 0 0mg和进口醋氯芬酸片 1 0 0mg,采用HPLC法测定给药后不同时间点的血浆醋氯芬酸浓度。用3p97程序计算其药代动力学参数 ,评价两种制剂的生物等效性和生物利用度。AUC0 - 2 4 ,AUC0 -inf和Cmax经方差分析和双单侧t检验。结果 :试验药和参比药的醋氯芬酸Cmax分别为 2 0±5mg·L- 1 和 2 0±6mg·L- 1 ;Tmax分别为 2 .7± 0 .5h和 2 .0±0 .5h;AUC0 - 2 4 分别为 5 5±2 6mg·h- 1 ·L- 1 和 5 2± 2 1mg·h- 1 ·L- 1 。试验药与参比药AUC0 - 2 4 之比和Cmax之比的 90 %可信区间分别为 92 .2 %～ 1 2 0 .7%和 91 .8%～ 1 1 8.9%。试验药的人体相对生物利用度为 1 1 2 %± 42 %。结论 :两种制剂的主要药代动力学参数均无显著性差异 ,具有生物等效性。试验药的生物利用度符合要求。AIM: To study the pharmacokinetics and bioequivalence of ac ec lofenac enter-coated tablets in healthy volunteers. METHODS: A single oral dose of 100 mg aceclofenac and the same dose of airtal were given t o 20 healthy male volunteers. Aceclofenac concentrations in plasma were determin ed by HPLC method. The parameters of pharmacokinetics were calculated by 3p97 pr ogram. The bioequivalence and bioavailability of the two formulations were analy sed. RESULTS: The C max of the test and re ference drug were 20±5 and 20±6 mg·L -1 , respectively; T max were 2.7 ± 0.5 and 2.0 ± 0.5 h, respectively; AUC 0-24 were 55±26 and 52±21 mg·h -1 ·L -1 . The 90% confident interval for AUC 0-24 -ratio and C max -ratio of the m ean values of test to reference formulations were 92.2 %- 120.7 % and 91. 8 %- 118.9 %, respectively. The bioavailability of the tested drug was 112%± 42%. CONCLUSIONS: There are no significant differences between the parameters of the two formulations, and the two formulations are bioequivale nce.

关 键 词：醋氯芬酸肠溶片 男性 药物代谢动力学 生物等效性 血浆 药理学 非甾体类抗炎药物 

分 类 号：R971.1[医药卫生—药品]