多剂量口服复方布洛芬缓释片与普通片的药代动力学及相对生物利用度  

Pharmacokinetics and Relative Bioavailability after Multiple Doses Oral of Sustained Release and Conventional Tablets of Ibuprofen in Male Volunters

作　　者：吴琳华[1] 赵红光[1] 樊宏伟[1] 曲福军[1] 金锐[1] 张一飞[1] 于景翠[1] 付红焱[1] 

机构地区：[1]哈尔滨医科大学附属第二医院,哈尔滨150086

出　　处：《中国临床药理学杂志》2001年第2期129-132,共4页The Chinese Journal of Clinical Pharmacology

摘　　要：目的：对２０名健康男性受试者分别多剂量交叉口服复方布洛芬缓释片２片，１２ｈ一次，普通片１片，６ｈ一次，共服６ｄ的药代动力学及相对生物利用度进行研究。方法：采用高效液相色谱法测定制剂中布洛芬及盐酸伪麻黄碱的血浆药物浓度。结果：缓释片与普通片中布洛芬的ＡＵＣｓｓ分别为２６３．３１± ２５．５５ｍｇ·ｈ·Ｌ－１和２７１．２６ ± ２９．７０ｍｇ·ｈ·Ｌ－１， ｔｍａｘ分别为７．４７ ± ０．８２ｈ和２．０５ ± ０．４９ｈ， Ｃｍａｘ分别为 １８４２± ２．６１ｍｇ·Ｌ－１和２５．７４ ± ５．０９ｍｇ·Ｌ－１， Ｃ分别为 １１．４４ ± １．４５ｍｇ·Ｌ－１和 １０．９１±１．９３ｍｇ·Ｌ－１。缓释片与普通片中盐酸伪麻黄碱的ＡＵＣｓｓ分别为３４６８．１４± １３６．４６μｇ·５·Ｌ－１和３４６６．７２±１６８．２０μｇ·ｈ·Ｌ－１，ｔｍａｘ分别为４．４１±０．２７ｈ和２．２７±０．７１ｈ，Ｃｍａｘ分别为 ２７５．２０± ２６．８２ｍｇ·Ｌ－１和 ３０７．８９± ２４．０９μｇ·Ｌ－１， Ｃｍｉｎ分别为 １４７．８９± １８．２４μｇ·Ｌ－１和１２６．６２±１８．２２μｇ·Ｌ－１。缓释片对普通片的相对生物利用度分别为９５．１％±９．０６％?OBJECTIVE:The pharmacokinetics and relative bioavailability of a new sustained release tablet(2 tablet q 12h ± 6d) of ibuprofen and d-peseudoephedrine hydrocholoride (PE) were investigated with a conventional tablet(1 tablet q 6h ± 6d) after multiple oral administration in twenty male healthy volunteers using an op en,randomized, two -way crossover design. ME THODS: The concentrations o f Ib and PE in plasma were determined by HPLC.RESULTS:The AUCss of sustained release tablet and conventioal tablet of Ibuprofen were (263.31 ± 25.55)mg·h·L-1 and (271 .26 ± 29.70) mg·h·L-1 respectively; tmax were (7.47 ± 0.82)h and (2.05 ± 0.49)h respectively; Cmax were (18.42 ± 2.61) mg·L-1 and (28.74 ± 5.09) mg·L-1 respectively, Cmin were (11 .44 ±11 .45) mg·L-1 and (10.91±11 .93) mg·L-1 respectively; The AUC of sustained release tablet and conventional tablet of PE-HCL were (3468. 14 ± 136.46)mg·L-1 and (3466.72 ± 168.20)μg·h·L-1 respectively; tmax weremg.L-1(4.41 ± 0.27)h and (2.27 ± 0.71)hrespectively, Cmax were (275.20 ± 26.82) μg.L-1 and (307.89 ± 24.09) μg·L-1 respectively; Cmin were (147.89 ± 18.24) μg·L-1 and (126.62 ± 18.22) μg·L-1 respectively, the relative bioavailability of sustained release tablet to conventional tablet were 95. 1% 1 9.06(Ibuprofen) and 97.44% ± 8.85(PE-HCL) respectively.CONCLUSION:The ibuprofen of sustained release tablet was less than that of conventional. talbet,the sustained release tablet had an effect of sustained release.

关 键 词：布洛芬 盐酸伪麻黄碱 缓释片 药代动力学 相对生物利用度 抗炎药 

分 类 号：R971.1[医药卫生—药品] R969.1[医药卫生—药学]