布洛芬缓释胶囊的人体相对生物利用度  

Relative Bioavailability of Ibuprofen Sustained-release Capsules in Human Subjects

作　　者：刘建芳[1] 邓鸣[1] 赵春丽[1] 刘会臣[1] 

机构地区：[1]白求恩国际和平医院临床药理室,河北石家庄050082

出　　处：《中国临床药理学杂志》2003年第2期113-116,共4页The Chinese Journal of Clinical Pharmacology

摘　　要：目的:比较布洛芬缓释胶囊和芬必得胶囊的人体生物利用度。方法:用随机交叉试验设计,20名健康男性受试者口服单剂量和多剂量两种制剂600 mg,高效液相色谱法测定血清中布洛芬的浓度,计算两药的药代动力学参数。结果:受试者口服单剂量国产布洛芬缓释胶囊与芬必得胶囊后布洛芬的AUC_(0-24)分别为208.74±43.74和205.54±39.43 mg·h·L^(-1),t_(max)分别为4.85±0.81和5.20±1.06 h,C_(max)分别为25.40±4.00和25.47±4.50mg·L^(-1),以AUC_(0-24)计算,国产布洛芬缓释胶囊的相对生物利用度为(104.13±25.50)％。口服多剂量国产布洛芬缓释胶囊与芬必得胶囊后布洛芬的AUC^(ss)分别为170.81±24.87和172.93±29.76 mg·h·L^(-1),t_(max)分别为4.90±0.97和4.65±1.09 h,C_(max)分别为27.31±5.45和26.87±3.79 mg·L^(-1);C_(min)分别为6.13±1.60和5.94±1.84 mg·L^(-1),波动度分别为(146.45±36.69)％和(149.10±22.61)％。以AUC^(ss)计算,国产布洛芬缓释胶囊的相对生物利用度为(99.68±10.22)％。结论:国产布洛芬缓释胶囊与芬必得胶囊具有生物等效性。OBJECTIVE: To compare the bioavailability of domestic ibuprofen sustained-release capsules and fenbid capsules in human subjects. METHODS: A single and multiple oral administration of 600mg test and reference capsules were given to 20 healthy male volunteers according to randomized crossover design. Ibuprofen concentrations in serum were determined by HPLC methods. The pharmacokinetics parameters and bioavailability of test capsules were compared with those of reference capsules. RESULTS: After a single oral administration of 600mg test and reference capsules, the pharmacokinetic parameters were as follows: AUC0-24 were 208.74 ± 43.74 and 205.54 ± 39.43 mg·L-1·h, tmax were 4.85 ± 0.81 and 5.20 ± 1.06 h , Cmax were 25.40 ± 4.00 and 25.47 ± 4.50 mg·L-1, respectively. The relative bioavailability of test capsules was (104.13 ± 25.50)%. After multiple oral administration of 600mg test and reference capsules , the pharmacokinetics parameters were as follows: AUCss were 170.81 ± 24.87 and 172.93 ± 29.76 mg·h·L-1, tmax were 4.90 ± 0.97 and 4.65 ± 1.09 h, Cmax were 27.31±5.45 and 26.87 ± 3.79 mg·L-1, Cmin were 6.13 ± 1.60 and 5.94 ± 1.84 mg·L-1, DF were ( 146.45 ± 36.69) %and(149.10±22.61)%,respectively.The relative bioavailability of test capsules was (99.68 ± 10.22)%. CONCLUSION: The two preparations were bioequivalent.

关 键 词：布洛芬缓释胶囊 人体相对生物利用度 高效液相色谱 药代动力学 

分 类 号：R971.1[医药卫生—药品] R969.1[医药卫生—药学]