单剂量及多剂量口服布洛芬缓释胶囊的药物动力学与生物等效性研究

Pharmacokinetics and Relative Bioequivalence of Single and Multiple Oral Doses of Ibuprofen Sustained-Release Capsules

在20名健康男性志愿者中研究两种布洛芬缓释胶囊的药动学和生物等效性。采用双周期随机交叉试验设计,LC-MS法测定人血浆中布洛芬的浓度。单剂量口服受试和参比制剂后血浆中布洛芬的Cmax分别为(19.21±3.49)和(16.86±4.30)μg/ml,tmax分别为(5.00±0.73)和(4.85±0.67)h,t1/2分别为(2.45±0.52)和(3.42±1.17)h,以AUC0→24h计算得受试制剂的相对生物利用度为(101.74±10.52)%;多剂量试验的Cmax分别为(17.58±4.38)和(14.46±3.61)μg/ml,tmax分别为(4.68±1.13)和(4.68±1.46)h,t1/2分别为(3.01±0.77)和(3.60±0.82)h,DF分别为(176.05±32.33)和(138.00±25.55)%,以AUC0→24h计算得受试制剂的相对生物利用度为(99.09±11.13)%。表明两种布洛芬缓释胶囊生物等效。

The pharmacokinetics and bioequivalence of two brands of ibuprofen sustained-release capsules was investigated in 20 healthy male volunteers, according to randomized crossover design. The concentrations of ibuprofen in plasma were determined by LC-MS method. The pharmacokinetic parameters for the single oral administration of 300mg test and reference capsules were Cmax （19.21±43.49） and （16.86±4.30） μg/mi, tmax（5.00±0.73） and （4.85±0.67） h, t1/2（2.45± 0.52） and （3.42 ± 1.17）h, respectively. The relative bioavailability of test capsules was （101.74±10.52 ）%. The pharmacokinetic parameters for the multiple oral administration of 300mg test and reference capsules were Cmax （ 17.58 ± 4.38） and （14.46 ± 3.61） μg/ml, tmax （4.68 ±1.13） and （4.684±1.46）h, DF （176.05±32.33） and （138.00±25.55）%, t1/2 （3.01±0.77） and （3.60±0.82） h, respectively. The relative bioavailability of test capsules was （99.09±11.13）%. The results showed that the test and reference preparations were bioequivalence.