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目的:建立高效液相色谱法测定人血浆中布洛芬浓度,并应用于两种布洛芬缓释制剂的人体生物等效性研究。方法:采用双周期自身随机交叉试验设计,24名男性健康志愿者分别单剂量、多剂量口服布洛芬缓释胶囊受试制剂和参比制剂300mg,采用高效液相色谱法测定人血浆中布洛芬浓度,利用DAS 2.0程序计算主要药动学参数,并对两种制剂进行生物等效性评价。结果:单剂量口服受试制剂和参比制剂后血浆中布洛芬的Cmax分别为(12.7±5.4)和(13.5±5.9)μg/mL,tmax分别为(5.5±1.4)和(5.1±1.0)h,AUC0→24分别为(96.8±50.2)和(95.7±45.4)μg·h·mL-1。多剂量口服受试制剂和参比制剂后血浆中布洛芬的Cmax分别为(14.1±5.3)和(14.9±6.4)μg/mL,tmax分别为(4.8±1.0)和(4.6±0.9)h,Cav分别为(8.3±3.4)和(8.6±4.3)μg/mL,DF值分别为(117.2±35.3)%和(131.7±35.1)%。经统计学检验,两种制剂主要药动学参数间无统计学差异(P>0.05)。结论:所建立的高效液相色谱法适合用于人体血浆中布洛芬测定。布洛芬受试制剂和参比制剂具有生物等效性。
OBJECTIVE: To establish a HPLC method for the determination of ibuprofen in human plasma and to study the bioequivalence of two ibuprofen sustained-release preparations. Methods: A double-cycle, randomized crossover trial was designed. Twenty-four male healthy volunteers received single or multiple doses of 300 mg ibuprofen sustained-release capsules and reference preparations, respectively. The contents of cloth in human plasma Lupine concentrations, the main pharmacokinetic parameters were calculated using the DAS 2.0 program and bioequivalence was evaluated for both formulations. RESULTS: The Cmax of ibuprofen in plasma after single-dose oral administration of test preparation and reference preparation were (12.7 ± 5.4) and (13.5 ± 5.9) μg / mL respectively, and the tmax were (5.5 ± 1.4) and ) h, AUC0 → 24 were (96.8 ± 50.2) and (95.7 ± 45.4) μg · h · mL-1, respectively. The Cmax values of ibuprofen in plasma after multiple doses of oral and reference preparations were (14.1 ± 5.3) and (14.9 ± 6.4) μg / mL, respectively, and the tmax were (4.8 ± 1.0) and (8.3 ± 3.4) and (8.6 ± 4.3) μg / mL for Cav, and the values of DF were (117.2 ± 35.3)% and (131.7 ± 35.1)%, respectively. Statistically, there was no significant difference between the two pharmacokinetic parameters (P> 0.05). Conclusion: The established HPLC method is suitable for the determination of ibuprofen in human plasma. Ibuprofen test and reference formulations are bioequivalent.