布洛芬缓释胶囊在健康人体的相对生物利用度研究

目的: 研究两种国产布洛芬的相对生物利用度。方法: 采用双周期随机交叉试验设计。分别给予24名男性健康受试者试验制剂或参比制剂布洛芬 300 mg,采用HPLC法测定给药后不同时间的血药浓度。结果: 参比制剂与试验制剂单剂量给药主要药代动力学参数C_max、t_max、AUC_0-24和AUC_0-∞分别为:(13.5±5.9)和(12.7±5.4) μg/mL;(5.1±1.0)和(5.5±1.5) h;(100.2±45.4)和(98.5±44.8) μg·h·mL^-1;(105.7±47.3)和(103.8±47.0) μg·h·mL^-1。参比制剂与试验制剂多剂量给药主要药代动力学参数C_max、C_av、t_max、AUC_ss分别为:(14.1±5.3)和(14.9±6.4) μg/mL;(8.2±3.4)和(8.6±4.3) μg/mL;(4.8±1.0)和(4.6±0.9) h;(99.0±40.4)和(103.3±51.3) μg·h·mL^-1。结论: 经统计学分析,布洛芬参比制剂与试验制剂具有生物等效性。

Study of the relative bioequivalence of sustained release capsules of Ibuprofen in healthy volunteers

AIM: To study the relative bioequivalence of sustained release capsules of Ibuprofen made by Jiangxi Pharmaceutical Co., Ltd.METHODS: A single dose of 300 mg domestic Ibuprofen, and its reference preparation made by Zhengzhou Fusheng Pharmaceuticals Co.,Ltd. were given to 24 healthy volunteers by oral in an open randomized two way crossover experiment.The plasma concentrations were determined by HPLC method.RESULTS: The main pharmacokinetic parameters of a single dose of Ibuprofen were as follows : C_max were (13.5±5.9) and (12.7±5.4) μg/mL; t_max were (5.1±1.0), (5.5±1.5) h; AUC_0-24 were (100.2±45.4) and (98.5±44.8) μg·h·mL^-1;AUC_0→∞ were (105.7±47.3) and (103.8±47.0) μg·h·mL^-1 for the reference drug and the test drug, respectively.The main pharmacokinetic parameters of muti-dose of Ibuprofen were as follows: C_max were (14.1±5.3) and (14.9±6.4) μg/mL;C_av were(8.2±3.4 )and (8.6±4.3) μg/mL; t_max were (4.8±1.0) and (4.6±0.9) h; AUC_ss were (99.0±40.4) and (103.3±51.3) μg·h·mL^-1 for the reference drug and the test drug, respectively.CONCLUSION: Statistic analysis shows that the reference preparation and the test preparation are bioequivalent.