萘丁美酮片药物动力学和生物利用度

Study of pharmacokinetics and bioavailability of nabumetone tablets

本文用反相高效液相色谱法研究了10名健康志愿受试者交叉口服单剂量萘丁美酮国产片和进口片1000mg的药物动力学和生物利用度。两制剂的药时曲线经计算机以非线性最小二乘法拟合,均符合二室开放模型。对两制剂的全部药物动力学参数用成对数据资料t—检验进行比较,结果表明:两制剂的全部药物动力学参数无显著差异(p<0.05)。进口萘丁美酮片的药物动力学参数分别为:T_(1/2)Ka6h,T_(1/2)α2.6h,T_(1/2)β29h,Cmax20μg/ml,Tp7h,Tlag0.49h,AUC1020(μg·h/ml);国产萘丁美酮片的药动学参数分别为:T_(1/2)Ka8h,T_(1/2)σ0.9h,T_(1/2)β30h,Cmax16μg/ml,TP11h,Tlag0.5h,AUC991(μg/ml),国产萘丁美酮片的相对生物利用度为97.1%。

The pharmacokineties and bioavailability of nabumetone tablets (home and Re- lifex) were studied in ten healthy volunteers after overcross oral single dose of 1000mg. The plasma concentration-time data of the two preparations was fitted by the nonlinear regression autogractic program and showed to be subjected to two- compartment open model. No significant difference was found between pharmaco- kinetic parameters of the two tablets (Relifex and home) (t-test, P>0.05). T1, 2ka T1/2α, T1/2β, Cmax, TP, Tlag and AUC of nabumetone tablet (home) were respe- ctively 8h, 0.9h, 30h, 16μg/ml, 11h, 0.5h, 991(μg·h/ml), T1/2ka, T1/2α, T1/2β. Cmax, TP, Tlag, AUC of nabumetone tablet (Relifex) werw repectively 6h, 2.6h, 29h, 20μg/ml, 7h. 0.9h, 1020(ng·h/ml). The relative bioavaibility of nabume- tone tablet (home) was 97.1%.