国产与进口美洛昔康片单次给药后人体药动学(英文)

目的 :比较健康志愿者国产与进口美洛昔康片的人体药动学和相对生物利用度。方法 :采用单次给药 2周期交叉设计 ,HPLC法测定 12名健康男性志愿者口服 15mg美洛昔康后血药浓度 ,计算药动学参数和国产片的相对生物利用度。结果 :2种制剂的药时曲线符合一级吸收的一室开放模型。国产与进口片的药动学参数分别是AUC0 - 96 为 (6 7±s 14 )mg·h·L- 1和 (6 4± 15 )mg·h·L- 1;AUC0 -∞ 为 (73± 19)mg·h·L- 1和 (70± 18)mg·h·L- 1;Cmax为 (2 .3± 0 .5 )mg·L- 1和 (1.6± 0 .3)mg·L- 1;Tmax为 (2 .0± 1.6 )h和 (6± 3)h ;T12 ke为 (2 5± 6 )h和 (2 4± 5 )h ;MRT为 (4 0± 13)hand (39±8)h。方差分析表明两者AUC之间无显著差异 (P>0 .0 5 ) ,但两者的Cmax和Tmax之间有显著差异 (P<0 .0 5 )。结论 :国产片的释药速率比进口片快 ,其相对生物利用度为 (10 5± 13) %。

Pharmacokinetics of domestic and imported meloxicam tablets following a single dose in healthy volunteers

AIM: To compare the pharmacokinetics and relative bioavailability of domestic and imported meloxicam tablets in healthy volunteers. METHODS: In a random two periods crossover study, 12 healthy male volunteers received a single dose of meloxicam 15 mg of two formulations respectively. The plasma concentration of meloxicam was determined by HPLC method. The pharmacokinetic parameters of the two preparations and the relative bioavailability of domestic tablets were calculated with statistical analysis. RESULTS: The concentration-time plots of the two preparations were in accordance with an open one-compartment model with first-order absorption. The main pharmacokinetic parameters of domestic and imported tablets were (67±s 14) mg·h·L-1 and (64±15) mg·h·L-1 for AUC0-96; (73±19) mg·h·L-1 and (70±18) mg·h·L-1 for AUC0-∞;(2.3±0.5) mg·L-1 and (1.6±0.3) mg·L-1 for Cmax;(2.0±1.6) h and (6±3) h for Tmax; (25±6) h and (24±5) h for T(1)/(2)ke; (40±13) h and (39±8) h for mean residence time (MRT), respectively. Variance analysis showed that there was significant difference in Cmax and Tmax but no significant difference in AUC between the two preparations. CONCLUSION: The release rate of the domestic meloxicam tablets is faster than that of the imported ones and the relative bioavailability of domestic tablets is (105±13) %.