【摘要】 目的:评价健康受试者在多次口服布洛芬片和多次同时口服阿兹夫定片及布洛芬片，阿兹夫定对布洛芬药动学的影响。方法:采用单中心开放平行序贯给药的试验设计。12例健康受试者连续口服布洛芬（0.2 g,qd） 5 d后，继续连续同时口服布洛芬（0.2 g,qd）与阿兹夫定（5 mg,qd） 5 d，采用高效液相色谱串联质谱法（LC-MS/MS）测定血浆中布洛芬和阿兹夫定的浓度，应用Phoenix WinNonlin 8.3软件计算主要药动学参数并应用SAS 9.4进行统计分析。结果:单独服用布洛芬和联用阿兹夫定后血浆中布洛芬的药动学参数中，C_max,ss分别为（15 250.00±3 127.735）和（16 133.33±2 694.214） ng·mL^-1,AUC_0-t,ss分别为（69 286.96±13 927.273）和（73 060.86±13 060.975） ng·h·m L^-1,AUC_0-∞，ss分别为（72 267.55±15 186.088）和（78 715.48±15 160.973） ng·h·mL^-1。与单用布洛芬相比，C_max,ss,AUC_0-t,ss和AUC_0-∞，ss的几何均值比值及其90%置信区间分别为106.59%（93.02%～122.14%）,105.81%（92.77%～120.67%）,109.20%（94.91%～125.65%）。结论:在健康受试者中，阿兹夫定对布洛芬的药动学影响一致且安全性良好。更多还原

【Abstract】 Objective: To evaluate the effect of azvudine on the pharmacokinetics of ibuprofen in healthy volunteers. Methods: The study adopted a single-center,open,sequential dosing design and was conducted in 12 healthy volunteers. Subjects took ibuprofen（ 0. 2 g,qd） for 5 consecutive days,followed by oral ibuprofen（ 0. 2 g,qd） and azvudine（ 5 mg,qd） for 5 consecutive days,and plasma samples were collected for the determination of drug concentrations by high performance liquid chromatography-tandem mass spectrometry（ LC-MS/MS）. The main pharmacokinetic parameters were calculated by using Phoenix WinNonlin 8. 3 and SAS 9. 4. Results: The pharmacokinetic parameters of ibuprofen in plasma after administration of ibuprofen alone and co-administration with azvudine were as follows,C_max,sswere（ 15 250. 00 ± 3 127. 735） and（ 16 133. 33 ± 2 694. 214） ng·m L^-1,AUC_0-t,sswere（ 69 286. 96 ± 13 927. 273） and（ 73 060. 86 ± 13 060. 975） ng·h·m L^-1,AUC_0-∞,sswere（ 72 267. 55 ±15 186. 088） and（ 78 715. 48 ± 15 160. 973） ng·h·m L^-1. Compared with administration of ibuprofen alone,the90% confidence intervals of the geometric mean ratios of C_max,ss,AUC_0-t,ssand AUC_0-∞,ss of ibuprofen in plasma after co-administration with azvudine were 106. 59%（ 93. 02% ～ 122. 14%）,105. 81%（ 92. 77% ～ 120. 67%）,and 109. 20%（ 94. 91% ～ 125. 65%）,respectively. Conclusion: The effect of azvudine on the pharmacokinetic profile of ibuprofen is consistent,without serious adverse events in healthy subjects.更多还原