空腹及餐后口服富马酸替诺福韦二吡呋酯片的人体生物等效性

发布时间：2019-08-14 10:20

【摘要】：建立了液相色谱-串联质谱法测定人血浆中的替诺福韦,考察空腹及餐后口服富马酸替诺福韦二吡呋酯片的人体生物等效性及药动学差异。采用随机自身交叉试验,将48名健康男性志愿者随机分为2组,每组再随机分为2个亚组,分别于空腹和餐后口服给予受试或参比制剂300 mg,清洗1周后交叉给药。空腹口服受试和参比制剂后,血浆中替诺福韦的主要药动学参数分别为:tmax(0.86±0.53)和(0.93±0.37)h,cmax(487.6±147.2)和(443.1±131.3)ng/ml,t1/2(20.09±3.97)和(20.39±4.78)h,以AUC0→∞计算,受试制剂的相对生物利用度为(103.38±23.53)%。餐后口服受试和参比制剂后,血浆中替诺福韦的主要药动学参数分别为:tmax(1.34±0.45)和(1.28±0.36)h,cmax(410.3±118.1)和(379.3±88.7)ng/ml,t1/2(15.57±4.12)和(16.47±4.96)h,以AUC0→∞计算,受试制剂的相对生物利用度为(107.91±15.34)%。空腹及餐后给药试验结果均表明受试制剂与参比制剂在健康志愿者体内具有生物等效性。
[Abstract]:A liquid chromatography-tandem mass spectrometry (LC-MS) was established for the determination of tenofovir in human plasma. The bioequivalence and pharmacokinetics of tenofovir fumarate dipyrifuroxime tablets were investigated by fasting and postprandial oral administration of tenofovir fumarate difurofuride tablets. Forty-eight healthy male volunteers were randomly divided into two groups. Each group was randomly divided into 2 subgroups. The subjects or reference preparations were given oral administration on an empty stomach and after meal for one week, and then the drug was cross-administered for one week. After fasting oral administration of tenofovir and reference preparation, the main pharmacokinetics parameters of tenofovir in plasma were: tmax (0.86 卤0.53) and (0.93 卤0.37) h, cmax (487.6 卤147.2) and (443.1 卤131.3) ng/ml,t1/2 (20.09 卤3.97) and (20.39 卤4.78) h, respectively. the relative bioavailability of tenofovir was (103.38 卤23.53)%. The main pharmacokinetics parameters of tenofovir in plasma were: tmax (1.34 卤0.45) and (1.28 卤0.36) h, cmax (410.3 卤118.1) and (379.3 卤88.7) ng/ml,t1/2 (15.57 卤4.12) and (16.47 卤4.96) h, respectively. the relative bioavailability of tenofovir was (107.91 卤15.34)%. The results of fasting and postmeal administration showed that the tested preparation and reference preparation were bioequivalent in healthy volunteers.
【作者单位】：四川大学华西药学院临床药学研究中心;同济大学附属第十人民医院;
【分类号】：R96

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