国产醋氯芬酸胶囊剂与片剂人体相对生物利用度研究

Study on bioequivalence of domestic aceclofenac capsule and tablet in healthy volunteers

目的 :评价国产醋氯芬酸胶囊剂、片剂和进口醋氯芬酸片剂 3种制剂的生物等效性。方法 :18名健康男性志愿者按 3个周期拉丁方交叉口服单剂量 (10 0mg)醋氯芬酸制剂 ,用HPLC法测定血清中醋氯芬酸的浓度 ,并对试验数据进行统计处理及对 3种制剂进行生物等效性评价。结果 :口服国产待测胶囊剂、片剂及进口醋氯芬酸片剂的Cmax分别为 (9.85± 3.2 1) ,(10 .11± 3.5 0 )及 (8.6 8± 2 .6 5 ) μg·mL- 1 ;Tmax分别为 (1.83± 1.0 0 ) ,(2 .31±1.2 5 )及 (2 .4 2± 1.2 9)h ;AUC0～ 1 2h分别为 (2 7.0 9± 5 .90 ) ,(2 8.16± 6 .4 7)及 (2 6 .0 0± 4 .87) μg·h·mL- 1 ;AUC0～∞ 分别为 (2 8.2 9± 6 .0 3) ,(2 9.39± 6 .6 6 )及 (2 7.11± 5 .15 ) μg·h·mL- 1 ;国产醋氯芬酸胶囊、片剂的相对生物利用度为(10 4 .83± 15 .5 4 ) %和 (10 8.97± 17.35 ) %。结论 :国产胶囊剂、片剂均与进口参比醋氯芬酸片剂具有生物等效性。

Objective:To evaluate the relative bioavailability and bioequivalence of domestic aceclofenac capsule,tablet and imported aceclofenac tablet in healthy volunteers.Methods:A single oral administration of 100mg domestic aceclofenac capsule,tablet and imported aceclofenac tablet were given to 18 healthy male volunteers in Latin square design study respectively.A HPLC assay method was developed to determine the concentration of aceclofenac in human serum.Results:The pharmacokinetics parameters after a single oral administration of 100mg domestic aceclofenac capsule,tablet and imported aceclofenac tablet were as follows: C max = (9.85± 3.21),(10.11±3.50) and (8.68±2.65)μg·mL -1 ; T max =(1.83±1.00),(2.31±1.25) and (2.42±1.29)h; AUC 0～12h =(27.09±5.90), (28.16± 6.47) and (26.00±4.87)μg·h·mL -1 ; AUC 0～∞ =(28.29±6.03 ),(29.39±6.66) and (27.11± 5.15)μg·h·mL -1 ; F 0～12h =(104.83±15.54)% and (108.97±17.35)% respectively.Conclusion:The three domestic and imported preparations were of bioequivalence.