氯雷他定胶囊和片剂的药动学及相对生物利用度

Pharmacokinetics and relative bioavailability of domestic Loratadine capsules and tablets in healthy volunteers

目的 研究氯雷他定胶囊与片剂的人体药动学和生物等效性。方法 选择 2 0名健康男性志愿者 ,随机交叉口服单剂量 (4 0mg)氯雷他定胶囊或片剂两种制剂 ,采用HPLC法测定血清中氯雷他定的浓度。结果 口服氯雷他定胶囊及片剂的Cmax分别为 (34.5± 1 5 .1 )ng·ml-1 和 (33.7± 1 5 .6 )ng·ml-1 ;Tmax 分别为 (1 .2± 0 .4 )h和 (1 .3± 0 .4 )h ;T1 / 2 β 分别为 (4 .3± 1 .2 )h和 (4 .5± 1 .4 )h ;AUC0 -2 4分别为 (99.1± 4 0 .2 )ng·h·ml-1 和 (99.6± 4 3.9)ng·h·ml-1 ;AUC0 -∞ 分别为 (1 0 4 .0± 39.2 )ng·h·ml-1 和 (1 0 5 .1± 4 3.4 )ng·h·ml-1 ;氯雷他定胶囊对片剂的相对生物利度为 (98.9± 31 .7) %。

Aim To study the pharmacokinetics and relative bioavailability of domestic loratadine capsules and tablets in healthy volunteers.Methods A reversed-phase high performance liquid chromatography was used for the determination of loratadine in serum after a single oral dose of 40mg domestic loratadine capsules and tablet in a crossover design.Results The main pharmacokinetic parameters of domestic loratadine capsule and tablet were as follows: C max were (34.5±15.1)ng·ml -1 and (33.7±15.6)ng·ml -1 ,respectively.T max were (1.2±0.4)h and (1.3±0.4)h,respectively。T 1/2β were (4.3±1.2)h and (4.5±1.4) h,respectively.AUC 0-24 were (99.1±40.2)ng·h·ml -1 and (99.6±43.9)ng·h·ml -1 ,respectively;AUC 0-∞ were (104.0±39.2)ng·h·ml -1 and (105.1±43.4)ng·h·ml -1 ,respectively.The relative bioavailability of the test capsule was (98.9±31.7)%.Conclusion The domestic loratadine capsule and tablet are bioequivalent.