国产盐酸西替利嗪片和胶囊的人体药动学及相对生物利用度

Pharmacokinetics and relative bioavailability of domestic cetirizine hydrochloride tablets and capsules in healthy volunteers

目的 :研究国产盐酸西替利嗪片和胶囊的人体药动学和生物等效性。方法 :选择 2 1名男性健康志愿者 ,采用反相高效液相色谱法 ,以紫外 2 2 9nm为检测波长 ,测定了单剂量 (2 0mg)口服国产盐酸西替利嗪片、胶囊和进口盐酸西替利嗪片在人体内的西替利嗪浓度。结果 :盐酸西替利嗪的体内动态过程呈一级吸收的二房室开放模型 ,国产片、胶囊和进口片的Cmax分别为 (6 4 8.5± 117.6 ) ,(6 78.8± 10 4 .6 )和 (6 6 1.5± 12 0 .6 )ng·ml-1,Tmax分别为 (1.0± 0 .4 ) ,(1.2± 0 .5 )和 (1.1± 0 .4 )h ,t1/ 2 β分别为 (7.8± 2 .6 ) ,(7.6± 2 .7)和 (9.4± 5 .2 )h ,MRT分别为 (7.2± 0 .6 ) ,(7.3± 0 .6 )和 (7.4± 0 .4 )h ,AUC0→ 2 5分别为(45 0 3.3± 6 89.5 ) ,(46 0 1.2± 739.1)和 (484 0 .5± 937.1)ng·h-1·ml-1,AUC0→∞ 分别为 (5 0 34.4± 84 1.4 ) ,(5 12 9.6± 776 .2 )和(5 4 32 .8± 10 2 4 .0 )ng·h-1·ml-1。结论

OBJECTIVE To study the pharmacokinetics and relative bioavailability of domestic cetirizine hydrochloride tablets and capsules in healthy volunteers.METHODS A reversed-phase high performance liquid chromatography was used for the determination of cetirizine in serum after a single oral dose of 20 mg domestic cetirizine hydrochloride tablet, capsule and imported cetirizine hydrochloride tablet (Zyrtec) in a crossover design.The detector was operated at UV 229 nm.RESULTS The dynamic course of cetirizine serum concentrations conformed to a two compartment open model and the main pharmacokinetic parameters of domestic cetirizine hydrochloride tablet and capsule and imported cetirizine hydrochloride tablet were as follows: C max were( 648.5 ± 117.6 ),( 678.8 ± 104.6 )and( 661.5 ± 120.6 )ng·ml -1 , T max were( 1.0 ± 0.4 ),( 1.2 ± 0.5 )and( 1.1 ± 0.4 ) h, t 1/2 β were( 7.8 ± 2.6 ),( 7.6 ± 2.7 )and ( 9.4 ± 5.2 ) h,MRT were( 7.2 ± 0.6 ),( 7.3 ± 0.6 ) and ( 7.4 ± 0.4 ) h,AUC 0→25 were ( 4503.3 ± 689.5 ),( 4601.2 ± 739.1 ) and ( 4840.5 ± 937.1 ) ng·h·ml -1 ,AUC 0→∞ were ( 5034.4 ± 841.4 ),( 5129.6 ± 776.2 )and ( 5432.8 ± 1024.0 ) ng·h·ml -1 ,respectively.CONCLUSIONS The domestic cetirizine hydrochloride and imported cetirizine hydrochloride tablets are bioequivalent.