氯雷他定3种制剂生物等效性研究

目的 :评价受试氯雷他定片 (T1)和颗粒(T2 )与参比氯雷他定片 (R)的生物等效性。方法 :2 4名健康男性受试者按体重配对、随机三交叉单次口服氯雷他定 4 0mg ,RT HPLC法测定血浆中药物浓度。结果 :T1,T2 及R的主要药动学参数Tmax分别为 (1.0±s 0 .5 ) ,(1.0± 0 .4 )和 (0 .9± 0 .3)h ;Cmax分别为 (36± 15 ) ,(37± 16 )和 (36± 15 ) μg·L- 1;T1/ 2 分别为 (3.5± 1.0 ) ,(3.6± 0 .8)和 (3.7±1.0 )h ;AUC0 - 12 分别为 (10 9± 4 6 ) ,(110± 5 1)和(10 8± 4 6 ) μg·h·L- 1,AUC0 ∞ 分别为 (118± 5 0 ) ,(12 0± 5 4)和 (119± 5 1) μg·h·L- 1。T1,T2 相对生物利用度分别为 (10 1± 12 ) %和 (10 1± 14 ) %。结论 :T1,T2 与R具有生物等效性。

Study on bioequivalence of three kinds of loratadine preparations

AIM: To evaluate the bioequivalence of three kinds of loratadine preparations in healthy volunteers. METHODS: A single oral dose of loratadine of reference or test preparations 40 mg was given to healthy male volunteers according to an open randomized three cross-over design. The plasma concentrations of loratadine were determined by a RP-HPLC method. The pharmacokinetic parameters and bioavailability of two test prepartions were compared with reference preparation. RESULTS: The main pharmacokinetic parameters were as follows: T_ max were (1.0±s 0.5), (1.0±0.4) and (0.9±0.3)h; C_ max were (36±15), (37±16) and (36±15) μg·L -1; T_ 1/2 were (3.5±1.0), (3.6±0.8) and (3.7±1.0)h; AUC_ 0-12 were (109±46), (110±51), and (108±46) μg·h·L -1; AUC_ 0～∞ were ( 118±50), (120±54), and (119±51)μg·h·L -1; The relative bioavailability of two test preparations reference preparation were (101±12)% and (101±14)%. CONCLUSION: The two test preparations and the reference preparation are bioequivalent.