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目的:研究健康受试者单剂量及多剂量口服氯酚伪麻缓释片后氯雷他定的药动学特征。方法:24名健康受试者随机分为Ⅰ、Ⅱ两组,每组男、女受试者各6名,Ⅰ组受试者首先单次口服氯酚伪麻缓释片1片;间隔1 wk清洗期后,该组继续进行多次给药试验,受试者连续5 d,每日2次,每次1片,d 6早晨服药1次;Ⅱ组受试者单次口服氯酚伪麻缓释片2片。用HPLC-MS法测定血浆中氯雷他定的浓度,计算药动学参数。结果:健康受试者单次口服氯酚伪麻缓释片1片、2片后,氯雷他定的药动学参数分别为:c_(max)为(1.5±s 0.7)和(3.1±1.3)μg·L~(-1),AUC为(5.7±2.7)和(11±5)μg·h·L~(-1),2组的t_(1/2)和t_(max)相近。多次给药后氯雷他定的药动学参数:AUC~(ss)为(5.9±2.4)μg·h·L~(-1),c_(max)~(ss)、c_(min)~(ss)和c_(av)~(ss)分别为(1.8±0.9)、(0.15±0.06)和(0.49±0.20)μg·L~(-1),D(F)为(3_3±0.8)%。结论:单次口服氯酚伪麻缓释片后,氯雷他定呈线性药动学特征;多次给药后氯雷他定的体内药动学特征无显著变化。
Objective: To study the pharmacokinetics of loratadine after single and multiple doses of oral chlorophenolate pseudoephedrine sustained-release tablets in healthy subjects. Methods: Twenty-four healthy subjects were randomly divided into two groups, Ⅰ and Ⅱ, each with 6 male and 6 female subjects. In group Ⅰ, wk washing period, the group continued to conduct multiple drug delivery tests, subjects for 5 consecutive days, 2 times a day, each time 1, d 6 medication once a day; Ⅱ subjects were single oral oral chlorophenylamine Ma sustained-release tablets 2 tablets. The concentration of loratadine in plasma was determined by HPLC-MS and the pharmacokinetic parameters were calculated. Results: The pharmacokinetic parameters of loratadine after single oral chlorophenolate pseudoephedrine sustained-release tablets (1 tablet) and 2 tablets (cmax) were (1.5 ± 0.7) and (3.1 ± 1.3) μg · L -1, the AUC was (5.7 ± 2.7) and (11 ± 5) μg · h · L -1, respectively. The t 1/2 and t max of the two groups were similar . The pharmacokinetic parameters of loratadine after multiple administrations were as follows: AUC ~ (5.9 ± 2.4) μg · h · L ~ (-1), cmax ~ (ss), c_ (min) The values of ~ (ss) and c_ (av) ~ (1.8 ± 0.9), (0.15 ± 0.06) and (0.49 ± 0.20) μg · L -1 and D (F) were (3_3 ± 0.8) )%. CONCLUSION: Loratadine has a linear pharmacokinetic profile after single oral administration of chlorophenylamine and pseudoephedrine sustained release tablets. There was no significant change in pharmacokinetics of loratadine after multiple administrations.