氯酚伪麻缓释片中氯雷他定在健康志愿者体内的药动学(英文)

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。

Pharmacokinetics of loratadine in loratadine, paracetamol and pseudoephedrine sustained-release tablets in healthy volunteers

AIM: To study the pharmacokinetics of loratadine in healthy volunteers after single and multiple oral administrations of loratadine, paracetamol and pseudoephedrine (LPP) sustained-release tablets.METHODS: Twenty-four volunteers were randomized into two groups which included six men and six women in each group. In the single dose design, volunteers received either one or two tablet (s) of LPP. After 1 wk wash out period, volunteers of one tablet group participated in multiple dose design in which each volunteer received one tablet of LPP twice per day for six consecutive days. The concentrations of loratadine in plasma were determined by HPLC-MS method and the pharmacokinetic parameters were calculated. RESULTS: In the single dose design, main pharmacokinetic parameters of one and two tablet group were as follow: cmax were ( 1.5 ±groups were similar to each other. The obtained multi-dose pharmacokinetic parameters were as follows: AUCssrespectively. D (F) was (3.3 ± 0.8) %. The pharmacokinetics of loratadine was linear. There were no significant difference in pharmacokinetics between single-dose and multi-dose. CONCLUSION: The release and absorption of loratadine in experimental tablet are close to those in loratadine tablet and not affected by the other two components, pseudoephedrine and paracetamol, in LPP sustained release tablet.