中国新药与临床杂志
中國新藥與臨床雜誌
중국신약여림상잡지
CHINESE JOURNAL OF NEW DRUGS AND CLINICAL REMEDIES
2007年
11期
801-804
,共4页
氯雷他定%色谱法,高压液相%光谱法,质谱,电喷雾电离%药动学
氯雷他定%色譜法,高壓液相%光譜法,質譜,電噴霧電離%藥動學
록뢰타정%색보법,고압액상%광보법,질보,전분무전리%약동학
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:cmax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t1/2和tmax相近.多次给药后氯雷他定的药动学参数:AUCss为(5.9±2.4)μg·h·L-1,css max、css min和css av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.
目的:研究健康受試者單劑量及多劑量口服氯酚偽痳緩釋片後氯雷他定的藥動學特徵.方法:24名健康受試者隨機分為Ⅰ、Ⅱ兩組,每組男、女受試者各6名,Ⅰ組受試者首先單次口服氯酚偽痳緩釋片1片;間隔1 wk清洗期後,該組繼續進行多次給藥試驗,受試者連續5 d,每日2次,每次1片,d 6早晨服藥1次;Ⅱ組受試者單次口服氯酚偽痳緩釋片2片.用HPLC-MS法測定血漿中氯雷他定的濃度,計算藥動學參數.結果:健康受試者單次口服氯酚偽痳緩釋片1片、2片後,氯雷他定的藥動學參數分彆為:cmax為(1.5±s 0.7)和(3.1±1.3)μg·L-1,AUC為(5.7±2.7)和(11±5)μg·h·L-1,2組的t1/2和tmax相近.多次給藥後氯雷他定的藥動學參數:AUCss為(5.9±2.4)μg·h·L-1,css max、css min和css av分彆為(1.8±0.9)、(0.15±0.06)和(0.49±0.20)μg·L-1,D(F)為(3.3±0.8)%.結論:單次口服氯酚偽痳緩釋片後,氯雷他定呈線性藥動學特徵;多次給藥後氯雷他定的體內藥動學特徵無顯著變化.
목적:연구건강수시자단제량급다제량구복록분위마완석편후록뢰타정적약동학특정.방법:24명건강수시자수궤분위Ⅰ、Ⅱ량조,매조남、녀수시자각6명,Ⅰ조수시자수선단차구복록분위마완석편1편;간격1 wk청세기후,해조계속진행다차급약시험,수시자련속5 d,매일2차,매차1편,d 6조신복약1차;Ⅱ조수시자단차구복록분위마완석편2편.용HPLC-MS법측정혈장중록뢰타정적농도,계산약동학삼수.결과:건강수시자단차구복록분위마완석편1편、2편후,록뢰타정적약동학삼수분별위:cmax위(1.5±s 0.7)화(3.1±1.3)μg·L-1,AUC위(5.7±2.7)화(11±5)μg·h·L-1,2조적t1/2화tmax상근.다차급약후록뢰타정적약동학삼수:AUCss위(5.9±2.4)μg·h·L-1,css max、css min화css av분별위(1.8±0.9)、(0.15±0.06)화(0.49±0.20)μg·L-1,D(F)위(3.3±0.8)%.결론:단차구복록분위마완석편후,록뢰타정정선성약동학특정;다차급약후록뢰타정적체내약동학특정무현저변화.
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.
