富马酸氯马斯汀注射液在健康人体内药物动力学研究  

Study on the Pharmacokinetics of Clemastine Fumarate Injection in Healthy Volunteers

作　　者：马忠英[1] 乔逸[1] 彭洁[2] 杨志福[1] 杨林[1] 文爱东[1] 

机构地区：[1]第四军医大学西京医院药剂科,西安710033 [2]第四军医大学预防医学系毒理学教研室

出　　处：《中国药师》2011年第5期620-624,共5页China Pharmacist

摘　　要：目的:研究富马酸氯马斯汀注射液在健康人体内单次和多次给药后药物动力学特征。方法:12名健康受试者单次肌内注射富马酸氯马斯汀注射液2 mg;间隔10 d后,连续3 d肌注富马酸氯马斯汀注射液2 mg,bid。给药后LC-MS/MS测定富马酸氯马斯汀血药浓度,DAS2.0药动学软件计算药动学参数。结果:单次和多次给药后主要药动学参数:C_(max)分别为(2.43±1.45)、(5.50±0.74)ng·ml^(-1);t_(max)分别为(0.40±0.24)、(0.43±0.26)h;AUC_(0～12)分别为(13.70±6.70)、(49.80±7.20)ng·h·ml^(-1);AUC_(0～96)分别为(65.10±15.70)、(256.90±33.00)ng·h·ml^(-1);AUC_(0～∞)分别为(82.50±18.00)、(355.10±116.00)ng·h·ml^(-1);t_(1/2)分别为(39.90±7.30)、(46.60±19.10)h。结论:连续3 d肌注富马酸氯马斯汀注射液,药物在体内存在蓄积。Objective： To study the pharmacokinetics of clemastine fumarate injection after single and multiple-dose intramuscular injection in Ghinese healthy volunteers. Method： 12 healthy volunteers were administrated 2 mg clemastine fumarate intramuscular injection once a day. After a 10-day washout period, they were administrated 2 nag clenaastine fumarate intramuscular injection twice a day for 3 days. The plasma concentrations were determined by LC-MS/MS method. The pharmacokinetic parameters were calculated hy BAS 2. 0 software. Result： The main pharmacokinetic parameters of clemastine fumaxate after a sing/eand nauhiple-dose were as fol- lows： Cmax were（2. 43 ± 1.45） and （5.50 ±0. 74） ng·ml^-1, tmax= were （0. 40 ±0.24） and （0. 43 ±0. 26） h, AUC0-12 were （13. 70 ± 6.70） and （49.80±7.20） ng·h·ml^-1, AUC0-96were （65. 10± 15.70） and （256.90±33.00） ng·h·ml^-1, AUC0-∞ were （82.50± 18.00） and （355. 10 ± 116. 00） ng·h·ml^-1, and t1/2 were （39. 90 ± 7. 30） and （46.60 ± 19. 10） h, respectively. Conclusion： There is significant accumulation after 2 mg intramuscular injection of clemastine fumarate twice a day for 3 days.

关 键 词：富马酸氯马斯汀 液质联用色谱法 单 多次给药 药物动力学 蓄积 

分 类 号：R969.1[医药卫生—药理学]