氢溴酸西酞普兰咀嚼片人体生物利用度和生物等效性研究  

Bioavailability and bioequivalence research for chewable tablet of citalopram hydrobromide in healthy volunteers

作　　者：张丽娟[1] 李海燕[1] 郝光涛[1] 刘泽源[1] 

机构地区：[1]军事医学科学院附属医院药学部,北京100071

出　　处：《实用药物与临床》2011年第6期480-483,共4页Practical Pharmacy and Clinical Remedies

摘　　要：目的比较国产氢溴酸西酞普兰咀嚼片与进口氢溴酸西酞普兰片的人体药动学参数及生物利用度,评价二者的生物等效性。方法 24名健康男性受试者随机交叉单剂量服用20 mg受试制剂和参比制剂,受试制剂空腹咀嚼30～60 s后直接吞咽,参比制剂空腹用200 mL温开水送服。血浆样品采用高效液相色谱-串联质谱法检测。结果受试制剂及参比制剂的主要药代动力学参数:Cmax分别为(16.56±4.12)、(18.30±4.72)μg/L;Tmax分别为(4.42±2.41)、(5.00±2.87)h;t1/2分别为(47.44±7.74)、(48.43±14.56)h;AUC0-tn分别为(819.74±261.18)、(885.38±216.22)μg.h/L;AUC0-∞分别为(939.00±336.16)、(1 016.04±315.32)μg.h/L;受试制剂的相对生物利用度F0-tn、F0-∞分别为91.92%±15.10%、92.09%±15.52%。结论受试制剂和参比制剂具有生物等效性。Objective To compare the relative bioavailability and the bioequivalence between domestic-made chewable tablets（to be tested）and imported tablets（reference）of citalopram hydrobromide and evaluate the bioequivalence of the two preparations.Methods A single dose of 20 mg of chewable tablets or referenced tablet of citalopram hydrobromide was administered with empty stomach by randomized crossover way in 24 healthy male volunteers.The chewable tablet was swallowed after been chewed for 30~60 s,while the referenced tablet was administered with warm water of 200 mL.The concentrations of the citalopram in plasma were detected by LC-MS/MS method.Results The main pharmacokinetics parameters of the chewable tablets and the referenced tablets were as follows：Cmax（16.56±4.12）vs.（18.30±4.72）μg/L,Tmax（4.42±2.41）vs.（5.00±2.87）h,t1/2（47.44±7.74）vs.（48.43±14.56）h,AUC0-tn（819.74±261.18）vs.（885.38±216.22）μg · h/L,AUC0-∞（939.00±336.16）vs.（1016.04±315.32）μg · h /L.The relative bioavailability F0-tn、F0-∞ of the citalopram hydrobromide chewable tablet were 91.92%±15.10% and 92.09%±15.52% respectively.Conclusion There are bioequivalence between domestic-made chewable tablets and imported tablets of citalopram hydrobromide.

关 键 词：西酞普兰 药动学 生物等效性 生物利用度 高效液相色谱-串联质谱 

分 类 号：R96[医药卫生—药理学]