佐米曲普坦片及胶囊的人体生物等效性研究  

Study on the bioequivalence of zolmitriptan preparations

作　　者：钱成兰[1] 王萍[1] 蒋金元 

机构地区：[1]南京医科大学第二附属医院,南京210011 [2]南京泽辰科技有限公司,南京210009

出　　处：《药学与临床研究》2007年第3期195-198,共4页Pharmaceutical and Clinical Research

摘　　要：目的:比较受试佐米曲普坦片和胶囊与阿斯利康公司生产的参比佐米曲普坦片在健康人体内的药代动力学过程,并评价其生物等效性。方法:24名健康男性志愿者按体重配对、随机三交叉单剂量口服佐米曲普坦5 mg,用高效液相色谱质谱选择性离子检测的内标法,测定血浆中药物浓度。结果:单剂量口服佐米曲普坦参比制剂和2种受试制剂5 mg后,三者的主要药代动力学参数:参比制剂、受试片剂、受试胶囊的AUC0-14分别为46.13±15.41 ng.h.mL-1,45.94±17.56 ng.h.mL-1,45.73±15.24 ng.h.mL-1;AUC0-∞分别为48.30±15.93 ng.h.mL-1,47.85±18.22 ng.h.mL-1,47.91±16.10 ng.h.mL-1;cm ax分别为8.84±2.86 ng.mL-1,8.90±3.23 ng.mL-1,8.42±2.53 ng.mL-1;tm ax分别为2.2±1.4 h,2.3±1.0 h,2.7±1.2 h;t1/2(Kel)分别为2.92±0.62 h,2.85±0.61 h,2.88±0.38 h;MRT分别为4.94±0.72 h,4.88±0.67 h,4.97±0.54 h。由AUC0-14计算2种受试制剂相对生物利用度分别为99.6%±17.5%,100.8%±15.9%。结论:2种受试制剂与参比制剂生物等效。Objective：To study the pharmacokinetics and bioequivalence of zolmitriptan in healthy volunteers. Methods： A single oral dose 5mg zolmitriptan of reference or test preparations were given to healthy male volun-teers according to an open randomized three cross-over design. The plasma concentrations of zolmitriptan were determined by a LC/MS method. The pharmacokinetic parameters and bioavailability of two test prepartions were compared with reference preparation. Results： The main pharmacokinetic parameters of reference sample, test tablets and capsules were as follows： AUCo-14 were 46.13±15.41 ng·h·mL^-1 and 45.94±17.56 ng·h·mL^-1, 45.73±15.24 ng·h·mL^-1 ;AUCo-∞ were 48.30±15.93 ng·h·mL^-1 and 47.85± 18.22 ng·h·mL^-1 ,47.91±16.10ng·h·mL^-1 ;Cmax were 8.84±2.86 ng·mL^-1 and 8.90±3.231 ng·mL^-1,8.42 ±2.53 ng·mL^-1 ;tmax were2.2±l.4h and 2.3±1.0 h,2.7±1.2 h;tl/2（Kel） were 2.92±0.62h and 2.85 ±0.61 h,2.88± 0. 38 h;MRT were 4. 94 ± 0. 72 h and 4. 88 ± 0. 67 h,4. 97± 0. 54 h. The relative bioavailability of two test preparations compared with reference preparation were （99.6 ±17.5 ） % and （ 100. 8 ± 15.9 ） % . Conclusion： Statistics showed that the two tested preparations and the reference preparation are bioequivalent.

关 键 词：佐米曲普坦 LC/MS 药代动力学 生物利用度 生物等效性 交叉设计 

分 类 号：R969.1[医药卫生—药理学]