国产与进口甲钴胺片剂在健康人体的生物等效性

Bioequivalence of domestic and imported mecobalamin tablets in healthy volunteers

目的研究甲钴胺片剂在健康人体内的药代动力学,并比较2种甲钴胺 片剂的生物等效性。方法20名健康男性受试者随机交叉口服单剂量试验和 参比甲钴胺片剂1500μg后,用微粒子捕捉酶免法测定血清中甲钴胺浓度,并 评价2种制剂的生物等效性。结果 口服试验和参比甲钴胺片剂后的Cmax分 别为(615．5±249．4)和(648．6±243．2)pg·mL-1;血清中甲钴胺浓度的增加 量△Cmax分别为(334．7±178．8)和(370．2±189．9)pg·mL-1;tmax分别为(3．2 ±2．4)和(2．7±1．2)h;t1／2分别为(25．1±10．5)和(28．8±11．2)h;△AUC0-t 分别为(7808．4±4628．8)和(7635．5±3430．2)pg·mL·h-1;△AUC0-∞分别 为(9897．5±6092．1)和(10464．3±5820．1)pg·mL·h-1;口服甲钴胺试验制 剂后的相对生物利用度F0-t为(101．52±19．38)％,F0-∞为(93．64±9．49)％。 结论试验和参比甲钴胺片剂具有生物等效性。

Objective To study the pharmacokinetics characteristic of mecobalamin tablets in healthy volunteers, compare the bioavailability and bioequivalence of two mecobalamin tablets. Methods A single oral dose 1500μg of tested and referenced mecobalamin tablets were given to 20 healthy volunteers in a randomized cross - over. The microparticle enzyme immunoassay（MEIA） method was used to assay the concentration of mecobalamin in serum. The pharmacokinetic parameters and bioequivalence were measured. Results The main pharmacokinetic parameters of mecobalamin by oral administration were as follow ： Cmax, were （ 615.5± 249.4 ） and （ 648.6 ± 243.2） pg · mL^- 1,△Cmax were （ 334. 7±178.8 ） and （ 370. 2 ± 189. 9 ） pg · mL^-1 ,tmax were（3.2 ±2. 4） and（2. 7 ±1.2） h,t1/2 were（25.1 ±10. 5）and （28.8± 11.2） h,△AUC0-t were （7808.4±4628.8） and（7635.5 ± 3430.2）pg · mL·h^-1, △AUC0-∞ were（9897.5±6092. 1）and（10464. 3 ± 5820. 1 ） pg ·mL· h^-1 for test and reference mecobalamin tablets, respectively. The relative bioavailability F0-t and F0-∞ were （101.52±19.38） % and （93.64±9.49 ） % , respectively. Conclusion Through the one two - sided test and the analysis of variance, the test and reference mecobalamin tablets are bioequivalence.