溴吡斯的明口腔崩解片和普通片在兔体内的生物等效性

Study on pharmacokinetics of pyridostigmine bromide orally disintegrating tablets and common tablets in rabbits

目的:研究新西兰大耳白兔口服溴吡斯的明口腔崩解片和普通糖衣片后的药动学。方法:12只新西兰大耳白兔随机分为2组,分别口服给予溴吡斯的明口腔崩解片和市售普通片(60mg),反相离子对色谱法测定血浆药物浓度,用DAS2.1.1药动学软件计算药动学参数。结果:口腔崩解片和普通片均符合一室开放模型,Cmax分别为(1.81±0.09)mg.L-1和(1.71±0.03)mg.L-1;tmax分别为(2.25±0.27)h和(2.67±0.26)h;t1/2分别为(3.0±0.8)h和(3.27±0.18)h;AUC0-24分别为(15.8±0.5)mg.h.L-1和(14.85±0.17)mg.h.L-1;AUC0-∞分别为(16.1±0.6)mg.h.L-1和(15.14±0.19)mg.h.L-1;口腔崩解片相对生物利用度F0-24为106.19%,F0-∞为106.07%;经方差分析、双单侧t检验和非参数检验,两制剂在兔体内无显著性差异。结论:两种制剂生物等效。

OBJECTIVE To compare the pharmacokinetic characteristics of pyridostigmine bromide orally disintegrating tablets with common tablets in rabbits by oral administration. METHODS Pyridostigmine bromide orally disintegrating tablets and common tablets were orally administrated to rabbits in a randomzied study. The concentration of pyridostigmine bromide in plasma was determined by reversed phase ion pair chromatography. Pharmacokinetic parameters were calculated by DAS 2. 1.1. RESULTS Pyridostigmine bromide orally disintegrating tablets and common tablets were fitted to the one compartment opened model. The pharmacokinetic parameters of pyridostigmine bromide orally disintegrating tablets and common tablets in rabbit plasma were as follows： Cmax （1. 81 ± 0. 09）mg· L^-1 and（ 1.71 ± 0. 03） mg·L^-1 ;tmax （2. 25 ± 0. 27）h and （2. 67 ± 0. 26）h;t1/2 （3. 0 ± 0. 8）h and （3.27 ± 0. 0. 18）h;AUG0-24, （15. 8 ± 0. 5）mg·h·L^-1 and （14. 85 ± 0. 17）mg·h·L^-1 ;AUC0-∞ （16. 1 ± 0. 6） mg·h·L^-1 and （15. 14 ± 0. 19）mg·h·L^-1. The relative bioavailability F0-24 was 106. 19% and F0-∞ was 106. 07%. The main pharmacokinetic parameters analyzea by variance, two side t-test and wilcoxon rank sum test, there was no significant difference between orally disintegrating tablets and market common tablets in viw. CONCLUSION The two preparations studied are bioequivalent.