摘要
Abstract
Objective To study the pharmacokinetics and relative bioavailability of N-trimethyl chitosan (TMC60) -coated pyridostigmine bromide liposomes ( PB-L) in rabbits. Methods Nine New Zealand rabbits were randomly divided into three groups. Based on the self-crossover control experiment, the rabbits were subjected to single-dose oral administration of TMC60-coated PB-L, uncoated PB-L and marketed PB tablets, respectively. The PB concentrations in the rabbit plasma were determined by HPLC, and the DAS 2. 1. 1 software was applied to calculate the pharmacokinetic parameters and relative bioavailability. Results The pharmaookinetic, property of TMC60-coated PB-L, uncoated PB-L and marketed PB tablets were fitted with two-compartment model with the main pharmacokinetic parameters as follows; Cmax of (15.131 ±0.244)mg · L-1,(15.430 ±0.512)mg · L-1 and( 17. 596 ±0. 484)mg · L-1, tmax of (4.52 ±0.24)h,(4. 05 ±0. 15) h and(2. 33 ±0.28) h, AUC0-∞ of (252.928 ±5. 014) mg · h · L-1 , (222.644+4.243) mg · h · L-1 and (196.553 ±2.982)mg · h · L-1. The relative bioavailability of TMC60-coated PB-L and uncoated PB-L was 128.682% and 101.573% , respectively. Through variance analysis, two one sided t-test and nonparametric test, the bioavailability of TMC60-coated PB-L was increased significantly ( P < 0. 05 ) while that of uncoated PB-L showed no notable difference when compared with that of PB tablets (P > 0. 05 ). Conclusion TMC60-coated PB-L showed the increased bioavailbility in rabbit.关键词
溴吡斯的明/N-三甲基壳聚糖/脂质体/药动学Key words
pyridostigmine bromide/ N-trimethyl chitosan/ liposomes/ pharmacokinetics分类
药学
