沙丁胺醇包合物缓释片在家犬体内药动学研究

Pharmacokinetics of Salbutamol-Ethylated β-Cyclodextrins Complexes Sustained Release Tablets in Dogs

对沙丁胺醇包合物缓释片和市售普通片进行了家犬单剂量交叉口服给药的药动学研究 ,采用高效液相色谱 -荧光法测定血药浓度。缓释片和普通片药动学参数 Tmax分别为 7.0± 2 .6和 2 .2± 0 .8h,Cmax分别为 12 8.5± 2 4.1和 2 0 1.2± 10 .6 ng/ m l,AUC分别为 116 2 .2± 2 0 0 .9和 10 5 4.4± 15 7.3ng· h· ml- 1。缓释片相对于普通片的生物利用度为 110 .1% 。

The pharmacokinetics and bioavailability of salbutamol ethylated β cyclodextrins complexes sustained release tablets (tested tablets) and salbutamol tablets (reference tablets) were investigated in dogs for single dose according to a randomized crossover design. Drug concentrations in dogs plasma were determined by HPLC with fluorescence detection. The pharmacokinetic parameters for the single dose of tested and reference tablets were T max 7.0±2.6 and 2.2±0.8 h, C max 128.5±24.1 and 201.2±10.6 ng/ml, AUC 1162.2±200.9 and 1054.4±157.3 ng·h·ml -1 , respectively. The relative bioavailability of tested tablets was 110.1% compared with reference tablets. The results showed that the tested tablets had correlation between in vivo absorption and in vitro release.