中国临床药理学杂志2024，Vol.40Issue(17)：2543-2547,5.DOI:10.13699/j.cnki.1001-6821.2024.17.018
泊沙康唑肠溶片碾碎给药对比口服混悬液家兔体内药代动力学研究
Pharmacokinetic study of crushed posaconazole enteric-coated tablets compared with oral suspension in rabbits
摘要
Abstract
Objective To compare the pharmacokinetics of crushed posaconazole enteric-coated tablets and oral suspension after intragastric administration in rabbits.Methods The experiment was designed in a randomized cross-over study.Six New Zealand rabbits were intragastrically administrated with crushed posaconazole enteric-coated tablets or suspension,and blood was collected at specific time points.The concentration of posaconazole in plasma was determined by high-performance liquid chromatography,and the pharmacokinetic parameters of both groups were calculated with DAS 2.0 software.Results The main pharmacokinetic parameters of posaconazole enteric-coated tablets and suspension were obtained as follows:AUC0-twere(40.03±5.04)and(49.92±16.09)µg·mL-1·h;AUC0-∞ were(44.00±4.50)and(51.10±16.80)μg·mL-1·h;t1/2 were(7.30±1.13)and(8.53±1.34)h;Cmrx were(3.12±0.57)and(2.78±0.60)μg·mL-1;apparent volume of distribution(Vd)were(2.40±0.34)and(2.59±0.76)L·kg-1;clearance rate(CL)were(0.23±0.02)and(0.22±0.08)L·h-1·kg.There were no statistic differences in AUC0-t,Cmax and Vd between posaconazole suspension and crushed enteric-coated tablets after intragastric administration(all P＞0.05).Conclusion There was no pharmacokinetic advantage for crushed enteric-coated tablets against oral suspension.关键词
泊沙康唑/混悬液/肠溶片碾碎/药代动力学Key words
posaconazole/oral suspension/crushed enteric-coated tablets/pharmacokinetic study分类
药学引用本文复制引用
刘凤喜,李斯雯,宗慧颖,张武林,黄欣,李妍..泊沙康唑肠溶片碾碎给药对比口服混悬液家兔体内药代动力学研究[J].中国临床药理学杂志,2024,40(17):2543-2547,5.基金项目
山东省自然科学基金资助项目(ZR2021QH145) （ZR2021QH145）
山东省药学会医院合理用药天际健康中青年科研学术活动基金资助项目(hlyy2021-04) （hlyy2021-04）
