Pharmacokinetic study of crushed posaconazole enteric-coated tablets compared with oral suspension in rabbits
10.13699/j.cnki.1001-6821.2024.17.018
- VernacularTitle: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
- Author:
Feng-Xi LIU
1
;
Si-Wen LI
;
Hui-Ying ZONG
;
Wu-Lin ZHAG
;
Xin HUANG
;
Yan LI
Author Information
1. 山东第一医科大学第一附属医院(山东省千佛山医院)临床药学,山东省儿童药物临床评价与研发工程技术究中心,山东省医药卫生临床药学重点实验室,山东济南 250014
- Keywords:
posaconazole;
oral suspension;
crushed enteric-coated tablets;
pharmacokinetic study
- From:
The Chinese Journal of Clinical Pharmacology
2024;40(17):2543-2547
- CountryChina
- Language:Chinese
-
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.
