Absorption mechanism of kirenol and pharmacokinetic analysis of its sustained-release pellets in beagles
HE Dong-mei
GUAN Shi-xia
FU Hong-zheng
LU Shu-fan
ZHOU Xiang-ping
Abstract：Objective:To investigate the absorption characteristics of kirenol in the gastrointestinal tract of rats,and the pharmacokinetics of kirenol stuff and homemade sustained-release pellets in Beagle dogs.Methods:The in situ closed loop method and everted gut sacs model were used to explore the absorption characteristics;A single oral dose of kirenol stuff and sustained-release pellets at a dosage of 2 mg· kg-1 was performed according to a two-period crossover design,The concentration of kirenol was determined by LC-MS.Results:Kirenol was absorbed by both the stomach and intestine,but the absorption was better in the intestine than in the stomach (P ＜0.01);The Ka of different intestine segments increased with the increase of the concentration of Kirenol;The characteristics of plasma concentration-time curve was fitted to a two-compartment model,The AUC0-t of sustainedrelease pellets was 6.56 times higher,compared with stuff.Conclusion:The intestinal was the main absorption site of kirenol,and the absorption pattern suggested that kirenol was passively transported;Compared with the stuff,the kirenol sustained-release pellets showed sustained-release characteristics,and the bioavailability was significantly improved.
Keywords：kirenolgastrointestinal absorptionsustained-release pelletsbeaglepharmacokinetics
Publication Date：2017-01-01
Online Publishing Date：2026-08-14(First online date of this platform, not the publication date of the document)
Pages：6( 2788-2793 )