Investigation in vitro Release Rate and in vivo Pharmacokinetics of Resveratrol/Hydroxypropyl- β-Cyclodextrin/Chitosan Sustained-release Pellets in Rats
- VernacularTitle:白藜芦醇/羟丙基-β-环糊精/壳聚糖缓释微球的体外释放度及其在大鼠体内药动学的考察
- Author:
Chenchen YU
1
;
Chungang ZHANG
1
;
Li YIN
1
;
Yixuan ZHOU
1
;
Lan CHENG
1
;
Tingguo KANG
1
Author Information
1. School of Pharmacy，Liaoning University of TCM，Liaoning Dali an 116620，China
- Publication Type:Journal Article
- Keywords:
Resveratrol;
Hydroxypropyl-β-cyclodextrin;
Chitosan;
Release rate;
Pharmacokinetics;
Rats
- From:
China Pharmacy
2019;30(19):2603-2607
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE： To investigate in vitro release rate and in vivo pharmacokinetics of Resveratrol/hydroxypropyl-β- cyclodextrin/chitosan sustained-release pellets （RES/HP-β-CD/Chitosan） in rats. METHODS： In vitro release rate of RES raw materials， RES-HP-β-CD complexes （RES/HP-β-CD） and RES/HP-β-CD/Chitosan in water within 12 h were investigated by paddle method. The pharmacokinetic characteristics of RES raw materials， RES/HP-β-CD and RES/HP-β-CD/Chitosan were compared within 720 min after intragastric administration. RESULTS： Compared with RES raw materials， in vitro release rate of RES/HP-β-CD was increased significantly， and 120 min accumulative release rate reached 87％. Compared with RES/HP-β-CD， in vitro release rate of RES/HP-β-CD/Chitosan were relieved significantly； release time prolonged significantly； 12 h accumulative release rate was 72％. The pharmacokinetic parameters of RES raw materials， RES/HP-β-CD and RES/HP-β-CD/Chitosan included that cmax were 473.3， 2 492.2， 590.5 ng/mL； t1/2 were 2.6， 0.5， 4.6 h； AUC0-12 h were 514.7， 824.6， 2 778.5 ng·h/mL. Compared with RES raw materials， relative bioavailability of RES/HP-β-CD and RES/HP-β-CD/Chitosan were 172.5％ and 540.0％. CONCLUSIONS： RES/HP-β-CD/Chitosan shows good sustained-release effect， and its bioavailability is significantly higher than that of RES raw materials， RES/HP-β-CD.
