Development of a Solid Dispersion System for Improving the Oral Bioavailability of Resveratrol in Rats.
OBJECTIVE
Resveratrol (3,4',5-trihydroxy-trans-stilbene; RES) produces a variety of pharmacological effects; however, its oral bioavailability (BA) approaches zero. In this study, grape peel extract (GPE) was incorporated into a solid dispersion delivery system to improve the solubility, dissolution and oral absorption of RES.


METHODS
The dripping pill (DP) oral delivery system was developed through the hot-melt method, and the optimal formulation consisted of GPE, propylene glycol monocaprylate, poloxamer 188, polyoxyl 35 castor oil and polyethylene glycol 6000.


RESULTS
The DPs enhanced the (mean ± SD) dissolution of RES from 23.3 ± 1.0 to 67.8 ± 0.4 %. The pharmacokinetic profiles in the rats revealed that the DPs increased the oral BA of RES from 0.9 ± 0.1 to 10.5 ± 0.9 %; this represented an approximately 12-fold increase in absorption.


CONCLUSIONS
Our results indicated that the DP formulation improves the dissolution and oral BA of RES. Thus, this could be an effective and practical technique for food and pharmaceutical applications.
School of Pharmacy, Kaohsiung Medical University, 100, Shih-Chuan 1st Road, Kaohsiung, 80708, Taiwan.
Chih-Wei
CW
Chang
School of Pharmacy, Kaohsiung Medical University, 100, Shih-Chuan 1st Road, Kaohsiung, 80708, Taiwan.
Cheng-Yu
CY
Wong
School of Pharmacy, Kaohsiung Medical University, 100, Shih-Chuan 1st Road, Kaohsiung, 80708, Taiwan. ytwu@kmu.edu.tw.
Yu-Tse
YT
Wu
Department of Sports Medicine, Kaohsiung Medical University, 100, Shih-Chuan 1st Road, Kaohsiung, 80708, Taiwan. meichich@kmu.edu.tw.
Mei-Chich
MC
Hsu
D000284:Administration, Oral; D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical / Q000379:methods; D016503:Drug Delivery Systems; D005079:Excipients / Q000737:chemistry; D008297:Male; D010936:Plant Extracts / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley; D000077185:Resveratrol; D012995:Solubility; D013267:Stilbenes / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D027843:Vitis / Q000737:chemistry
D000975:Antioxidants; D005079:Excipients; D010936:Plant Extracts; D013267:Stilbenes; D000077185:Resveratrol