Chih-Wei Chang1, Cheng-Yu Wong1, Yu-Tse Wu2, Mei-Chich Hsu3. 1. School of Pharmacy, Kaohsiung Medical University, 100, Shih-Chuan 1st Road, Kaohsiung, 80708, Taiwan. 2. School of Pharmacy, Kaohsiung Medical University, 100, Shih-Chuan 1st Road, Kaohsiung, 80708, Taiwan. ytwu@kmu.edu.tw. 3. Department of Sports Medicine, Kaohsiung Medical University, 100, Shih-Chuan 1st Road, Kaohsiung, 80708, Taiwan. meichich@kmu.edu.tw.
Abstract
BACKGROUND AND 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.
BACKGROUND AND 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.
Authors: M H Criqui; R D Langer; A Fronek; H S Feigelson; M R Klauber; T J McCann; D Browner Journal: N Engl J Med Date: 1992-02-06 Impact factor: 91.245
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