Abstract
Methods for a dissolution study by ultra-high performance liquid chromatography/triple quadrupole mass spectrometry (UHPLC-QqQ/MS) analysis of grape polyphenol dietary supplements, namely, grape seed extract (GSE) and resveratrol (RSV) capsules, were developed following the guidance of United States Pharmacopeia (USP) <2040>. Two dissolution media, 0.1 N hydrochloric acid (pH 1.2) and 0.05 M acetate buffer (pH 4.6), were evaluated with dissolution apparatus (USP 1), 100 rpm rotation speed, and 900 ml dissolution medium volume. Dissolution profiling was performed over 120 min. Major phenolic compounds of gallic acid, catechin, epicatechin, and procyanidin B2 were quantitated to obtain the dissolution profile of GSE capsules, and trans-RSV was used for RSV capsules. Results indicated that the released trans-RSV for RSV capsules in both of the dissolution media meets the USP standards, and that for the GSE capsules, all the four marker compounds passed the dissolution test in the HCl medium but did not reach a 75% release within 60 min in the acetate buffer. These promising results suggest that the general USP dissolution protocols are adequate for the successful release of RSV capsules in HCl medium and acetate buffer and GSE capsules (in HCl medium), but may be inadequate for GSE capsules in acetate buffer. These results showed that under a low pH of 1.2 (simulated stomach environment), bioactive compounds were released on time from the GSE capsules and met the USP guidelines; however, under a higher pH of 4.6 (simulated duodenum environment), the same biomarkers failed, suggesting the need to further improve the dissolution of GSE over a wider range of pH environments to enhance bioavailability and efficacy.
Highlights
Grape (Vitis vinifera) is native to southern Europe and Western Asia and is grown all over the world today
For all the tested grape seed extract (GSE) capsules, the percentage of four marker compounds released from GSE capsules was calculated based on analytically measured amounts
A novel dissolution test and LC/MS analysis were developed to evaluate the performance of grape polyphenol dietary supplements, namely, GSE and RSV capsules
Summary
Grape (Vitis vinifera) is native to southern Europe and Western Asia and is grown all over the world today. It has gained a high level of interest from the public health sector because of its numerous active components [1]. The United States Pharmacopeia (USP) has established performance standards to detect their release from dosage forms in capsules and tablets that may occur as a result of formulation design or manufacturing processes in order to ensure safety and bioavailability [10, 11]. The USP general chapter describes a set of standardized test protocols tailored for specific combinations of dosage form and ingredient content category and dissolution protocols for vitamin/mineral DSs, it does not specify a dissolution protocol for testing grape-based DSs [10]
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