Rapid and cost‐effective LC–MS/MS method for determination of hydroxycitric acid in plasma: Application in the determination of pharmacokinetics in commercial Garcinia preparations

Abstract

Garcinia cambogia is one of the most commonly used anti‐obesity dietary supplements, and hydroxycitric acid (HCA) is a major constituent in the commercial preparations of Garcinia. High doses of HCA are often consumed without much awareness of its pharmacokinetic and toxicokinetic parameters, and therefore, a complete understanding of its effects is lacking. The first step in understanding these parameters is the availability of a reliable bioanalytical method. Here, we present the first report on a UPLC–MS/MS method for analysis of HCA in rat plasma after a simplified and cost‐effective protein precipitation. Chromatographic separation of the analytes in the supernatant was achieved using hydrophilic interaction liquid chromatography, where mass parameters were optimized and a rapid 5‐min quantitative assay was developed. The method was highly sensitive, accurate, precise and linear in the concentration range of 10.5–5000 ng/mL (validated according to the United States Food and Drug Administration guidelines). Further, the method was successfully used to describe the pharmacokinetic profile of HCA in rat plasma after the administration of pure HCA and commercial Garcinia preparations.

Statistical Design of Sustained-Release Tablet Garcinia cambogia Extract and Bioconverted Mulberry Leaf Extract for Anti-Obesity

“…We consider the GABMUL tablet to be an oral tablet. The half-lives of hydroxycitric acid (an indicator of GA) and polyphenol (an indicator of BMUL) are around 5.4 and 4 h in rats, according to the literature [ 23 , 24 ]. In the release test, the GA + BMUL tablet showed a sustained-release profile.…”

Recent Advances in Garcinia cambogia Nutraceuticals in Relation to Its Hydroxy Citric Acid Level. A Comprehensive Review of Its Bioactive Production, Formulation, and Analysis with Future Perspectives

“…Likewise, HCA was analyzed in rat plasma after i.v. administration of a dose of 1 mg/kg, where the half-life and the apparent volume of distribution of HCA reached 2.1 ± 0.4 h and 0.6 ± 0.15 L/kg, respectively, whereas with oral administration of 20 mg/kg, HCA showed maximum plasma concentration C max at 14.4 μg/mL reached at 1 h. The method was reproducible, sensitive, accurate, precise, and linear in the concentration range of 10–5000 ng/mL . Further, the method was successfully used to determine HCA pharmacokinetics (PKs) in rat plasma after the administration of pure HCA and a commercial Garcinia preparation.…”

“…The method reported can be further used routinely for the analysis of HCA and could be helpful for further toxicological evaluation of Garcinia products alone or in a mixture. 59 A validated analytical method for quantification of HCA in rat plasma and fetal homogenate using LC-MS/MS analysis was reported. Results revealed that at a range of 20–800 ng/mL the method was linear with limits of quantitation (LOQ) and detection (LOD) equal to 20.0 and 3.9 ng/mL plasma, respectively.…”

“…The quantification of HCA in humans and rats was evaluated using a rapid, selective, and sensitive UPLC-MS/MS method. , HCA was analyzed in 16 healthy subjects after oral administration of G. cambogia extract revealing an excellent mean peak area ratio of 0.98 and coefficient of variation CV% of 7.17 from normal, lipemic, and hemolyzed plasma samples . Excellent intra-assay and inter-assay precision were achieved, ranging from 5.02% to 12.01% (CV%) as well as intra- and interassay accuracy ranging from 0.29% to 9.20% relative errors (RE%).…”

“…The method was successfully used to determine in vivo PKs of HCA revealing that it is rapidly absorbed with moderate apparent volume of distribution and a good bioavailability. The method reported can be further used routinely for the analysis of HCA and could be helpful for further toxicological evaluation of Garcinia products alone or in a mixture . A validated analytical method for quantification of HCA in rat plasma and fetal homogenate using LC-MS/MS analysis was reported.…”