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快速且经济高效的 LC-MS/MS 法测定血浆中羟基柠檬酸:在商业藤黄属制剂药代动力学测定中的应用。

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.

机构信息

Department of Pharmacy, Birla Institute of Technology and Science (BITS) Pilani, Pilani, India.

Pharmaceutical Candidate Optimization, Biocon Bristol Myers Squibb R&D Centre, Syngene International Limited, Bangalore, India.

出版信息

Biomed Chromatogr. 2020 Oct;34(10):e4902. doi: 10.1002/bmc.4902. Epub 2020 Jun 11.

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.

摘要

藤黄果是最常用的抗肥胖饮食补充剂之一,而羟基柠檬酸(HCA)是藤黄果商业制剂中的主要成分。人们在服用 HCA 高剂量时,往往对其药代动力学和毒代动力学参数没有太多了解,因此对其作用缺乏全面的认识。了解这些参数的第一步是要有可靠的生物分析方法。在这里,我们首次报道了一种用于分析大鼠血浆中 HCA 的 UPLC-MS/MS 方法,该方法经过简化和具有成本效益的蛋白沉淀处理。在亲水作用色谱中,对上清液中的分析物进行了色谱分离,对质谱参数进行了优化,并开发了快速的 5 分钟定量分析方法。该方法灵敏度高、准确、精密且线性范围在 10.5-5000ng/mL 之间(根据美国食品和药物管理局的指南进行验证)。此外,该方法还成功地用于描述纯 HCA 和商业藤黄果制剂给药后大鼠血浆中 HCA 的药代动力学特征。

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