高效液相色谱-荧光检测法研究胃保护剂量辣椒素的毒代动力学。
Toxicokinetic Study of a Gastroprotective Dose of Capsaicin by HPLC-FLD Method.
机构信息
Institute of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Pécs, Rókus str. 2, H-7624 Pécs, Hungary.
Department of Forensic Medicine, Medical School, University of Pécs, Szigeti str. 12, H-7624 Pécs, Hungary.
出版信息
Molecules. 2019 Aug 5;24(15):2848. doi: 10.3390/molecules24152848.
BACKGROUND
A low dose of capsaicin and its natural homologs and analogs (capsaicinoids) have shown to prevent development of gastric mucosal damage of alcohol and non-steroid anti-inflammatory drugs. Based on this experimental observation, a drug development program has been initiated to develop applicable capsaicin containing drugs to eliminate gastrointestinal damage caused by non-steroid anti-inflammatory drugs.
METHODS
As a part of this program, a sensitive and selective reverse-phase high-performance liquid chromatography-based method with fluorescence detection has been developed for quantification of capsaicin and dihydrocapsaicin in experimental dog's plasma.
RESULTS
The method was evaluated for a number of validation characteristics (selectivity, repeatability, and intermediate precision, LOD, LOQ, and calibration range). The limit of detection (LOD) was 2 ng/mL and the limit of quantification (LOQ) was 10 ng/mL for both capsaicin and dihydrocapsaicin. The method was used for analysis of capsaicin and dihydrocapsaicin in the plasma samples obtained after administration of low doses (0.1, 0.3, and 0.9 mg/kg bw) of Capsaicin Natural (USP 29) to the experimental animals.
CONCLUSIONS
The obtained results indicated that the administered capsaicinoids did not reach the general circulation.
背景
低剂量的辣椒素及其天然同系物和类似物（辣椒素类）已被证明可预防酒精和非甾体抗炎药引起的胃黏膜损伤。基于这一实验观察，已经启动了一项药物开发计划，以开发含有适用辣椒素的药物来消除非甾体抗炎药引起的胃肠道损伤。
方法
作为该计划的一部分，开发了一种基于反相高效液相色谱法和荧光检测的灵敏、选择性方法，用于定量实验犬血浆中的辣椒素和二氢辣椒素。
结果
该方法经过了多项验证特性（选择性、重复性和中间精密度、检测限、定量限和校准范围）的评估。辣椒素和二氢辣椒素的检测限（LOD）均为 2 ng/mL，定量限（LOQ）均为 10 ng/mL。该方法用于分析在实验动物中给予低剂量（0.1、0.3 和 0.9 mg/kg bw）辣椒素天然品（USP 29）后获得的血浆样品中的辣椒素和二氢辣椒素。
结论
所得结果表明，给予的辣椒素类物质未到达体循环。
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