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用一种新的全面稳定性指示 HPLC 方法比较熊果苷在越桔中的稳定性。

Comparative stability of arbutin in Arctostaphylos uva-ursi by a new comprehensive stability-indicating HPLC method.

机构信息

Departamento de Produtos Farmacêuticos, Faculdade de Farmácia, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil.

出版信息

Phytochem Anal. 2020 Nov;31(6):884-891. doi: 10.1002/pca.2953. Epub 2020 Jun 4.

Abstract

INTRODUCTION

Arbutin is a phenol glucoside found in high concentrations in bearberry leaves and associated with the antimicrobial activity of the plant. Hydroquinone can also be found in leaves or be formed by degradation of arbutin. Lengthy exposure to free hydroquinone is associated with induction of toxicity in different organs.

OBJECTIVE

To develop and validate a stability-indicating method by high-performance liquid chromatography diode array detector (HPLC-DAD) for simultaneous quantification of arbutin and hydroquinone in bearberry leaves and perform a comprehensive forced degradation study comparing synthetic arbutin and the arbutin in bearberry leaves.

METHODS

Separation was performed using a C18 column, mobile phase with water-methanol (95:5), flow rate 1.0 mL/min and detection at 280 nm. Bearberry leaves were assayed and a forced degradation study of arbutin was performed in different conditions.

RESULTS

The method complied with all required validation parameters. Contents varied from 1.19 to 4.15% (w/w) of arbutin and from 0.022 to 0.604% (w/w) of hydroquinone. Synthetic arbutin was susceptible to acid hydrolysis and oxidative degradation, forming hydroquinone as the main degradation product. The same study using bearberry leaves showed that constituents of the plant matrix may act as antioxidants, reducing the oxidative degradation of arbutin, however acid hydrolysis of arbutin occurred in higher intensity.

CONCLUSION

Analysis of bearberry leaves evidenced high variation in arbutin and hydroquinone levels, demonstrating the need for standardisation and control. The stability profiles of synthetic arbutin and the arbutin in bearberry leaves were considerably different and the results may be useful for determining the most appropriate conditions for extraction and production of bearberry-based formulations.

摘要

简介

熊果苷是一种苯丙素糖苷,在熊果叶中含量很高,与植物的抗菌活性有关。氢醌也可以在叶子中找到,或者由熊果苷降解形成。长时间接触游离氢醌会导致不同器官的毒性诱导。

目的

建立并验证一种高效液相色谱二极管阵列检测器(HPLC-DAD)的稳定性指示方法,用于同时定量测定熊果叶中的熊果苷和氢醌,并对合成熊果苷和熊果叶中的熊果苷进行全面的强制降解研究。

方法

采用 C18 柱,水-甲醇(95:5)为流动相,流速 1.0 mL/min,检测波长 280nm。对熊果叶进行测定,并在不同条件下对熊果苷进行强制降解研究。

结果

该方法符合所有要求的验证参数。熊果苷的含量为 1.19%至 4.15%(w/w),氢醌的含量为 0.022%至 0.604%(w/w)。合成熊果苷易发生酸水解和氧化降解,形成氢醌为主要降解产物。对熊果叶的相同研究表明,植物基质的成分可能起到抗氧化剂的作用,降低熊果苷的氧化降解,但熊果苷的酸水解强度更高。

结论

对熊果叶的分析表明,熊果苷和氢醌的含量差异很大,需要进行标准化和控制。合成熊果苷和熊果叶中熊果苷的稳定性曲线有很大的不同,结果可能有助于确定最适合熊果叶提取和生产熊果叶制剂的条件。

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