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人参皂苷Re作为评估微晶纤维素对活性药物成分降解催化潜力的探针。

Ginsenoside Re as a Probe for Evaluating the Catalytic Potential of Microcrystalline Cellulose for the Degradation of Active Pharmaceutical Ingredients.

作者信息

Gao Xinyu, Xiao Shengyuan

机构信息

Engineering Center of Chinese Ministry of Education for Edible and Medicinal Fungi, Jilin Agricultural University, Changchun 130118, China.

出版信息

Pharmaceuticals (Basel). 2025 Jun 11;18(6):869. doi: 10.3390/ph18060869.

Abstract

Microcrystalline cellulose (MCC) is a commonly used pharmaceutical excipient. At present, the catalytic potential of MCCs for the degradation of active pharmaceutical ingredients (APIs) has not been paid adequate attention. This study aims to investigate the representativeness of the pH value of an MCC determined in accordance with the pharmacopeia method to the acidity on its surface. We tested the differences between the catalytic activities of different MCCs and their supernatant prepared in accordance with the pharmacopeia method for the hydrolysis of ginsenoside Re, which is relatively stable in neutral or weak alkaline aqueous solutions but sensitive to acid. The sulfur content of the sulfuric acid-prepared MCC was measured using an ICP-OES. All of the five tested commercially available and two self-prepared MCCs have been found to significantly promote the hydrolysis of ginsenoside Re. But their supernatants were neutral and chemically inert to Re. The sulfur content of the MCC prepared in this experiment using sulfuric acid hydrolysis was determined to be 109.60 µg/g, which is equivalent to 186 to 465 µM of sulfuric acid on the surface. The pH value of an MCC determined in accordance with the pharmacopeia method is not representative of the acidity on its surface. The primary reason should be that there is immobilized acid that is not so easily dissociated into the media. Ginsenoside Re is sensitive and applicable as a probe for the evaluation of the catalytic potential of pharmaceutically used MCCs.

摘要

微晶纤维素(MCC)是一种常用的药用辅料。目前,MCC对活性药物成分(API)降解的催化潜力尚未得到足够关注。本研究旨在探讨按照药典方法测定的MCC的pH值对其表面酸度的代表性。我们测试了不同MCC及其按照药典方法制备的上清液对人参皂苷Re水解的催化活性差异,人参皂苷Re在中性或弱碱性水溶液中相对稳定,但对酸敏感。使用电感耦合等离子体发射光谱仪(ICP-OES)测量硫酸制备的MCC的硫含量。已发现所有测试的五种市售MCC和两种自制MCC均能显著促进人参皂苷Re的水解。但其上清液呈中性,对Re化学惰性。本实验通过硫酸水解制备的MCC的硫含量测定为109.60μg/g,相当于表面硫酸浓度为186至465μM。按照药典方法测定的MCC的pH值不能代表其表面酸度。主要原因应该是存在固定化酸,不易解离到介质中。人参皂苷Re敏感,可作为评估药用MCC催化潜力的探针。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c172/12195823/f82520393496/pharmaceuticals-18-00869-g001.jpg

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