| 张靖,李盼盼,杨锐,肖新月,邹健,涂家生.口服药物中药用辅料对胃肠渗透影响的研究进展[J].中国药事,2021,35(12):1383-1390 |
| 口服药物中药用辅料对胃肠渗透影响的研究进展 |
| Research Progress on the Effect of Oral Drug Excipients on Gastrointestinal Permeability |
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| DOI：10.16153/j.1002-7777.2021.12.009 |
| 中文关键词: 药用辅料 口服制剂 胃肠吸收 渗透性 |
| 英文关键词: pharmaceutical excipients oral preparations gastrointestinal absorption permeability |
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| 中文摘要: |
| 目的： 汇总分析国内外对于药用辅料影响口服药物胃肠渗透的相关研究，及其常用的体外吸收预测模型，为药物制剂的研发、处方的筛选等提供参考。方法：对药用辅料影响药物胃肠渗透的方式进行分类、归纳和整理，同时对几种常用于体外吸收预测的模型进行分析。结果：药用辅料可以通过改变胃肠蠕动、影响肠细胞P-糖蛋白介导的外排和影响药物的溶出，从而影响药物活性成分在胃肠道内的渗透吸收。常用的体外吸收预测模型主要有人结肠腺癌细胞模型、动物在体和离体模型及利用平行人工膜的实验模型。结论：在对口服药物的体内吸收进行研究时，区别于以往辅料作为惰性物质的观念，应更加注重辅料对药物在胃肠吸收过程中的影响。在体内外吸收预测模型方面，平行人工膜通透性测定以其分析快速且重现性好等优点引起了越来越多的关注。 |
| 英文摘要: |
| Objective: To summarize and analyze the relevant researches about the effect of oral drug excipients on the gastrointestinal penetration at home and abroad, and the commonly-used in vitro absorption prediction models in order to provide references for the development of pharmaceutical preparations and prescription screening. Methods: The ways in which pharmaceutical excipients affect the gastrointestinal penetration of drugs were classified, summarized and sorted out, and several models commonly used in in vitro absorption prediction were analyzed. Results: Pharmaceutical excipients could affect the osmotic absorption of active ingredients in the gastrointestinal tract by changing gastrointestinal peristalsis, affecting the efflux mediated by intestinal cells P-glycoprotein and affecting the dissolution of drugs. The commonly-used in vitro absorption prediction models are mainly human colon adenocarcinoma cell (Caco-2) models, in vivo and in vitro animal models and experimental models using parallel artificial membranes. Conclusion: In the study of the in vivo absorption of oral drugs, different from the previous concept of excipients as inert substances, more attention should be paid to the influence of excipients on the gastrointestinal absorption process. In terms of in vivo and in vitro absorptionprediction models, parallel artificial membrane permeability assay (PAMPA) has attracted more and more attention due to its rapid analysis and good reproducibility. |
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