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黏膜生物转化

Mucosal biotransformation.

作者信息

Schwenk M

机构信息

Department of Pharmacology, Medizinische Hochschule Hannover, Federal Republic of Germany.

出版信息

Toxicol Pathol. 1988;16(2):138-46. doi: 10.1177/019262338801600206.

Abstract

About 4 million compounds have been described by chemists, and some 60,000 are presently on the market. The search for new chemicals with better properties and less toxicity continues, and future life quality will depend on our ability to find the safest compounds in each field of application. During development of new drugs and chemicals, studies on biotransformation should be done very early, and with adequate analytical tools, in order to get an early understanding of data on bioavailability, metabolic pattern, and toxicity. Though the liver is generally the organ with the highest drug metabolizing activity, it becomes increasingly evident that some extrahepatic organs, such as intestine, kidney, skin, and lung also participate in drug metabolism. The peculiar property of intestinal metabolism is the fact that it modifies chemicals before they enter the circulation. Therefore, an understanding of intestinal metabolism is important for proper interpretation of all pharmacological and toxicological data during development of a new compound. Mucosal biotransformation has recently been reviewed. The present work gives a schematic survey on the topic, shows new trends, and discusses the consequences for toxicological testing of new chemicals.

摘要

化学家已描述了约400万种化合物,目前约有6万种投放市场。对具有更好性能和更低毒性的新化学品的探索仍在继续,未来的生活质量将取决于我们在每个应用领域找到最安全化合物的能力。在新药和新化学品的研发过程中,应尽早使用适当的分析工具开展生物转化研究,以便尽早了解生物利用度、代谢模式和毒性数据。虽然肝脏通常是药物代谢活性最高的器官,但越来越明显的是,一些肝外器官,如肠道、肾脏、皮肤和肺也参与药物代谢。肠道代谢的独特之处在于它在化学物质进入循环之前就对其进行修饰。因此,了解肠道代谢对于在新化合物研发过程中正确解读所有药理学和毒理学数据非常重要。黏膜生物转化最近已有综述。本文对该主题进行了简要概述,展示了新趋势,并讨论了其对新化学品毒理学测试的影响。

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