非甾体抗炎药的原药:综述。

Q2 Pharmacology, Toxicology and Pharmaceutics Open Medicinal Chemistry Journal Pub Date : 2017-11-30 eCollection Date: 2017-01-01 DOI:10.2174/1874104501711010146
Kamal Shah, Jeetendra K Gupta, Nagendra S Chauhan, Neeraj Upmanyu, Sushant K Shrivastava, Pradeep Mishra
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引用次数: 0

摘要

内吸法:原药方法涉及化学生物转化或酶转化,或涉及活性药物分子的非活性或活性较低的生物可逆衍生物。它们必须经过酶或化学生物转化才能发挥药理作用:两种不同的药理作用结合在一起,可产生协同活性,或有助于将活性药物靶向作用于靶点。原药超级种子解决了原药设计的各种问题,例如提高溶解度、生物利用度、化学稳定性、系统前代谢、特定部位给药、毒性掩蔽、提高病人接受度或消除不良反应:结果:近年来,人们一直在寻找毒性降低的原药或互利原药。结果:近年来,人们一直在寻找具有减毒作用的原药或互效原药。本综述强调了这一共同的帮助,以改善药物的理化、制药和治疗效果:结论:这为研究人员提供了一个共同的平台,使他们可以找到常用非甾体抗炎药的原药,以克服胃肠道毒性(刺激、溃疡和出血)。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Prodrugs of NSAIDs: A Review.

Intoroduction: Prodrug approach deals with chemical biotransformation or enzymatic conversion or involves inactive or less active bio-reversible derivatives of active drug molecules. They have to pass through enzymatic or chemical biotransformation before eliciting their pharmacological action.

Methods & materials: The two different pharmacophores combine to give synergistic activity or may help in targeting the active drug to its target. Prodrug super seeds the problems of prodrug designing, for example solubility enhancement, bioavailability enhancement, chemical stability improvement, presystemic metabolism, site specific delivery, toxicity masking, improving patient acceptance, or eradicating undesirable adverse effects.

Results: As an outcome the search for a prodrug or mutual prodrug with reduced toxicity has continued during recent years. This present review emphasizes the common help to revamp physiochemical, pharmaceutical and therapeutic effectiveness of drugs.

Conclusion: This gives the researcher a common platform where they can find prodrugs of commonly used NSAIDs to overcome the gastrointestinal toxicity (irritation, ulcergenocity and bleeding).

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来源期刊
Open Medicinal Chemistry Journal
Open Medicinal Chemistry Journal Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
4.40
自引率
0.00%
发文量
4
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