水溶性差药物的溶解度:技术和替代方案

Komal Singh, P. Singh, Amanda Frank, Saahil Arora, Rajiv Sharma, Neha Bajwa
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引用次数: 1

摘要

影响药物生物利用度的最重要变量是其水溶性。制药企业面临的最大问题之一是提高水溶性,这是提高疗效的关键。在第一次筛选过程中,超过50%的新开发药物被发现是不溶性或弱溶性的。该药物的溶解度可通过多种技术加以提高。该方法需要化学和物理药物修饰。任何被吸收的药物都必须以溶液的形式存在于吸收部位。难溶性药物可以通过多种方法使其更容易溶解,比如对药物进行物理和化学改变以及其他策略。使用表面活性剂、络合等都是固体分散的例子。提高溶解度技术的选择受药理学性质、吸收部位和剂型要求的影响。为了提供快速参考,本研究试图收集各种改善溶解度方法的资料并进行系统整理。
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Solubility, the Main Concern for Poorly Water-soluble Drugs: Techniques and Alternatives
The most important variable that affects a drug's bioavailability is its aqueous solubility. One of the biggest issues facing the pharmaceutical business is improving water solubility, which is the key to improving therapeutic efficacy. During the first screening procedure, over 50% of recently created medications are discovered to be insoluble or weakly soluble. The solubility of the medicine can be increased using a variety of techniques. The method entails both chemical and physical drug modifications. Any medicine that is absorbed must be present at the absorption site in the form of a solution. Poorly soluble medications can be made more soluble using a variety of approaches, like physical and chemical alterations to the drug and other strategies. Using a surfactant, complexation, and so on are examples of solid dispersion. The choice of a solubility-improving technology is influenced by pharmacological properties, absorption sites, and the requirements for the dosage form. In order to serve as a quick reference, this study attempted to gather information on various solubility improvement methods and organize it systematically.
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