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水增溶物在低溶解度药物增溶中的作用:分子动力学模拟和实验透视的见解。

Role of Hydrotropes in Sparingly Soluble Drug Solubilization: Insight from a Molecular Dynamics Simulation and Experimental Perspectives.

机构信息

Department of Chemistry, Indian Institute of Technology, Guwahati, Assam 781039, India.

出版信息

Langmuir. 2021 Apr 27;37(16):4745-4762. doi: 10.1021/acs.langmuir.1c00169. Epub 2021 Apr 14.

DOI:10.1021/acs.langmuir.1c00169
PMID:33853331
Abstract

Drug molecules' therapeutic efficacy depends on their bioavailability and solubility. But more than 70% of the formulated drug molecules show limited effectiveness due to low water solubility. Thus, the water solubility enhancement technique of drug molecules becomes the need of time. One such way is hydrotropy. The solubilizing agent of a hydrophobic molecule is generally referred to as a hydrotrope, and this phenomenon is termed hydrotropy. This method has high industrial demand, as hydrotropes are noninflammable, readily available, environmentally friendly, quickly recovered, cost-effective, and not involved in solid emulsification. The endless importance of hydrotropes in industry (especially in the pharmaceutical industry) motivated us to prepare a feature article with a clear introduction, detailed mechanistic insights into the hydrotropic solubilization of drug molecules, applications in pharma industries, and some future directions of this technique. Thus, we believe that this feature article will become an adequate manual for the pharmaceutical researchers who want to explore all of the past perspectives of the hydrotropic action of hydrotropes in pharmaceutics.

摘要

药物分子的治疗效果取决于其生物利用度和溶解度。但由于水溶解度低,超过 70%的已配药物分子显示出有限的效果。因此,提高药物分子的水溶解度技术成为当务之急。其中一种方法是变亲水性。通常将疏水分子的增溶剂称为变亲水剂,这种现象称为变亲水性。这种方法具有很高的工业需求,因为变亲水剂不易燃、易得、环保、可快速回收、具有成本效益,并且不涉及固体乳化。变亲水剂在工业中的重要性(特别是在制药工业中)促使我们编写了一篇专题文章,其中对药物分子的变亲水性增溶作用进行了清晰的介绍,详细的机制见解,在制药工业中的应用,以及该技术的一些未来方向。因此,我们相信这篇专题文章将成为希望探索变亲水剂在药剂学中变亲水性的所有过去观点的制药研究人员的充分手册。

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