药物溶解度增强技术综述

Vaishnavi B. Borgaonkar, Chetan M. Jain, Amit R. Jaiswal, Poonam Irache, Achal H. Yelane, Hanuman P. Tattu
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引用次数: 0

摘要

溶解度是影响药物化合物生物利用度和疗效的一个关键参数,通常是药物开发过程中的一个重大挑战。这篇综述文章深入探讨了用于改善低溶解度药物溶解度的几种方法,以克服其局限性。文章讨论了传统方法和新兴方法,强调了这些方法的机制、优势和局限性。本研究探讨了粒度减小、固体分散和共溶等传统方法,重点介绍了这些方法的历史重要性和广泛应用。研究还讨论了纳米技术的进展,包括纳米悬浮剂、纳米晶体和脂基纳米载体,因为它们有可能通过改进给药系统彻底改变溶解度的提高。实现循环系统最佳药物剂量吸收的一个重要决定因素是药理作用的显示与物质的溶解度直接相关。配制新药物化学制剂的主要挑战在于其有限的水溶性。水溶性低的药物需要大剂量口服才能在血液中达到最高有效浓度。生物制药分类系统(BCS)根据物质的溶解度和渗透性对其进行分类。监管机构和卫生组织采用这种分类方法,通过溶解度作为一种确认形式,来验证高溶解度和高渗透性化学品的生物等效性。溶解于水的能力差的药物分解速度慢,导致口服时可被血液吸收的药物量减少。
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A review on solubility enhancement technique for pharmaceutical drugs
Solubility, a critical parameter governing the bioavailability and therapeutic efficacy of pharmaceutical compounds, often poses a significant challenge in drug development. This review article offers a thorough examination of several methods used to improve the solubility of medications that have low solubility, in order to overcome their limits. The discussion encompasses both conventional and emerging strategies, highlighting their mechanisms, advantages, and limitations. The study examines conventional methods such as particle size reduction, solid dispersion, and cosolvency, focusing on their historical importance and extensive use. Advances in nanotechnology, including nanosuspensions, nanocrystals, and lipid-based nanocarriers, are discussed for their potential to revolutionize solubility enhancement through improved drug delivery systems. An essential determinant in achieving optimal medication dosage absorption into the circulatory system is the demonstration of a pharmacological action is directly linked to the solubility of a substance. The primary challenge in formulating the new medicinal chemical is its limited water solubility. Medications with low solubility in water need large doses in order to achieve their highest effective concentration in the bloodstream when taken orally. The biopharmaceutical categorization system (BCS) classifies substances according to their solubility and permeability. Regulatory agencies and health organizations have used this categorization approach to validate bioequivalence for chemicals that are both highly soluble and very permeable by using dissolution as a form of confirmation. Medications that have a poor capacity to dissolve in water have a slow pace of breaking down, which results in a reduction in the amount of the medication that may be absorbed into the bloodstream when taken orally.
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