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Strategies for Solubility Enhancement of Anthelmintics (Review)
Pharmaceutical Chemistry Journal ( IF 0.9 ) Pub Date : 2020-08-01 , DOI: 10.1007/s11094-020-02229-4
S. S. Khalikov , A. V. Dushkin

Most drug substances are poorly soluble in water so that their efficacies must be improved by increasing the dosage, which not only creates economic problems but also increases the toxicity of the future medicine. These problems can be solved by developing various dosage forms, which involves additional financial costs, complicates the technology, increases development times to introduce the future medicine, etc. Another approach to improving the solubility of such drug substances is the development of methods and technologies for producing solid dispersions of these drug substances with excipients (polymers, dispersants, surfactants, etc.). The present review covers the development and application of mechanochemical technology to modify sparingly soluble anthelmintic drugs. The technology consists essentially of joint mechanical treatment of a drug substance and polymer in grinder-activators of controlled energy. This technology uses one stage and avoids the use of solvents, heating, evaporation, etc. The resulting solid dispersions include supramolecular systems with increased solubility and better bioavailability and are also highly active with reduced consumption of the active ingredients.

中文翻译:

提高驱虫药溶解度的策略(综述)

大多数原料药难溶于水,因此必须通过增加剂量来提高其功效,这不仅造成经济问题,而且增加了未来药物的毒性。这些问题可以通过开发各种剂型来解决,这涉及额外的财务成本,使技术复杂化,增加引入未来药物的开发时间等。 提高此类药物溶解度的另一种方法是开发方法和技术用赋形剂(聚合物、分散剂、表面活性剂等)生产这些药物的固体分散体。本综述涵盖了机械化学技术在修饰微溶性驱虫药物方面的发展和应用。该技术主要包括在受控能量的研磨活化剂中对原料药和聚合物进行联合机械处理。该技术使用一个阶段,避免使用溶剂、加热、蒸发等。由此产生的固体分散体包括具有更高溶解度和更好生物利用度的超分子系统,并且还具有高活性,减少了活性成分的消耗。
更新日期:2020-08-01
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