4.7 Article

The antisolvent coprecipitation method for enhanced bioavailability of poorly water-soluble drugs

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出版社

ELSEVIER
DOI: 10.1016/j.ijpharm.2022.122043

关键词

Antisolvent coprecipitation; Poorly water-soluble drugs; Cocrystals; Nanocrystals; Amorphous solid dispersions; Nanoparticles

资金

  1. Hunan Provincial Natural Science Foundation of China [2021JJ30761]
  2. Changsha platform and talent plan [KQ2203002]
  3. Key R & D Program of Hunan Province, China [2022WK2008]
  4. Natural Science Foundation of Jiangsu Province, China [BK 20200573]

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In recent years, the poor solubility of drug candidates in the pharmaceutical industry has posed a challenge. To overcome this issue, various delivery systems, including nanocrystals, cocrystals, nanoparticles, and amorphous solid dispersions, have been developed. Among them, the antisolvent coprecipitation method stands out as a relatively simple and cost-effective approach. This review provides an overview of the recent developments in solubility enhancement using the antisolvent coprecipitation method, emphasizing the process, properties, and factors influencing the efficacy of this approach.
In recent years, poorly water-soluble drug candidates in the drug development pipeline have been a challenging issue for the pharmaceutical industry. Many delivery systems, such as nanocrystals, cocrystals, nanoparticles, and amorphous solid dispersions (ASDs) have been developed to overcome these problems. A large number of methods are utilized to realize the above delivery systems. Among all the preparation methods, the antisolvent coprecipitation method is a relatively simple, cost-effective method, offering many advantages over conventional methods. An overview of recent developments for each solubility enhancement approach using the antisolvent coprecipitation method is presented. This current review details a comprehensive overview of the antisolvent coprecipitation process and its properties, as well as the fundamentals for enhancing the solubility and bioavailability of poorly water-soluble drugs by nanotization, polymorph control with polymers and/or surfactants. Furthermore, this review also presents insights into the factors affecting the antisolvent coprecipitation process.

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