Strategies for Solubility Enhancement of Anthelmintics (Review)

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 additi...

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Bibliographic Details
Published in:Pharmaceutical chemistry journal 2020-08, Vol.54 (5), p.504-508
Main Authors: Khalikov, S. S., Dushkin, A. V.
Format: Article
Language:English
Subjects:
Drug Synthesis Methods and Manufacturing Technology
Medicine
Organic Chemistry
Pharmacology/Toxicology
Pharmacy
Phenylbutazone
Polymers
Povidone
Surface active agents
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Summary: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.
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-020-02229-4