Solubility of Diclofenac Acid Form from Solid Dispersions

The influence of solid dispersions (SD) on diclofenac solubility was determined by studying diclofenac (acid form) and its SD with polyethyleneglycol-1500 (PEG) and polyvinylpyrrolidone-10000 (PVP). SD formation increased the solubility and dissolution rate of the non-steroidal anti-inflammatory dru...

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Bibliographic Details
Published in:Pharmaceutical chemistry journal 2015-02, Vol.48 (11), p.733-737
Main Authors: Krasnyuk, I. I., Ovsyannikova, L. V., Nikulina, O. I., Belyatskaya, A. V., Kharitonov, Yu. Ya, Grikh, V. V., Korol’, L. A., Obidchenko, Yu. A., Vorob’ev, A. N.
Format: Article
Language:English
Subjects:
Chemical properties
Comparative analysis
Drug Synthesis Methods and Manufacturing Technology
Medicine
Nonsteroidal anti-inflammatory agents
Organic Chemistry
Pharmacology/Toxicology
Pharmacy
Polymers
Solid solutions
Steroidal anti-inflammatory agents
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Summary:The influence of solid dispersions (SD) on diclofenac solubility was determined by studying diclofenac (acid form) and its SD with polyethyleneglycol-1500 (PEG) and polyvinylpyrrolidone-10000 (PVP). SD formation increased the solubility and dissolution rate of the non-steroidal anti-inflammatory drug (NSAID). Diclofenac solubility from the SD with PVP increased by 2.5 times; from the SD with PEG (solvent evaporation method), by 8 times compared with diclofenac drug substance. A combination of physicochemical methods showed that the improved release of diclofenac from the SD occurred because of reduced crystallinity, formation of drug solid solutions in the polymer matrix, and formation of a colloidal drug solution.
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-015-1183-2