Репозиторий Университета

© 2019, Springer Science+Business Media, LLC, part of Springer Nature. Water solubility of prothionamide and its solid dispersions with polyethylene glycol-1500, polyvinylpyrrolidone-10000, and β-cyclodextrin was studied. The most promising results were obtained with the solid dispersion with polyvinylpyrrolidone, which provided a 2.6-fold general increase of drug’s solubility and about a 6-fold dissolution rate increase, the maximal values among the studied drug forms. The results of complex physicochemical studies suggested that the improved drug release was due to micronization and solubilizing action of the polymer. A principal factor was the destruction of the crystal lattice and formation of amorphous particles in the solid dispersion. The obtained data can be useful for the development of modified pharmaceutical forms of prothionamide with improved drug release profile.

© 2018, Springer Science+Business Media, LLC, part of Springer Nature. Technology development for solid dosage forms with a solid dispersion of diclofenac is a crucial problem in pharmaceutical science and practice. The goal of the work was science-based and experimental technology development for tablets containing a solid dispersion of diclofenac with improved biopharmaceutical indicators as an equivalent to the substance. The obtained granulates and tablets had indicators that met the corresponding standards of the Russian SP XIIIth Ed. Almost 100% of the diclofenac was released from the developed tablets. This was 1.3 times greater than from commercial tablets. The recommended shelf life under these conditions is two years. The proposed technology could not only increase the bioavailability of the slightly soluble non-salt form of diclofenac but also facilitate further development of new medicinal preparations with improved bioavailability.

© 2018, Springer Science+Business Media, LLC, part of Springer Nature. Solid dispersions (SDs) of indomethacin with polyethylene glycol 1500 (PEG-1500) were studied to determine their effect on indomethacin solubility. Production of SDs increased the solubility and dissolution rate of indomethacin in H2O. The solubility and dissolution rate of indomethacin from SDs increased by 1.8 – 2.2 and 3.1 – 4.4 times, respectively. Indomethacin became less crystalline and then amorphous during preparation of the SDs. Dissolution of the SDs solubilized indomethacin and formed colloidal solutions.