Polyvinyl alcohol extrudates for improving the dissolution of main protease and reverse-transcriptase inhibitors

• Published in: Journal of excipients and food chemicals Vol. 13; no. 1
• Main Authors: Sergey A Zolotov, Natalia B Demina, Igor A Dain, Anna S Zolotova, Grigorii A Buzanov, Vasilii M Retivov, Alexander M Cheremisin
• Format: Journal Article
• Language: English
• Published: International Pharmaceutical Excipients Council 01.03.2022
• ISSN: 2150-2668

The aim of this work was to improve the solubility of various anti-HIV APIs extruding them with polyvinyl alcohol to allow a reduction in patient drug burden. There are no previously known cases of successful use of this polymer to improve the solubility of APIs using a convenient industrial technology. Anti-HIV API solid dispersion samples were obtained using hot melt extrusion with polyvinyl alcohol, and were studied with solubility testing, as well as various methods of confirming amorphousness (differential scanning calorimetry, X-ray powder diffraction). This study confirmed the presence of amorphousness and a significant increase in the solubility of the API in various dissolution media. According to the obtained data, the best samples were selected and utilized in tablet formulations, which successfully passed in vitro dissolution testing. The results of in vitro dissolution testing showed the improvement of dissolution kinetics for all APIs. These results howed the usefulness of hot melt extrusion with polyvinyl alcohol in a ratio of at least 1-3 or 1-5 for the studied APIs and improved the dissolution kinetics of the proposed tablet formulations compared to the controls.