The solubility of darunavir (D) and darunavir ethanolate (DE) at physiological pH values and temperatures in solutions of pharmaceutically acceptable polymeric excipients was studied to substantiate dosage form formulations. Both substances were determined to dissolve better in HCl at pH 1.2 and 37°C. Use of PVP 90 in peroral dosage form formulations was shown to be unadvisable because of a negative effect on the solubility of the substances. The effect of Soluplus® on the solubility of D and DE was complicated by multifactor and heteropolar effects. PVP 12 – 30, HPMC 606, and Kollidon® VA64 HPC had positive effects on the solubility of D and DE substances. The best results were obtained for Eudragit® E PO solutions.
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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 54, No. 12, pp. 44 – 47, December, 2020.
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Zolotov, S.A., Demina, N.B. & Zolotova, A.S. Influence of Water-Soluble Pharmaceutically Acceptable Polymers on the Solubility of Darunavir and Darunavir Ethanolate. Pharm Chem J 54, 1274–1277 (2021). https://doi.org/10.1007/s11094-021-02354-8
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DOI: https://doi.org/10.1007/s11094-021-02354-8