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Article

Enhancing the Solubility and Dissolution Performance of Safinamide Using Salts

School of Chemical Engineering and Resource Recycling, Wuzhou University, Wuzhou 543000, China
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Crystals 2020, 10(11), 989; https://doi.org/10.3390/cryst10110989
Received: 16 September 2020 / Revised: 24 October 2020 / Accepted: 29 October 2020 / Published: 31 October 2020
Safinamide (SAF) is an anti-Parkinson’s disease (PD) drug that has selective monoamine oxidase type-B (MAO-B) inhibition activity. In 2017, SAF was approved by the U.S. Food and Drug Administration (FDA) as safinamide mesylate (SAF-MS, marketed as Xadago). Owing to its poor solubility in water, SAF is a Biopharmaceutics Classification System BCS Class II compound. In this study, four salts of safinamide (with hydrochloric acid (HCl), hydrobromic acid (HBr), and maleic acid (MA)) were obtained and characterized using single crystal X-ray diffraction (SCXRD), powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), and thermogravimetry (TG). The solubility and dissolution rate of all salts were systematically studied in water and phosphate buffer (pH 6.86) solutions. The accelerated stability tests indicated that all salts, except SAF-MA, had good stability under high humidity conditions. View Full-Text
Keywords: safinamide; salts; X-ray diffraction; solubility; dissolution rate safinamide; salts; X-ray diffraction; solubility; dissolution rate
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MDPI and ACS Style

Gao, L.; Liu, Q.; Zhang, X.-R. Enhancing the Solubility and Dissolution Performance of Safinamide Using Salts. Crystals 2020, 10, 989. https://doi.org/10.3390/cryst10110989

AMA Style

Gao L, Liu Q, Zhang X-R. Enhancing the Solubility and Dissolution Performance of Safinamide Using Salts. Crystals. 2020; 10(11):989. https://doi.org/10.3390/cryst10110989

Chicago/Turabian Style

Gao, Lei, Qian Liu, and Xian-Rui Zhang. 2020. "Enhancing the Solubility and Dissolution Performance of Safinamide Using Salts" Crystals 10, no. 11: 989. https://doi.org/10.3390/cryst10110989

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