Work

Enhancing the Solubility and Dissolution Performance of Safinamide Using Salts

Year: 2020
Type: article
Abstract: 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.
Source: Crystals
Institution: Wuzhou University
Language: English
Open Access status: gold
Estimated APC paid: $1,690
OpenAlex ID: W3097618656
FWCI:
Cites: 29
Cited by: 2
Related to: 10