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Spherical Agglomeration of Safinamide Mesylate: A Case Study of a Simultaneous Control of Crystalline Landscape and Micromeritic Properties
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2023-03-17 , DOI: 10.1021/acs.oprd.2c00396
Aurélien Lemercier 1, 2 , Yohann Cartigny 1 , Pierrick Morice 2 , Elise Vanbiervliet 2 , Massimiliano Forcato 2 , Gérard Coquerel 1
Affiliation  

Safinamide mesylate (SAFIM) is a drug used in its anhydrous form as an add-on treatment for Parkinson′s disease. This work demonstrates the feasibility of a spherical agglomeration process on a molecule exhibiting an agglomeration′s unfavorable crystalline landscape, due to the high stability of SAFIM hydrate. After a comprehensive characterization of the crystalline landscape of SAFIM, conditions to obtain anhydrous SAFIM during the agglomeration process are presented. Temperature, stirring rate, the concentration of the slurry, and the amount of bridging liquid were studied to obtain spherical agglomerates with desirable micromeritic properties.

中文翻译:

Safinamide Mesylate 的球形团聚:同时控制结晶景观和微晶特性的案例研究

Safinamide mesylate (SAFIM) 是一种以无水形式使用的药物,可作为帕金森病的辅助治疗药物。由于 SAFIM 水合物的高稳定性,这项工作证明了在表现出团聚不利的结晶景观的分子上进行球形团聚过程的可行性。在对 SAFIM 的结晶景观进行全面表征后,提出了在团聚过程中获得无水 SAFIM 的条件。研究了温度、搅拌速率、浆料的浓度和桥接液的量以获得具有理想微晶特性的球形附聚物。
更新日期:2023-03-17
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