Development of Screening Methodology for the Assessment of the Agglomeration Potential of APIs

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• 作者：Charles D. Papageorgiou ; Marianne Langston ; Frederick Hicks ; David am Ende ; Eric Martin ; Sarah Rothstein ; Jerry Salan ; Robert Muir
• 刊名：Organic Process Research & Development
• 出版年：2016
• 出版时间：August 19, 2016
• 年：2016
• 卷：20
• 期：8
• 页码：1500-1508
• 全文大小：550K
• 年卷期：0
• ISSN：1520-586X

文摘

A simple screening protocol has been developed for assessing the agglomeration potential of active pharmaceutical ingredients (APIs) using resonant acoustic mixing that minimizes the quantity of API used. This methodology improves upon existing ones as it allows for multiple conditions to be screened in parallel, saving time and allowing for the study of agglomeration and optimization of the drying unit operation to take place early in development. In addition to a qualitative (visual) assessment, quantitative data can be obtained after the material has been dried therefore accounting for a measure of cake hardening. This methodology was also extended to assess the friability of the generated agglomerates and was validated using a scaled-down agitated filter dryer (AFD). The impact of particle size, particle size distribution, solvent selection, and solvent loading on the agglomeration potential for a Takeda API is also discussed which allowed for the development of an improved drying process that was successfully scaled-up in the pilot plant.