Darren L. Reid, Margaret M. Faul, Vilmalí López-Mejías, Prashant Agarwal, Markus Bergauer, Laura E. Blue, Mary K. Chaves, John Chung, Melanie Cooke, Robert P. Farrell, James E. Huckle, Ron C. Kelly, Y.-H. Kiang, Weikun Li, Adrian Ortiz, Qiong Wu
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引用次数: 0
Abstract
Selecting the development form of an active pharmaceutical ingredient (API) in drug development is key to determining the final performance of the drug substance and drug product. Form selection requires an interdisciplinary approach involving a complex process to discover, monitor, and evaluate the solid-state characteristics, biopharmaceutical properties, stability, and processability of numerous forms. This Perspective discusses the importance of aligning critical material attributes with the desired quality target product profile to ensure drug safety and efficacy. It discusses how the form selection strategy is dependent on factors related to the administration route, dosage form, and therapeutic indication and provides an interdisciplinary framework with four prioritized sets of target attributes for oral delivery: solid-state properties, biopharmaceutical performance, stability, and processability. A classification system to guide form selection, particularly for immediate-release oral medications, is reviewed. The benefits of crystalline forms in terms of stability and processability are highlighted, emphasizing the role of solution crystallization in controlling their development. The interdisciplinary form selection process will be demonstrated through case studies highlighting how each set of target attributes were evaluated leading to the selection of ideal forms for development.
期刊介绍：
The journal Organic Process Research & Development serves as a communication tool between industrial chemists and chemists working in universities and research institutes. As such, it reports original work from the broad field of industrial process chemistry but also presents academic results that are relevant, or potentially relevant, to industrial applications. Process chemistry is the science that enables the safe, environmentally benign and ultimately economical manufacturing of organic compounds that are required in larger amounts to help address the needs of society. Consequently, the Journal encompasses every aspect of organic chemistry, including all aspects of catalysis, synthetic methodology development and synthetic strategy exploration, but also includes aspects from analytical and solid-state chemistry and chemical engineering, such as work-up tools，process safety, or flow-chemistry. The goal of development and optimization of chemical reactions and processes is their transfer to a larger scale; original work describing such studies and the actual implementation on scale is highly relevant to the journal. However, studies on new developments from either industry, research institutes or academia that have not yet been demonstrated on scale, but where an industrial utility can be expected and where the study has addressed important prerequisites for a scale-up and has given confidence into the reliability and practicality of the chemistry, also serve the mission of OPR&D as a communication tool between the different contributors to the field.
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