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KMID : 1146920220520020175
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Journal of Pharmaceutical Investigation
2022 Volume.52 No. 2 p.175 ~ p.194
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Tableting process-induced solid-state polymorphic transition
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Park Hee-Jun
Kim Jeong-Soo
Hong Seong-Woo
Ha Eun-Sol
Nie Haichen
Zhou Qi Tony
Kim Min-Soo
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Abstract
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Background: Polymorphism is that a substance exists into more than two crystalline forms with different molecular arrangements and/or conformations. It has been reported that the polymorphic transition significantly influences several important qualities of a solid drug product such as physical properties of dosage form, physicochemical stability, dissolution rate, permeability and absorption, bioavailability, manufacturability, and commercial scalability. Polymorphic transition can be altered by several pharmaceutical processes.
Area covered: This review paper discussed the tableting process-induced solid-state polymorphic transition in detail. In particular, the basic principles of solid-state polymorphic transition, theoretical hypotheses for their mechanism, solid-state characterization methods for the analysis of polymorphic transition, and research cases for various drugs in relation to polymorphic transition were reviewed.
Expert opinion: For the proper selection of the solid phase of raw materials, formulation design, and robust production process to assure the quality and performance of a final tablet product, the following are essential: (i) an in-depth knowledge based on fundamental understanding of the polymorphic transition mechanisms, (ii) development of a promising analytical technology as a process analytical technology (PAT) available for in situ and in-die real-time measurement of a very small quantity of polymorphic transformation with high sensitivity, and iii) development of a complete technology in the formulation and process that can finely control the undesired polymorphic transition.
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KEYWORD
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Polymorphic transition, Stability, Solid-state, Tableting, Compaction, Process analytical technology (PAT)
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