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Tableting process-induced solid-state polymorphic transition

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Abstract

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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Acknowledgements

This research was supported by the Basic Science Research Program through the National Research Foundation of Korea funded by the Ministry of Education (2016R1A6A1A03007648). This work was supported by the National Research Foundation of Korea (NRF) grant funded by the Korea government (MSIT) (No. 2020R1A2C4002166). This research was supported by Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education (No. 2020R1I1A1A01074378). We would like to thank Eunseo Kang and Yerin Oh for helping search for literature with this review paper.

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  1. Heejun Park and Jeong-Soo Kim have contributed equally to this work.

Authors and Affiliations

  1. College of Pharmacy, Duksung Women’s University, 33, Samyangro 144-gil, Dobong-gu, Seoul, 01369, Republic of Korea

    Heejun Park & Seongwoo Hong

  2. Dong-A ST Co. Ltd., Giheung-gu, Yongin, Gyeonggi, 446-905, Republic of Korea

    Jeong-Soo Kim

  3. College of Pharmacy, Pusan National University, 2, Busandaehak-ro 63beon-gil, Geumjeong-gu, Busan, 46241, Republic of Korea

    Eun-Sol Ha & Min-Soo Kim

  4. Center for Materials Science and Engineering, Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA, 19486, USA

    Haichen Nie

  5. Department of Industrial and Physical Pharmacy, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, IN, 47907, USA

    Qi Tony Zhou

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  1. Heejun Park
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Park, H., Kim, JS., Hong, S. et al. Tableting process-induced solid-state polymorphic transition. J. Pharm. Investig. 52, 175–194 (2022). https://doi.org/10.1007/s40005-021-00556-6

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