Study of the identity of the polymorphic form of API – dapagliflosin derivative and of its permanency structure under the influence of the tableting process

Authors

DOI:

https://doi.org/10.15587/2519-4852.2024.289293

Keywords:

polymorphism, critical technological parameter, tabletting, polymorphic transition, structural stability, bioequivalence

Abstract

The aim. To investigate the polymorphic structure of the API – Dapagliflozin propanediol monohydrate and to reveal the absence of an effect of the tabletting process on the polymorphic structure of the API in model compositions of tablets.

Materials and methods. Model mixtures of API - dapagliflozin propanediol monohydrate and excipients were studied. The research used the method of designing pharmaco-technological parameters of solid dosage forms, the method of quantum-chemical modelling of the mechanical properties of polymorphic modifications of APIs, the modelling of shear deformation, the nanoindentation method, the Rietveld method for calculating X-ray patterns, X-ray structural analysis of API and selected model compositions of tablets.

Results. The polymorphic structure of API - dapagliflozin propanediol monohydrate and its polymorphic structure in selected model compositions of tablets produced by the pressing method were studied and analyzed. An X-ray structural study was carried out, and the qualitative and phase composition of samples and polymorphic modifications of API and model series of tablets were determined. According to the results of the X-ray structural analysis, it was established that there is no polymorphic transition and that the polymorphic structure of API is invariant under the influence of pressing pressure, which ensures the quality of the tablet form.

Conclusions. The design of an experimental study was determined based on the application of the QbD concept, design of experiments – DoE, for designing and ensuring a high-quality technological process – tabletting of API - Dapagliflozin propanediol monohydrate and excipients.

To manage a critical technological parameter - the stability of the polymorphic structure of the API, which guarantees the quality of the tablet form, its bioavailability and bioequivalence, it is necessary to use a set of methods for studying structural changes and polymorphic modifications of the API during the tableting process.

According to the results of the X-ray structural study of API and selected model compositions of tablets, it was established that during the process of tabletting under pressure, the structure of the polymorphic modification of dapagliflozin propanediol monohydrate does not change, and no polymorphic transition is observed

Author Biographies

Yevhenii Bohuslavskyi, Kyiv National University of Technology and Design

PhD Student

Department of Industrial Pharmacy

Halyna Voskoboinikova, Kyiv International University; JSC Farmak

Doctor of Pedagogical Sciences, PhD, Professor

Department of Pharmacy, Drug Technology and Pharmaceutical Management

Andriy Goy, Kyiv National University of Technology and Design; JSC Farmak

PhD, Associate Professor

Department of Industrial Pharmacy

Svetlana Shishkina, State Scientific Institution «Institute for Single Crystals» of National Academy of Sciences of Ukraine; V. N. Karazin Kharkiv National University

PhD, Senior Researcher, Head of  Department

Department of X-ray Structural Research and Quantum Chemistry

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Study of the identity of the polymorphic form of API – dapagliflosin derivative and of its permanency structure under the influence of the tableting process

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Published

2024-06-30

How to Cite

Bohuslavskyi, Y., Voskoboinikova, H., Goy, A., & Shishkina, S. (2024). Study of the identity of the polymorphic form of API – dapagliflosin derivative and of its permanency structure under the influence of the tableting process. ScienceRise: Pharmaceutical Science, (3 (49), 86–95. https://doi.org/10.15587/2519-4852.2024.289293

Issue

No. 3 (49) (2024)

Section

Pharmaceutical Science

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Copyright (c) 2024 Yevhenii Bohuslavskyi, Halyna Voskoboinikova, Andriy Goy, Svetlana Shishkina

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