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Production of the Amorphous Form of Ibrutinib and Study of its Physicochemical Properties

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Pharmaceutical Chemistry Journal Aims and scope

The main lyophilization parameters enabling the production of amorphous ibrutinib active pharmaceutical ingredient (API) are presented. The amorphous and crystalline APIs were studied using x-ray powder diffractometry, scanning electron microscopy, and differential scanning calorimetry. The particle size, melting point, hygroscopicity, moisture content, and solubility in organic solvents and aqueous solutions were determined for both API forms. Lyophilization from a binary DMSO/t-BuOH mixture made it possible to obtain an amorphous form of ibrutinib without adding any crystallization inhibitors and to eliminate their effects on the API. The amorphous form exhibited enhanced solubility as compared to the crystalline form A used in the original drug.

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  1. LLC AMEDART, 42/24 Volgogradskii Prosp., Moscow, 109316, Russia

    S. A. Zolotov, G. K. Sazonov, I. A. Dain, E. S. Ponomarev & A. S. Zolotova

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  1. S. A. Zolotov
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  2. G. K. Sazonov
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Correspondence to E. S. Ponomarev.

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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 57, No. 2, pp. 45 – 51, February, 2023.

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Zolotov, S.A., Sazonov, G.K., Dain, I.A. et al. Production of the Amorphous Form of Ibrutinib and Study of its Physicochemical Properties. Pharm Chem J 57, 300–305 (2023). https://doi.org/10.1007/s11094-023-02880-7

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  • DOI: https://doi.org/10.1007/s11094-023-02880-7

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