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Preparation and Characterization of Ibrutinib Amorphous Solid Dispersions: a Discussion of Interaction Force

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Abstract

The aim of this study was to improve the solubility and dissolution of Ibrutinib (IBR), a biopharmaceutical classification system (BCS) class II drug, by preparing binary and ternary amorphous solid dispersions (ASDs). The physicochemical properties of the ASD formulations were evaluated. Compared with crystalline IBR Form A, ASDs showed prominent improvement both in solubility and dissolution. The solubility and dissolution of IBR-HPMCAS (1:3) ASD were increased up to 9 times and 15 times than IBR Form A in the pH 6.8 buffer. Moreover, IBR-HPMCAS (1:3) ASD kept a stable amorphous state for 180 days under the accelerated stability condition (40 °C/75% RH). From Fourier Transform-Infrared spectra and ΔTg analysis, the possible hydrogen-bond interactions in IBR ASDs were pointed out to explain the improvement of solubility and stability. The results of this study demonstrated that ASD is a promising strategy to improve solubility and dissolution of poorly water soluble IBR.

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Acknowledgements

This work was supported by Project 21606203 of the Natural Science Foundation of China. The authors offer their sincere thanks to Shengjie Song (Zhejiang University of Technology) for his assistance.

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Authors and Affiliations

  1. National Engineering Research Center for Process Development of Active Pharmaceutical Ingredients, Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou, 310014, People’s Republic of China

    Xiangjun Shi, Baibai Fan, Xiyue Zhou, Qifeng Chen, Shuimei Shen, Xiaoyi Xing & Yu Deng

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  1. Xiangjun Shi
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Shi, X., Fan, B., Zhou, X. et al. Preparation and Characterization of Ibrutinib Amorphous Solid Dispersions: a Discussion of Interaction Force. J Pharm Innov 17, 1074–1083 (2022). https://doi.org/10.1007/s12247-021-09585-y

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