Preparation and Characterization of Ibrutinib Amorphous Solid Dispersions: a Discussion of Interaction Force
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.
Article information: Shi, X., Fan, B., Zhou, X. et al. Preparation and Characterization of Ibrutinib Amorphous Solid Dispersions: a Discussion of Interaction Force. J Pharm Innov (2021). https://doi.org/10.1007/s12247-021-09585-y
Interested in amorphous solid dispersions? Have a look at our ASD webinar series:
![easer Shin Etsu Webinar 2 Spray Drying]()
![Shin-Etsu - Downstream Processing Webinar Teaser]()
