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- Title
Dissolution performance enhancement of poorly water-soluble API by crystallization from phase-separated melt.
- Authors
Tumurbaatar, Bolor-Uyanga; Amari, Shuntaro; Takiyama, Hiroshi
- Abstract
For dissolution enhancement of poorly water-soluble APIs, a novel production method for multi-component solids was proposed by developing the melt crystallization concept into multi-component raw material in which the target API and matrix component were immiscible, and phase separated. The dispersion of the target API in the matrix component is required for dissolution enhancement of the target API. However, the coalescence of the dispersed droplets, which negatively affected API dispersion, occurred in the phase-separated melt. Therefore, the crystallization phenomenon of the matrix component was applied to prevent the coalescence of droplets and keep the API dispersion. The shear force was given to the phase-separated melt to achieve the irreversible phenomenon. As the results of dissolution tests, the multi-phase solid formed using high shear force to the phase-separated melt shows a large amount of API dissolved and an extremely high dissolution rate. Additionally, it was found that the multi-phase solid with a high dissolution rate had the smallest crystal particle size. These results suggest that the dissolution performance of poorly water-soluble API can be enhanced by the synergistic effect of both dispersion of droplets and the precipitation of fine crystals obtained by using high shear force to phase-separated melt. [Display omitted] • A new production method for multi-component solids of pharmaceutical products. • The raw materials were melted to phase-separated melt and then crystallized. • Giving High shear force to the melt enhanced the dissolution rate of the product. • The high shear force has a synergistic effect of improving dissolution.
- Subjects
CRYSTALLIZATION; SHEARING force; MELT crystallization; MELTING; PRODUCTION methods
- Publication
Chemical Engineering Research & Design: Transactions of the Institution of Chemical Engineers Part A, 2024, Vol 203, p538
- ISSN
0263-8762
- Publication type
Article
- DOI
10.1016/j.cherd.2024.02.009