Complex methodology for rational design of Apremilast-benzoic acid co-crystallization process

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22310%2F19%3A43917915" target="_blank" >RIV/60461373:22310/19:43917915 - isvavai.cz</a>
Alternative codes found
RIV/60461373:22340/19:43917915
Result on the web
<a href="https://www.sciencedirect.com/science/article/pii/S0378517319306842?via%3Dihub" target="_blank" >https://www.sciencedirect.com/science/article/pii/S0378517319306842?via%3Dihub</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.ijpharm.2019.118639" target="_blank" >10.1016/j.ijpharm.2019.118639</a>

Result language
angličtina
Original language name
Complex methodology for rational design of Apremilast-benzoic acid co-crystallization process
Original language description
A new co-crystal of pharmaceutical active ingredient Apremilast was successfully designed in this work. The discovered co-crystal with benzoic acid significantly improves key properties like the dissolution and stability of an otherwise poorly soluble Apremilast. A crystallization process was developed, which includes efficient solvent selection and ternary phase diagram construction to minimize risks during scale up. To increase efficiency, we propose that both steps be combined into a single methodology based on solubility data. A suitable solvent for the co-crystallization process was selected and ternary phase diagrams were constructed using three different modifications of thermodynamic model of solid-liquid equilibria. Based on the obtained information, the co-crystallization process was scaled-up to 100 mL. This provides a feasible process to produce larger amounts of this promising pharmaceutical solid form of Apremilast necessary for further drug development.
Czech name
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Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
—
OECD FORD branch
10403 - Physical chemistry

Project
<a href="/en/project/GA17-23196S" target="_blank" >GA17-23196S: In situ monitoring and modeling of the solvation processes of active pharmaceutical ingredients</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year
2019
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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