Salt formation of cabozantinib with hydrochloric and hydrobromic acids – influence on the in vitro dissolution behavior and food effect

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F68378271%3A_____%2F25%3A00618712" target="_blank" >RIV/68378271:_____/25:00618712 - isvavai.cz</a>
Alternative codes found
RIV/60461373:22340/25:43933252
Result on the web
<a href="https://hdl.handle.net/11104/0365608" target="_blank" >https://hdl.handle.net/11104/0365608</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1039/d4ce01278j" target="_blank" >10.1039/d4ce01278j</a>

Result language
angličtina
Original language name
Salt formation of cabozantinib with hydrochloric and hydrobromic acids – influence on the in vitro dissolution behavior and food effect
Original language description
The aim of this study was to prepare stable novel crystalline salts of cabozantinib, a tyrosine kinase inhibitor used to treat medullary thyroid cancer, to improve its dissolution properties and thereby reduce the positive food effect associated with its marketed salt form (L-malate). Five novel multi-component solid forms were obtained. In addition to the detailed physicochemical characterization, we report the crystal structures of the saccharinate, hydrochloride, and hydrobromide salts. The hydrobromide and hydrochloride salts of cabozantinib were chosen for further studies based on promising preliminary results from dissolution rate measurements. The potential of the hydrochloride and hydrobromide salts to be used for drug formulation was determined by testing their physical stability using hygroscopicity tests and by observing their melting properties.
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
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OECD FORD branch
10302 - Condensed matter physics (including formerly solid state physics, supercond.)

Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2025
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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