Pharmaceutical salts of venetoclax with dicarboxylic and sulfonic acids: solid-state characterization and dissolution performance
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F68378271%3A_____%2F25%3A00618406" target="_blank" >RIV/68378271:_____/25:00618406 - isvavai.cz</a>
Alternative codes found
RIV/60461373:22340/25:43933248
Result on the web
<a href="https://hdl.handle.net/11104/0365786" target="_blank" >https://hdl.handle.net/11104/0365786</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1039/d4ce01121j" target="_blank" >10.1039/d4ce01121j</a>
Alternative languages
Result language
angličtina
Original language name
Pharmaceutical salts of venetoclax with dicarboxylic and sulfonic acids: solid-state characterization and dissolution performance
Original language description
This study focuses on enhancing the aqueous dissolution of venetoclax through salt formation. Venetoclax, a BCS class IV B-cell lymphoma-2-selective inhibitor, exhibits very low solubility and bioavailability. Given its multiple protonable groups, salt formation was explored to improve its dissolution properties. Dicarboxylic and sulfonic acids were selected as counterions for salt screening. Ten salts were synthesized and characterized using powder X-ray diffraction, nuclear magnetic resonance spectroscopy, thermogravimetric analysis, and differential scanning calorimetry. Intrinsic dissolution rate measurements demonstrated that all salts dissolve faster than the parent drug. The crystal structures of venetoclax, venetoclax fumarate, venetoclax oxalate, and venetoclax napsylate, which all solvated with acetonitrile, and unsolvated venetoclax tosylate were elucidated and described.
Czech name
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Czech description
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Classification
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.)
Result continuities
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
Others
Publication year
2025
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
CrystEngComm
ISSN
1466-8033
e-ISSN
1466-8033
Volume of the periodical
27
Issue of the periodical within the volume
12
Country of publishing house
GB - UNITED KINGDOM
Number of pages
14
Pages from-to
1816-1829
UT code for WoS article
001433029400001
EID of the result in the Scopus database
2-s2.0-105001085637