Pharmaceutical salts of venetoclax with dicarboxylic and sulfonic acids: solid-state characterization and dissolution performance

Kód výsledku v 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>

Nalezeny alternativní kódy

RIV/60461373:22340/25:43933248

Výsledek na webu

<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>

Jazyk výsledku

angličtina

Název v původním jazyce

Pharmaceutical salts of venetoclax with dicarboxylic and sulfonic acids: solid-state characterization and dissolution performance

Popis výsledku v původním jazyce

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.

Název v anglickém jazyce

Pharmaceutical salts of venetoclax with dicarboxylic and sulfonic acids: solid-state characterization and dissolution performance

Popis výsledku anglicky

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.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

10302 - Condensed matter physics (including formerly solid state physics, supercond.)

Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2025

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

CrystEngComm

ISSN

1466-8033

e-ISSN

1466-8033

Svazek periodika

27

Číslo periodika v rámci svazku

12

Stát vydavatele periodika

GB - Spojené království Velké Británie a Severního Irska

Počet stran výsledku

14

Strana od-do

1816-1829

Kód UT WoS článku

001433029400001

EID výsledku v databázi Scopus

2-s2.0-105001085637