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

Kód výsledku v 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>

Nalezeny alternativní kódy

RIV/60461373:22340/25:43933252

Výsledek na webu

<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>

Jazyk výsledku

angličtina

Název v původním jazyce

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

Popis výsledku v původním jazyce

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.

Název v anglickém jazyce

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

Popis výsledku anglicky

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.

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

7

Stát vydavatele periodika

GB - Spojené království Velké Británie a Severního Irska

Počet stran výsledku

8

Strana od-do

1026-1033

Kód UT WoS článku

001401254800001

EID výsledku v databázi Scopus

2-s2.0-85215956086