Amorphous Enzalutamide - Non-isothermal recrystallization kinetics and thermal stability

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216275%3A25310%2F18%3A39913353" target="_blank" >RIV/00216275:25310/18:39913353 - isvavai.cz</a>

Výsledek na webu

<a href="http://dx.doi.org/10.1016/j.tca.2018.05.020" target="_blank" >http://dx.doi.org/10.1016/j.tca.2018.05.020</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.tca.2018.05.020" target="_blank" >10.1016/j.tca.2018.05.020</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Amorphous Enzalutamide - Non-isothermal recrystallization kinetics and thermal stability

Popis výsledku v původním jazyce

Recrystallization kinetics of amorphous Enzalutamide (two batches prepared by hot-melt extrusion and thermal evaporation of the solvent) was studied by differential scanning calorimetry. The preparation route was found to have significant effect on material thermal stability and initial degree of crystallinity - solvent evaporation led to formation of partially crystalline matrix with residual solvent content causing plasticization and the ongoing thermally induced crystallization was largely accelerated. Thermal recrystallization of both Enzalutamide batches led to a similar polymorphic form. The recrystallization kinetics was evaluated by means of modified multivariate kinetic analysis and described in terms of the autocatalytic gestak-Berggren and the nth order autocatalytic reaction models. The recrystallization kinetics were found to be dependent on applied heating rate, gradually shifting from the nucleation-growth kinetics to the autocatalyzed 0th order kinetics (with the effective order of reaction changing from 1 to 0.2). The autocatalytic Sestak-Berggren model appears to be more suitable for predictions of the Enzalutamide recrystallization behavior due to the constancy of the autocatalytic term (M = 0.55) with regard to the experimental conditions. In addition, the kinetic predictions of crystallization in pharmaceuticals were discussed in general based on theoretical simulations - importance of the aspects influencing the kinetic predictions was demonstrated.

Název v anglickém jazyce

Amorphous Enzalutamide - Non-isothermal recrystallization kinetics and thermal stability

Popis výsledku anglicky

Recrystallization kinetics of amorphous Enzalutamide (two batches prepared by hot-melt extrusion and thermal evaporation of the solvent) was studied by differential scanning calorimetry. The preparation route was found to have significant effect on material thermal stability and initial degree of crystallinity - solvent evaporation led to formation of partially crystalline matrix with residual solvent content causing plasticization and the ongoing thermally induced crystallization was largely accelerated. Thermal recrystallization of both Enzalutamide batches led to a similar polymorphic form. The recrystallization kinetics was evaluated by means of modified multivariate kinetic analysis and described in terms of the autocatalytic gestak-Berggren and the nth order autocatalytic reaction models. The recrystallization kinetics were found to be dependent on applied heating rate, gradually shifting from the nucleation-growth kinetics to the autocatalyzed 0th order kinetics (with the effective order of reaction changing from 1 to 0.2). The autocatalytic Sestak-Berggren model appears to be more suitable for predictions of the Enzalutamide recrystallization behavior due to the constancy of the autocatalytic term (M = 0.55) with regard to the experimental conditions. In addition, the kinetic predictions of crystallization in pharmaceuticals were discussed in general based on theoretical simulations - importance of the aspects influencing the kinetic predictions was demonstrated.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

10403 - Physical chemistry

Projekt

<a href="/cs/project/GA17-11753S" target="_blank" >GA17-11753S: Kinetická analýza komplexních fyzikálně chemických procesů</a><br>

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Rok uplatnění

2018

Kód důvěrnosti údajů

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

Název periodika

Thermochimica Acta

ISSN

0040-6031

e-ISSN

—

Svazek periodika

665

Číslo periodika v rámci svazku

July

Stát vydavatele periodika

NL - Nizozemsko

Počet stran výsledku

8

Strana od-do

134-141

Kód UT WoS článku

000437372400017

EID výsledku v databázi Scopus

2-s2.0-85047544744