Controlled Crystallization Enables Facile Fine-Tuning of Physical–Chemical Properties of Nicergoline Toward Easier Processability

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F25%3A73632628" target="_blank" >RIV/61989592:15310/25:73632628 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/61989592:15640/25:73632628 RIV/61989100:27740/25:10258745

Výsledek na webu

<a href="https://www.mdpi.com/1424-8247/18/10/1465" target="_blank" >https://www.mdpi.com/1424-8247/18/10/1465</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.3390/ph18101465" target="_blank" >10.3390/ph18101465</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Controlled Crystallization Enables Facile Fine-Tuning of Physical–Chemical Properties of Nicergoline Toward Easier Processability

Popis výsledku v původním jazyce

Background/Objectives: Crystallization is a key process in the manufacturing of active pharmaceutical ingredients (APIs), as it significantly affects the physical and chemical properties of the final product. Nicergoline, a clinically relevant ergot derivative, was chosen as a model compound to investigate how different crystallization strategies affect particle attributes. The objective of this study was to compare controlled and uncontrolled crystallization techniques and evaluate their impact on the physicochemical properties of nicergoline. Methods: Nicergoline was crystallized using controlled methods, including sonication-induced and seeding-induced crystallization, and uncontrolled methods, namely cubic and linear cooling, as well as acetone evaporation. The resulting powders were characterized by using a range of physicochemical techniques to assess particle morphology, size distribution, agglomeration behavior, and surface properties. Results: Uncontrolled crystallization methods produced particles prone to agglomeration, resulting in a broader particle size distribution ranging from 8 to 720 mu m and heterogeneous surface characteristics. In contrast, controlled crystallization generated more uniform particles with reduced agglomeration and narrower particle size distributions. Among the evaluated methods, sonocrystallization provided the most effective control over particle size and morphology, demonstrated by a narrow size distribution ranging from 16 to 39 mu m which correlated with improved flowability and surface energy. Conclusions: The study demonstrates that the choice of crystallization method significantly influences the structural and physicochemical properties of nicergoline. These findings highlight the importance of method selection for tailoring API properties to enhance downstream processing and product quality.

Název v anglickém jazyce

Controlled Crystallization Enables Facile Fine-Tuning of Physical–Chemical Properties of Nicergoline Toward Easier Processability

Popis výsledku anglicky

Background/Objectives: Crystallization is a key process in the manufacturing of active pharmaceutical ingredients (APIs), as it significantly affects the physical and chemical properties of the final product. Nicergoline, a clinically relevant ergot derivative, was chosen as a model compound to investigate how different crystallization strategies affect particle attributes. The objective of this study was to compare controlled and uncontrolled crystallization techniques and evaluate their impact on the physicochemical properties of nicergoline. Methods: Nicergoline was crystallized using controlled methods, including sonication-induced and seeding-induced crystallization, and uncontrolled methods, namely cubic and linear cooling, as well as acetone evaporation. The resulting powders were characterized by using a range of physicochemical techniques to assess particle morphology, size distribution, agglomeration behavior, and surface properties. Results: Uncontrolled crystallization methods produced particles prone to agglomeration, resulting in a broader particle size distribution ranging from 8 to 720 mu m and heterogeneous surface characteristics. In contrast, controlled crystallization generated more uniform particles with reduced agglomeration and narrower particle size distributions. Among the evaluated methods, sonocrystallization provided the most effective control over particle size and morphology, demonstrated by a narrow size distribution ranging from 16 to 39 mu m which correlated with improved flowability and surface energy. Conclusions: The study demonstrates that the choice of crystallization method significantly influences the structural and physicochemical properties of nicergoline. These findings highlight the importance of method selection for tailoring API properties to enhance downstream processing and product quality.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

10403 - Physical chemistry

Projekt

<a href="/cs/project/EH22_008%2F0004587" target="_blank" >EH22_008/0004587: Technologie za hranicí nanosvěta</a><br>

Návaznosti

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

Rok uplatnění

2025

Kód důvěrnosti údajů

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

Název periodika

Pharmaceuticals

ISSN

1424-8247

e-ISSN

—

Svazek periodika

18

Číslo periodika v rámci svazku

10

Stát vydavatele periodika

CH - Švýcarská konfederace

Počet stran výsledku

16

Strana od-do

nestránkováno

Kód UT WoS článku

001601571200001

EID výsledku v databázi Scopus

2-s2.0-105020196214