Modeling of the Aqueous Solubility of N-butyl-N-methyl-1-phenylpyrrolo[1,2-a] pyrazine-3-carboxamide: From Micronization to Creation of Amorphous-Crystalline Composites with a Polymer.
antidepressants
anxiolytics
micronization
polymorphism
polyvinylpyrrolidone
solubility
Journal
Polymers
ISSN: 2073-4360
Titre abrégé: Polymers (Basel)
Pays: Switzerland
ID NLM: 101545357
Informations de publication
Date de publication:
18 Oct 2023
18 Oct 2023
Historique:
received:
05
09
2023
revised:
13
10
2023
accepted:
16
10
2023
medline:
28
10
2023
pubmed:
28
10
2023
entrez:
28
10
2023
Statut:
epublish
Résumé
N-butyl-N-methyl-1-phenylpyrrole[1,2-a] pyrazine-3-carboxamide (GML-3) is a potential candidate for combination drug therapy due to its anxiolytic and antidepressant activity. The anxiolytic activity of GML-3 is comparable to diazepam. The antidepressant activity of GML-3 is comparable to amitriptyline. GML-3 is an 18 kDa mitochondrial translocator protein (TSPO) ligand and is devoid of most of the side effects of diazepam, which makes the research on the creation of drugs based on it promising. However, its low water solubility and tendency to agglomerate prevented its release. This research aimed to study the effect of dry grinding, the rapid expansion of a supercritical solution (RESS), and the eutectic mixture (composite) of GML-3 with polyvinylpyrrolidone (PVP) on the particle size, dissolution rate, and lattice retention of GML-3. The use of supercritical CO
Identifiants
pubmed: 37896380
pii: polym15204136
doi: 10.3390/polym15204136
pmc: PMC10611044
pii:
doi:
Types de publication
Journal Article
Langues
eng
Subventions
Organisme : RUDN
ID : RUDN University Strategic Academic Leadership Program
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