Composites of N-butyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide with Polymers: Effect of Crystallinity on Solubility and Stability.

amorphous solid dispersions antidepressants anxiolytics bioavailability composite solubility

Journal

International journal of molecular sciences
ISSN: 1422-0067
Titre abrégé: Int J Mol Sci
Pays: Switzerland
ID NLM: 101092791

Informations de publication

Date de publication:
30 Jul 2023
Historique:
received: 01 06 2023
revised: 19 07 2023
accepted: 28 07 2023
medline: 14 8 2023
pubmed: 12 8 2023
entrez: 12 8 2023
Statut: epublish

Résumé

This work aimed to develop and characterize a water-soluble, high-release active pharmaceutical ingredient (API) composite based on the practically water-insoluble API N-butyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide (GML-3), a substance with antidepressant and anxiolytic action. This allows to ensure the bioavailability of the medicinal product of combined action. Composites obtained by the method of creating amorphous solid dispersions, where polyvinylpyrrolidone (PVP) or Soluplus

Identifiants

pubmed: 37569589
pii: ijms241512215
doi: 10.3390/ijms241512215
pmc: PMC10418436
pii:
doi:

Substances chimiques

Polymers 0
polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer 0
Povidone FZ989GH94E
Water 059QF0KO0R
Pyrazines 0

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

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Auteurs

Vladimir B Markeev (VB)

V.V. Zakusov Research Institute of Pharmacology, 8 Baltiyskaya St., 125315 Moscow, Russia.

Evgenia V Blynskaya (EV)

V.V. Zakusov Research Institute of Pharmacology, 8 Baltiyskaya St., 125315 Moscow, Russia.
Institute of Biochemical Technology and Nanotechnology, Peoples' Friendship University of Russia n.a. P. Lumumba (RUDN), 6 Miklukho-Maklaya St., 117198 Moscow, Russia.

Sergey V Tishkov (SV)

V.V. Zakusov Research Institute of Pharmacology, 8 Baltiyskaya St., 125315 Moscow, Russia.

Konstantin V Alekseev (KV)

V.V. Zakusov Research Institute of Pharmacology, 8 Baltiyskaya St., 125315 Moscow, Russia.

Anna I Marakhova (AI)

Institute of Biochemical Technology and Nanotechnology, Peoples' Friendship University of Russia n.a. P. Lumumba (RUDN), 6 Miklukho-Maklaya St., 117198 Moscow, Russia.

Alexandre A Vetcher (AA)

Institute of Biochemical Technology and Nanotechnology, Peoples' Friendship University of Russia n.a. P. Lumumba (RUDN), 6 Miklukho-Maklaya St., 117198 Moscow, Russia.
Complementary and Integrative Health Clinic of Dr. Shishonin, 5, Yasnogorskaya St., 117588 Moscow, Russia.

Alexander Y Shishonin (AY)

Complementary and Integrative Health Clinic of Dr. Shishonin, 5, Yasnogorskaya St., 117588 Moscow, Russia.

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Classifications MeSH