Crystalline and amorphous famotidine malate as pathways to prevent polymorphic transformation with improved dissolution.


Journal

International journal of pharmaceutics
ISSN: 1873-3476
Titre abrégé: Int J Pharm
Pays: Netherlands
ID NLM: 7804127

Informations de publication

Date de publication:
25 Jul 2023
Historique:
received: 12 10 2022
revised: 09 05 2023
accepted: 11 05 2023
medline: 24 7 2023
pubmed: 18 5 2023
entrez: 17 5 2023
Statut: ppublish

Résumé

Famotidine (FMT) is an orally administered histamine H2-receptor blocker with limited bioavailability since it exhibits low solubility and low permeability. In addition, the recent withdrawal of ranitidine from the market, makes famotidine an interesting candidate to obtain solid forms with improved pharmacokinetic performance. In this work, crystal engineering concepts and the co-amorphous formation strategy were applied to obtain two novel solids. Crystalline famotidine malate (FMT-MT) and a vitreous phase (FMT-MTa) were prepared by solvent evaporation and mechanochemical synthesis, respectively. FMT-MT (monoclinic, S.G. P2

Identifiants

pubmed: 37196883
pii: S0378-5173(23)00473-8
doi: 10.1016/j.ijpharm.2023.123053
pii:
doi:

Substances chimiques

Famotidine 5QZO15J2Z8
malic acid 817L1N4CKP
Malates 0
Histamine H2 Antagonists 0

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

123053

Informations de copyright

Copyright © 2023 Elsevier B.V. All rights reserved.

Déclaration de conflit d'intérêts

Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Auteurs

Marcos G Russo (MG)

Instituto de Investigaciones en Tecnología Química (INTEQUI, UNSL-CONICET), Facultad de Química, Bioquímica y Farmacia, Universidad Nacional de San Luis (UNSL), Almirante Brown 1455, D5700HGC, San Luis, Argentina. Electronic address: mgrusso@unsl.edu.ar.

Elena V Brusau (EV)

Instituto de Investigaciones en Tecnología Química (INTEQUI, UNSL-CONICET), Facultad de Química, Bioquímica y Farmacia, Universidad Nacional de San Luis (UNSL), Almirante Brown 1455, D5700HGC, San Luis, Argentina. Electronic address: ebrusau@unsl.edu.ar.

Javier Ellena (J)

São Carlos Institute of Physics, Avenida Trabalhador São-carlense 400, Parque Arnold Schimidt, CEP 13566-590, São Carlos, São Paulo, Brazil.

Griselda E Narda (GE)

Instituto de Investigaciones en Tecnología Química (INTEQUI, UNSL-CONICET), Facultad de Química, Bioquímica y Farmacia, Universidad Nacional de San Luis (UNSL), Almirante Brown 1455, D5700HGC, San Luis, Argentina.

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Classifications MeSH