Fluorobenzoic acid coformers to improve the solubility and permeability of the BCS class IV drug naftopidil

Fluorobenzoic acid coformers to improve the solubility and permeability of the BCS class IV drug naftopidil

Crystalline salts of the low solubility and low permeability drug naftopidil were investigated with mono-, di-, tri-, and tetrafluorobenzoic acids as coformers to show that 245TFBA (2,4,5-trifluorobenzoic acid) is the optimal salt with faster dissolution and high permeability, thereby opening the st...

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Veröffentlicht in:Chemical communications (Cambridge, England) England), 2022-05, Vol.58 (37), p.5582-5585
Hauptverfasser: Mannava, M K Chaitanya, Bommaka, Manish K, Dandela, Rambabu, Solomon, K Anand, Nangia, Ashwini K
Format: Artikel
Sprache:eng
Schlagworte:
Crystallization
Naphthalenes
Permeability
Piperazines
Salts - chemistry
Solubility
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Zusammenfassung:Crystalline salts of the low solubility and low permeability drug naftopidil were investigated with mono-, di-, tri-, and tetrafluorobenzoic acids as coformers to show that 245TFBA (2,4,5-trifluorobenzoic acid) is the optimal salt with faster dissolution and high permeability, thereby opening the study of fluorinated coformers in pharmaceutical cocrystals and salts.
ISSN:1359-7345
1364-548X
DOI:10.1039/d1cc07187d