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Enhancing the solubility and permeability of the diuretic drug furosemide via multicomponent crystal forms.

Abstract：

:Furosemide (FSM) is a biopharmaceutical classification system (BCS) class IV drug, being a potent loop diuretic used in the treatment of congestive heart failure and edema. Due to its low solubility and permeability, FSM is known for exhibiting poor oral bioavailability. In order to overcome or even minimize these undesirable biopharmaceutical attributes, in this work we have focused on the development of more soluble and permeable multicomponent solid forms of FSM. Using solvent evaporation as crystallization method, a salt and a cocrystal of FSM with imidazole (IMI) and 5-fluorocytosine (5FC) coformers, named FSM-IMI and FSM-5FC, respectively, were successfully prepared. A detailed structural study of these new solid forms was conducted using single and powder X-ray diffraction (SCXRD, PXRD), Fourier Transform Infrared (FT-IR) and proton Nuclear Magnetic Resonance (1H NMR) spectroscopy and thermal analysis (thermogravimetry, differential scanning calorimetry and hot-stage microscopy). Both FSM-IMI and FSM-5FC showed substantial enhancements in the solubility (up 118-fold), intrinsic dissolution (from 1.3 to 2.6-fold) and permeability (from 2.1 to 2.8-fold), when compared to the pure FSM. These results demonstrate the potential of these new solid forms to increase the limited bioavailability of FSM.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Diniz LF,Carvalho PS Jr,Pena SAC,Gonçalves JE,Souza MAC,de Souza Filho JD,Bomfim Filho LFO,Franco CHJ,Diniz R,Fernandes C

doi

10.1016/j.ijpharm.2020.119694

subject

Has Abstract

pub_date

2020-09-25 00:00:00

pages

119694

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(20)30678-5

journal_volume

587

pub_type

杂志文章

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