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Perphenazine-fumaric acid salts with improved solubility: preparation, physico-chemical characterization and in vitro dissolution
Research Area: | Uncategorized | Year: | 2012 |
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Type of Publication: | Article | ||
Authors: |
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Journal: | CRYSTENGCOMM | Volume: | 14 |
Number: | 18 | Pages: | 6035-6044 |
ISSN: | 1466-8033 | ||
Abstract: | New compounds of perphenazine and fumaric acid in 2:1 and 1:2 molar
ratios have been prepared by solvent evaporation with the aim of
increasing the drug solubility. Their physico-chemical properties were
thoroughly characterized by differential scanning calorimetry, powder
X-ray diffraction, Fourier infrared spectroscopy and scanning electron
microscopy coupled with energy dispersive X-ray spectrometry. In
addition, the crystal structure of the 2:1 salt was determined by
single-crystal X-ray diffraction. The pharmaceutical characterization
included solubility and dissolution studies in comparison with the
commercial product Trilafon (R). Perphenazine solubility is strongly
pH-dependent: the binary systems show improved solubility and intrinsic
dissolution rate compared with perphenazine, but only the capsule
formulation containing the 1 : 2 dihydrate sample shows a quick and
complete dissolution behaviour at neutral pH. This sample could
represent an interesting perphenazine formulation to improve drug
bioavailability and perhaps reduce in vivo variability even when the
gastric fluid pH is increased by the presence of food. |
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