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2000
Volume 12, Issue 6
  • ISSN: 2210-6812
  • E-ISSN: 2210-6820

Abstract

Background: The current investigation contributes to the development of novel Paliperidone (PPD) co-crystals (CCs) using benzamide (BZ) as a conformer. The CCs were synthesized using the solvent evaporation technique. Methods: The enhancement in solubility was studied by saturation solubility studies. Structural characterization of CCs was performed by Fourier Transform Infra-Red Spectroscopy (FTIR), powder X-ray diffraction (PXRD), Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM) and Proton Nuclear Magnetic Resonance (1H- FT NMR) to verify CC formation. Results: CCs exhibited a higher aqueous solubility of 2.067±0.004mg/ml when compared to pure drug 0.473±0.012mg/ml. This designated aqueous solubility enhancement of CCs by 4.36 folds. In vitro dissolution data of the CCs exhibited a drug release of 96.5±1.63% in 60min, while pure drug showed a poor release of 37.8±1.76% in the same time period In vivo studies resulted in enhanced rate and extent of drug absorption from CCs when compared to drug suspension. Conclusion: CCs formed between PPD and BZ present a novel approach in overcoming the hurdles in the solubility of PPD that exhibits poor aqueous solubility.

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/content/journals/nanoasi/10.2174/2210681213666221031150449
2022-12-01
2024-12-12
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/content/journals/nanoasi/10.2174/2210681213666221031150449
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  • Article Type:
    Research Article
Keyword(s): bioavailability; coformer; drug; Paliperidone; solvent evaporation; structural analysis
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