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Improvement of opipramol base solubility by complexation with β-cyclodextrin

Opipramol (OPI), a tricyclic antidepressant and anxiolytic compound, is administered orally in the form of a dihydrochloride. Salt form of the drug has a higher solubility in water and hence bioavailability and stability. A similar effect can be achieved by closing the hydrophobic part of the drug molecule in the cyclodextrin cavity. The paper presents opipramol inclusion complexes with beta-cyclodextrin (β-CD) in 1:1 molar ratio. Studies on the formation of inclusion complexes were carried out both in solution and in the solid state. The formation and physicochemical characterisation of the complexes were determined by UV spectroscopic measurement (UV–vis), Fourier Transform Infrared (FTIR) Spectroscopy, 1H Nuclear Magnetic Resonance (1H NMR, 2D NOESY NMR), thermoanalytical methods (TGA – Termogravimetric analysis, DSC – differential scanning calorimetry), X-ray diffractometry (XRD) and scanning electron microscopy (SEM). The phase solubility profile with β-CD was classified as the AN- type, indicating the formation of the inclusion complex with a drug.

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DOI
Digital Object Identifier link open in new tab 10.1080/10610278.2017.1350677
Category
Publikacja w czasopiśmie
Type
artykuł w czasopiśmie wyróżnionym w JCR
Language
angielski
Publication year
2018

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