Abstract
The aim of this study is to prepare and characterize binary systems of aceclofenac (AC) with hydroxypropyl β-cyclodextrin (HPβCD) in equimolar ratio. Solid binary systems of aceclofenac with HPβCD were prepared using cogrinding, kneading, and coevaporating methods, and a physical mixture was prepared for comparison. The binary systems were characterized by differential scanning calorimetry, thermogravimetric analysis, mass spectroscopy, 1H nuclear magnetic resonance (NMR) spectroscopy, scanning electron microscopy, and in vitro dissolution studies. 1H NMR studies showed that AC partially fits into the HPβCD torus cavity with a preferential inclusion of the phenyl ring of the drug. All the binary systems showed superior dissolution and lower dose:solubility ratio (D:S ratio) as compared to pure AC, but the kneaded product exhibited the best dissolution, with complete drug release within 10 min and a D:S ratio of 5 mL. Hence, it was suggested that complexation of aceclofenac with HPβCD may be used as an approach to change the drug from Biopharmaceutics Classification System BCS Class II to BCS Class I without changing its intrinsic permeability.
- Aceclofenac
- Phase solubility studies
- Dissolution enhancement
- Inclusion complexation
- Poorly water soluble drugs
- BCS classification
Footnotes
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