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Enhancing the dissolution of hydrophobic guests using solid state inclusion complexation: characterization and in vitro evaluation

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Abstract

The objectives of the present investigation were to prepare and characterize solid inclusion complexes of Etodolac (ETD) with β-cyclodextrin (β-CD) in order to study the effect of complexation on the dissolution rate of ETD, a hydrophobic guest molecule. Phase solubility curve was classified as a typical AL-type for the cyclodextrins (CD’s), showing that soluble complex was formed. The inclusion complexes in the molar ratio of 1:1 and 1:2 (β-CD–ETD) were prepared by various methods such as kneading, co-evaporation and in molar ratio of 1:1 by spray dried technique respectively. The molecular behaviors of ETD in all samples were characterized by nuclear magnetic resonance (NMR) spectroscopy, fourier-transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) studies and Scanning Electron microscopy (SEM) analysis. The results of these studies indicated that complexes prepared by kneading, co-evaporation and spray drying techniques showed inclusion of the ETD molecule into the CD’s cavities. The highest improvement in in vitro dissolution profiles was observed in complexes prepared with spray dried technique. Mean in vitro dissolution time indicated significant difference between the release profiles of ETD from complexes and physical mixtures and from pure ETD.

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Acknowledgements

We would like to thank Ranbaxy Pvt. Ltd. for donating us the gift sample of ETD. We are grateful to S.A Chemicals Pvt. Ltd. for providing us the formulation excipients.

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  1. Department of Pharmaceutics, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, 160014, India

    V. R. Sinha,  Amita, Renu Chadha & Honey Goel

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  1. V. R. Sinha
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  2. Amita
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Correspondence to V. R. Sinha.

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Sinha, V.R., Amita, Chadha, R. et al. Enhancing the dissolution of hydrophobic guests using solid state inclusion complexation: characterization and in vitro evaluation. J Incl Phenom Macrocycl Chem 66, 381–392 (2010). https://doi.org/10.1007/s10847-009-9655-1

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  • DOI: https://doi.org/10.1007/s10847-009-9655-1

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