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Preparation, Characterization, and In Vitro Evaluation of Ezetimibe Binary Solid Dispersions with Poloxamer 407 and PVP K30

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Abstract

Ezetimibe (EZE), a water insoluble drug, depicts variable bioavailability. The objective of the present investigation was to improve dissolution characteristics of EZE, which might offer improved bioavailability. The solid dispersions were prepared using poloxamer 407 (L 127) and polyvinyl pyrrolidone by melt and solvent method, respectively. Phase solubility studies indicated linear relationship between drug solubility and carrier concentration. In vitro release studies revealed improvement in the dissolution characteristics of EZE in solid dispersions. Solid dispersion with L 127 gave better rate and extent of dissolution. The best fit model indicating the probable mechanism of drug release from solid dispersions was found to be Korsemeyer–Peppas. The results of characterization of solid dispersions by Fourier transform infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffraction revealed reduction in drug crystallinity which might be responsible for improved dissolution properties. The tablets of solid dispersion, containing L 127 prepared by direct compression, exhibited better drug release as compared to marketed formulation.

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Acknowledgments

The authors are thankful to Mepro Pharmaceuticals Ltd. (Surendranagar, India) and BASF Ltd. (Mumbai, India) for providing EZE and L 127, respectively, as gift samples.

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Authors and Affiliations

  1. Department of Pharmaceutical Sciences, Saurashtra University, Rajkot, 360 005, Gujarat, India

    Komal R. Parmar, Sunny R. Shah & Navin R. Sheth

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  1. Komal R. Parmar
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  2. Sunny R. Shah
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  3. Navin R. Sheth
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Correspondence to Sunny R. Shah.

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Parmar, K.R., Shah, S.R. & Sheth, N.R. Preparation, Characterization, and In Vitro Evaluation of Ezetimibe Binary Solid Dispersions with Poloxamer 407 and PVP K30. J Pharm Innov 6, 107–114 (2011). https://doi.org/10.1007/s12247-011-9104-8

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  • DOI: https://doi.org/10.1007/s12247-011-9104-8

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