Amorphous Solid Dispersion Based Oral Disintegrating Film of Ezetimibe: Development and Evaluation

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Author(s): Sangam Shrestha, Preethi Sudheer*, A.N Kavitha

Journal Name: Drug Metabolism Letters

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Background: Ezetimibe is a cholesterol lowering agent with an oral bioavailability of 50 % by the virtue of its poor solubility, extensive hepatic and intestinal metabolism.

Objective: The study is aimed to overcome low bioavailability issues of ezetimibe by formulating an oral disintegrating film.

Method: The low solubility of ezetimibe was tackled preparing solid dispersions using mannitol, β-cyclodextrin and urea. The mannitol solid dispersion assimilated oral disintegrating film was prepared and optimized using 2 3 factorial design, where concentration of film formers hydroxypropyl methyl cellulose (K5& K15) (X1and X2) and super disintegrant, sodium starch glycolate (X3) was used as factors on the response disintegration time (Y). The films were evaluated for physical properties, time of disintegration and drug release profiles.

Results and Discussions: Mannitol solid dispersion (1:2 ratio) on the basis of the superior drug content, solubility and in vitro release profile was preferred in film formation. The low crystalline nature of the solid dispersion was very evident by the absence of prominent peaks in the X Ray diffraction pattern and the reduced peak intensity of melting endotherms. The correlation coefficient (R2 ) and statistical parameter analysis of variance specifies implication of linear factors on responses, which is apparent from confidence intervals (Pvalues) less than 0.05. The in vitro release profile of all the eight formulations (F1-F8) in phosphate buffer solution pH 6.8 revealed a significant increment in comparison to ezetimibe.

Conclusion: The study revealed that the formulation approach could overcome the biopharmaceutical challenge of solubility as well as low bioavailability issues of ezetimibe.

Keywords: Ezetimibe, HPMC, ODF, Solid dispersion, BCS, Mannitol, In vitro release, Factors.

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(E-pub Ahead of Print)
DOI: 10.2174/1872312814666200901182517
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