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Miconazole Nitrate Oral Disintegrating Tablets: In Vivo Performance and Stability Study

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Abstract

The interest in and need for formulating miconazole nitrate (MN), a broad-spectrum antifungal, as an oral disintegrating tablet for treatment of some forms of candidiasis have increased. Formulation of MN in this dosage form will be more advantageous, producing dual effect: local in the buccal cavity and systemic with rapid absorption. Four formulations were prepared utilizing the foam granulation technique. The prepared tablets were characterized by measuring the weight uniformity, thickness, tensile strength, friability, and drug content. In addition, tablet disintegration time, in vitro dissolution, and in vivo disintegration time were also evaluated. Stability testing for the prepared tablets under stress and accelerated conditions in two different packs were investigated. Each pack was incubated at two different elevated temperature and relative humidity (RH), namely 40 ± 2°C/75 ± 5% RH and 50 ± 2°C/75 ± 5% RH. The purpose of the study is to monitor any degradation reactions which will help to predict the shelf life of the product under the defined storage conditions. Finally, in vivo study was performed on the most stable formula to determine its pharmacokinetic parameters. The results revealed that all the prepared tablets showed acceptable tablet characteristics and were stable under the tested conditions. The most stable formula was that containing magnesium stearate as lubricant, hydrophobic Aerosil R972 as glidant, low urea content, mannitol/microcrystalline cellulose ratio 2:1, and 9% Plasdone XL100 as superdisintegrant. The in vivo results revealed that the tested formula showed rapid absorption compared to the physical blend (t max were 1 and 4 h, respectively), while the extent of absorption was almost the same.

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ACKNOWLEDGMENTS

The authors highly appreciated the cooperation of DEEF Pharmaceutical Industries Company for giving the research team the permission to use the foam granulation machine.

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Authors and Affiliations

  1. Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, P.O. Box 80200, Zip Code 21589, Jeddah, Kingdom of Saudi Arabia

    Tarek A. Ahmed & Khalid M. El-Say

  2. Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar university, Cairo, Egypt

    Tarek A. Ahmed, Khalid M. El-Say, Maged F. Mahmoud & Ahmed M. Samy

  3. Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt

    Alia A. Badawi

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  1. Tarek A. Ahmed
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  2. Khalid M. El-Say
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Correspondence to Tarek A. Ahmed.

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Ahmed, T.A., El-Say, K.M., Mahmoud, M.F. et al. Miconazole Nitrate Oral Disintegrating Tablets: In Vivo Performance and Stability Study. AAPS PharmSciTech 13, 760–771 (2012). https://doi.org/10.1208/s12249-012-9798-z

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  • DOI: https://doi.org/10.1208/s12249-012-9798-z

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