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Studies on Formulation Development of Mucoadhesive Sustained Release Itraconazole Tablet Using Response Surface Methodology

  • Research Article/Theme: Oral Controlled Release Development and Technology/Guest Editors: Stephen A. Howard and Jian-Xin Li
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Abstract

The purpose of this research was to prepare and evaluate sustained release mucoadhesive tablets of Itraconazole. It is practically insoluble in aqueous fluids hence its solid dispersion with Eudragit E100 was prepared by spray drying. This was formulated in matrix of hydrophilic mucoadhesive polymers Carbopol 934P (CP) and Methocel K4M (HPMC). The formulation was optimized using a 32 factorial design. Amounts of CP and HPMC were taken as formulation variables for optimizing response variables i.e. mucoadhesion and dissolution parameters. The optimized mucoadhesive formulation was orally administered to albino rabbits, and blood samples collected were used to determine pharmacokinetic parameters. The solid dispersion markedly enhanced the dissolution rate of itraconazole. The bioadhesive strength of formulation was found to vary linearly with increasing amount of both polymers. Formulations exhibited drug release fitting Peppas model with value of n ranging from 0.61 to 1.18. Optimum combination of polymers was arrived at which provided adequate bioadhesive strength and fairly regulated release profile. The experimental and predicted results for optimum formulations were found to be in close agreement. The formulation showed C max 1898 ± 75.23 ng/ml, t max of the formulation was 2 h and AUC was observed to be 28604.9 ng h/ml

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Authors and Affiliations

  1. Poona College of Pharmacy, Bharti Vidyapeeth University, Erandwane, Pune, 411038, India

    Ashwini Madgulkar, Shivajirao Kadam & Varsha Pokharkar

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  1. Ashwini Madgulkar
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  2. Shivajirao Kadam
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  3. Varsha Pokharkar
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Correspondence to Ashwini Madgulkar.

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Madgulkar, A., Kadam, S. & Pokharkar, V. Studies on Formulation Development of Mucoadhesive Sustained Release Itraconazole Tablet Using Response Surface Methodology. AAPS PharmSciTech 9, 998–1005 (2008). https://doi.org/10.1208/s12249-008-9119-8

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  • DOI: https://doi.org/10.1208/s12249-008-9119-8

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