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Formulation and evaluation of taste-masked paracetamol-lipid sachets and chewable tablets

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Abstract

The use of lipids as taste-masking excipients in paracetamol sachets and chewable tablets without compromising drug release was investigated. Twelve paracetamol granule formulations were prepared by melt granulation, using Precirol® (glyceryl palmitostearate), cetyl alcohol and stearic acid, at different paracetamol-lipid ratios. Based on efficient taste-masking results coupled with minimum retardation of drug release, paracetamol-Precirol (1:1), paracetamol-cetyl alcohol (1:2) and paracetamol-stearic acid (1:2) granules were selected for preparation of chewable tablets and sachets. Formulations were evaluated for the effect of storage, at 40 °C and 75 % RH for 6 months, on their performance. Results inferred that paracetamol sachets, after reconstitution in 100 ml water, showed efficient taste-masking compared to control sachets (without lipids). The sachets released more than 90 % of their drug content in 30 min, when tested in 900 ml of phosphate buffered saline, pH 5.8. Chewable tablets exhibited comparable taste-masking effect to a reference product, Tylenol® 80 mg chewable tablets, and yielded similar drug dissolution profiles (similarity factor f 2 > 50). Differential scanning calorimetry indicated the absence of interaction between paracetamol and lipids. Scanning electron micrographs supported the obtained results. Upon storage at 40 °C and 75 % RH for 6 months, all the prepared sachets and chewable tablets were found to be stable except cetyl alcohol-based tablets that showed decrease in the efficiency of taste masking with increase in release rate. In conclusion, selected lipids, Precirol®, cetyl alcohol and stearic acid, could be efficiently used in formulation of taste masked paracetamol sachets and chewable tablets without adversely delaying drug release.

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Acknowledgments

This article does not contain any studies with animal subjects performed by any of the authors. All authors (W.M. El-Refaie, M.A. El-Massik, O.Y. Abdallah, and N.M. Khalafallah) declare that they have no conflict of interest.

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Authors and Affiliations

  1. Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt

    Ossama Y. Abdallah & Nawal M. Khalafallah

  2. Department of Pharmaceutics, Faculty of Pharmacy and Drug Manufacturing, Pharos University in Alexandria, P.O. Box 37. Sidi Gaber, Alexandria, 21311, Egypt

    Wessam M. El-Refaie & Magda A. El-Massik

Authors
  1. Wessam M. El-Refaie
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  2. Magda A. El-Massik
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  3. Ossama Y. Abdallah
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  4. Nawal M. Khalafallah
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Correspondence to Magda A. El-Massik.

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El-Refaie, W.M., El-Massik, M.A., Abdallah, O.Y. et al. Formulation and evaluation of taste-masked paracetamol-lipid sachets and chewable tablets. Journal of Pharmaceutical Investigation 44, 431–442 (2014). https://doi.org/10.1007/s40005-014-0137-0

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  • DOI: https://doi.org/10.1007/s40005-014-0137-0

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