Enhancement of the aqueous solubility and masking the bitter taste of famotidine using drug/SBE-β-CyD/povidone K30 complexation approach

  1. Fatma M. Mady1,2,
  2. Ahmed E. Abou-Taleb3,
  3. Khaled A. Khaled1,
  4. Keishi Yamasaki4,
  5. Daisuke Iohara4,
  6. Takako Ishiguro4,
  7. Fumitoshi Hirayama4,
  8. Kaneto Uekama4,
  9. Masaki Otagiri2,4,*

Article first published online: 12 APR 2010

DOI: 10.1002/jps.22153

Issue

Journal of Pharmaceutical Sciences

Journal of Pharmaceutical Sciences

Volume 99, Issue 10, pages 4285–4294, October 2010

Additional Information

How to Cite

Mady, F. M., Abou-Taleb, A. E., Khaled, K. A., Yamasaki, K., Iohara, D., Ishiguro, T., Hirayama, F., Uekama, K. and Otagiri, M. (2010), Enhancement of the aqueous solubility and masking the bitter taste of famotidine using drug/SBE-β-CyD/povidone K30 complexation approach. Journal of Pharmaceutical Sciences, 99: 4285–4294. doi: 10.1002/jps.22153

Author Information

  1. 1

    Department of Pharmaceutics, Faculty of Pharmacy, El-Minia University, El-Minia Governate 61732, Egypt

  2. 2

    Department of Biopharmaceutics, Graduate School of Pharmaceutical Sciences, Kumamoto University, 5-1 Oe-honmachi, Kumamoto 862-0973, Japan

  3. 3

    Department of Industrial Pharmacy, Faculty of Pharmacy, Assuit University, Assuit City 71515, Egypt

  4. 4

    Department of Clinical Pharmacy, Faculty of Pharmaceutical Sciences, Sojo University, 4-22-1 Ikeda, Kumamoto 860-0082, Japan

*Department of Biopharmaceutics, Graduate School of Pharmaceutical Sciences, Kumamoto University, 5-1 Oe-honmachi, Kumamoto 862-0973, Japan. Telephone: +81-96-371-4150; Fax: +81-96-362-7690

Publication History

  1. Issue published online: 18 AUG 2010
  2. Article first published online: 12 APR 2010
  3. Manuscript Accepted: 23 FEB 2010
  4. Manuscript Revised: 14 JAN 2010
  5. Manuscript Received: 4 NOV 2009

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Keywords:

  • famotidine;
  • cyclodextrins;
  • sulfobutyl ether β-cyclodextrin;
  • Povidone K30;
  • dissolution;
  • masking of bitter taste

Abstract

The objective of the present study was to evaluate the potential of ternary system (comprised of famotidine, β-cyclodextrin (β-CyD) or its derivatives and a hydrophilic polymer) as an approach for enhancing the aqueous solubility and masking the bitter taste of famotidine. The aqueous solubility of famotidine increased in the presence of β-CyDs, particularly sulfobutyl ether β-CyD (SBE-β-CyD), and it was further enhanced by the combination of SBE-β-CyD and polyvinyl pyrrolidone (Povidone) K30. The solid binary (drug-β-CyDs) and ternary (drug-β-CyDs-Povidone K30) systems were prepared by the kneading and freeze-drying methods. The dissolution rates of these solid systems were much faster than that of the drug alone. A taste perception study was carried out, initially using a taste sensory machine and subsequently on human volunteers to evaluate the taste masking ability of the ternary complexation. Our results indicated that the combination of SBE-β-CyD and Povidone K30 is effective not only in the enhancement of the solubility and dissolution rate of famotidine, but also in masking of the bitter taste of the drug. This technique may be of value for the pharmaceutical industries, especially in preparation of rapidly disintegrating tablets dealing with bitter drugs to improve patient compliance and thus effective pharmacotherapy. © 2010 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 99:4285–4294, 2010

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