Design and evaluation of gastroretentive levofloxacin floating mini-tablets-in-capsule system for eradication of Helicobacter pylori

Sally A. El-Zahaby, Abeer A. Kassem, Amal H. El-Kamel

Research output: Contribution to journalArticleResearchpeer-review

33 Citations (Scopus)

Abstract

Gastroretentive levofloxacin (LVF) floating mini-tablets for the eradication of Helicobacter pylori (H. pylori) were prepared using the matrix forming polymer hydroxypropyl methylcellulose (HPMC K100M), alone or with Carbopol 940P in different ratios by wet granulation technique. Buoyancy of mini-tablets was achieved by an addition of an effervescent mixture consisting of sodium bicarbonate and anhydrous citric acid to some formulations. The prepared mini-tablets were evaluated for weight variation, thickness, friability, hardness, drug content, in vitro buoyancy, water uptake and in vitro release. The optimized formula was subjected to further studies: FT-IR, DSC analysis and in vivo examination in healthy volunteers. The prepared mini-tablets exhibited satisfactory physicochemical characteristics. Incorporation of gas-generating agent improved the floating parameters. HPMC K100M mini-tablet formulation (F1) offered the best controlled drug release (>8 h) along with floating lag time <1 s and total floating time >24 h. The obtained DSC thermograms and FT-IR charts indicated that there is no positive evidence for the interaction between LVF and ingredients of the optimized formula. The in vivo test confirmed the success of the optimized formula F1 in being retained in the stomach of the volunteers for more than 4 h. LVF floating mini-tablets based on HPMC K100M is a promising formulation for eradication of H. pylori.

Original languageEnglish
Pages (from-to)570-579
Number of pages10
JournalSaudi Pharmaceutical Journal
Volume22
Issue number6
DOIs
Publication statusPublished - 1 Jan 2014

Fingerprint

Levofloxacin
Helicobacter pylori
Tablets
Capsules
Sodium Bicarbonate
Hardness
Citric Acid
Volunteers
Stomach
Healthy Volunteers
Polymers
Gases
Weights and Measures
Water
Pharmaceutical Preparations

Keywords

  • Floating
  • Fluoroquinolones
  • Gastroretentive
  • Helicobacter pylori
  • Levofloxacin
  • Mini-tablets

Cite this

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title = "Design and evaluation of gastroretentive levofloxacin floating mini-tablets-in-capsule system for eradication of Helicobacter pylori",
abstract = "Gastroretentive levofloxacin (LVF) floating mini-tablets for the eradication of Helicobacter pylori (H. pylori) were prepared using the matrix forming polymer hydroxypropyl methylcellulose (HPMC K100M), alone or with Carbopol 940P in different ratios by wet granulation technique. Buoyancy of mini-tablets was achieved by an addition of an effervescent mixture consisting of sodium bicarbonate and anhydrous citric acid to some formulations. The prepared mini-tablets were evaluated for weight variation, thickness, friability, hardness, drug content, in vitro buoyancy, water uptake and in vitro release. The optimized formula was subjected to further studies: FT-IR, DSC analysis and in vivo examination in healthy volunteers. The prepared mini-tablets exhibited satisfactory physicochemical characteristics. Incorporation of gas-generating agent improved the floating parameters. HPMC K100M mini-tablet formulation (F1) offered the best controlled drug release (>8 h) along with floating lag time <1 s and total floating time >24 h. The obtained DSC thermograms and FT-IR charts indicated that there is no positive evidence for the interaction between LVF and ingredients of the optimized formula. The in vivo test confirmed the success of the optimized formula F1 in being retained in the stomach of the volunteers for more than 4 h. LVF floating mini-tablets based on HPMC K100M is a promising formulation for eradication of H. pylori.",
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Design and evaluation of gastroretentive levofloxacin floating mini-tablets-in-capsule system for eradication of Helicobacter pylori. / El-Zahaby, Sally A.; Kassem, Abeer A.; El-Kamel, Amal H.

In: Saudi Pharmaceutical Journal, Vol. 22, No. 6, 01.01.2014, p. 570-579.

Research output: Contribution to journalArticleResearchpeer-review

TY - JOUR

T1 - Design and evaluation of gastroretentive levofloxacin floating mini-tablets-in-capsule system for eradication of Helicobacter pylori

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