Development and in vitro/in vivo evaluations of bioadhesive buccal tablets for nicotine replacement therapy

Pharmazie. 2006 Mar;61(3):203-7.

Abstract

Buccal bioadhesive tablet formulations of nicotine hydrogen tartrate (NHT) for nicotine replacement therapy (NRT) were developed using chitosan and carbomer at different ratios. Magnesium hydroxide was incorporated into the formulations as pH increasing agent. In vitro release and bioadhesion properties of the tablets were investigated. Release of NHT from the tablets was increased with the increasing amount of chitosan in formulations whilst the bioadhesion of the tablet was decreased. In vivo studies were carried out in healthy, non-smoker volunteers in comparison to a commercially available transdermal patch. Plasma nicotine and cotinine levels were determined using gas chromatography-mass spectrophotometry. No significant difference was found between the maximum plasma nicotine concentrations (Cmax) obtained with the buccal tablet and the transdermal patch (p > 0.05). Time to reach the Cmax was 2.9 +/- 0.2 h and 11.5 +/- 1.3 h, and AUC0-24 values were 59.3 +/- 5.1 ng x h x mL(-1) (0-12 h) and 204.1 +/- 31.2 ng x h x mL(-1) for buccal tablet and transdermal patch, respectively.

MeSH terms

  • Acrylic Resins
  • Adhesiveness
  • Adhesives
  • Adult
  • Chemistry, Pharmaceutical
  • Chitosan
  • Cotinine / blood
  • Dosage Forms
  • Female
  • Humans
  • Kinetics
  • Magnesium Hydroxide / chemistry
  • Male
  • Mouth Mucosa
  • Nicotine / administration & dosage*
  • Nicotine / blood
  • Nicotine / therapeutic use
  • Nicotinic Agonists / administration & dosage*
  • Nicotinic Agonists / blood
  • Nicotinic Agonists / therapeutic use
  • Smoking Cessation*
  • Solubility

Substances

  • Acrylic Resins
  • Adhesives
  • Dosage Forms
  • Nicotinic Agonists
  • carbomer
  • Nicotine
  • Chitosan
  • Cotinine
  • Magnesium Hydroxide