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

Ikinci G., ŞENEL S. , Tokgozoglu L., Wilson C., Sumnu M.

PHARMAZIE, cilt.61, sa.3, ss.203-207, 2006 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 61 Konu: 3
  • Basım Tarihi: 2006
  • Dergi Adı: PHARMAZIE
  • Sayfa Sayıları: ss.203-207


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 (C-max) obtained with the buccal tablet and the transdermal patch (p > 0.05). Time to reach the C-max was 2.9 +/- 0.2 h and 11.5 +/- 1.3 h, and AUC(0-24) values were 59.3 +/- 5.1 ng - h - mL(-1) (0-12 h) and 204.1 +/- 31.2 ng - h - mL(-1) for buccal tablet and transdermal patch, respectively.