Investigation of formulation factors affecting in vitro and in vivo characteristics of a galantamine transdermal system

Int J Pharm. 2012 Oct 15;436(1-2):32-40. doi: 10.1016/j.ijpharm.2012.06.057. Epub 2012 Jul 5.

Abstract

Because of low treatment compliance with the Alzheimer disease patients, there have been clinical needs for the alternative administration route to effective and well-tolerated approaches of galantamine (Small and Dubois, 2007). In this study, drug-in-adhesive transdermal patches with galantamine were prepared and evaluated in vitro and in vivo. The in vitro permeation studies indicated that DT-2510 was the most suitable pressure-sensitive-adhesive and oleic acid was the most promising enhancer for galantamine drug-in-adhesive patch. The optimized galantamine drug-in-adhesive patch could be physicochemically stable for 28 days at 40 °C/75% RH. The in vivo studies of the optimized galantamine drug-in-adhesive patch showed high absolute bioavailability of around 80% and sustained effect on the drug plasma levels for 24 h. The in vitro and in vivo studies of galantamine drug-in-adhesive patches with different pressure-sensitive-adhesive functional groups showed a strong correlation between the skin permeation rate and the area under the curve. The results suggest that the transdermal application of galantamine drug-in-adhesive patches might be the alternative dosage form to have good efficacy and tolerability for the treatment of Alzheimer disease.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adhesives / administration & dosage
  • Adhesives / chemistry*
  • Administration, Cutaneous
  • Animals
  • Chemistry, Pharmaceutical
  • Cholinesterase Inhibitors / administration & dosage
  • Cholinesterase Inhibitors / chemistry*
  • Cholinesterase Inhibitors / pharmacokinetics
  • Galantamine / administration & dosage
  • Galantamine / chemistry*
  • Galantamine / pharmacokinetics
  • In Vitro Techniques
  • Male
  • Oleic Acid / administration & dosage
  • Oleic Acid / chemistry*
  • Oleic Acid / pharmacokinetics
  • Rabbits
  • Rats
  • Rats, Sprague-Dawley
  • Skin Absorption
  • Transdermal Patch*

Substances

  • Adhesives
  • Cholinesterase Inhibitors
  • Galantamine
  • Oleic Acid