Bioadhesive, rheological, lubricant and other aspects of an oral gel formulation intended for the treatment of xerostomia

Int J Pharm. 2004 Jul 8;278(2):391-406. doi: 10.1016/j.ijpharm.2004.03.022.

Abstract

Xerostomia is commonly known as 'dry mouth' and is characterised by a reduction or loss in salivary production. A bioadhesive gel for its localised treatment was formulated to help enhance the residence time of the product, based on the polymer Carbopol 974P. The bioadhesion of various formulations was evaluated on different mucosal substrates, as simulations of the oral mucosa of xerostomic patients. Depending on the type of model substrate used, the mechanism of bioadhesion could alter. When the rheology of various formulations was examined, changes in bioadhesion were more easily interpreted, as the presence of other excipients caused an alteration in the rheological profile, with a change from a fully expanded and partially cross-linked system to an entangled system. Improving the lubricity of the product was considered important, with optimum incorporation of vegetable oil causing a desirable lowering of the observed friction of the product. The final complex formulation developed also contained salivary levels of electrolytes to help remineralisation of teeth, fluoride to prevent caries, zinc to enhance taste sensation, triclosan as the main anti-microbial/anti-inflammatory agent and non-cariogenic sweeteners with lemon flavour to increase the palatability of the product while stimulating any residual salivary function.

MeSH terms

  • Acrylates / chemistry*
  • Acrylates / therapeutic use
  • Adhesiveness
  • Excipients / chemistry
  • Excipients / therapeutic use
  • Mucous Membrane / chemistry
  • Rheology
  • Saliva, Artificial / chemistry*
  • Saliva, Artificial / therapeutic use
  • Xerostomia / drug therapy

Substances

  • Acrylates
  • Excipients
  • Saliva, Artificial
  • carbopol 974P NF