Influence of Polymer Type, Active Substance, and Experimental Model on Mucoadhesive Properties of Selected Drug Formulations

Abstract

Texture analyzer equipped with mucoadhesive rig has been used for determination of mucoadhesiveness of solid and semisolid drug formulations: lyophilizates, compressed tablets, and gels. Two different mucosa surrogates: mucin solution on a cellulose support and gelatin discs have been employed. The results obtained for different polymers are inconsistent and depend not only on the experimental model but also on the drug formulation. Addition of an excipient (e.g., lactose) or a drug (tramadol HCl, telmisartan) to the lyophilized polymer matrix generally resulted in decrease of observed adhesive forces which depended more on the polymer used than on the composition of the preparation. Due to low predictability of the effect of pharmaceutical formulation (type and composition) on the mucoadhesiveness of the polymer it has been concluded that individually designed experiments have to be applied for each preparation.

Keywords:

• Drug formulations
• mucoadhesiveness
• polymers
• texture analyzer

Notes

*Molecular weight: L – low, M – medium, H – high, (a) – acidic form, (alc) – alcalised form; CP – carbomer, CMC – sodium carmellose, HPMC – hypromellose, AlgNa – sodium alginate, HEC – hydroxyethylcellulose, Pec – pectin.

From the Proceedings from Formula VI in Stockholm 2010.