Development and in-vivo characterization of novel trans buccal formulations of Amiloride hydrochloride

Abstract

Objectives

Formulation development and characterization of novel trans-buccoadhesive patches and bilayer tablets of Amiloride hydrochloride (AMHCL) with the objectives to avoid the first-pass effect, incomplete absorption from GIT, improve the bioavailability, minimize the dose, improve the duration of action and hence produce controlled drug delivery.

Methods

AMHCL patches were prepared by solvent casting method, using hydroxy propyl methyl cellulose (HPMC), Carbopol, Chitosan, and polyvinylpyrrolidone-K30 (PVP). Tablets were prepared by direct compression method, using sodium carboxy methyl cellulose (SCMC), HPMC K100, sodium alginate, Carbopol 934 P, Eudragit RL 100, PVP and ethyl cellulose (EC) as a backing layer. The both formulations were evaluated for their thickness uniformity, folding endurance, weight uniformity, content uniformity, swelling behavior, tensile strength, buccoadhesive strength, surface pH and in vitro release studies.

Results

Data of in vitro release from both patches and tablets were fit to different equations and kinetic models to explain release profiles. In vivo drug release studies in rabbits showed 91.65% of drug release from HPMC-Chitosan patch, while it was 82.63–90.21% release from sodium alginate-SCMC buccal tablets. Good correlation among in vitro release and in vivo release of AMHCL was observed in both formulations.

Conclusion

The satisfactory results were obtained in all prepared formulations and based on the results, it can be concluded, Amiloride hydrochloride oral mucoadhesive buccal formulations which can be used mainly in minimizing dose and mainly help to improve the patient compliance and Amiloride hydrochloride is a drug of choice for delivery through the control release via buccal route.