Abstract

DESIGN AND EVALUATION OF BUCCOADHESIVE COMPACTS OF ENALAPRIL MALEATE

G.S. Shantha Kumar*, R. Narayanacharyulu, Divakar Goli, Roopa Karki,Venkatesh D.P.

ABSTRACT

Compacts containing the drug layer were developed by direct compression method using combination of polymers (HPMC and Carbopol 934P) and ethyl cellulose as an impermeable backing layer to release the drug in a unidirectional way toward the mucosa, thus avoiding loss of drug due to wash out by saliva. Formulations were evaluated for precompressional parameters, physical parameters, drug content uniformity, in vitro release studies, ex vivo residence time, stability studies in human saliva and in vivo mucoadhesion test. Physicochemical parameters and content uniformity were found within IP limits. The bioadhesive force of compacts was found in the range of 2.59 to 4.34 N. Formulation F2 exhibited controlled drug release of 90.92% in 8h and selected as optimized formulation follows zero order drug release. FTIR studies showed no evidence on interaction between drug, polymers and other excipients. Ex vivo residence time was found in the range of 375 to 655 min. The results of stability studies in human saliva showed that compacts stable in human saliva. In vivo mucoadhesion studies indicated that compacts were retained for more than 8h. It was revealed that there are no changes in color, irritancy, redness and dryness of mouth was found in rabbits after mucoadhesion studies. Short-term stability studies (40 2C/755% for 3 months) on the optimized formulation indicated that there are no significant changes in drug content and in vitro dissolution characteristics. The results indicate that suitable buccoadhesive compacts of enalapril maleate with in vivo residence time and control release could be developed.

Keywords: Enalapril maleate, Carbopol 934P, in vivo residence time, bioadhesive force.