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.
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