چکیده (انگلیسی):

The aim of the current study was to design oral controlled
release mucoadhesive compressed hydrophilic matrices of
atenolol and to optimize the drug release profile and bioadhesion
using response surface methodology. Tablets were
prepared by direct compression and evaluated for bioadhesive
strength and in vitro dissolution parameters. A central
composite design for 2 factors at 3 levels each was employed
to systematically optimize drug release profile and
bioadhesive strength. Carbopol 934P and sodium carboxymethylcellulose
were taken as the independent variables.
Response surface plots and contour plots were drawn, and
optimum formulations were selected by feasibility and
grid searches. Compressed matrices exhibited non-Fickian
drug release kinetics approaching zero-order, as the value
of release rate exponent (n) varied between 0.6672 and
0.8646, resulting in regulated and complete release until
24 hours. Both the polymers had significant effect on the
bioadhesive strength of the tablets, measured as force of
detachment against porcine gastric mucosa (P < .001).
Polynomial mathematical models, generated for various
response variables using multiple linear regression analysis,
were found to be statistically significant (P < .01). Validation
of optimization study, performed using 8 confirmatory runs,
indicated very high degree of prognostic ability of response
surface methodology, with mean percentage error (± SD)
as −0.0072 ± 1.087. Besides unraveling the effect of the
2 factors on the various response variables, the study helped
in finding the optimum formulation with excellent bioadhesive
strength and controlled release.