چکیده (انگلیسی):

The purpose of this research was to study mucoadhesive
bilayer buccal tablets of propranolol hydrochloride using the
bioadhesive polymers sodium alginate (Na-alginate) and
Carbopol 934P (CP) along with ethyl cellulose as an impermeable
backing layer. The tablets were evaluated for
weight variation, thickness, hardness, friability, surface pH,
mucoadhesive strength, swelling index, in vitro drug release,
ex vivo drug permeation, ex vivo mucoadhesion, and
in vivo pharmacodynamics in rabbits. Tablets containing
Na-alginate and CP in the ratio of 5:1 (F2) had the maximum
percentage of in vitro drug release without disintegration
in 12 hours. The swelling index was proportional to
Na-alginate content and inversely proportional to CP content.
The surface pH of all tablets was found to be satisfactory
(7.0 ± 1.5), close to neutral pH; hence, buccal cavity
irritation should not occur with these tablets. The mechanism
of drug release was found to be non-Fickian diffusion
and followed zero-order kinetics. The formulation F4 was
optimized based on good bioadhesive strength (28.9 ± 0.99 g)
and sustained in vitro drug permeation (68.65% ± 3.69% for
12 hours). The behavior of formulation F4 was examined in
human saliva, and both the drug and the buccal tablet were
found to be stable. The formulation F4 was applied to rabbit
oral mucosa for in vivo studies. The formulation inhibited
isoprenaline-induced tachycardia. The studies conducted in
rabbits confirmed the sustained release as compared with
intravenous administration.