چکیده (انگلیسی):

The aim of the present study was to prepare and evaluate a
novel buccal adhesive system (NBAS) containing propranolol
hydrochloride (PH). A special punch was fabricated
and used while preparing an NBAS. Solubility of PH in
phosphate buffer solution (pH 6.6), partition coefficient
between phosphate buffer (pH 6.6) and 1-octanol, and permeability
coefficient through the porcine buccal mucosa
were performed and found to be 74.66 mg/mL, 5.17, and 5.6,
respectively. Stability of NBAS was determined in natural
human saliva, and it was found that both PH and device are
stable in human saliva. NBAS was evaluated by weight uniformity,
thickness, hardness, friability, swelling, mucoadhesive
strength, in vitro drug release, and in vivo human acceptability
studies. Swelling index was higher (4.4) for formulations
containing hydroxyl propyl methyl cellulose (HPMC)
K4M alone, and it decreases with its decreasing concentration
in the NBAS. Mucoadhesive strength (MS) was measured
by using a modified apparatus. All NBASs showed
higher MS with porcine buccal mucosa when compared with
that of rabbit buccal mucosa. NBASs containing carbopol
(CP) 934P and HPMC K4M at the ratio of 1:1 showed higher
MS (44.76 g) with porcine buccal mucosa when compared
with 1:2 (39.76 g), 0:1 (23.29 g), and 1:0 (22.22 g) ratios,
respectively. The mechanism of PH release was found to be
by non-Fickian diffusion (value of "n" between 0.5 and 1.0)
and followed first order kinetics. In vivo human acceptability
study showed that the newly prepared NBAS was comfortable
in the human buccal cavity. It can be concluded that
NBAS is a superior, novel system that overcomes the drawback
associated with the conventional buccal adhesive tablet.