PREPARATION AND EVALUATION OF BUCCOADHESIVE COMPACTS OF LERCANIDIPINE HYDROCHLORIDE
GS Shantha Kumar*, R Narayanacharyulu, Divakar Goli
ABSTRACT
In the present study, an attempt was made to formulation and
evaluation of Buccoadhesive compacts of LER(LER) in order to
overcome bioavailability problems, to reduce dose dependent side
effects and frequency of administration. Nine formulations were
developed with varying concentrations of polymers like Carbopol 934P
and HPMC by direct compression method. The compacts were tested
for Physical parameters, surface pH, drug content uniformity, swelling
index, bioadhesive strength and in-vitro drug dissolution study. FTIR
studies showed no evidence on interactions between drug, polymers,
and excipients. The surface pH, bioadhesive strength and swelling
index of formulation F2 was found to be 6.27 - 7.00, 3.466 - 5.624N
and 39.21% - 98.54%. The compacts (F2) which contain the Carbopol
934p and HPMC 4KM in the ratio of 1:1 exhibited drug release of
90.17 % in 8h. Ex vivo residence time of all formulations was found in the range of 460 to
680 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 ±
2°C/75±5% for 3 months) on the optimized formulation indicated that there are no significant
changes in drug content and in vitro dissolution characteristics. The prepared compacts of
LER were able to stay in the buccal cavity for a longer period of time, which indicates a
potential use of buccoadhesive compacts of LER for treating blood pressure.
Keywords: Lercanidipine HCl, HPMC 35KM, Bioadhesive strength, Surface pH, in vivo mucoadhesion.
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