Abstract

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.