Abstract

CARBOPOL BASED MUCOADHESIVE FORMULATION OF DILTIAZEM HYDROCHLORIDE

Channawar Madhuri* and Kshirsagar Mahendra

ABSTRACT

Diltiazem hydrochloride, is a drug which is widely used in the treatment of hypertension. However, its extensive first pass metabolism results in poor bioavailability. The objective of present research work is to design and evaluate the controlled release mucoadhesive buccal tablets of Diltiazem hydrochloride with a goal to increase the bioavailability, reduce dosing frequency and improve patient compliance. The tablets were prepared using primary mucoadhesive polymers such as Carbopol‐940P along with secondary polymers such as Hydroxy propyl methyl cellulose (HPMC), Psyllium husk. Six formulations were developed with varying concentration of polymers. The tablets were evaluated for hardness, weight variation, thickness, percentage of drug content, Surface pH, invitro swelling, mucoadhesive strength, mucoadhesion time and percentage drug release. Formulation (A3) containing Carbopol‐940 and HPMC K4M in the ratio of (1 : 5) showed good mucoadhesive strength (39.43gm) and maximum drug release of 87.33% in 8 hrs. Swelling increase with increase in concentration of HPMC K4M in tablets. Surface pH was found to be 6.10. Drug release pattern was found to be Higuchi in formulation A3. FTIR study showed no evidence of interaction between drug and polymers. The results indicate that the mucoadhesive buccal tablets of Diltiazem may be good choice to bypass the extensive hepatic first pass metabolism with an improvement in the bioavailability.

Keywords: Diltiazem, Mucoadhesive, Control release, Swelling index, HPMC, Carbopol.