Design and characterisation of sustain release gastro retentive floating tablets of Diltiazem Hydrochloride

By Margret Chandira, Chandramohan, Debjit,  Chiranjib, B.Jayakar, K.P.Sampath Kumar

Abstract

Gastroretentive drug delivery systems are the systems which are retained in the stomach for a longer period of time and thereby improve the bioavailability of drugs. Diltiazem Hydrochloride, is a Calcium channel blocker, an anti-hypertension and anti-anginal drug, Diltiazem Hydrochloride undergoes an extensive biotransformation, mainly through cytochrome P-450 CYP3A, which results in less than 4% of its oral dose being excreted unchanged in urine. Suffers from poor bioavailability (~30% to 40%) owing to an important first pass metabolism. It has an elimination half-life of 3.5 hrs and an absorption zone from the upper intestinal tract. Thus the present work is aimed to formulate floating tablets of Diltiazem Hydrochloride using an effervescent approach for gastroretentive drug delivery system.Floating tablets were prepared using direct compression technique using Hydrophilic polymer like HPMC K4M, HPMC K15M and hydrophobic polymer like Ethylcellulose as matrix materials in various quantities (%w/w), sodium bicarbonate, citric acid, magnesium stearate, talc and lactose in varying ratio to formulate the floating tablets. Observations of all formulations for physical characterization had shown that, all of them comply with the specification of official pharmacopoeias and/or standard reference. It was observed that tablets of batch F6 followed the results obtained, it was concluded that the formulation F6 is the best formulations as the extent of drug release was found to be around 99.81 % at the desired time 12 hrs.

 

Key Words : Floating tablets, swelling index, Diltiazem Hydrochloride, in-vitro buoyancy studies

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