Controlled release tablet formulations of carvedilol
ABSTRACT:
The present investigation was undertaken with an objective
of formulating controlled release (CR) oral matrix tablet formulations of
Carvedilol (CAR), an antihypertensive using cellulose ether polymer, Hydroxy
Propyl Methyl Cellulose (HPMC K4M, HPMC K15M) of different viscosity grades as
drug release retardants. The tablets were prepared by direct compression
technique and evaluated for various physico-chemical/mechanical parameters.
Based on the viscosity and gel formation during dissolution, HPMC K4M was
selected as release retardant. The effect of different fillers like Avicel PH
101, Avicel PH 105 and Avicel PH 200 (microcrystalline cellulose), pre gelatinized
starch (PGS), maize starch with spray dried lactose (FLOWLAC) on CAR release
was studied and percent release of CAR at the end of 24h is in the order of
FLOWLAC > Avicel PH 101 > Avicel PH 105 > Avicel PH 200 > PGS.
Based on the dissolution data obtained with different fillers and keeping in
view of the results from the pre-compression studies, and gel layer retaining
with the matrix tablets, Avicel PH 105 was selected to carry out further
formulation development. The formulation containing 25%w/w HPMC K4M as release
retardant and Avicel PH 105 gave 96.59 ± 3.1% release at the end of 24h and
fulfils regulatory requirement. The dissolution data was also evaluated for
drug release kinetics and mechanism.
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