Abstract
In this study, a novel approach for compression of matrix pellets into disintegrating tablets has been studied in an attempt to overcome the issues pertaining to rupture of polymer coat during compression of reservoir-type pellets. Extended release matrix pellets were prepared by the extrusion/spheronization technique using commercially available aqueous dispersions of ethyl cellulose, acrylic polymers and sodium alginate at 10%, 20% and 30%w/w levels. Sertraline hydrochloride was used as the model drug and an in vitro release profile of 12 h was targeted. Tablets containing matrix pellets were prepared by the direct compression process. Acceptance Value, a pharmacopeial test, was applied to study the uniformity of drug distribution. Effect of compression force (2-6 kN), extrusion screen aperture size, diluent blend composition and pellet percentage on drug release and acceptance value were studied. As polymer is uniformly distributed within each pellet, the drug release pattern from uncompressed pellets was comparable to compressed tablets. Surface morphological changes due to calcium chloride treatment were observed using Scanning electron microscopy. The pellet segregated from the surface of the tablet was found to be flattened in the direction of applied compression force with minor deformities. In conclusion, matrix pellets can constitute an alternative approach to reservoir-type pellets in obtaining disintegrating tablets for extended delivery of drugs.
Highlights
Multiple unit extended release dosage forms are preferred over single unit dosage forms as they spread uniformly throughout the gastrointestinal tract producing less variability and lower risk of local irritation due to the minute amount of drug carried (Bodmeier, 1997; Bechgaard, Nielsen, 1978)
The concept of compression of matrix pellets into disintegrating tablet dosage form was derived as a response to issues pertaining to compression of reservoir-type pellets coated with polymers for extended release of drug
Most of the studies on compression of pellets coated with polymers have shown damage to the coating with loss of the extended release properties due to rupture of the coat (Dashevsky, Kotler, Bodmeier, 2004) resulting in faster drug release (Sarisuta, Punpreuk, 1994)
Summary
Multiple unit extended release dosage forms are preferred over single unit dosage forms as they spread uniformly throughout the gastrointestinal tract producing less variability and lower risk of local irritation due to the minute amount of drug carried (Bodmeier, 1997; Bechgaard, Nielsen, 1978). Most of the studies on the compression of pellets coated with ethyl cellulose and acrylic polymers have revealed damage to the coating with loss of the extended release properties (Bansal, Vasireddy, Parikh, 1993). Compression of pellets at higher force is reported to reduce the release from the tablets due to fusion of pellets (Lopez-Rodriguez et al, 1993) whereas the release of drug was found to be faster from tablets due to the brittle nature of pellets (Branka et al, 2009). Use of microcrystalline cellulose and polyethylene glycol 3350 produced rapidly disintegrating tablets containing pellets, with lowest change in the drug release pattern after tableting (Torrado, Paronen, 1994). A recent study involved the use of polyethylene glycol as a cushioning agent and tablet compression at elevated temperature as an alternative to using reservoir-type pellets (Wieslaw, Jaroslaw, Ilona, 2010)
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