Design and evaluation of mul tip articulate. systems prepared using sieving-spheronisation and extrusionspheronisation
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Date
2011
Authors
Karim, Sabiha
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Abstract
Pelletised dosage forms can be prepared by different methods which, in general,
are time consuming and labor intensive. The current study was carried out to assess the
feasibility of preparing spherical pellets by sieving the wet powder mass followed by
spheronisation. This method was compared with extrusion-spheronisation process in
terms of physical characteristics and in-vitro dissolution profile of the developed
fommlations. The fast release paracetamol pellets were comprised of, microcrystalline
cellulose, Iactose, crosp6vidone and polyvinyl pyrrolidone-K90. The percentage yield of
paracetamol pellets produced by sieving-spheronisation was- higher (p<0.05) in
companson with that produced by extrusion-spheronisation. The extrusionspheronisation
showed better flowability (p<0.05) than sieving-spheronisation. However,
no significant difference was found in other physical properties of two methods. The
dissolution profile was slightly higher in sieving-spheronisation technique, the similarity
factors showed that dissolution profiles can be considered comparable in the
formulations prepared by two methods and followed first order kinetics. The rate of drug
release was essentially independent of pH and agitation rate. Omeprazole spherical
pellets with required release rate were developed using sieving-spheronisation process.
Pellets with desired characteristics were obtained with minimum amount of
microcrystalline cellulose (16% ), lactose, polyvinylpyrrolidone K30, polyethylene
glycol 6000 and sodium lauryl sulfate. Pellets prepared by sieving-spheronisation
showed significantly higher (p<0.05) percentage yield as compared to that of extrusionspheronisation.
Omeprazole delay release system was develope'd by Kollicoat 30DP,
using bottom spray fluidised bed system. Coating level of 17.5 % prevented the drug
release less than 10% at pH 1 for initial 2 hours and at pH 6.8 release was 80 to 84%
within 45 minutes, following the first order release kinetics. In accelerated stability
studies, both drugs followed the zero order degradation. The estimated shelf life of
paracetamol and omeprazole was 24.42 and 21.00 months respectively at 25 °C. Coated
omeprazole pellets prepared by sieving-spheronisation and the reference drug (Zimor®
20mg) were evaluated for bioequivalence, using rabbits in cross-over design, and both
formulations were found to be equivalent.
In conclusion, the pelletised dosage forms can be formulated- through si·eving
followed by spheronisation method, which is simple, easy, less time consuming and
economical as compared to extrusion-spheronisation process.
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Keywords
Multiparticulate systems , Sieving-spheronisation