A NOVEL APPROACH OF ENTERIC COATED PELLETS FORIMMEDIATE RELEASE BY USING EXTRUSION-SPHERONIZATIONTECHNIQUE

Abstract

In the present study, an attempt was made to prepare immediate-release enteric-coated pellets of
a NSAID class of drug, a poorly soluble nonsteroidal anti-inflammatory drug that has a gastrointestinal intolerance as its serious side effect. Formulation of enteric-coated pellets with
improved solubility of drug could address both of these problems. To achieve these goals, pellets
were prepared by extrusion–spheronization method using pelletizing agents that can contribute to
the faster disintegration and thereby improve the solubility of the drug. Different disintegrants
like β-cyclodextrin, cross carmellose sodium, sodium starch glycolate, Prosolve, crospovidone
were tried in order to further improve disintegration time. The pellets were characterized for drug
content, particle size distribution, flow properties, infrared spectroscopy, surface morphology,
disintegration rate, and dissolution profile. The Formulation was Coated with an enteric-coated
polymer which does not dissolve at gastric pH but dissolves at intestinal pH, releasing the drug
immediately in dissolution medium. The improvement was substantial when it was compared
with solubility of pure drug under the same conditions. Here in this review article these topics
are discussed briefly.
Keywords: NSAID class of Drug,enteric-coating, Immediate release, Super disintegrant, pellets, Extrusion-Spheronization technique
INTRODUCTION
Pellets are small free flowing, spherical particulate, manufactured by the agglomeration of fine
powder or granules. In recent years, there has been a growing interest in the field of pelletization
to produce spherical pellets which can be changed into several dosages forms like tablet and
capsule or can be administered as such. Pelletization involves size enlargement process and if the
final agglomerates are spherical in shape in the size range of 0.5-2.0 mm, they are called pellets.
(1) Pellets have numerous therapeutic as well as technical advantages such as enhanced drug
absorption due to involvement of large GI surface in absorption process, less gastric irritation by
limiting localized buildup and dose dumping, good flow ability due to uniform size and shape,
high tensile strength, low friability, narrow particle size distribution, and uniform packing
characteristics.(2)
The pelletized products can improve the safety and efficacy of the active agent. The pellets are
directly filled into capsule and can also be compressed into tablets. The compression of pellets
into tablets is much more ideal than enclosing them in a hard gelatin capsule.(3)In multiple unit
IJARR, 2(12), 2017; 68-75
68
International Journal of Advanced Research and Review
www.ijarr.in
A NOVEL APPROACH OF ENTERIC COATED PELLETS FORIMMEDIATE RELEASE BY USING EXTRUSION-SPHERONIZATIONTECHNIQUE
Bipin Bholani1*
, Dr. Manish Goyani2
1Shree Dhanvantary Pharmacy College, Kim, Surat, Gujarat, India. Email: bipinbholani@gmail.com
ABSTRACT
In the present study, an attempt was made to prepare immediate-release enteric-coated pellets of
a NSAID class of drug, a poorly soluble nonsteroidal anti-inflammatory drug that has a gastrointestinal intolerance as its serious side effect. Formulation of enteric-coated pellets with
improved solubility of drug could address both of these problems. To achieve these goals, pellets
were prepared by extrusion–spheronization method using pelletizing agents that can contribute to
the faster disintegration and thereby improve the solubility of the drug. Different disintegrants
like β-cyclodextrin, cross carmellose sodium, sodium starch glycolate, Prosolve, crospovidone
were tried in order to further improve disintegration time. The pellets were characterized for drug
content, particle size distribution, flow properties, infrared spectroscopy, surface morphology,
disintegration rate, and dissolution profile. The Formulation was Coated with an enteric-coated
polymer which does not dissolve at gastric pH but dissolves at intestinal pH, releasing the drug
immediately in dissolution medium. The improvement was substantial when it was compared
with solubility of pure drug under the same conditions. Here in this review article these topics
are discussed briefly.