2014, Number 2
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Rev Cubana Farm 2014; 48 (2)
In vitro evaluation of oral tablets of copper-non steroidal anti inflammatory complexes
Benavides AJF, Tobón ZGE
Language: Spanish
References: 17
Page: 239-249
PDF size: 321.85 Kb.
ABSTRACT
Introduction: non-steroidal anti-inflammatory drugs (NSAIDs) are a diverse and chemically heterogeneous group of analgesic, antipyretic and inflammatory drugs;
however their performance is affected by low aqueous solubility and the incidence of side gastrointestinal effects. As an alternative to manage this problem, the
copper-NSAIDS complex in a tablet formulation shows adequate
in vitro behavior and might have minor side effects compared to those of the single non-complexed anti-inflammatory drug.
Objective: to evaluate the tablet disintegration and dissolution behaviors of copper-NSAIDS complex.
Methods: copper-NSAIDS complexes were synthesized and characterized. The
effect of morphology, particle size and surface characteristics on the dissolution
process was assessed through the optic microscopy. These results were further
considered for the complex formulation and allowed the right selection of a
disintegrator, a flow modifier, a lubricant and a binder together with production of
tablets through direct compression. The mechanical and physical properties and the
dissolution and disintegration behaviors of these compacts were also evaluated.
Results: complex tablets showed disintegration times from 5 to 15 min and
in vitro release of 75 % to 93 %.
Conclusions: NSAIDs dissolution improved due to complexation with copper, smaller particle size, presence of pores and cracks on the particle surface and the
inclusion of excipients in the formulation of oral tablets.
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