Purpose:
To formulate prolonged-release floating
microparticles that would minimise the
irritant effect of weakly acidic drugs, such as
nimesulide, on the stomach by avoiding direct contact
with gastric mucosa.
Methods:
Sustained release floating microparticles of nimesulide
was prepared by a coacervation (non-solvent addition
technique. Three different ratios of the coacervating
polymer, low-viscosity hydroxypropyl methylcellulose (HPMC),
were used, and the dissolution characteristics of the
floating microparticles in simulated gastric and
intestinal media were evaluated. In order to determine
whether there was drug – polymer interaction, the
microparticles were also assessed by infra-red (FTIR)
spectroscopy and x-ray diffraction (XRD). Micromeritic
properties of the microparticles were also assessed.
Results:
The drug content of the floating microparticles
increased with increase in the level of HPMC
incorporated. All floating microparticles formulations
showed good flow properties while particle size analysis
revealed that the appearance and size distribution of
the formulations varied with polymer concentration. FTIR
and XRD data indicated the crystalline nature of the
drug but there was no chemical interaction between the
drug and the polymer in the microparticles. Nimesulide
release was faster in simulated intestinal fluid (pH
6.8) than in simulated gastric fluid (pH 1.2) and
distilled water (pH 6.5).
Conclusion:
Coacervation non-solvent addition is a suitable
technique for preparing floating microparticles of
nimesulide using low-viscosity HPMC.
Keywords:
Floating microparticles, Nimesulide, HPMC, Coacervation,
Non-solvent addition, Sustained release.