Enhancement of Bioavailability of Cefpodoxime Proxetil Using Different Polymeric Microparticles

Poorly water-soluble drugs such as cefpodoxime proxetil (400 μg/ml) offer a challenging problem in drug formulation as poor solubility is generally associated with poor dissolution characteristics and thus poor oral bioavailability. According to these characteristics, preparation of cefpodoxime proxetil microparticle has been achieved using high-speed homogenization. Polymers (methylcellulose, sodium alginate, and chitosan) were precipitated on the surface of cefpodoxime proxetil using sodium citrate and calcium chloride as salting-out agents. The pure drug and the prepared microparticles with different concentrations of polymer (0.05–1.0%) were characterized in terms of solubility, drug content, particle size, thermal behavior (differential scanning calorimeter), surface morphology (scanning electron microscopy), in vitro drug release, and stability studies. The in vivo performance was assessed by pharmacokinetic study. The dissolution studies demonstrate a marked increase in the dissolution rate in comparison with pure drug. The considerable improvement in the dissolution rate of cefpodoxime proxetil from optimized microparticle was attributed to the wetting effect of polymers, altered surface morphology, and micronization of drug particles. The optimized microparticles exhibited excellent stability on storage at accelerated condition. The in vivo studies revealed that the optimized formulations provided improved pharmacokinetic parameter in rats as compared with pure drug. The particle size of drug was drastically reduced during formulation process of microparticles

Industrially feasible alternative approaches in the manufacture of solid dispersions: A technical report

The purpose of this report was to compile relevant technical information on various alternative strategies that can be used as feasible approaches in the development of solid dispersions. The technologies discussed in the report are spray coating on sugar beads with a fluidized bed coating system, hot melt extrusion, direct capsule filling, electrostatic spinning, surface active carriers, and supercritical fluid technology. The focus is on basic principles, the equipment involved, and the relevant scale-up work. These technologies have been found to eliminate several drawbacks posed by the conventional methods of manufacturing of solid dispersions such as laborious preparation methods, reproducibility, scaling up of manufacturing processes, stability of drug, and vehicle