Inclusion complexes of nicardipine-HCL for oral administration

Inclusion complexes of nicardipine HCl [NIC] with beta-cyclodextrin [beta-CD] and hydroxypropyl-beta-cyclodextrin [HP-beta-CD] were prepared using different methods: co-evaporation, kneading and co-precipitation. Inclusion complexation in aqueous solution and in solid state was studied by the solubility method, Fourier transform-infrared spectroscopy [FTIR], Differential scanning calorimetry [DSC] and X-ray diffractometry [XRD]. The solubility of [NIC] increased as a function of cyclodextrin concentration, showing B s and AL type diagrams for [beta-CD] and [HP-beta-CD], respectively. The dissolution rate of [NIC] / cyclodextrin complexes were investigated and compared with those of the physical mixtures and pure drug. The dissolution efficiency of [NIC] increased by complexation with cyclodextrins to 2.8-2.9 fold than [NIC] alone. Oral bioavailability in rabbits increased to 6 fold by complexation with [beta-CD]

Preparation and physicochemical characterization of solid dispersions of piroxicam with phospholipids

Solid dispersions of piroxicam with dimyristoylphosphatidylcholine [DMPC], dipalmitoylphosphatidylcholine [DSPC] and distearoylphosphatidylcholine [DSPC] in ratios of 20:1, 10:1 and 5:1 [drug-to-phospholipids w/w], were prepared by the solvent evaporation method. Coprecipitation was done from a chloroform solution of the appropriate quantities of piroxicam and each phospholipid according to the previously mentioned w/w ratios. The physicochemical characteristics of piroxicam-phospholipids coprecipitates were evaluated using differential scanning calorimetric analysis [DSC], X- ray diffraction analysis [XRD] and Fourier transform infrared analysis [FTlR]. Results were compared with the pure drug and the corresponding physical mixtures in the same weight ratios

Enhancement of dissolution and bioavailability of firoxicam via solid dispersion with phospholipids

In this work physical mixtures [PMs] and coprecipitates [COPPTs] of piroxicam [PIR] with each of L-alpha-dimyristoylphosphatidylcholine [DPPC] and L-alpha-distearoylphosphatidycholine [DSPC] in ratios of 20:1, 10:1 and 5:1 [drug-to-phospholipids w/w] were prepared. The effect of the method of preparation, the type of phospholipids [PL] and the drug-to-PL w/w ratios on the rate and extent of dissolution of PIR was investigated. The effect of the previously mentioned factors on the dissolution efficiency [DE%] was analyzed using two-way analysis of variance [ANOVA]. The most significant effect on the dissolution rate and extent was due to the method of preparation followed by the drug-to-PL ratio and finally the PL type. All PIR-PL systems improved the dissolution rate of piroxicam, but coprecipitates of 5:1 w/w ratio showed the superior effect on the drug dissolution profile