Improvement in physicochemical properties of ezetimibe using a crystal engineering technique

Solubility Enhancement of Lornoxicam by Crystal Engineering

“…The formation of cocrystal was also confirmed on the basis of powder XRD studies, which indicated completely different diffractograms for cocrystals and lornoxicam. Thus the strength of hydrogen bonding will definitely influence the melting point characteristic of a cocrystal [41] .…”

Kinetics of co-crystal formation with caffeine and citric acid via liquid-assisted grinding analyzed using the distinct element method

“…3f). Mulye et al (2012) reported that co-crystals of ezetimibe-benzoic acid and ezetimibe-salicylic acid have altered morphologies compared with those of the original crystals. Morphological analysis of the particles revealed marked differences among CF, CF hydrate, CTA, CTA hydrate, co-crystal-1, and co-crystal-2, indicating that different crystal forms may be obtained.…”

Understanding peroral absorption: regulatory aspects and contemporary approaches to tackling solubility and permeability hurdles

“…OMS formulation compares well with the marketed product (sporanox) thus considered as better carrier.136Porous silicon based microparticles–Antipyrene, ibuprofen, griseofulvin, ranitidine, furosemideII, IVDrug loaded in mesoporous silicon microparticle increased the dissolution rate and reduced the pH dependency dissolution.137MicelleThin film hydrationAmphotericinIISelf-assembled lecithin-based mixed polymeric micelle containing pluronic, kolliphor RH40,TPGS and DSPE-PEG2K showed 2.18- and 1.50-fold increased in bioavailability when administered i.v. and orally.138MicelleDialysis methodPaclitaxelIVPluronic F127, P188 and heparin-all- trans -retinoid acid conjugate mixed micelle exhibited higher AUC, C max and 5- to 6-fold increase in effective permeability.139Co-crystal–QuercetinIIQuercetin–caffeine, quercetin–caffeine–methanol, quercetin–isonicotinamide and quercetin–theobromine dihydrate co-crystals exhibited pharmacokinetic properties that are vastly superior than quercetin alone.140Co-crystalAnti-solvent crystallizationIndomethacinIISaccharine-indomethacin cocrystals were hygroscopic and found to have significantly higher dissolution rate than pure indomethacin.141Co-crystalAnti-solvent crystallizationDiflunisalIINicotinamide–diflunisal cocrystal improves intrinsic dissolution rate by 20%.142Co-crystalAnti-solvent crystallizationIbuprofenIIHighly soluble molecule in crystallographic pattern of ibuprofen enhances the solubility more than 7.5 times.143Co-crystalAnti-solvent crystallizationEzetimibeIIBenzoic acid and salicylic acid ezetimibe co-crystal showed significant enhancement in the dissolution profile as compared to pure ezetimibe.144Dendrimer–CamptothecinIIG.4 and G.3.5 PAMAM dendrimer increased camptothecin solubilization in simulated gastric fluid and caused 2-fold to 3-fold increase in oral absorption suggested increased bioavailability.145Dendrimer–Famotidine, indomethacin, amphotericinIIG.5 PPI dendrimer–drug complex demonstrated increase in solubility due to hydrophobic and electrostatic interactions for acidic, basic and amphoteric drug.146Dendrimer…”