ChemistrySelect · 2019 · 13 citations · 25 references
PharmacyPharmaceuticsPharmacologyDissolution TestingDrug DeliveryPharmaceutical FormulationChromatographyDissolution MediaDrug SolubilityFormulation Effects On DissolutionLiquid ChromatographySpectroscopic Analysis Of PharmaceuticalsChemical Stability AssessmentChemical Stability TestingCo-crystal CharacterizationCo-crystal FormationCo-crystal FormulationsCocrystal FormationMicrowave-assisted PreparationPowder X-ray Diffraction
Abstract In this study, we developed a novel and simple method to prepare an established diclofenac‐proline co‐crystal (DPC) using microwave. In addition, we also evaluate the pharmaceutical properties of the co‐crystal, including dissolution, diffusion, and anti‐inflammatory profile. The kinetics of co‐crystal formation was investigated using Fourier‐transform infrared spectroscopy. The co‐crystal yield was confirmed physically by differential scanning calorimetry and powder x‐ray diffraction, while the chemical stability of the drug during and after microwaving was confirmed using thin layer chromatography, ultraviolet spectrophotometry and high‐performance liquid chromatography. Experiment results demonstrated that microwave can generate the stable and uniform quality of diclofenac‐proline co‐crystal efficiently. Furthermore, the process was investigated to follow a second order kinetic, which is different than the neat‐grinding process previously reported. Moreover, our findings revealed that co‐crystals with L‐proline can significantly improve the dissolution, diffusion, and anti‐inflammation activity of diclofenac acid.
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