Abstract

Azelnidipine, an anti-hypertensive drug of dihydropyridine class, has low solubility and high permeability drug (class-2) and thus often shows dissolution rate-limited oral absorption and high variability in pharmacological effects. The purpose of study was to prepare co-crystals of AZL to enhance its solubility. Co-crystals were prepared by solvent evaporation method using different co-crystal formers. The prepared co-crystals were evaluated for solubility. The solid state property was characterized by microscopy, differential scanning calorimetry (DSC) and Fourier transfer infrared spectroscopy (FTIR). It was observed that the solubility of AZL co-crystals was significantly more than AZL. Co-crystal using succinic acid and saccharine gave maximum solubility. The microscopy, FTIR and DSC and studies of cocrystal confirmed the formation of co-crystals and indicated that new interactions were formed. In conclusion, co-crystals of AZL lead to the solubility enhancement and this can be further explored to study the impact of increased solubility on the bioavailability of AZL.

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