Development, Characterization
and Analysis of Azelnidipine Co-Crystals
Patel Ekta C., Patel Hemangi S., Patel Mehul N., Christian Jenee R. and Suhagia
B.N.
Res. J. Chem. Environ; Vol. 26(6); 15-23;
doi: https://doi.org/10.25303/2606rjce15023; (2022)
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.