Cocrystallization of Loratadine With Succinic Acid Using Neat Grinding Method

Abstract

Cocrystal of loratadine (L) was produced using succinic acid (SA), in order to improve the poor aqueous solubility profile. This was prepared in molar ratio of 1:1 (CC1) and 1:2 (CC2), applying the neat grinding method, therefore, the physicochemical properties and in vitro dissolution of both were characterized in free CO2 aquadest. The thermogram DSC of CC1 exhibited single endothermic peak at 116.8°C, two peaks were seen in CC2, at 90.2 and 152.2°C, and L had one, at 137.5°C. In addition, the results of XRPD showed a new peak at 2θ 21.93° and 21.88°, respectively, while C=O and –OH band shifts were identified in the FTIR spectra of both preparations. SEM photomicrographs revealed particle size reduction without habit alteration, while physicochemical characterization confirmed the incomplete cocrystal formation of loratadine with succinic acid, which promotes efficiency dissolution (DE15), in contrast with loratadine.

Keywords: loratadine, succinic acid, cocrystal, physical characterization, dissolution