Preparation and Characterization of Novel Pharmaceutical Co-Crystals: Ticagrelor with Nicotinamide

Two new co-crystals, Ticagrelor with Nicotinamide, have been prepared with improved solubility. Because Ticalegor has a poor solubility and dissolution rate, a novel co-crystallization method with structurally homogenous crystalline material, an active pharmaceutical ingredient (API), and co-former...

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Bibliographic Details
Main Authors: Muhammad Inam, Jiajia Wu, Jie Shen, Chi Uyen Phan, Guping Tang, Xiurong Hu
Format: Article
Language:English
Published: MDPI AG 2018-08-01
Series:Crystals
Subjects:
Online Access:http://www.mdpi.com/2073-4352/8/9/336
Description
Summary:Two new co-crystals, Ticagrelor with Nicotinamide, have been prepared with improved solubility. Because Ticalegor has a poor solubility and dissolution rate, a novel co-crystallization method with structurally homogenous crystalline material, an active pharmaceutical ingredient (API), and co-former indefinite stoichiometric amount has been made to improve Ticagrelor’s solubility. The co-crystal of Ticagrelor (TICA) with Nicotinamide (NCA) was prepared in ratio (1:1) and confirmed by FTIR, DSC, and XRD characterization. Furthermore, the single crystal structure of TICA-NCA hydrate was analyzed. The solubility of co-crystals was investigated in pH 2 acidic medium, which was a significant improvement as compared to the solubility of a free drug. The in vitro dissolution rate of co-crystal was larger than that of the commercial product.
ISSN:2073-4352