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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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:	co-crystal ticagrelor nicotinamide solubility dissolution
Online Access:	http://www.mdpi.com/2073-4352/8/9/336

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spelling	doaj-afd6698d510a43118439c5f1379232722020-11-24T21:17:19ZengMDPI AGCrystals2073-43522018-08-018933610.3390/cryst8090336cryst8090336Preparation and Characterization of Novel Pharmaceutical Co-Crystals: Ticagrelor with NicotinamideMuhammad Inam0Jiajia Wu1Jie Shen2Chi Uyen Phan3Guping Tang4Xiurong Hu5Department of Chemistry, Zhejiang University, Hangzhou 310028, ChinaDepartment of Chemistry, Zhejiang University, Hangzhou 310028, ChinaDepartment of Chemistry, Zhejiang University, Hangzhou 310028, ChinaDepartment of Chemistry, Zhejiang University, Hangzhou 310028, ChinaDepartment of Chemistry, Zhejiang University, Hangzhou 310028, ChinaDepartment of Chemistry, Zhejiang University, Hangzhou 310028, ChinaTwo 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.http://www.mdpi.com/2073-4352/8/9/336co-crystalticagrelornicotinamidesolubilitydissolution
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Muhammad Inam Jiajia Wu Jie Shen Chi Uyen Phan Guping Tang Xiurong Hu
spellingShingle	Muhammad Inam Jiajia Wu Jie Shen Chi Uyen Phan Guping Tang Xiurong Hu Preparation and Characterization of Novel Pharmaceutical Co-Crystals: Ticagrelor with Nicotinamide Crystals co-crystal ticagrelor nicotinamide solubility dissolution
author_facet	Muhammad Inam Jiajia Wu Jie Shen Chi Uyen Phan Guping Tang Xiurong Hu
author_sort	Muhammad Inam
title	Preparation and Characterization of Novel Pharmaceutical Co-Crystals: Ticagrelor with Nicotinamide
title_short	Preparation and Characterization of Novel Pharmaceutical Co-Crystals: Ticagrelor with Nicotinamide
title_full	Preparation and Characterization of Novel Pharmaceutical Co-Crystals: Ticagrelor with Nicotinamide
title_fullStr	Preparation and Characterization of Novel Pharmaceutical Co-Crystals: Ticagrelor with Nicotinamide
title_full_unstemmed	Preparation and Characterization of Novel Pharmaceutical Co-Crystals: Ticagrelor with Nicotinamide
title_sort	preparation and characterization of novel pharmaceutical co-crystals: ticagrelor with nicotinamide
publisher	MDPI AG
series	Crystals
issn	2073-4352
publishDate	2018-08-01
description	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.
topic	co-crystal ticagrelor nicotinamide solubility dissolution
url	http://www.mdpi.com/2073-4352/8/9/336
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Preparation and Characterization of Novel Pharmaceutical Co-Crystals: Ticagrelor with Nicotinamide

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