Fabrication and solid state characterization of ticagrelor Co-Crystals with improved solubility and dissolution

Shane, Nazare Lobo John and Chamle, Ashish Hanumantrao and Vasantharaju, * and Pai, Aravinda and Pai, Girish K and Muddukrishan, BS (2017) Fabrication and solid state characterization of ticagrelor Co-Crystals with improved solubility and dissolution. International Journal of Pharmaceutical Quality Assurance, 8 (1). pp. 1-8. ISSN 0975 9506

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Abstract

In the present study a new co-crystal of Ticagrelor with L-Tartaric acid has been prepared with improved solubility. Ticagrelor is a class VI drug with poor solubility and permeability; hence an attempt has been made to improve its solubility by co-crystallization technology.A co-crystal is a structurally homogeneous crystalline material containing an API and the co-former in definite stoichiometric amounts. In this study the conformer selected was L-Tartaric acid based on ease of hydrogen bond formation. The co-crystal of Ticagrelor with L-Tartaric acid was prepared in different ratios (1:1, 2:1, 1:2). Ticagrelor formed stable co-crystals in the ratios 1:1&2:1. The formation of co-crystal was confirmed by FTIR, DSC and PXRD. The dynamic solubility of co-crystals in the ratios 1:1 and 2:1 was increased by approximately 2.7 and 2.6 fold respectively as compared to pure drug. The in-vitrodissolution study demonstrated a 1.5 fold increase in the solubility for selected TIC:L-TAR (1:1) as compared to its TIC active pharmaceutical ingredient and TIC physical mixture.

Item Type: Article
Uncontrolled Keywords: Ticagrelor; L-Tartaric acid; slow evaporation method; dynamic solubility; co-crystal.
Subjects: Pharmacy > MCOPS Manipal > Pharmaceutical Chemistry
Pharmacy > MCOPS Manipal > Pharmaceutical Quality Assurance
Pharmacy > MCOPS Manipal > Pharmaceutics
Depositing User: KMC Library
Date Deposited: 24 May 2017 11:10
Last Modified: 24 May 2017 11:10
URI: http://eprints.manipal.edu/id/eprint/148938

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