Abstract

In this study a new co-crystal of ticagrelor with quercetin has been fabricated 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 active pharmaceutical ingredient and the co-former in definite stoichiometric amounts. In this study the conformer selected was quercetin based on ease of hydrogen bond formation and also as quercetin will provide a synergistic effect with ticagrelor. The co-crystal of ticagrelor with quercetin was prepared in two ratios (1:1, 2:1). Ticagrelor formed stable co-crystals in the ratios 1:1 and 2:1. The formation of co-crystal was confirmed by PXRD, DSC, and FTIR. The dynamic solubility of co-crystals in the ratios 1:1 and 2:1 increased by approximately 1.6 fold as compared to pure drug.

Original languageEnglish
Pages (from-to)2051-2056
Number of pages6
JournalLatin American Journal of Pharmacy
Volume38
Issue number10
Publication statusPublished - 01-01-2019

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Solubility
Quercetin
Technology
Pharmaceutical Preparations
Fourier Transform Infrared Spectroscopy
Crystallization
Hydrogen
Permeability
Ticagrelor

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science
  • Drug Discovery

Cite this

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title = "Solubility enhancement of ticagrelor by co-crystal technology: Preparation, solid state characterization and solubility studies",
abstract = "In this study a new co-crystal of ticagrelor with quercetin has been fabricated 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 active pharmaceutical ingredient and the co-former in definite stoichiometric amounts. In this study the conformer selected was quercetin based on ease of hydrogen bond formation and also as quercetin will provide a synergistic effect with ticagrelor. The co-crystal of ticagrelor with quercetin was prepared in two ratios (1:1, 2:1). Ticagrelor formed stable co-crystals in the ratios 1:1 and 2:1. The formation of co-crystal was confirmed by PXRD, DSC, and FTIR. The dynamic solubility of co-crystals in the ratios 1:1 and 2:1 increased by approximately 1.6 fold as compared to pure drug.",
author = "Shane, {Nazare L.J.} and Aravind Pai and Girish Pai and Vasudev Pai and Vasanthraju Sg and Sathyanarayana, {Muddukrishna B.}",
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Solubility enhancement of ticagrelor by co-crystal technology : Preparation, solid state characterization and solubility studies. / Shane, Nazare L.J.; Pai, Aravind; Pai, Girish; Pai, Vasudev; Sg, Vasanthraju; Sathyanarayana, Muddukrishna B.

In: Latin American Journal of Pharmacy, Vol. 38, No. 10, 01.01.2019, p. 2051-2056.

Research output: Contribution to journalArticle

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T1 - Solubility enhancement of ticagrelor by co-crystal technology

T2 - Preparation, solid state characterization and solubility studies

AU - Shane, Nazare L.J.

AU - Pai, Aravind

AU - Pai, Girish

AU - Pai, Vasudev

AU - Sg, Vasanthraju

AU - Sathyanarayana, Muddukrishna B.

PY - 2019/1/1

Y1 - 2019/1/1

N2 - In this study a new co-crystal of ticagrelor with quercetin has been fabricated 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 active pharmaceutical ingredient and the co-former in definite stoichiometric amounts. In this study the conformer selected was quercetin based on ease of hydrogen bond formation and also as quercetin will provide a synergistic effect with ticagrelor. The co-crystal of ticagrelor with quercetin was prepared in two ratios (1:1, 2:1). Ticagrelor formed stable co-crystals in the ratios 1:1 and 2:1. The formation of co-crystal was confirmed by PXRD, DSC, and FTIR. The dynamic solubility of co-crystals in the ratios 1:1 and 2:1 increased by approximately 1.6 fold as compared to pure drug.

AB - In this study a new co-crystal of ticagrelor with quercetin has been fabricated 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 active pharmaceutical ingredient and the co-former in definite stoichiometric amounts. In this study the conformer selected was quercetin based on ease of hydrogen bond formation and also as quercetin will provide a synergistic effect with ticagrelor. The co-crystal of ticagrelor with quercetin was prepared in two ratios (1:1, 2:1). Ticagrelor formed stable co-crystals in the ratios 1:1 and 2:1. The formation of co-crystal was confirmed by PXRD, DSC, and FTIR. The dynamic solubility of co-crystals in the ratios 1:1 and 2:1 increased by approximately 1.6 fold as compared to pure drug.

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