TY - JOUR
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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M3 - Article
AN - SCOPUS:85075626160
SN - 0326-2383
VL - 38
SP - 2051
EP - 2056
JO - Latin American Journal of Pharmacy
JF - Latin American Journal of Pharmacy
IS - 10
ER -