scholarly journals Anticrystal Engineering of Ketoprofen and Ester Local Anesthetics: Ionic Liquids or Deep Eutectic Mixtures?

Pharmaceutics ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 368 ◽  
Author(s):  
Anita Umerska ◽  
Klaudia Bialek ◽  
Julija Zotova ◽  
Marcin Skotnicki ◽  
Lidia Tajber
Keyword(s):  
Ionic Liquids ◽  
Supercooled Liquids ◽  
Glass Forming Ability ◽  
Molar Ratios ◽  
Glass Forming ◽  
Eutectic Mixtures ◽  
Carboxylate Anions ◽  
Quench Cooling ◽  
Crystallization Tendency ◽  
Low Solubility

Ionic liquids (ILs) and deep eutectic mixtures (DEMs) are potential solutions to the problems of low solubility, polymorphism, and low bioavailability of drugs. The aim of this work was to develop and investigate ketoprofen (KET)-based ILs/DEMs containing an ester local anesthetic (LA): benzocaine (BEN), procaine (PRO) and tetracaine (TET) as the second component. ILs/DEMs were prepared via a mechanosynthetic process that involved the mixing of KET with an LA in a range of molar ratios and applying a thermal treatment. After heating above the melting point and quench cooling, the formation of supercooled liquids with Tgs that were dependent on the composition was observed for all KET-LA mixtures with exception of that containing 95 mol% of BEN. The KET-LA mixtures containing either ≥ 60 mol% BEN or 95 mol% of TET showed crystallization to BEN and TET, respectively, during either cooling or second heating. KET decreased the crystallization tendency of BEN and TET and increased their glass-forming ability. The KET-PRO systems showed good glass-forming ability and did not crystallize either during the cooling or during the second heating cycle irrespective of the composition. Infrared spectroscopy and molecular modeling indicated that KET and LAs formed DEMs, but in the KET-PRO systems small quantities of carboxylate anions were present.

scholarly journals Influence of Carboxylate Anions on Phase Behavior of Choline Ionic Liquid Mixtures

Molecules ◽  
2020 ◽  
Vol 25 (7) ◽  
pp. 1691 ◽  
Author(s):  
Fred Elhi ◽  
Mikhail Gantman ◽  
Gunnar Nurk ◽  
Peter S. Schulz ◽  
Peter Wasserscheid ◽  
...  
Keyword(s):  
Ionic Liquids ◽  
Liquid Mixtures ◽  
Melting Point Depression ◽  
Melting Points ◽  
Thermal Stabilities ◽  
Application Range ◽  
Practical Applications ◽  
Eutectic Mixtures ◽  
Carboxylate Anions ◽  
Pure Compounds

Mixing ionic liquids is a suitable strategy to tailor properties, e.g., to reduce melting points. The present study aims to widen the application range of low-toxic choline-based ionic liquids by studying eight binary phase diagrams of six different choline carboxylates. Five of them show eutectic points with melting points dropping by 13 to 45 °C. The eutectic mixtures of choline acetate and choline 2-methylbutarate were found to melt at 45 °C, which represents a remarkable melting point depression compared to the pure compounds with melting points of 81 (choline acetate) and 90 °C (choline 2-methylbutarate), respectively. Besides melting points, the thermal stabilities of the choline salt mixtures were investigated to define the thermal operation range for potential practical applications of these mixtures. Typical decomposition temperatures were found between 165 and 207 °C, with choline lactate exhibiting the highest thermal stability.

Crystal packing and crystallization tendency from the melt of 2-((2-ethylphenyl)amino)nicotinic acid

2018 ◽  
Vol 233 (1) ◽  
pp. 9-16 ◽  
Author(s):  
Arjun Kalra ◽  
Mingtao Zhang ◽  
Sean Parkin ◽  
Tonglei Li
Keyword(s):  
Nicotinic Acid ◽  
Crystal Packing ◽  
Amorphous State ◽  
Glass Forming Ability ◽  
Melt Quenching ◽  
Scanning Calorimetry ◽  
Glass Forming ◽  
Planar Conformation ◽  
Acid Acid ◽  
Crystallization Tendency

Abstract2-((2-ethylphenyl)amino)nicotinic acid (2EPNA) was synthesized and its crystal structure was determined. It was observed that alkylation of the phenyl ring with ethyl group disrupts the planar conformation of the molecule by steric repulsion, resulting in formation of an acid-pyridine heterosynthon (instead of acid-acid homosynthon) in the crystal. Crystallization tendency from the melt state of the polymorph was studied by differential scanning calorimetry (DSC). It was revealed that this compound could form a very stable amorphous phase on melt quenching and not crystallize even on re-heating. The formation of acid-pyridine hydrogen bonding in the amorphous state is believed to be responsible for its good glass forming ability.

scholarly journals Computational Predictions of Glass-Forming Ability and Crystallization Tendency of Drug Molecules

2014 ◽  
Vol 11 (9) ◽  
pp. 3123-3132 ◽  
Author(s):  
Amjad Alhalaweh ◽  
Ahmad Alzghoul ◽  
Waseem Kaialy ◽  
Denny Mahlin ◽  
Christel A. S. Bergström
Keyword(s):  
Glass Forming Ability ◽  
Glass Forming ◽  
Drug Molecules ◽  
Crystallization Tendency ◽  
Computational Predictions

Crystallization and Glass-Forming Ability of Ionic Liquids: Novel Insights into Their Thermal Behavior

2019 ◽  
Vol 7 (3) ◽  
pp. 2989-2997 ◽  
Author(s):  
Ana I. M. C. Lobo Ferreira ◽  
Ana S. M. C. Rodrigues ◽  
Miguel Villas ◽  
Emília Tojo ◽  
Luís Paulo N. Rebelo ◽  
...  
Keyword(s):  
Ionic Liquids ◽  
Thermal Behavior ◽  
Glass Forming Ability ◽  
Glass Forming

Green Chemistry and Green Solvents: An Overview

2020 ◽  
Vol 7 (3) ◽  
pp. 314-325
Author(s):  
Barla Karuna Devi ◽  
Swathi Naraparaju ◽  
Chaganti Soujanya ◽  
Sayan Dutta Gupta
Keyword(s):  
Ionic Liquids ◽  
Green Chemistry ◽  
Chemical Reaction ◽  
Supercritical Co2 ◽  
Environmental Problems ◽  
Green Solvents ◽  
Eutectic Mixtures ◽  
Organic Carbonates

: Green chemistry emphasizes designing novel routes to overcome health and environmental problems that occur during a chemical reaction. Green solvents are used in place of conventional solvents that are hazardous to both human and the environment. Solvents like water, ionic liquids, supercritical CO2, biosolvents, organic carbonates, and deep eutectic mixtures can be used as green solvents. The review focuses on the properties, applications, and limitations of these solvents.

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