Melting point–solubility–structure correlations in multicomponent crystals containing fumaric or adipic acid

Batisai, Eustina; Ayamine, Alban; Kilinkissa, Ornella E. Y.; Báthori, Nikoletta B.

doi:10.1039/c4ce01298d

Cited by 56 publications

(47 citation statements)

References 34 publications

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“…Moreover, an inverse correlation between the melting points and their aqueous solubilities has also been observed (Figure ) in these multicomponent solid forms. This correlation gives an idea about their thermodynamic stability and can be attributed to significant solubility improvement in eutectic over cocrystal solid form.…”

Section: Resultsmentioning

confidence: 96%

Multicomponent solid forms of felodipine: preparation, characterisation, physicochemical and in-vivo studies

Chadha

Sharma

Haneef

2017

Journal of Pharmacy and Pharmacology

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Section: Resultsmentioning

confidence: 96%

Multicomponent solid forms of felodipine: preparation, characterisation, physicochemical and in-vivo studies

Chadha

Sharma

Haneef

2017

Journal of Pharmacy and Pharmacology

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“…It is the temperature at which solid material is at equilibrium with liquid phase [53]. The melting point of a drug is also related to its solubility, stability, tablet ability, flow property, and processability of a drug formulation.…”

Section: Melting Pointmentioning

confidence: 99%

Cocrystals: A Complete Review on Conventional and Novel Methods of Its Formation and Its Evaluation

Yadav

Khursheed

Singh

2019

Asian J Pharm Clin Res

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The active moiety with poor solubility is posing a challenge in drug development which may reduce the effectiveness in patients when administered orally. Cocrystal formation is one of the latest approaches for improving the various parameters of a drug molecule such as solubility, melting point, pharmacokinetic, pharmacodynamic, and bioavailability. Cocrystals are crystalline single state materials composed of two or more than two different molecular amalgams held together in a fixed stoichiometric ratio. There are various techniques used for the preparation of cocrystals such as solvent evaporation, grinding, and cooling crystallization. The quantitative and qualitative aspects of these cocrystals are evaluated using various validated instruments such as nuclear magnetic resonance, powder X-ray diffraction, and differential scanning calorimetry.

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“…Pure substances or solid melt at sharp meting point with narrow range 15 . Thermodynamic stability of any API can be govern by its meting point so utility of high melting point conformer for its better stability and also useful in case of thermolabile drugs, so selection of conformer is very important in case of synthesis of cocrystals 16 . Differential scanning calorimetry (DSC) and thermal gravimetric analysis (TGA) are most common techniques used to determine melting point.…”

Section: Melting Pointmentioning

confidence: 99%

Co-Crystals: A Review

Chaudhari¹,

Nikam

Khatri³

et al. 2018

J. Drug Delivery Ther.

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In development of new product major constraints are poor aqueous solubility and low oral bioavailability. Crystallization is one the approach has been used for enhancement of solubility of poorly aqueous soluble drugs also helps to improve physicochemical properties such as melting point, tabletability, solubility, stability, bioavailability and permeability with preserving the pharmacological properties of the active pharmaceutical ingredient. Different methods have been used for the synthesis of cocrystal such as grinding, slurry, antisolvent, hot melt extrusion, sonocrystallization, supercritical fluid, spray drying etc. The article highlights the co-crystallization, its methods and significance.

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Melting point–solubility–structure correlations in multicomponent crystals containing fumaric or adipic acid

Abstract: The relationships between the melting point, solubility and structure was investigated in a series of multicomponent crystals of fumaric and adipic acid.

Cited by 56 publications

References 34 publications

Multicomponent solid forms of felodipine: preparation, characterisation, physicochemical and in-vivo studies

Multicomponent solid forms of felodipine: preparation, characterisation, physicochemical and in-vivo studies

Cocrystals: A Complete Review on Conventional and Novel Methods of Its Formation and Its Evaluation

Co-Crystals: A Review

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