What is the difference between Cocrystal and salt?
LTG-NCT cocrystal is more soluble than drug at pH > 3 and reaches solubilities 18 times the drug solubility at pH ≥ 6. The cocrystal is also more soluble than the SAC salt at pH < 7, and is orders of magnitude more soluble than the salt at pH < 3.
What is the difference between crystal and Cocrystal?
The difference between a crystalline salt and a cocrystal lies merely in the transfer of a proton. The transfer of protons from one component to another in a crystal is dependent on the environment.
What are Coformers?
Cocrystals are multicomponent system in which one component is Active Pharmaceutical Ingredient (API) and another is called coformer. So coformer selection is one of the main challenge in cocrystal development which is compatible with API.
Is a Cocrystal a salt?
If so, the above definition might be modified as follows: cocrystals are solids that are crystalline single phase materials composed of two or more different molecular and/or ionic compounds generally in a stoichiometric ratio which are neither solvates nor simple salts.
What are solvates with example?
A solvate is a compound that forms between a solute and its solvent. Hydrates: A wide range of salts form hydrates when dissolved in water. The liquid water can then be evaporated to leave the solid hydrate. For example, ferrous chloride FeCl2 forms the hydrate FeCl2(H2O)4.
What are conformers and regulators?
Conformers- The body of the organism depends upon the changes in its external environment. Regulators- The organisms are capable of controlling their internal environment irrespective of their external surroundings to an extent.
How do cocrystals facilitate a reaction?
The mechanism by which cocrystals go into solution involves three main steps: (1) breaking intermolecular bonds in the cocrystal, (2) breaking intermolecular bonds in the solvent, and (3) forming intermolecular bonds between cocrystal molecules and solvent molecules.
What is co crystallized ligand?
One of the common methods of obtaining crystals of a protein–ligand complex is cocrystallization, where the ligand is added to the protein to form a complex that is subsequently used in crystallization trials. This is often the method of choice when the compounds are quite insoluble or the protein aggregates easily.
How do you identify solvates?
Hydrates and solvates can be prepared by crystallization in water or an organic solvent or by conversion of the anhydrous material through moisture or solvent adsorption. In quality control testing, hydrates or solvates are identified by the assay of water of crystallization or solvent found in the crystal.
What is a conformer?
A conformer is an isomer of a molecule that differs from another isomer by the rotation of a single bond in the molecule. A conformer is also known as a conformational isomer. The isomers that are formed are known as conformation.
What is an example of a conformer?
Conformers are referred to as cold-blooded animals. Examples of this class – amphibians, reptiles, insects etc.
How do cocrystals increase solubility?
In contrast to amorphous pharmaceutical forms, cocrystals can achieve thermodynamic stability in the solid state while providing large solubility advantage over drug. Compared to polymorphs, cocrystals have the ability to increase solubility by orders of magnitude above the drug solubility.
What is co crystallisation?
Co-crystallization is a process by which the molecular interactions can be altered to optimize the drug properties. Co-crystals comprise a multicomponent system of active pharmaceutical ingredient (API) with a stoichiometric amount of a pharmaceutically acceptable coformer incorporated in the crystal lattice.
How do Cocrystals facilitate a reaction?
What is conformer chemistry?
A conformer is a conformation of a molecule that lies at an energy minimum in a potential energy diagram. eg: Shown below is the potential energy diagram of conformations of ethane.
What is conformation in chemistry?
conformation, any one of the infinite number of possible spatial arrangements of atoms in a molecule that result from rotation of its constituent groups of atoms about single bonds.
What is the difference between salts and cocrystals?
Salts and cocrystals are multicomponent crystals that can be distinguished by the location of the proton between an acid and a base. At the salt end of the spectrum proton transfer is complete, and on the opposite end proton transfer is absent in cocrystals.
What is a cocrystal?
The following definition of cocrystals was proposed by the FDA in the draft guidance: Solids that are crystalline materials composed of two or more molecules in the same crystal lattice.
Why is melting behavior important when selecting a salt or cocrystal?
Also, the melting behavior is particularly important when selecting a salt or cocrystal for a drug product, since processing steps, such as milling or micronization, can generate considerable heat which not all salt and cocrystal forms are equally able to tolerate.
What are the sub-groups of cocrystals?
An interesting sub-group of cocrystals is the one composed of charged cocrystal systems, namely salt cocrystals (SCCs) [9], [10], [11], ionic cocrystals (ICCs) [12], [13], [14], [15], [16], [17], and zwitterionic cocrystals [18], [19].
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