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Establishment of cocrystal cocktail grinding method for rational screening of pharmaceutical cocrystals

International Journal of Pharmaceutics, 2012
Cocrystals (CCs) used in the pharmaceutical industry are defined as complex crystals formed by reaction between an API and a cocrystal former (CCF); unlike salts, CCs do not show proton transfer. Recently, pharmaceutical CCs have been used to improve the drug-likeness of APIs, such as solubility and stability.
Katsuhiko, Yamamoto   +2 more
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On the thermodynamics of cocrystal formation

International Journal of Pharmaceutics, 2009
The thermodynamics underpinning cocrystal formation are derived. The results provide the pharmaceutical scientist with the foundation to experimentally assess the thermodynamic stability of a cocrystal with respect to its component forms. Data for the carbamazepine-nicotinamide system are discussed as an example.
openaire   +2 more sources

Three cocrystals and a cocrystal salt of pyrimidin-2-amine and glutaric acid

Acta Crystallographica Section C Structural Chemistry, 2015
Four new cocrystals of pyrimidin-2-amine and propane-1,3-dicarboxylic (glutaric) acid were crystallized from three different solvents (acetonitrile, methanol and a 50:50 wt% mixture of methanol and chloroform) and their crystal structures determined. Two of the cocrystals, namely pyrimidin-2-amine–glutaric acid (1/1), C4H5N3·C6H8O4, (I) and (II), are ...
Isaac, Odiase   +5 more
openaire   +2 more sources

Polymorphs and Polymorphic Cocrystals of Temozolomide

Chemistry – An Asian Journal, 2008
AbstractCrystal polymorphism in the antitumor drug temozolomide (TMZ), cocrystals of TMZ with 4,4′‐bipyridine‐N,N′‐dioxide (BPNO), and solid‐state stability were studied. Apart from a known X‐ray crystal structure of TMZ (form 1), two new crystalline modifications, forms 2 and 3, were obtained during attempted cocrystallization with carbamazepine and 3‐
N Jagadeesh, Babu   +3 more
openaire   +2 more sources

Five pseudopolymorphs and a cocrystal of nitrofurantoin

Acta Crystallographica Section C Crystal Structure Communications, 2010
The antibiotic nitrofurantoin {systematic name: (E)-1-[(5-nitro-2-furyl)methylideneamino]imidazolidine-2,4-dione} is not only used for the treatment of urinary tract infections, but also illegally applied as an animal food additive. Since derivatives of 2,6-diaminopyridine might serve as artificial receptors for its recognition, we crystallized one ...
Maya, Tutughamiarso   +3 more
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Cocrystals and Salts of Gabapentin: pH Dependent Cocrystal Stability and Solubility

Crystal Growth & Design, 2008
Thirteen new multicomponent crystals (cocrystals and salts) of an anticonvulsant drug gabapentin with various carboxylic acid coformers have been discovered using the reaction crystallization method (RCM). These new forms are characterized by X-ray powder diffraction (XRPD), Raman and infrared spectroscopy, and differential scanning calorimetry (DSC ...
L. Sreenivas Reddy   +3 more
openaire   +1 more source

Chrysin cocrystals: Characterization and evaluation

Journal of Pharmaceutical and Biomedical Analysis, 2017
Solvent free mechanochemical approach is utilized to synthesise new cocrystals of chrysin using supramolecular chemistry based upon reliable synthons. Chrysin, a flavone nutraceutical with wide range of beneficial effects has critically low bioavailability on account of its poor aqueous solubility and consequently poor absorption from the ...
Renu, Chadha   +4 more
openaire   +2 more sources

A melt castable energetic cocrystal

Chemical Communications, 2017
Cocrystallization leads to melt-state stabilization of the thermally unstable energetic 4-amino-3,5-dinitropyrazole, allowing for production of a melt castable cocrystalline explosive.
Jonathan C. Bennion   +2 more
openaire   +2 more sources

Furosemide Cocrystals with Pyridines: An Interesting Case of Color Cocrystal Polymorphism

Crystal Growth & Design, 2015
Furosemide (FS), a loop diuretic drug commonly used for the treatment of hypertension and edema, exhibited color cocrystal polymorphism with coformer 4,4′-bipyridine (4BPY) in the stoichiometry 2:1, albeit both the API and the cocrystal former are colorless.
Ekta Sangtani   +6 more
openaire   +1 more source

Understanding and Predicting the Effect of Cocrystal Components and pH on Cocrystal Solubility

Crystal Growth & Design, 2009
Understanding how cocrystal solubility−pH dependence is affected by cocrystal components is important to engineer cocrystals with customized solubility behavior. Equations that describe cocrystal solubility in terms of solubility product, cocrystal component ionization constants, and solution pH are derived for cocrystals with acidic, basic, amphoteric,
Sarah J. Bethune   +3 more
openaire   +1 more source

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