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Publikācija: Crystal Structures and Physicochemical Properties of Diltiazem Base

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Publikācijas valoda English (en)
Nosaukums oriģinālvalodā Crystal Structures and Physicochemical Properties of Diltiazem Base, Acetylsalicylate, Nicotinate and L-Malate
Pētniecības nozare 1. Dabaszinātnes
Pētniecības apakšnozare 1.4. Ķīmija
Autori Dmitrijs Stepanovs
Māra Jure
Marina Gosteva
Yuris Popelis
Glebs Kiselovs
Anatolijs Mišņovs
Atslēgas vārdi Crystal structures and physicochemical properties of diltiazem base, acetylsalicylate, nicotinate and L-malate
Anotācija Diltiazem is a drug used as a calcium channel blocker in the treatment of cardiovascular disorders. Because of poor aqueous solubility of the drug, hydrochloride salt has been marketed. Due to the short elimination half-life of diltiazem, extended-release formulations were developed. In the present work, the crystal engineering approach has been employed to obtain diltiazem forms with lower water solubility by treating with carboxylic acids. Three molecular salts of diltiazem with aspirin, niacin and L-malic acid were synthesized and characterized by a single crystal and powder XRD, DTA, solid state CP-MAS, NMR and UV/vis techniques. The single crystal structure determination allowed us to study supramolecular structures and proton transfer interactions from carboxylic acids to diltiazem in the solid state, while NMR studies – interaction in solution. In crystal, the N,N-(dimethyl)ethylamine fragment of the drug molecule interacts with carboxylic groups of the acids to form heterosynthons. The maximum 40-fold decrease of aqueous solubility is achieved for diltiazem acetylsalicylate hydrate in comparison with the solubility of diltiazem hydrochloride.
DOI: 10.1039/C5CE01204J
Hipersaite: http://pubs.rsc.org/en/content/articlelanding/2016/ce/c5ce01204j#!divAbstract 
Atsauce Stepanovs, D., Jure, M., Gosteva, M., Popelis, Y., Kiselovs, G., Mišņovs, A. Crystal Structures and Physicochemical Properties of Diltiazem Base, Acetylsalicylate, Nicotinate and L-Malate. CrystEngComm, 2016, Vol.18, Iss.7, 1235.-1241.lpp. ISSN 1499-8033. Pieejams: doi:10.1039/C5CE01204J
Papildinformācija Citējamību skaits:
ID 21738