Vibrational study of polymorphism of tetralin derivative for treatment of cardiovascular diseases.
Vibrational spectroscopy coupled with thermogravimetry (TG) and differential scanning calorimetry (DSC) was used to characterize racemic propanoic acid, 2-methyl-5,6,7,8-tetrahydro-6-(methylamino)-1,2-naphthalenediyl ester hydrochloride (CHF-1035), which is a new DA2 dopaminergic receptor/alpha2 agonist and beta blocker under clinical investigation for the treatment of congestive heart failure. Raman spectroscopy disclosed at least two different CHF-1035 polymorphs; the marker bands characteristic of each form were identified. The modifications undergone by the CHF-1035 drug as a consequence of grinding and heating were investigated. Mechanical and gentle thermal treatments caused a polymorphic transformation of the drug crystal form. Raman spectroscopy proved suitable for investigating the possible presence of different polymorphic forms, their relative stability, and interconversion tendency in relation to industrial manufacturing processes undergone by the drug (i.e., grinding, compression, and heating).
Taddei
Paola
P
Dipartimento di Biochimica G. Moruzzi, Sezione di Chimica e Propedeutica Biochimica, University of Bologna, Via Belmeloro 8/2, 40126, Italy.
Torreggiani
Armida
A
Fini
Giancarlo
G
D002152:Calorimetry, Differential Scanning; D002318:Cardiovascular Diseases / Q000378:metabolism / Q000628:therapy*; D004952:Esters / Q000737:chemistry* / Q000378:metabolism*; D006801:Humans; D008956:Models, Chemical; D011110:Polymorphism, Genetic; D011487:Protein Conformation; D017366:Serotonin Receptor Agonists / Q000737:chemistry; D013053:Spectrophotometry; D013696:Temperature; D013764:Tetrahydronaphthalenes / Q000737:chemistry* / Q000378:metabolism*
D004952:Esters; D017366:Serotonin Receptor Agonists; D013764:Tetrahydronaphthalenes; C457559:nolomirole; C095210:tetralin