Enhancement of the efficacy of dihydropyridines by deuteration

Details Enhancement of the efficacy of dihydropyridines by deuteration Enhancement of the efficacy of dihydropyridines by deuteration

C - Chemistry, Metallurgy

07

D

C07D 211/90 (2006.01) A61K 31/44 (2006.01) C07B 59/00 (2006.01) G01N 33/15 (2006.01)

Patent

CA 2186371

A method of enhancing the efficiency and increasing the duration of action of drugs (e.g. dihydropyridines) and particularly of nifedipine wherein one or more hydrogen atoms are deuterated and wherein the deuterated nifedipine has unexpectedly improved hypotensive properties when used in much lower concentrations than nifedipine per se. A method for determining the identity and bioequivalency of a new drug is also disclosed wherein the molecular and isotope structure of a new drug is determined by gas chromatography-isotope ratio mass spectrometry and compared with the molecular and isotope structure of a known human drug.

Un procédé permet de potentialiser des médicaments, des dihydropyridines, par exemple, et particulièrement la nifédipine, ainsi que d'en prolonger l'activité. Un ou plusieurs atomes d'hydrogène sont deutérés et la nifédipine ainsi deutérée présente des propriétés hypotensives étonnamment améliorées à des concentration bien plus faibles que la nifédipine elle-même. De plus un procédé qui permet de déterminer l'identité et la bioéquivalence d'un nouveau médicament recourt, pour en établir la structure moléculaire et isotopique, à la spectrométrie de masse à rapport isotopique et à la chromatographie en phase gazeuse, après quoi cette structure est comparée à la structure moléculaire et isotopique d'un médicament connu utilisé chez l'homme.

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