Method of using deuterated calcium channel blockers
Therapeutic methods and compositions using deuterated enriched 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylic acid 3-ethyl 5-methyl ester and other deuterated dihydropyridine compounds are described. The deuterated compounds exhibit enhanced efficacy in blocking calcium channels over non-deuterated dihydropyridines.
-
(2008/06/13)
Enhancement of the efficacy of nifedipine by deuteration
A method of enhancing the efficiency and increasing the duration of action of drugs (e.g. dihydropyridines and anti-bacterials) and particularly of nifedipine and penicillins wherein one or more hydrogen atoms are deuterated and wherein the deuterated drug has unexpectedly improved properties when used in much lower concentrations than unmodified drug. 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 isotope ratio mass spectrometry and compared with the molecular and isotope structure of a known human drug.
-
(2008/06/13)
Enhancement of pharmaceutical activity
The invention encompasses mixtures of antimicrobial agents coencapsulated in liposomes which when administered in vivo exert an enhanced therapeutic effect. The therapeutic effectiveness of the coencapsulated antimocrobial agents is greater than that of the same combination administered either in solution or as a mixture of liposome populations each containing one of the antimicrobial agents.
-
(2008/06/13)
β-lactam antibiotics
Alpha-carboxy-3-thienylmethyl penicillin having either the R- or the S- configuration at C-10 is obtained in cyrstalline form. The isomers show improved stability and higher biological activity as compared to the amorphous RS material.