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Influence of cyclodextrins on nitrosation of drugs
Authors:K -H Frömming  V Wedelich  W Mehnert
Institution:(1) Pharmaceutical Institute of the Free University of Berlin, Königin-Luise-Str. 2+4, 1000 Berlin 33, FRG
Abstract:The World Health Organization issued a nitrosation procedure (NAP Test) which allows to carry out nitrosation under standard conditions. It has proved that the in vitro reaction rates of the fast nitrosatable drugs piperazine, cimetidine and ethambutol are not influenced by agr-, beta- and gamma-cyclodextrin. On the contrary, beta-, gamma-cyclodextrin and heptakis-2,6-di-O-methyl-beta-cyclodextrin enhance the nitrosation of the slower nitrosatable 1-ephedrine and fencamfamine significantly. This possible reaction must be considered if nitrosatable drugs are formulated with cyclodextrins to be administered to human beings.
Keywords:Nitrosation reactions: agr-" target="_blank">gif" alt="agr" align="BASELINE" BORDER="0">-  beta-" target="_blank">gif" alt="beta" align="MIDDLE" BORDER="0">-  gamma-cyclodextrin" target="_blank">gif" alt="gamma" align="MIDDLE" BORDER="0">-cyclodextrin  dimethyl-beta-cyclodextrin" target="_blank">gif" alt="beta" align="MIDDLE" BORDER="0">-cyclodextrin  piperazine  ethambutol  cimetidine  1-ephedrine  fencamfamine
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