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Influence of cyclodextrins on nitrosation of drugs

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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 α-, β- and γ-cyclodextrin. On the contrary, β-, γ-cyclodextrin and heptakis-2,6-di-O-methyl-β-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.

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Frömming, K.H., Wedelich, V. & Mehnert, W. Influence of cyclodextrins on nitrosation of drugs. Journal of Inclusion Phenomena 2, 605–611 (1984). https://doi.org/10.1007/BF00662226

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  • DOI: https://doi.org/10.1007/BF00662226

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