Hydrolysis of oxaliplatin—evaluation of the acid dissociation constant for the oxalato monodentate complex

Authors

  • Elin Jerremalm,

    1. Karolinska Pharmacy, Karolinska Hospital, SE-171 76 Stockholm, Sweden
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  • Staffan Eksborg,

    1. Karolinska Pharmacy, Karolinska Hospital, SE-171 76 Stockholm, Sweden
    2. Department of Woman and Child Health, Karolinska Institutet, Stockholm, Sweden
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  • Hans Ehrsson

    Corresponding author
    1. Karolinska Pharmacy, Karolinska Hospital, SE-171 76 Stockholm, Sweden
    2. Department of Oncology-Pathology, Karolinska Institutet, Stockholm, Sweden
    • Karolinska Pharmacy, Karolinska Hospital, SE-171 76 Stockholm, Sweden. Telephone: 46-8-51775326; Fax: 46-8-307346
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Abstract

Alkaline hydrolysis of the platinum anticancer drug oxaliplatin gives the oxalato monodentate complex and the dihydrated oxaliplatin complex in two consecutive steps. The acid dissociation constant for the oxalato monodentate intermediate was determined by a kinetic approach. The pKa value was estimated as 7.23. The monodentate intermediate is assumed to rapidly react with endogenous compounds, resulting in a continuous conversion of oxaliplatin via the monodentate form. © 2003 Wiley-Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 92:436–438, 2003

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