Method for stabilizing duocarmycin derivatives

Details Method for stabilizing duocarmycin derivatives Method for stabilizing duocarmycin derivatives

A - Human Necessities

61

K

A61K 31/495 (2006.01) A61K 9/14 (2006.01) A61K 9/19 (2006.01) A61K 31/496 (2006.01) A61K 47/02 (2006.01) A61K 47/26 (2006.01)

Patent

CA 2190635

Stabilized duocarmycin derivatives represented by formula (I), wherein R is lower alkyl, allyl or benzyl, and X is Cl or Br, are prepared by adding at least a compound selected from the group consisting of a saccharide, an electolyte, a water-soluble polymer, a polyhydric alcohol and a surfactant to a solution containing the duocarmycin derivatives. Also provided are freeze-dried pharmaceutical preparations containing the stabilized duocarmycin derivatives.

L'invention concerne des dérivés de la duocarmycine stabilisés représentés par la formule (I). Dans cette formule, R représente un alkyle inférieur, un allyle ou un benzyle et X représente Cl ou Br. Ces dérivés sont préparés par l'addition d'au moins un composé choisi dans le groupe constitué par un saccharide, un électrolyte, un polymère hydrosoluble, un alcool polyhydrique et un tensioactif, à une solution contenant les dérivés de la duocarmycine. On décrit également des préparations pharmaceutiques lyophilisées contenant les dérivés stabilisés de la duocarmycine.

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