Parenteral formulations of elacytarabine derivatives

摘要

The present invention relates to parenteral formulations for certain long chain saturated and monounsaturated fatty acid derivatives of 1-β-D-arabinofuranosylcytosine (cytarabine). In particular, the present invention relates to a parenteral pharmaceutical composition and a method of the preparation thereof, in order to accommodate therapeutically effective doses of the said derivatives ameliorating compliance in treatment of cancer.

主权项

1. A pharmaceutical composition, comprising a cytarabine derivative of formula I: wherein R1 and R3 are hydrogen and R2 is a C18- or C20-saturated or monounsaturated acyl group, or a pharmaceutically acceptable salt thereof as an active ingredient; wherein the active ingredient is dissolved or dispersed in a formulation comprising: a solubilizer comprising one or more phospholipids, a co-solubilizer comprising a surfactant, and an isotonicity agent selected from the group consisting of glycerol, propylene glycol, sugars, amino acids, proteins, salts and combinations thereof, wherein the formulation has a particle size between 5 nm and 45 nm.