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US 8,912,162 B2Granted
Parenteral formulations of elacytarabine derivatives
AssigneeClavis Pharma Asa
InventorsSayeh Ahrabi, Finn Myhren, Ole Henrik Eriksen
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Abstract
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.
Claims18
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.
3 more elements
Dependencies are inferred from the claim text.