Taxoid-based compositions

• US 5,438,072 A
• Filed: 11/22/1993
• Issued: 08/01/1995
• Est. Priority Date: 12/02/1992
• Status: Expired due to Term

• Current Assignee: Aventis Pharma SA (Sanofi )
• Original Assignee: Rhone-Poulenc Rorer S.A. (Sanofi )
• Inventors: Bobee, Jean-Marc, de Lanty, Patrick, Guerin, Gilles, Veillard, Michel
• Primary Examiner(s): Raymond, Richard L.
• Assistant Examiner(s): LAMBKIN, DEBORAH C
• Application Number:
  US08/155,543
• Time in Patent Office: 617 Days
• Field of Search: 514/449, 549/510
• US Class Current: 514/449
• CPC Class Codes: A61K 31/335 having oxygen as the only ring hetero atom, e.g. fungichromin
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• CPC Class Codes: A61K 47/44 Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14
• CPC Class Codes: A61K 9/0019 Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner non-active ingredients are additionally classified in A61K47/00
• CPC Class Codes: A61P 35/00 Antineoplastic agents

Abstract

The present invention relates to new taxoid-based compositions consisting of solutions of these derivatives in a surface-active agent.

These solutions are used for preparing perfusion solutions.

Claims

1. Injectable compositions useful for the preparation of perfusion solutions comprising taxane derivatives, wherein formation of a gelled phase during mixing of the compositions with an aqueous solution is avoided or wherein any gelled phase formed during mixing of the composition with an aqueous solution can be broken, said composition comprising a solution convenient for storage of said taxane derivatives in a surface active agent selected from polysorbates, ethylene oxide esters-ethers and fatty acids glycerides, and a water solution of an effective amount of a dilution additive selected from organic compounds having a hydroxyl group an amine functional group and a molecular weight of less than 200 or sodium chloride.

2. Injectable compositions according to claim 1, wherein the dilution additive is an amino acid.

3. Compositions according to claim 1, wherein the weight ratio between the additive and the surface-active agent is greater than 6%.

4. Compositions according to claim 1, wherein the weight ratio between the additive and the surface-agent is greater than 15%.

5. Compositions according to claim 1, wherein the additive is selected from glucose, glycerol, sorbitol, mannitol, glycine, polyethylene glycols, propylene glycol, benzyl alcohol and ethanol.

6. Compositions according to claim 1, wherein the derivative of the class of taxanes is selected from the derivatives of formula (I) ##STR2## in which R represents a hydrogen atom or an acetyl radical, the symbol R₁ represents a terbutoxycarbonylamino or benzoylamino radical.

7. Compositions according to claim 6, wherein in the compound of formula (I) R represents an acetyl group and R₁ represents a benzoylamino radical.

8. Compositions according to claim 6, wherein in the compound of formula (I) R represents hydrogen and R₁ a tert-butoxycarbonylamino radical.