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Claims for Patent: 5,438,072

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Claims for Patent: 5,438,072

Title: Taxoid-based compositions
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.
Inventor(s): Bobee; Jean-Marc (Verrieres-le-Buisson, FR), de Lanty; Patrick (Paris, FR), Guerin; Gilles (Eaubonne, FR), Veillard; Michel (Sceaux, FR)
Assignee: Rhone-Poulenc Rorer S.A. (Antony Cedex, FR)
Application Number:08/155,543
Patent 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 R.sub.1 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 R.sub.1 represents a benzoylamino radical.

8. Compositions according to claim 6, wherein in the compound of formula (I) R represents hydrogen and R.sub.1 a tert-butoxycarbonylamino radical.
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