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Last Updated: April 18, 2024

Claims for Patent: 5,403,858


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Summary for Patent: 5,403,858
Title: New compositions containing taxane derivatives
Abstract:Compositions containing taxane derivatives, consist of a solution of such derivative in a surfactant consisting of polysorbate, polyethelene glycol or hydrogenated castor oil. These compositions can be used to prepare perfusion solutions essentially free of ethanol.
Inventor(s): Bastard; Jean-Pierre (Lesigny, FR), Dupechez; Thierry (Villemoisson sur Orge, FR), Fabre; Jean-Louis (Paris, FR)
Assignee: Rhone-Poulenc Rorer, S.A. (Antony, FR)
Application Number:07/930,392
Patent Claims: 1. A composition consisting essentially of a compound of formula: ##STR2## in which R represents a hydrogen atom or an acetyl radical and R.sub.1 represents a tert-butoxycarbonylamino or benzoylamino radical, dissolved in a surfactant selected from the group consisting of polysorbate, polyoxyethylene glycol and hydrogenated castor oil, and essentially free of ethanol.

2. A composition according to claim 1, which contains less than 5% by volume of ethanol.

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

4. A composition according to claim 1, wherein, in the compound of formula (I), R represents an acetyl group and R.sub.1 represents a benzoyloxyamino radical.

5. A composition according to claim 1, which contains up to 200 mg/ml of compound of formula (I).

6. A composition according to claim 3, which contains 20 to 80 mg/ml of compound of formula (I).

7. A composition according to claim 4, which contains 6 to 20 mg/ml of compound of formula (I).

8. A composition according to claim 2, wherein the composition contains less than 2% of ethanol.

9. A composition according to claim 5, which contains up to 80 mg/ml of compound of formula (I).

10. Composition consisting essentially of a taxane derivative of the formula: ##STR3## in which R represents a hydrogen atom or an acetyl radical and R.sub.1 represents a tert-butoxycarbonylamino or benzoylamino radical dissolved in a surfactant selected from the group consisting of polysorbate, polyoxyethylene glycol and hydrogenated castor oil, said composition containing less than 5% by volume ethanol.

11. Composition according to claim 10, wherein ethanol is less than 2% by volume.

12. A perfusion comprising less than 0.5 mg/ml of compound as defined in claim 3 and less than 1 ml/l of ethanol and less than 15 ml/l of surfactant.

13. A perfusion, comprising 1 mg/ml or less of compound as defined in claim 4 and less than 1 ml/l of ethanol.

14. A perfusion according to claim 12, wherein the perfusion contains 0.1 to 0.3 mg/ml of a compound of formula (I) wherein R represents hydrogen and R.sub.1 represents a tert-butoxycarbonylamino radical.

15. A method for preparing a composition according to claim 1, which comprises dissolving a compound of formula (I) in ethanol, adding the surfactant and removing the ethanol.

16. A method for preparing a composition according to claim 1, which comprises slowly adding a compound of formula (I) to a solution of the surfactant containing 1 to 2% by volume of ethanol.

17. A method for preparing a composition according to claim 15, wherein ethanol is removed by evaporation.

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