Patent EA-005314-B1 (EA)
Title: Pharmaceutical dronedarone composition for parenteral administration
Inventor: BOURRIAGUE-SEVE FREDERIQUE
IPC: A61K9/00
Filed: 2001-12-10
Abstract: 1. Pharmaceutical composition for parenteral administration, characterized in that it comprises: dronedarone or one of its pharmaceutically acceptable salts as active principle, a physiologically acceptable buffer solution capable of maintaining the pH of the composition between 3 and 5, a physiologically acceptable water-soluble [beta]-cyclodextrin derivative. 2. Pharmaceutical composition according to claim 1, characterized in that it comprises from 0.01% to 4% of active principle. 3. Pharmaceutical composition according to claim 2, characterized in that it comprises from 0.4 to 0.8% of active principle. 4. Pharmaceutical composition according to one of claims 1 to 3, characterized in that the buffer solution is an aqueous solution comprising a buffer system chosen from the following: acetic acid/alkali metal acetate, fumaric acid/alkali metal fumarate, succinic acid/alkali metal succinate, citric acid/alkali metal citrate, tartaric acid/alkali metal tartrate, lactic acid/alkali metal lactate, maleic acid/alkali metal maleate, methanesulphonic acid/alkali metal methanesulphonate, monoalkali metal phosphate. 5. Pharmaceutical composition according to claim 4, characterized in that the buffer system is a monoalkali metal phosphate. 6. Pharmaceutical composition according to claim 4, characterized in that the monoalkali metal phosphate buffer solution maintains the pH at 4.5. 7. Pharmaceutical composition according to one of claims 1 to 6, characterized in that the ionic strength of the buffer solution is between 0.005 molar and 0.5 molar. 8. Pharmaceutical composition according to claim 7, characterized in that the ionic strength of the buffer solution is between 0.01 molar and 0.2 molar. 9. Pharmaceutical composition according to claim 7 or 8, characterized in that the ionic strength of the buffer solution is between 0.05 and 0.15 molar. 10. Pharmaceutical composition according to claims 1 to 9, characterized in that the buffer solution is a 0.05 to 0.15 molar aqueous solution of monoalkali metal phosphate. 11. Pharmaceutical composition according to claim 4, 5, 6 or 10, characterized in that the alkali metal is sodium or potassium. 12. Pharmaceutical composition according to one of claims 1 to 11, characterized in that the water-soluble [beta]-cyclodextrin derivative is chosen from hydroxypropyl-[beta]-cyclodextrin, the sulphobutyl ether derivative of [beta]-cyclodextrin, dimethyl-[beta]-cyclodextrin, trimethyl-[beta]-cyclodextrin, and their mixtures. 13. Pharmaceutical composition according to one of claims 1 to 12, characterized in that the water-soluble [beta]-cyclodextrin derivative is hydroxypropyl-[beta]-cyclodextrin. 14. Pharmaceutical composition according to one of claims 1 to 13, characterized in that the water-soluble [beta]-cyclodextrin derivative is present in a proportion of 0.5 to 50%. 15. Pharmaceutical composition according to one of claims 1 to 14, characterized in that the water-soluble [beta]-cyclodextrin derivative is present in a proportion of 5 to 20 times the weight of dronedarone or of one of its pharmaceutically acceptable salts. 16. Pharmaceutical composition according to claim 15, characterized in that the water-soluble [beta]-cyclodextrin derivative is present in a proportion of 12 to 13 times the weight of dronedarone or of one of its pharmaceutically acceptable salts. 17. Pharmaceutical composition according to one of claims 1 to 16, characterized in that it additionally comprises a preservative or a protective agent. 18. Pharmaceutical composition according to one of claims 1 to 17, characterized in that it additionally comprises a compound which makes it possible to maintain the isotonicity. 19. Pharmaceutical composition according to one of claims 1 to 18, characterized in that the active principle is dronedarone hydrochloride.