TH81540A - Pharmaceutical compounds of vinflune for non-gastrointestinal administration, preparation process and use of this compound. - Google Patents

Abstract

DC60 (21/03/48) This invention relates to a pharmaceutical mixture of vinflunine, in the form of a stable and sterile aqueous solution of water-soluble vinflunine salts at pH between 3 and 4. This invention also relates to the process for preparing this mixture and to its use as a pharmaceutical product for non-intestinal administration in the treatment of cancer. This invention relates to a pharmaceutical mixture of vinflunine, in the form of a stable and sterile aqueous solution of water-soluble vinflunine salts at pH between 3 and 4. This invention also relates to the process for preparing this mixture and to its use as a pharmaceutical product for non-intestinal administration in the treatment of cancer.

Claims (13)

1. Pharmaceutical mixtures of vinflunine are characterized by the presence of a stable, sterile aqueous solution of water-soluble vinflunine salts at a pH between 3 and 4. 2. A mixture as defined in Claim 1, characterized by a salt of vinflunine, namely vinflunine ditartrate. 3. The mixture as defined in claim 2, which is characterized by the composition of vinflune tartrate and water for the preparation of a ready-to-use injectable drug. 4. A mixture as defined in claim 1 or 2, characterized by the inclusion of a pH buffer system to maintain the pH between 3 and 4. 5. A mixture as defined in claim 4, characterized by a molarity of the pH buffer system between 0.002 molar and 0.2 molar. 6. A mixture as defined in one of the claims of Claims 4 and 5, characterized by a pH buffer system consisting of an acetic acid/sodium acetate or citric acid/sodium citrate buffer. 7. A mixture defined in one of the claims of Claims 2 through 6, which is characterized by the presence of vinflunine ditartrate with a vinflunine concentration between 1 and 50 mg/ml, with a beneficial effect when between 25 and 30 mg/ml, particularly 25 mg/ml. 8. A mixture as defined in any of the claims of Claims 2 through 7, which is characterized as being a mixture of the following formulations: 68.35 mg of vinflunine ditartrate in water to a total volume of 2 ml, 136.70 mg of vinflunine ditartrate in water to a total volume of 4 ml, or 341.75 mg of vinflunine ditartrate in water to a total volume of 10 ml, where the vinflunine ditartrate corresponds to 50 mg of vinflunine base, 100 mg of vinflunine base, and 250 mg of vinflunine base, respectively. 9. A mixture as defined in one of the claims of a prior claim, which is characterized by the mixture remaining stable for at least 3 months at a temperature of 5°C ± 3°C. 10. The use of mixtures as defined in any one of the claims of claims 1 through 9 in the manufacture of a pharmaceutical product for non-intravenous administration, where the benefit is advantageous when administered intravenously. 11. Use as defined in claim 10, which is specifically intended for the treatment of cancer. 12. The process for preparing the mixture as defined in one of the claims of claims 1 through 9 consists of the following sequential steps: (a) dissolution of the vinflunine salt in the water used to make the ready-to-use injectable drug; (b) addition of a pH buffer as an optional step; (c) sterilization by filtration of the bulk solution; (d) aseptic dispensing in a nitrogen atmosphere of the sterile mixture obtained in step (c) into a container, which would have an advantage in the choice of container from pre-filled glass vials, glass bottles, and syringes. 13. Containers or packaging holding the mixture as defined in any one of Claims 1 through 9.