Injectable pharmaceutical formulations of lefamulin
The present invention relates to an injectable pharmaceutical formulation comprising a compound of formula (I) the formulation being buffered to a pharmaceutically acceptable pH-value, especially a pH-value of from 2 to 6, in particular a pH value of from 3 to 5.5, preferred a pH-value of about 4 to 5, particularly preferred about 5.
1. An injectable pharmaceutical formulation comprising a compound of formula (I)
or a pharmaceutically acceptable salt thereof, said formulation being buffered to a pharmaceutically acceptable pH-value of from 4 to 6, wherein the buffer is a citrate buffer.
2. The formulation according to claim 1 , wherein the buffered formulation comprises a pharmaceutically acceptable vehicle.
3. The formulation according to claim 1 , wherein the citrate buffer is 10 mM to 20 mM, the pH-value of the formulation is from 4 to 5.5, the concentration of the compound of formula (I) is between 0.2 to 3 mg/ml (calculated as free base form), and the formulation comprises a pharmaceutically acceptable vehicle.
4. The formulation according to claim 3 , wherein the citrate buffer is 10 mM and the concentration of the compound of formula (I) is between 0.3 to 1.2 mg/ml.
5. The formulation according to claim 4 , wherein the concentration of the compound of formula (I) is between 0.3 to 0.6 mg/ml.
6. The formulation according claim 1 , wherein the compound of formula (I) is employed as a pharmaceutically acceptable salt.
7. A method of treating diseases mediated by microbes comprising administering the formulation according to claim 1 to a subject in need of said treatment.
8. The method according to claim 7 , wherein the formulation is administered via intravenous application.
9. A pharmaceutical composition, comprising an injectable formulation comprising a compound of formula (I),
or a pharmaceutically acceptable salt thereof, said formulation being buffered to a pharmaceutically acceptable pH-value of from 4 to 5.5, wherein the buffer is a citrate buffer.
10. The injectable pharmaceutical formulation according to claim 1 , wherein the pharmaceutically acceptable pH-value is from 4 to 5.5.
11. The injectable pharmaceutical formulation according to claim 10 , wherein the pharmaceutically acceptable pH-value is from 4 to 5.
12. The injectable pharmaceutical formulation according to claim 1 , wherein the pharmaceutically acceptable pH-value is about 5.
13. The formulation according to claim 1 , wherein the citrate buffer is a 10 to 20 mM citrate buffer.
14. The formulation according to claim 13 , wherein the citrate buffer is a 10 mM citrate buffer.
15. The formulation according to claim 2 , wherein the pharmaceutically acceptable vehicle is selected from the group consisting of normal saline solution, 5% dextrose solution and mixtures thereof.
16. The formulation according to claims 3, 4 or 5 , wherein the pH-value of the formulation is 5.
17. The formulation according claim 6 , wherein the pharmaceutically acceptable salt is selected from the group consisting of acetate and L-lactate.