Claims for Patent: 12,121,582

Summary for Patent: 12,121,582

Title:	Injectable pharmaceutical formulations of lefamulin
Abstract:	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.
Inventor(s):	Mathias Ferencic, Werner Heilmayer, Peter Hinsmann, Wolfgang Wicha
Assignee:	Hong Kong King Friend Industrial Co Ltd
Application Number:	US15/736,865
Patent Claims:	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.