INJECTABLE PHARMACEUTICAL FORMULATIONS OF LEFAMULIN
The present invention relates to an injectable pharmaceutical formulation comprising a compound of formula (I) said 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)
said formulation being buffered to a pharmaceutically acceptable pH-value.
2 . The injectable pharmaceutical formulation according to claim 1 , wherein a buffer solution is employed for buffering the compound of formula (I), said buffer solution containing at least one constituent with a pKa value within the range of from 2 to 6 and the resultant pH value of the buffer solution being lower than or equal to said pKa value.
3 . The injectable pharmaceutical formulation according to claim 1 , wherein the buffer is selected from the group consisting of citrate buffers, phosphate buffers and mixtures thereof.
4 . The injectable pharmaceutical formulation according to claim 3 , wherein the buffer is a citrate buffer.
5 . The injectable pharmaceutical formulation according to claim 1 , wherein the buffered injectable pharmaceutical formulation comprises a pharmaceutically acceptable vehicle.
6 . The injectable pharmaceutical formulation according to claim 4 , wherein the citrate buffer is a 10 mM to 20 mM citrate buffer, the pH-value of the injectable pharmaceutical formulation is from 3 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 injectable pharmaceutical formulation comprises a pharmaceutically acceptable vehicle.
7 . The injectable pharmaceutical formulation according to claim 6 , wherein the citrate buffer is a 10 mM citrate buffer, the pH-value of the formulation is from 3 to 5.5, the concentration of the compound of formula (I) is between 0.3 to 1.2 mg/ml (calculated as free base form) and the injectable pharmaceutical formulation comprises a pharmaceutically acceptable vehicle.
8 . The injectable pharmaceutical formulation Formulation according to claim 7 , wherein the concentration of the compound of formula (I) is between 0.3 to 0.6.
9 . The injectable pharmaceutical formulation according to claim 1 , wherein the compound of formula (I) is employed as a pharmaceutically acceptable salt.
10 . A method of treating diseases mediated by microbes comprising administering the injectable pharmaceutical formulation according to claim 1 to a subject in need of said treatment.
11 . The method according to claim 10 , wherein the injectable pharmaceutical formulation is administered via intravenous application.
12 . A pharmaceutical composition, comprising the injectable pharmaceutical formulation according to claim 1 .
13 - 14 . (canceled)
15 . The injectable pharmaceutical formulation according to claim 1 , wherein the pharmaceutically acceptable pH-value is from 2 to 6.
16 . The injectable pharmaceutical formulation according to claim 1 , wherein the pharmaceutically acceptable pH-value is from 3 to 5.5.
17 . The injectable pharmaceutical formulation according to claim 1 , wherein the pharmaceutically acceptable pH-value is from 4 to 5.
18 . The injectable pharmaceutical formulation according to claim 1 , wherein the pharmaceutically acceptable pH-value is about 5.
19 . The injectable pharmaceutical formulation according to claim 4 , wherein the citrate buffer is a 10 to 20 mM citrate buffer. 20 (New) The injectable pharmaceutical formulation according to claim 4 , wherein the citrate buffer is a 10 mM citrate buffer.
21 . The injectable pharmaceutical formulation according to claim 5 , wherein the pharmaceutically acceptable vehicle is selected from the group consisting of normal saline solution, 5% dextrose solution and mixtures thereof.
22 . The injectable pharmaceutical formulation according to claim 6 , wherein the pH-value of the formulation is 5.
23 . The injectable pharmaceutical formulation according to claim 7 , wherein the pH-value of the formulation is 5.
24 . The injectable pharmaceutical formulation according to claim 8 , wherein the pH-value of the formulation is 5.
25 . The injectable pharmaceutical formulation according to claim 9 , wherein the pharmaceutically acceptable salt is selected from the group consisting of acetate and L-lactate.