Claims for Patent: 10,039,804

Summary for Patent: 10,039,804

Title:	Glycopeptide compositions
Abstract:	Solutions comprising a glycopeptide antibiotic, for example Vancomycin, and an amino acid or amino acid derivative such as N-acetyl-Glycine or N-acetyl-D-Alanine are provided. These solutions are stable or stabilized for long-term periods at conditions of normal use and storage, and can be formulated as pharmaceutical solutions for use in subjects. Methods of manufacturing and using these solutions are also provided, as are methods of stabilizing a glycopeptide antibiotic, for example Vancomycin, using amino acids or amino acid derivatives such as N-acetyl-Glycine or N-acetyl-D-Alanine.
Inventor(s):	Jasprica; Ivona (Zagreb, HR), Keser; Sabina (Zagreb, HR), Pindric; Katarina (Sesvete, HR)
Assignee:	XELLIA PHARMACEUTICALS APS (Copenhagen S., DK)
Application Number:	15/827,719
Patent Claims:	1. An aqueous pharmaceutical composition comprising vancomycin and N-acetyl-D-Alanine, wherein the molar ratio of N-acetyl-D-Alanine to vancomycin is from about 5:1 to about 40:1, and wherein the composition comprises about 0.5% w/V of vancomycin. 2. An aqueous pharmaceutical composition comprising vancomycin and N-acetyl-D-Alanine, wherein the molar ratio of N-acetyl-D-Alanine to vancomycin is from about 0.1:1 to about 10:1, and wherein the composition comprises about 5% w/V of vancomycin. 3. An aqueous pharmaceutical composition comprising vancomycin and N-acetyl-D-Alanine and an amino acid. 4. The aqueous pharmaceutical composition of claim 3, wherein the amino acid is selected from Glycine, Alanine, Serine, Leucine, Valine, Lysine, Arginine and Ornithine. 5. The aqueous pharmaceutical composition of claim 4, wherein the amino acid is selected from L-Lysine and D-Lysine. 6. The aqueous pharmaceutical composition of claim 3, comprising about 0.5-15% w/V vancomycin, wherein the vancomycin and N-acetyl-D-Alanine are in a molar ratio of about 1:1-1:40. 7. An aqueous pharmaceutical composition comprising vancomycin, N-acetyl-D-Alanine, and, an organic solvent selected from ethanol and polyethylene glycol. 8. The aqueous pharmaceutical composition of claim 7, wherein a concentration of the organic solvent is up to 50% V/V. 9. An aqueous pharmaceutical composition comprising vancomycin and N-acetyl-D-Alanine, comprising about 0.5-15% w/V vancomycin, wherein the vancomycin and N-acetyl-D-Alanine are in a molar ratio of about 1:1-1:40; wherein the pharmaceutical composition has a pH of about 3-6; wherein the pharmaceutical composition comprises an amino acid selected from D-Serine, D-Leucine, D-Valine, L-Lysine, D-Lysine, L-Arginine, D-Ornithine and L-Ornithine in a molar ratio to vancomycin of about 1:1-30:1; and wherein the pharmaceutical composition further comprises up to 50% V/V of a pharmaceutically acceptable organic solvent. 10. The aqueous pharmaceutical composition of claim 9, wherein the pharmaceutically acceptable organic solvent comprises polyethylene glycol. 11. The aqueous pharmaceutical composition of claim 5, wherein the amino acid comprises L-Lysine; wherein the pharmaceutical composition comprises the vancomycin in a concentration of about 0.5% w/V; wherein the vancomycin, L-Lysine and N-acetyl-D-Alanine are present in a molar ratio of about 1:20:30; wherein the composition has a pH of about 4.5-5.5; and wherein the composition comprises 1.8% V/V of polyethylene glycol. 12. A method of treating bacterial infections in a subject in need thereof, comprising administering to the subject an aqueous pharmaceutical composition comprising vancomycin and N-acetyl-D-Alanine. 13. The method of claim 12, wherein the aqueous pharmaceutical composition further comprises an amino acid. 14. The method of claim 13, wherein the aqueous pharmaceutical composition comprises about 0.5-15% w/V vancomycin; wherein the vancomycin and N-acetyl-D-Alanine are in a molar ratio of 1:1-1:40; wherein the pharmaceutical composition has a pH of about 3-6; wherein the amino acid is selected from D-Serine, D-Leucine, D-Valine, L-Lysine, D-Lysine, L-Arginine, D-Ornithine and L-Ornithine in a molar ratio to vancomycin of about 1:1-30:1; and wherein the pharmaceutical composition comprises up to 50% v/v of polyethylene glycol. 15. The method of claim 13, wherein the amino acid comprises L-Lysine; wherein the pharmaceutical composition comprises the vancomycin in a concentration of about 0.5% w/V; wherein the vancomycin, L-Lysine and N-acetyl-D-Alanine are present in a molar ratio of about 1:20:30; wherein the composition has a pH of about 4.5-5.5; and wherein the composition comprises 1.8% V/V of polyethylene glycol. 16. The method of claim 12, wherein the aqueous pharmaceutical composition is administered parenterally. 17. The method of claim 12, wherein the vancomycin in the pharmaceutical composition administered to the subject is present in an amount sufficient to treat the bacterial infection.