In one aspect, the invention provides a stabilized lipid-based glycopeptide antibiotic composition and a process for producing the same. In another aspect, the invention provides methods for treating a bacterial pulmonary infection by administering to a subject in need thereof a therapeutically effe
In one aspect, the invention provides a stabilized lipid-based glycopeptide antibiotic composition and a process for producing the same. In another aspect, the invention provides methods for treating a bacterial pulmonary infection by administering to a subject in need thereof a therapeutically effective amount of the stabilized lipid-based glycopeptide antibiotic composition.
대표청구항▼
1. A stabilized lipid-based glycopeptide antibiotic composition comprising: a lipid component;a glycopeptide antibiotic component; andan amino acid or derivative thereof,wherein the amino acid or the derivative thereof reduces the degradation rate of the glycopeptide antibiotic, and wherein the anti
1. A stabilized lipid-based glycopeptide antibiotic composition comprising: a lipid component;a glycopeptide antibiotic component; andan amino acid or derivative thereof,wherein the amino acid or the derivative thereof reduces the degradation rate of the glycopeptide antibiotic, and wherein the antibiotic composition is at least 44% more stable than an antibiotic composition comprising the same lipid component and the same glycopeptide antibiotic component, that does not comprise an amino acid or a derivative thereof. 2. The stabilized lipid-based glycopeptide antibiotic composition according to claim 1, wherein the stabilized glycopeptide antibiotic-amino acid complex is entrapped by the lipid component. 3. The stabilized lipid-based glycopeptide antibiotic composition according to claim 1, wherein the antibiotic composition is at least 77% more stable, or at least 88% more stable, than an antibiotic composition comprising the same lipid component and the same glycopeptide antibiotic component, that does not comprise an amino acid or a derivative thereof. 4. The stabilized lipid-based glycopeptide antibiotic composition according to claim 1, wherein the composition produces product degradants at a rate less than 0.05% by weight per week at 4° C., or a rate less than 0.02% by weight per week at 4° C., or a rate less than 0.01% by weight per week at 4° C. 5. The stabilized lipid-based glycopeptide antibiotic composition according to claim 1, wherein the lipid component comprises a phospholipid. 6. The stabilized lipid-based glycopeptide antibiotic composition according to claim 5, wherein the phospholipid is selected from the group consisting of phosphatidylcholine (PC), phosphatidylglycerol (PG), phosphatidylinositol (PI), phosphatidylserine (PS), phosphatidylethanolamine (PE), phosphatidic acid (PA), and a mixture thereof. 7. The stabilized lipid-based glycopeptide antibiotic composition according to claim 1, wherein the lipid component comprises a sterol. 8. The stabilized lipid-based glycopeptide antibiotic composition according to claim 7, wherein the sterol is cholesterol. 9. The stabilized lipid-based glycopeptide antibiotic composition according to claim 1, wherein the lipid component comprises a phospholipid and a sterol. 10. The stabilized lipid-based glycopeptide antibiotic composition according to claim 1, wherein the lipid component comprises dipalmitoylphosphatidylcholine (DPPC). 11. The stabilized lipid-based glycopeptide antibiotic composition according to claim 1, wherein the lipid component comprises dipalmitoylphosphatidylcholine (DPPC) and cholesterol. 12. The stabilized lipid-based glycopeptide antibiotic composition according to claim 1, wherein the lipid component comprises dipalmitoylphosphatidylglycerol (DPPG). 13. The stabilized lipid-based glycopeptide antibiotic composition according to a claim 1, wherein the lipid component comprises dipalmitoylphosphatidylglycerol (DPPG) and cholesterol. 14. The stabilized lipid-based glycopeptide antibiotic composition according to claim 1, wherein the lipid component comprises dipalmitoylphosphatidylcholine (DPPC), dipalmitoylphosphatidylglycerol (DPPG), and cholesterol. 15. The stabilized lipid-based glycopeptide antibiotic composition according to claim 2, wherein the lipid component is a liposome, a lipid clathrate or a proliposome. 16. The stabilized lipid-based glycopeptide antibiotic composition according to claim 1, wherein the glycopeptide antibiotic is vancomycin. 17. The stabilized lipid-based glycopeptide antibiotic composition according to claim 1, wherein the amino acid is D-alanine, aspartic acid, bicine, D-glutamic acid, glycylglycine (Gly-Gly) or iminodiacetic acid. 18. The stabilized lipid-based glycopeptide antibiotic composition according to claim 1, wherein a molar ratio of the glycopeptide antibiotic component to the amino acid or derivative thereof is from about 1:1 to about 1:4, from about 1:1 to about 1:2, about 1:1 or about 1:2. 19. The stabilized lipid-based glycopeptide antibiotic composition according to claim 1, wherein the composition comprises an amino acid or derivative thereof is a dipeptide or a tripeptide. 20. A method for treating a bacterial infection in a patient in need thereof, the method comprising administering to the patient, a therapeutically effective amount of a stabilized lipid-based glycopeptide antibiotic composition comprising a lipid component, a glycopeptide antibiotic component, and an amino acid or derivative thereof, wherein the amino acid or the derivative thereof reduces the degradation rate of the glycopeptide antibiotic, and wherein the antibiotic composition is at least 44% more stable than an antibiotic composition comprising the same lipid component and the same glycopeptide antibiotic component, that does not comprise an amino acid or a derivative thereof.
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