Aerosol fluoroquinolone formulations for improved pharmacokinetics
View Patent ↗The present invention relates to the field of antimicrobial agents. In particular, the present invention relates to the use of aerosolized fluoroquinolones formulated with divalent or trivalent cations and having improved pulmonary availability for the treatment and management of bacterial infections of the lung and upper respiratory tract.
1. An aqueous pharmaceutical solution comprising about 100 mg/ml of levofloxacin and about 200 mM of magnesium chloride.
2. The solution of claim 1 having a pH from about 5 to about 7 and an osmolality from about 300 mOsmol/kg to about 500 mOsmol/kg.
3. The solution of claim 1 , comprising a dose of about 240 mg of the levofloxacin.
4. An aqueous pharmaceutical solution comprising about 90 mg/ml to about 110 mg/ml of levofloxacin and about 190 mM to about 210 mM of a magnesium cation.
5. The solution of claim 4 , wherein the magnesium cation is in the form of magnesium chloride.
6. The solution of claim 4 , wherein the magnesium cation is in the form of magnesium sulfate.
7. The solution of claim 4 having a pH from about 5 to about 7 and an osmolality from about 300 mOsmol/kg to about 500 mOsmol/kg.
8. The solution of claim 4 having a pH from about 6.0 to about 6.5 and an osmolality from about 350 mOsmol/kg to about 400 mOsmol/kg.
9. The solution of claim 4 , comprising a dose of about 240 mg levofloxacin.
10. An aqueous pharmaceutical solution comprising about 80 mg/ml to about 120 mg/ml of levofloxacin and about 160 mM to about 240 mM of a cation, wherein the cation is magnesium, calcium, zinc, copper, aluminum, or iron.
11. The solution of claim 10 , comprising about 175 mM to about 225 mM of the cation.
12. The solution of claim 10 , comprising about 90 mg/ml to about 110 mg/ml of the levofloxacin and about 190 mM to about 210 mM of the cation.
13. The solution of claim 10 , comprising about 100 mg/ml of levofloxacin and about 200 mM of the cation.
14. The solution of claim 10 , wherein the cation is magnesium.
15. The solution of claim 14 , wherein the cation is in the form of magnesium chloride.
16. The solution of claim 10 having a pH from about 5 to about 7 and an osmolality from about 300 mOsmol/kg to about 500 mOsmol/kg.
17. The solution of claim 16 having a pH from about 6.0 to about 6.5 and an osmolality from about 350 mOsmol/kg to about 400 mOsmol/kg.
18. The solution of claim 10 , comprising a dose of about 180 mg to about 300 mg of the levofloxacin.
19. The solution of claim 18 , comprising a dose of about 240 mg of the levofloxacin.
20. A nebulizer comprising the aqueous pharmaceutical solution of claim 1 .