Topical administration of antimicrobial agents for the treatment of systemic bacterial diseases

• US 5,929,086 A
• Filed: 05/05/1997
• Issued: 07/27/1999
• Est. Priority Date: 05/10/1996
• Status: Expired due to Fees

• Current Assignee: Pharmacia & Upjohn Company (Pfizer Inc.)
• Original Assignee: Pharmacia & Upjohn Company (Pfizer Inc.)
• Inventors: Wardley, Richard C., Watts, Jeffrey L., Stehle, Randall G.
• Primary Examiner(s): Cook, Rebecca
• Application Number:
  US08/851,307
• Time in Patent Office: 813 Days
• Field of Search: 514/312, 514/772
• US Class Current: 514/312
• CPC Class Codes: A61K 31/4709 Non-condensed quinolines and containing further heterocyclic rings
• CPC Class Codes: A61K 31/546 containing further heterocyclic rings, e.g. cephalothin
• CPC Class Codes: C07D 401/04 directly linked by a ring-member-to-ring-member bond

Abstract

The present invention provides a method of topically administering antimicrobial agents such as premafloxacin, premafloxacin-like compound, premafloxacin ester, ciprofloxacin, enrofloxacin, cefquinome, cefpodoxime, gentamicin or erythromycin for the treatment of systemic bacterial diseases in mammals.

Claims

1. A method of treating a systemic bacterial disease in a mammnal in need thereof which comprises topically administering to said mammal an effective amount of an antimicrobial agent in a propylene glycol/oleyl alcohol (PG/OA) carrier wherein said antimicrobial agent is selected from the group consisting of premafloxaciin or a premafloxacin ester wherein propylene glycol and oleyl alcohol is in a ratio at least about 80% of propylene, glycol by volume.

3. The method of claim 1 or 2 wherein said PG/OA carrier comprises about 95% of PG and about 5% OA by volume.

4. The method of claim 1 wherein said premafloxacin ester is a compound of formula II or a pharmaceutically acceptable acid addition salt thereof ##STR9## wherein R is C_1-10 alkyl, C_1-10 alkenyl, C_1-6 cycloalkyl, phenyl, benzyl, or napthyl.

5. The method of claim 4 wherein R is C_1-4 alkyl.

6. The method of claim 4 wherein R is ethyl or butyl.

7. The method of claim 1 or 2 wherein said antimicrobial agent is topically administered in an amount of from about 0.1 to about 100 mg/kg body weight/per day.

8. The method of claim 1 or 2 wherein said antimicrobial agent is topically administered in an amount of from about 1.0 to about 50 mg/kg body weight/per day.

2. A method of treating a systemic bacterial disease in a mammal in need thereof which comprises topically administering to said mammal an effective amount of an antimicrobial agent in a propylene glycol/oleyl alcohol (PG/OA) carrier wherein said antimicrobial agents is a compound of formula III or a pharmaceutically acceptable salt thereof ##STR8## wherein R₁ is ethyl, cyclopropyl or 2,4-difluorophenyl;

R₂ is hydrogen or C_1-4 alkyl;

R₃ is hydrogen, amino or methyl;

R₄ and R₅ are each independently hydrogen or methyl; and

wherein propylene glycol and oleyl alcohol is in a ratio at least about 80% of propylene glycol by volume.