Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Web – sheet or filament bases; compositions of bandages; or...
Reexamination Certificate
1999-05-26
2003-09-02
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Web, sheet or filament bases; compositions of bandages; or...
C424S443000, C424S448000
Reexamination Certificate
active
06613349
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention is a method of treating topical application of known pharmaceutically useful Oxazolidinone antibacterials to treat non-topical infections.
2. Description of the Related Art
U.S. Pat. Nos. 5,164,510, 5,231,188, 5,565,571, 5,652,238, 5,688,792, 5,698,574 and 5,627,181 all disclose various oxazolidinone antibiotics which are well known to those skilled in the art.
U.S. Pat. No. 5,688,792 discloses various oxazolidinone antibiotics which can be administered orally, parenterally or topically. The topical application being by gel or cream vehicle.
PCT patent application PCT/US97/07124 published as International Publication WO97/42954 discloses a method of transdermal administration of a number of antimicrobial agents for treating or preventing systemic bacterial diseases which comprised use of DMSO/water carrier which comprised at least 10% DMSO. None of the antimicrobial agents of International Publication WO97/42954 included Oxazolidinones and the present invention does not use any DMSO.
U.S. Pat. No. 3,743,727 discloses a method of enhancing the penetration into and across the external membrane barrier of an animal subject of an antimicrobial agent of various types which comprised sufficient DMSO to sufficiently enhance the penetration of the antimicrobial agent. None of the antimicrobial agents included oxazolidinones and the present invention does not use any DMSO.
PCT patent application PCT/US84/00899 published as International Publication WO85/00108 discloses a method of treating acne with topical preparations comprising an antibacterial agent in DMSO. None of the antibacterial agents included oxazolidinones and the present invention does not use any DMSO.
U.S. Pat. No. 4,943,435 discloses a transdermal patch for controlled delivery of nicotine. This is a small molecule and not an antibacterial agent.
SUMMARY OF INVENTION
Disclosed is a method of treating a non-topical infection selected from the group consisting of ear infections, skin and soft tissue infections, acne, infected wounds, bacteremia, in a useful warm blooded mammal who is in need of such treatment which comprises topical administration of a pharmaceutical formulation containing a transdermally effective amount of an Oxazolidinone.
DETAILED DESCRIPTION OF THE INVENTION
U.S. Pat. No. 5,688,792 which disclosed various oxazolidinone antibiotics disclosed they could be administered orally, parenterally or topically. Topical administration is not specifically defined but used in its ordinary meaning. Dorland's Illustrated Medical Dictionary (twenty-sixth edition, 1981, page 1377) defines topical as, “pertaining to a particular surface area, as a topical anti-infective applied to a certain area of the skin and affecting only the area to which it is applied.” Therefore, topical administration is administration to a certain area of the skin where the applied item only affects the area to which it is applied. This differs significantly from transdermal. Topical differs from transdermal in that transdermal administration refers to topical administration of an agent, for the purpose of delivering the agent to an adjacent, underlying or distant site or tissue which is different than the site of application. With the Oxazolidinones of the present invention, it is understood that the topical application is to the top of the skin which is not the site of antibacterial activity, which is below or away from the site of topical application. The Oxazolidinone may have antibacterial activity at the top of the skin where [applied] it is applied but that is incidental to the site of intended action. The infection being treated is a non-topical infection.
The claimed invention is a method of treating an infection selected from the group consisting of ear infections, skin and soft tissue infections, acne, infected wounds, bacteremia, in a useful warm blooded mammal who is in need of such treatment which comprises topical administration of a transdermally effective amount of an Oxazolidinone.
Useful warm blooded mammals which are within the scope of the present invention include humans, pets such as dogs, cats and commercially important mammals such as horses, cattle, pigs. It is preferred that the mammal be a human, dog or cat; more preferably a human.
The Oxazolidinones of the present invention are known, see EXAMPLES 1 thru 6 (Oxazolidinones). It is preferred that the Oxazolidinone be selected from the group consisting of:
(S)-N-[[3-[3-fluoro-4-[4-(hydroxyacetyl)-1-piperazinyl]-phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide,
(S)-N-[[3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide,
[4(S)-cis]-(−)-N-[[3-[3-fluoro-4-(tetrahydro-1-oxido-2H-thiopyran-4-yl)phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide,
N-((5S)-3-(3-fluoro-4-(4-(2-fluoroethyl)-3-oxopiperazin-1-yl)phenyl)-2-oxooxazolidin-5-ylmethyl)acetamide,
(S)-N-[[3-[5-(3-pyridyl)thiophen-2-yl]-2-oxo-5-oxazolidinyl]methyl]acetamide and
(S)-N-[[3-[5-(4-pyridyl)pyrid-2-yl]-2-oxo-5-oxazolidinyl]methyl]acetamide hydrochloride. It is more preferred that the Oxazolidinone be selected from the group consisting of:
(S)-N-[[3-[3-fluoro-4-[4-(hydroxyacetyl)-1-piperazinyl]-phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide,
(S)-N-[[3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide and
[4(S)-cis]-(−)-N-[[3-[3-fluoro-4-(tetrahydro-1-oxido-2H-thiopyran-4-yl)phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide; and it is even more preferred that the Oxazolidinone be (S)-N-[[3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide.
The infections treated by the present invention include ear infections, skin and soft tissue infections, acne, infected wounds and bacteremia which are not topical infections but rather infections of the underlying tissue.
Ear infections can be caused by either gram positive or gram negative bacteria or mixture of both. About 60% of the time, the ear infection is caused by gram positive bacteria and in those cases the method of the present invention will be useful in treating the ear infection. If not treated successfully, the two important consequences are the ear drum can rupture leading to a reduction in hearing, and the surrounding tissues including bone can become infected and lead to a more life threatening condition. Ear infections are most often caused by
Streptococcus pneumoniae
and sometimes by
Streptococcus pneumoniae
and
Haemophilus influenzae
at the same time. It is apparent to one skilled in the art that a subject is in need of treatment for an ear infection when there is a fever and the patient has pain in the ear or the patient has pain in the ear and an ear exam discloses a swollen ear rum and fluid is observed behind the ear drum. Ear infections are treated by administering the desired Oxazolidinone(s) directly to the affected ear by use of a pharmaceutical formulation which is a solution, suspension or emulsion. It is preferred that the transdermally effective amount of the Oxazolidinone for treatment of ear infections is from about 0.1 to about 10%; it is more preferred that the transdermally effective amount is from about 0.2 to about 2%. The Oxazolidinone should be administered two thru four times daily for 3 to 14 days. It is preferable if 0.25 to 1 ml of the pharmaceutical formulation is containing the Oxazolidinone is administered each time it is administered.
Skin and soft tissue infections are infections which are most often caused by staphylococci and streptococci. Such infections are very difficult to treat with known antibiotics because of their location and treatment failures occur often requiring additional courses of therapy. These infections include skin (cellulitis and super
Ford Charles W.
Watts Jeffrey L.
Ghali Isis
Hosley Mary J.
Page Thurman K.
Pharmacia & Upjohn Company
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