Drug – bio-affecting and body treating compositions – Solid synthetic organic polymer as designated organic active... – Aftertreated polymer
Reexamination Certificate
2000-05-11
2002-11-19
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Solid synthetic organic polymer as designated organic active...
Aftertreated polymer
C424S078080, C424S078070, C424S078020
Reexamination Certificate
active
06482402
ABSTRACT:
BACKGROUND OF THE INVENTION
The resistance of pathogens to various antimicrobial agents has increased at an alarming rate in recent years rendering many important therapeutics for the treatment of microbial infections ineffective. There exist multiple mechanisms for resistance that have been well studied. Pathogens may employ one or more modes of resistance rendering them polyresistant. Polyresistant pathogens are found among a variety of microorganisms including rendering some treatable by only a single class of clinically available antimicrobial agents, if at all.
In response to the rapid development of polyresistant pathogens, combinations of active antimicrobial therapeutic agents are being employed to treat disease. The most useful combination therapies appear to be capable of inhibiting or killing microbes via multiple mechanisms thereby circumventing microbial resistance.
Thus there is a need for antimicrobial agents or a combination of agents that together possess potent broad spectrum antimicrobial activity to which the microbe can not easily become resistant, and can be administered at lower concentrations while maintaining or improving therapeutic activity, and have reduced toxicity, and are inexpensive to produce.
SUMMARY OF THE INVENTION
In one aspect, the present invention relates to antimicrobial compositions.
Another aspect of the invention deals with pharmaceutical compositions comprising a broad group of known antibacterial agents in combination with polymers of the invention as defined herein and a pharmaceutically acceptable carrier.
Yet another aspect of the invention is a treatment regimen (also referred to herein as the “treatment regimen” or “method” of the invention) for treating a microbial infection in a mammal, comprising administering to the mammal a therapeutically effective amount of polymer as defined herein in combination with a therapeutically effective amount of an antibacterial agent.
The polymer to be administered can be a homopolymer or a copolymer. In one embodiment, the polymer further includes a monomer comprising a hydrophobic group, such as an aryl group or a normal or branched C
3
-C
18
-alkyl group.
The polymer to be administered can, optionally, further include a monomer comprising a neutral hydrophilic group, such as a hydroxyl group or an amide group.
The polymer can further have a backbone which is interrupted at one or more points by a nitrogen containing functional group such as a quaternary ammonium group, phosphorus containing functional groups, or sulfur containing functional groups.
Preferred polymers of the invention include amine or ammonium functional groups attached to the polymer backbone via aliphatic spacer groups.
The term “antimicrobial agents” are intended to include antibacterial agents, antifungal agents, antiseptics and the like.
The treatment regimen of the invention represents a new approach to antibacterial therapy to which a polymer can be administered in combination with an antibacterial agent to provide a therapeutically effective treatment of an infection, particularly an infection involving resistant or polyresistant bacteria, and/or to reduce the overall amount of antibacterial agent, or polymer necessary to treat an infection.
Furthermore, the treatment regimen of the invention may reduce the need to develop new antibacterial agents as bacteria and other microbes develop resistance to known antibacterial and antimicrobial agents.
In addition, the polymers employed in the invention are easily prepared using standard techniques of polymer synthesis and inexpensive starting materials. Preferably, the polymers will not be substantially degraded in the digestive tract and, therefore, can be administered orally or topically. Polymer compositions can also be readily varied, to optimize properties such as solubility or water swellability and antimicrobial activity.
DETAILED DESCRIPTION OF THE INVENTION
A description of preferred embodiments of the invention follows.
The present invention relates to antimicrobial compositions including pharmaceutical compositions and treatment regimens for preventing or treating a microbial infection in a mammal, such as a human, by administering to the mammal, a therapeutically effective amount of an cationic polymer and a therapeutically effective amount of an antibacterial agent.
As used herein, a “therapeutically effective amount” is a first amount of a polymer in combination with a second amount of an antimicrobial agent that is sufficient to therapeutically inhibit, partially or totally, a microbial infection, or to reverse development of a microbial infection, or prevent or reduce its further progression.
The term “antimicrobial agent” is intended to include antibacterial agents, antifungal agents, antiseptics and the like. The term “antibacterial agent” includes but is not limited to: naturally occurring antibiotics produced by microorganisms to suppress the growth of other microorganisms, and agents synthesized or modified in the laboratory which have either bacteriocidal or bacteriostatic activity, e.g., &bgr;-lactam antibacterial agents including, e.g. carbencillim; ampicillin, cloxacillin, oxacillin and pieracillin, cephalosporins and other cephems including, e.g. cefaclor, cefamandole, cefazolin, cefoperazone, ceftaxime, cefoxitin, ceftazidime, ceftriazone and carbapenems including, e.g., imipenem and meropenem; and glycopeptides, macrolides, quinolones (e.g. nalidixic acid), tetracyclines, aminoglycosides (e.g. Gentamicin and Paromomycin) and further includes antifungal agents. In general if an antibacterial agent is bacteriostatic, it means that the agent essentially arrests or inhibits bacterial cell growth (but does not kill the bacteria); if the agent is bacteriocidal, it means that the agent kills bacterial cells (and may stop growth before killing the bacteria).
The term “polymer” refers to a macromolecule comprising a plurality of repeat units or monomers. The term includes homopolymers, which are formed from a single type of monomer, and copolymers, which are formed of two or more different monomers. A “terpolymer” is a copolymer formed from three different monomers. The term polymer, as used herein, is intended to exclude proteins, peptides, polypeptides and proteinaceous materials.
As used herein, the term “polymer backbone” or “backbone” refers to that portion of the polymer which is a continuous chain, comprising the bonds which are formed between monomers upon polymerization. The composition of the polymer backbone can be described in terms of the identity of the monomers from which it is formed, without regard to the composition of branches, or side chains, off of the polymer backbone. Thus, a poly(acrylamide) polymer is said to have a poly(acrylamide) backbone, without regard to the substituents on the acrylamide nitrogen atom, which are components of the polymer side chains. A poly(acrylamide-co-styrene) copolymer, for example, is said to have a mixed acrylamide/styrene backbone.
The term “polymer side chain” or “side chain” refers to the portion of a monomer which, following polymerization, forms a branch off of the polymer backbone. In a homopolymer all of the polymer side chains are identical. A copolymer can comprise two or more distinct side chains. When a side chain comprises an ionic unit, for example, the ionic unit depends from, or is a substituent of, the polymer backbone, and is referred to as a “pendant ionic unit”. The term “spacer group”, as used herein, refers to a polyvalent molecular fragment which is a component of a polymer side chain and connects a pendant moiety to the polymer backbone. The term “aliphatic spacer group” refers to a spacer group which does not include an aromatic unit, such as a phenylene unit.
The term “addition polymer”, as used herein, is a polymer formed by the addition of monomers without the consequent release of a small molecule. A common type of addition polymer is formed by polymerizing olefinic monomers, wherein monomers are joined by the formation of a carbon-carbon bonds between monomers, without
Kurtz Caroline
Neenan Thomas X.
Fubara Blessing
GelTex Pharmaceuticals Inc.
Hamilton Brook Smith & Reynolds P.C.
Page Thurman K.
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