Drug – bio-affecting and body treating compositions – Solid synthetic organic polymer as designated organic active... – Aftertreated polymer
Reexamination Certificate
1999-03-25
2001-05-15
Kulkosky, Peter F. (Department: 1615)
Drug, bio-affecting and body treating compositions
Solid synthetic organic polymer as designated organic active...
Aftertreated polymer
C424S617000, C424S618000, C424S615000
Reexamination Certificate
active
06231848
ABSTRACT:
The present invention relates to topical compositions for the prophylaxis and treatment of bacterial infections of skin which comprise at least one polymer complex which is essentially composed of hydrogen peroxide, a polymer suitable for complex formation with hydrogen peroxide, with or without another bactericidal compound, and with or without a metal salt or metal colloid.
The bactericidal action of hydrogen peroxide is utilized in a variety of ways for the disinfection of liquids and articles and for the topical therapy of infectious diseases in human and veterinary medicine. It can be used topically in the form of liquid preparations, for example aqueous solutions for irrigating body cavities or fistulas, in the form of solid preparations, e.g. as complexes of hydrogen peroxide with urea, or in the form of salts or compounds which form hydrogen peroxide on hydrolysis or decomposition. The bactericidal action of such preparations extends to Gram-positive and Gram-negative cocci, bacilli or spirochetes, and to a number of yeasts and fungi. In addition, hydrogen peroxide is also used, because of its cleansing and hemostatic action, for viral infections and inflammations not caused by microorganisms.
However, the use of hydrogen peroxide is restricted in principle by its tendency to decompose on exposure to heat or light or in the presence of impurities such as dust, various metal salts and alkaline substances. Although its bactericidal action derives from these decomposition reactions, there are limitations on the storability and utilizability of its preparations because the hydrogen peroxide content decreases.
It has emerged that hydrogen peroxide can be stabilized in the form of complexes with polymers, preferably polyvinylpyrrolidones. Complexes of this type are described, for example, in U.S. Pat. No. 3,376,110, U.S. Pat. No. 3,480,557, U.S. Pat. No. 5,077,047, U.S. Pat. No. 5,108,742, WO-A 91/07184 and WO-A 92/17158. These complexes are, as a rule, stable powders which are easy to handle and can be incorporated into a large number of preparations. Their use for the treatment of acne vulgaris is described in U.S. Pat. No. 5,130,124. These complexes may have the disadvantageous effect that the release of hydrogen peroxide depends on the strength of binding to the polymer, but its action depends on its decomposition and thus on the decomposition catalysts present in the system (dust particles, basic impurities, traces of metals).
It is often necessary, for comprehensive therapy of bacterial infections of skin, to combine the bactericidal action of hydrogen peroxide with other therapeutic effects. Thus, in the cosmetic treatment of acne there is often use of keratolytic substances such as salicylic acid or sulfur (see G. A. Novak in “Die kosmetischen Präparate”, Volume 1, Verlag für chemische Industrie, Augsburg, 1982, pages 202 ff) or vitamin A acid. It is furthermore known that &agr;-hydroxy carboxylic acids have a keratolytic effect (see W. Smith, SÖFW-Journal, 121 (1995)1013 ff). However, said substances may result in skin irritation, erythema or allergies, and less commonly in severe inflammatory reactions. On the other hand, it is known that &agr;-hydroxy acids or salicylic acid form complexes with polyvinylpyrrolidone (see D. Horn and W. Ditter, J. Pharm. Sci. 71, 1982, 1021 ff).
It is furthermore known that polyvinylpyrrolidone can be employed as protective polymer for metallic colloid solutions, for example of copper, silver (Hirai et al., Makromol. Chem. Rapid Commun. 5 (1984) 381), palladium, gold, rhodium or platinum. Esumi et al. describe the preparation of colloidal silver solutions in the presence of vinyl alcohol and N-vinylpyrrolidone (J. Appl. Polym. Sci. 44 (1992) 1003) or polyvinylpyrrolidone homopolymers (Hirai et al. J. Macromol. Sci. Chem. A13 (1979) 633). Bimetallic colloids have also been described, especially for use as catalysts, by Wang et al. (Polymer Bulletin 25 (1991) 139).
It is furthermore known that silver ions in the form of silver salts represent toxicologically acceptable antiseptics with a broad spectrum of action. Thus, 1% strength silver nitrate solution is, in Credé's method (prevention of gonoblennorrhea), administered into the conjunctival sac of neonates immediately after birth.
It is an object of the present invention to provide a topical composition for the treatment of bacterial or viral infections of the skin which, on the one hand, ensures a controlled effect of the bactericidal ingredient and, at the same time, shows other therapeutically worthwhile effects without the prior art disadvantages.
We have found that this object is achieved by polymer-bound hydrogen peroxide, where another therapeutically active substance is additionally bound in the polymer, with or without a metal colloid or metal salt.
The present invention therefore relates to a composition for the prophylaxis or treatment of bacterial or viral infections of skin, comprising at least one polymer complex which is essentially composed of
a) hydrogen peroxide
b) at least one polymer suitable for binding the hydrogen peroxide,
c) with or without another therapeutically active compound and
d) with or without a metal colloid or metal salt
with the proviso that the polymer complexes comprise at least one of components c) or d).
C
1
-C
n
-alkyl means hereinafter linear, branched or cyclic alkyl groups with 1 to n carbon atoms. Examples are methyl, ethyl, n-propyl, i-propyl, n-butyl, 2-butyl, i-butyl, t-butyl, n-hexyl, 2-hexyl, 2-ethylhexyl or n-decyl, cyclopentyl or cyclohexyl. C
1
-C
n
-alkylene means linear or branched alkylene units, for example methylene, ethylene, ethylidene, 1,1-, 1,2-, 1,3-, 2,2-propylene, 1,1-, 1,2-, 1,3-, 1,4-, 2,2-, 2,3-butylene. Aryl groups are phenyl or naphthyl which are unsubstituted or substituted by 1 to 3 C
1
-C
4
-alkyl groups or halogen atoms.
The polymeric component b) of the polymer complexes present in the composition according to the invention is preferably a homo- or copolymer of one or more N-vinyllactams. Preferred N-vinyllactams are N-vinylpyrrolidone, N-vinylpiperidone, N-vinylcaprolactam, N-vinyl-3-morpholinone, N-vinyl-4-oxazolidinone and mixtures thereof. Particularly suitable comonomers are N-vinylheterocycles, e.g. vinylpyridines or vinylimidazoles, which may carry one or more C
1
-C
4
-alkyl radicals or phenyl radicals. Examples which may be mentioned are: N-vinylimidazole and 2-methyl-1-vinylimidazole, 4-methyl-1-vinylimidazole, 5-methyl-1-vinylimidazole, 2-ethyl-1-vinylimidazole, 2-propyl-1-vinylimidazole, 2-isopropyl-1-vinylimidazole, 2-phenyl-1-vinylimidazole, 2-vinylpyridine, 4-vinylpyridine and 2-methyl-5-vinylpyridine.
It is furthermore possible to employ C
1
-C
8
-alkyl vinyl ethers, e.g. methyl vinyl ether, ethyl vinyl ether, n-propyl vinyl ether, i-propyl vinyl ether, n-butyl vinyl ether, i-butyl vinyl ether, t-butyl vinyl ether, 2-ethylhexyl vinyl ether, vinyl esters of C
1
-C
10
-alkyl- or C
6
-C
10
-arylcarboxylic acids, e.g. vinyl acetate, vinyl propionate, vinyl butyrate, vinyl hexanoate, vinyl-2-ethylhexanoate, vinyl decanoate, vinyl laurate, vinyl stearate or vinyl benzoate. Also suitable are esters of acrylic acid or of methacrylic acid with C
1
-C
12
-alkanols, preferably C
1
-C
4
-alkanols. Examples thereof are methyl (meth)acrylate, ethyl (meth)acrylate, n-butyl (meth)acrylate. Further possible comonomers are conjugated C
4
-C
8
-dienes such as butadiene or isoprene, vinylaromatic compounds such as styrene, &agr;-methylstyrene or vinyltoluenes and cationically modified vinyl monomers. Examples of the latter are monoethylenically unsaturated C
3
-C
5
-carboxylic esters with amino alcohols of the formula
where R is C
2
-C
5
-alkylene, R
1
, R
2
and R
3
are, independently of one another, H, CH
3
, C
2
H
5
, C
3
H
7
, and X
⊖
is an anion. Also suitable are amides of these carboxylic acids derived from amines of the formula
The substituents in formula II and X
⊖
have the same meaning as in formula I. Examples of suitable carboxylic acids are acrylic acid, methacrylic acid, cr
Breitenbach Jorg
Fussnegger Bernhard
Lang Siegfried
BASF - Aktiengesellschaft
Keil & Weinkauf
Kulkosky Peter F.
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