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Claims for Patent: 4,844,902

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Claims for Patent: 4,844,902

Title: Topically applicable formulations of gyrase inhibitors in combination with corticosteroids
Abstract:Topically applicable formulations comprising known ciprofloxacin-type antibacterials of the formula ##STR1## in which and corticosteroids are especially effective in therapy, particularly in the oral cavity. The formulations can be used in the form of plasters, gels, suspensions, emulsions and solutions.
Inventor(s): Grohe; Klaus (Odenthal, DE)
Assignee: Bayer Aktiengesellschaft (Leverkusen, DE)
Application Number:07/154,835
Patent Claims: 1. A topically applicable formulation comprising by weight about 0.05 to 30% of an antibacterially active compound of the formula ##STR6## in which R.sup.1 represents methyl, ethyl, propyl, isopropyl, cyclopropyl, vinyl, 2-hydroxyethyl, 2-fluoroethyl, methoxy, amino, methylamino, dimethylamino, ethylamino, phenyl, 4-fluorophenyl or 2,4-difluorophenyl,

R.sup.2 represents hydrogen, alkyl with 1 to 4 carbon atoms or (5-methyl-2-oxo-1,3-dioxol-4-yl)-methyl,

R.sup.3 represents methyl or a cyclic amino group of the formula ##STR7## wherein R.sup.4 represents hydrogen, alkyl with 1 to 4 carbon atoms, 2-hydroxyethyl, allyl, propargyl, 2-oxopropyl, 3-oxobutyl, phenacyl, formyl, CFCL.sub.2 -S-, CFCL.sub.2 -SO.sub.2 -, CH.sub.3 O-CO-S-, benzyl, 4-aminobenzyl or ##STR8## R.sup.5 represents hydrogen or methyl, R.sup.6 represents hydrogen, alkyl with 1 to 4 carbon atoms, phenyl or benzyloxymethyl,

R.sup.7 represents hydrogen, amino, methylamino, ethylamino, aminomethyl, methylaminomethyl, ethylaminomethyl, dimethylaminomethyl, hydroxyl or hydroxymethyl and

R.sup.8 represents hydrogen, methyl, ethyl or chlorine,

X represents hydrogen, fluorine, chlorine or nitro and

A represents N or C-R.sup.9,

wherein

R.sup.9 represents hydrogen, halogen, such as fluorine or chlorine, methyl or nitro, or

A, together with R.sup.1, can also form a bridge with the structure ##STR9##

0. 01 to 10% of a corticosteroid, and a carrier.

2. A topically applicable formulation according to claim 1, wherein the antibacterially active compound is selected from the group consisting of ciprofloxacin, norfloxacin, perfloxacin, amifloxacin, pirfloxacin, ofloxacin and enoxacin, and the corticosteroid is selected from the group consisting of

A beclomethasone dipropionate

B clobetasol propionate

C diflucortolone valerate

D fluocinolone acetonide

E beclomethasone dipropionate

F betamethasone benzoate

G betamethasone dipropionate

H betamethasone valerate

I desonide

J desoxymethasone

K diflorasone diacetate

L diflucortolone valerate

M fluclorolone acetonide

N fluocinolone acetonide

O fluocinonide

P fluocortolone

Q fluprednidene (fluprednylidene) acetate

R flurandrenolone

S halcinonide

T hydrocortisone butyrate

X triamcinolone acetonide

Y clobetasone butyrate

Z flumethasone pivalate

A.sup.1 fluocinolone acetonide

B.sup.1 fluocortine butyl ester

C.sup.1 fluocortolone

D.sup.1 flurandrenalone

E.sup.1 hydrocortisone (urea)

F.sup.1 dexamethasone

G.sup.1 hydrocortisone (alcohol or acetate) and

H.sup.1 methylprednisolone.

3. A topically applicable formulation according to claim 1, in the form of a solution, spray, lotion, gel, ointment, cream, powder, dusting powder spray, paste, suspension, emulsion, foam.

4. A topically applicable formulation according to claim 1, comprising by weight about

(a.sup.1) 0.1 to 20% of an active compound of the formula I,

(a.sup.2) 0.01 to 10% of a corticosteroid,

(b) 1 to 40% of a water-soluble gel- or lacquer-forming polymer,

(c) 40 to 98% of an organic water-miscible solvent which evaporates faster than water and in which the polymer does not dissolve, and

(d) 0.1 to 10% of at least one of a plasticizer, suspending auxiliary, antioxidant, spreading agent or dyestuff.

5. A topically applicable formulation according to claim 1, comprising by weight about

(a.sup.1) 0.1 to 5% of an active compound of the formula I,

(a.sup.2) 0.02 to 5% of a corticosteroid,

(b) 1 to 20% of a water-soluble gel- or lacquer-forming polymer,

(c) 60 to 90% of an organic water-miscible solvent which evaporates faster than water and in which the polymer does not dissolve, and

(d) 0.1 to 10% of at least one of a plasticizer, suspending auxiliary, antioxidant, spreading agent or dyestuff.

6. A topically applicable formulation according to claim 1, further containing a spreading agent.

7. A composition according to claim 1 in the form of a gel, the carrier including as a gel-forming agent, cellulose ether, polyacrylic acid, polymethacrylic acid, sodium alginate or propylene glycol alginate, sodium amylopectin semiglycolate, alginic acid, gum arabic or guar gum.

8. A composition according to claim 7 further containing a linear high molecular weight polysaccharide as a stabilizing gel-forming agent.

9. A composition according to claim 1 in the form of a suspension having solid particles of 0.1 to 100 .mu.m and a solids content of about 0.5 to 40% by weight.

10. A composition according to claim 1 in the form of an emulsion.

11. A composition according to claim 1 in the form of a solution, the carrier comprising at least one solvent selected from the group consisting of ethanol, isopropyl alcohol, propylene glycol, polyethylene glycol, glycerol, methylcellosolve, cellosolve, an ester, morpholine, dioxane, dimethylsulphoxide, water and cyclohexanone.
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