Formulations with a controlled release of perfumes for dermal application

Abstract

An odorant and flavoring formulation for topical application comprising, as matrix former, a mixture of at least one water-insoluble polymer from the group of homo- or co-polymers of C1-C4-carboxylic acid vinyl esters and at least one water-soluble polymer from the group of homo- or copolymers of N-vinyllactams.

Claims

1. An odorant and flavoring formulation for topical application comprising, as a matrix former, a mixture of a water-insoluble polyvinyl acetate, having an average molecular weight Mw of 200,000 to 700,000 daltons and a water-soluble homopolymer of N-vinylpyrrolidone having a K value of 30; wherein a weight ratio of the polyvinyl acetate to the homopolymer of N-vinylpyrrolidone is about 4:1 to about 10:1.

2. The formulation according to claim 1, said formulation comprising the polyvinyl acetate having an average molecular weight M.sub.w of 400 000 to 500 000 daltons as the water-insoluble polymer and the homopolymer of N-vinylpyrrolidone having a K value of 30 as water-soluble polymer.

3. The formulation according to claim 1, said formulation additionally comprising 0.1 to 2 wt % sodium dodecylsulfate, based on the solids content of the formulation.

4. The formulation according to claim 1, said formulation additionally comprising 0.05 to 2 wt % silicon dioxide, based on the solids content of the formulation.

5. The formulation according to claim 1, said formulation comprising (i) 0.5 to 10 wt % matrix formers, (ii) 60 to 99.4 wt % solvent and (iii) 0.1 to 20 wt % of one or more perfumes, wherein the amounts are based on the total weight of the formulation.

6. The formulation according to claim 1, said formulation comprising a synthetic odorant from the group consisting of geraniol, linalool, linalyl acetate, pyranol, geranyl acetate, anisaldehyde, citral, citronellal, lysmeral, citronellol, rose oxide, tetrahydrolinalool, hydroxycitronellal, beta-ionone, and menthol.

7. The formulation according to claim 1 for use as a spray for topical applications.

8. The formulation according to claim 1 for use as a dermal spray for pharmaceutical or cosmetic applications to humans and animals.

9. The formulation according to claim 1 for use as a textile treatment.

10. The formulation according to claim 1, said formulation additionally comprising 0.1 to 2 wt % sodium dodecylsulfate, based on the solids content of the formulation; 0.05 to 2 wt % silicon dioxide, based on the solids content of the formulation; and (i) 0.5 to 10 wt % matrix formers, (ii) 60 to 99.4 wt % solvent and (iii) 0.1 to 20 wt % of one or more perfumes, wherein the amounts are based on the total weight of the formulation.

Description

EXAMPLES

(1) Kollidon® SR:

(2) 80% polyvinyl acetate (MW 450 000 D), 19% Povidone K30, 0.8% sodium laurylsulfate and 0.2% silica

(3) Kollicoat® SR30D: 30 wt % aqueous dispersion (used as dispersion in the examples) 90% polyvinyl acetate (MW 450 000 D), 9% Povidone K30, 1% sodium laurylsulfate, based on solids

(4) All percentages are wt %.

Examples 1-4: Aerosol Spray

(5) General Procedure

(6) Menthol was dissolved beforehand in abs. ethanol. Kollicoat SR 30 D was then added with stirring to the abs. ethanol/menthol mixture. This preparation was used to fill an aerosol can, the aerosol was can sealed with the aid of a crimping press and dimethyl ether was added under pressure through the valve. The fill level was 100 g.

(7) TABLE-US-00001 Ingredients Example 1 Example 2 Kollicoat SR 13.33% 13.33% 30D Abs. ethanol 36.67% 36.67% Dimethyl ether 49.00% 48.00% Menthol 1.00% 2.00% Total 100.00% 100.00%

Examples 3-4: Pump Sprays with Ethyl Acetate

(8) General Procedure

(9) Menthol was dissolved beforehand in abs. ethanol. Kollicoat SR 30 D was then added with stirring to the abs. ethanol/menthol mixture. Ethyl acetate was then added and the resulting solution was stirred for a few minutes. This preparation was dispensed into plastic pump spray bottles. The fill level was 100 g.

(10) TABLE-US-00002 Ingredients Example 3 Example 4 Kollicoat SR 13.33% 13.33% 30D Abs. ethanol 36.67% 36.67% Ethyl acetate 49.00% 48.00% Menthol 1.00% 2.00% Total 100.00% 100.00%

(11) All pump and aerosol sprays prepared (Examples 1-4) were sprayed onto filter paper and PE film. After a brief drying time, sensory testing was carried out, and also after 2 h and 24 h and the results were documented.

(12) Aerosol Spray

(13) General Procedure

(14) The aroma was firstly dissolved in an ethanol/water mixture (9:1 v/v). Kollidon SR was then added with constant stirring to the ethanol/water mixture. This preparation was used to fill an aerosol can, the aerosol can was crimped and dimethyl ether was added under pressure through the valve. The fill level was 50 g.

(15) The sensory properties were tested as described above by spraying the sprays onto a carrier and after the periods of time specified in the tables.

(16) Geraniol-containing sprays and sensory properties thereof

Example 5-7 Aerosol Spray with Geraniol

(17) TABLE-US-00003 Ingredients Example 5 Example 6 Example 7 Kollidon SR 2.00% 3.00% 5.00% Ethanol/water 58.00% 57.00% 55.00% (9:1) Dimethyl ether 35.00% 35.00% 35.00% Geraniol 5.00% 5.00% 5.00% Total 100.00% 100.00% 100.00%

(18) Aerosol Spray with Geraniol

(19) TABLE-US-00004 8-11 12-14 Formulation Start 7 h 1 day 5 days 6-7 days days days Geraniol ✓ ✓ X X X X X Extra (5% in EtOH) 2% ✓ ✓ ✓ ✓ ✓ ✓ ✓ Koll.SR/5% geraniol 3% ✓ ✓ ✓ ✓ ✓ ✓ ✓ Koll.SR/5% geraniol 5% ✓ ✓ ✓ ✓ ✓ ✓ ✓ Koll.SR/5% geraniol ✓ odor perceptible X odor no longer perceptible

(20) Menthol-containing sprays and sensory properties thereof

(21) Aerosolspray mit Menthol in Ethanol

Examples 8-11: Aerosol Spray with Menthol

(22) TABLE-US-00005 Ingredients Example 8 Example 9 Example 10 Example 11 Kollidon SR 1.00% 2.00% 3.00% 5.00% Ethanol/water 59.00% 58.00% 57.00% 55.00% (9:1) Dimethyl 39.00% 39.00% 39.00% 39.00% ether Menthol 1.00% 1.00% 1.00% 1.00% Total 100.00% 100.00% 100.00% 100.00%

(23) Aerosol Spray with Menthol

(24) TABLE-US-00006 6-7 9-12 13-14 Formulation Start 1 h 4 h 7 h 1 day 5 days days days days Menthol ✓ ✓ X X X Stopped after 24 h, (5% in residue-free drying EtOH) 1% ✓ ✓ ✓ ✓ ✓ ✓ ✓ X X Koll.SR/1% menthol 2% ✓ ✓ ✓ ✓ ✓ ✓ ✓ ✓ X Koll.SR/1% menthol 3% ✓ ✓ ✓ ✓ ✓ ✓ ✓ ✓ ✓ Koll.SR/1% menthol 5% ✓ ✓ ✓ ✓ ✓ ✓ ✓ ✓ ✓ Koll.SR/1% menthol ✓ odor perceptible X odor no longer perceptible

(25) Menthol perfume-containing sprays and sensory properties thereof

(26) Aerosolspray mit Menthol

Examples 12-13: Aerosol Spray with Menthol Perfume

(27) TABLE-US-00007 Ingredients Example 12 Example 13 Kollidon SR 2.00% 3.00% Ethanol/water 58.00% 57.00% (9:1) Dimethyl ether 35.00% 35.00% Menthol perfume 5.00% 5.00% Total 100.00% 100.00%

(28) Aerosol Spray with Menthol Perfume

(29) TABLE-US-00008 8-11 12-14 Formulation Start 7 h 1 day 5 days 6-7 days days days 2% ✓ ✓ ✓ ✓ ✓ ✓ ✓ Koll.SR/5% menthol perfume 3% ✓ ✓ ✓ ✓ ✓ ✓ ✓ Koll.SR/5% menthol perfume ✓ odor perceptible X odor no longer perceptible

(30) Pump Sprays without Ethyl Acetate

(31) General Procedure

(32) The aroma was firstly dissolved in an ethanol/water mixture (9:1 v/v). Kollidon SR was then added with constant stirring to the ethanol/water mixture.

(33) Geraniol-containing sprays and sensory properties thereof

Examples 14-16: Pump Spray with Geraniol

(34) TABLE-US-00009 Ingredients Example 14 Example 15 Example 16 Kollidon SR 2.00% 3.00% 5.00% Ethanol/water 93.00% 92.00% 90.00% (9:1) Geraniol 5.00% 5.00% 5.00% Total 100.00% 100.00% 100.00%

(35) Pump Spray with Geraniol

(36) TABLE-US-00010 12-14 Formulation Start 7 h 1 day 5 days 6-7 days 8-11 days days Geraniol ✓ ✓ X X X X X (5% in EtOH) 2% ✓ ✓ ✓ ✓ ✓ ✓ X Koll.SR/5% geraniol 3% ✓ ✓ ✓ ✓ ✓ ✓ ✓ Koll.SR/5% geraniol 5% ✓ ✓ ✓ ✓ ✓ ✓ ✓ Koll.SR/5% geraniol ✓ odor perceptible X odor no longer perceptible

(37) Menthol perfume-containing sprays and sensory properties thereof

Example 17-18 Pump Spray with Menthol Perfume

(38) TABLE-US-00011 Ingredients Example 17 Example 18 Kollidon SR 2.00% 3.00% Ethanol/water 93.00% 92.00% (9:1) Menthol perfume 5.00% 5.00% Total 100.00% 100.00%

(39) Pump Spray with Menthol Perfume

(40) TABLE-US-00012 8-11 12-14 Formulation Start 7 h 1 day 5 days 6-7 days days days 2% ✓ ✓ ✓ ✓ ✓ ✓ ✓ Koll.SR/5% menthol perfume 3% ✓ ✓ ✓ ✓ ✓ ✓ ✓ Koll.SR/5% menthol perfume ✓ odor perceptible X odor no longer perceptible

(41) All pump and aerosol sprays prepared (Example 5-18) were sprayed onto glass plates. After a brief drying time, sensory testing was carried out, and also after 7 h, 1 day, 5 days, 6-7 days, 8-11 days and 12-14 days. The films were stored for two days at 33° C. in a drying cabinet and subsequently at an ambient temperature of 23° C.