Cosmetic or pharmaceutical composition, to be applied topically

Abstract

A cosmetic or pharmaceutical composition, to be applied topically is described, which has a hydrophilic outer phase, at least one cosmetic and/or pharmaceutical active ingredient and at least one carrier substance for the active ingredient. The carrier substance here forms such structures, which comprises at least two lamellar double membrane layers arranged one over another in the manner of a sandwich, wherein between adjacent double membrane layers, aligned parallel to each other, a layer of an inner phase is respectively arranged. The active ingredient is distributed in the double membrane layer and in the layer of the inner phase such that the layer of the inner phase contains the active ingredient in a concentration range between 2% by weight and 98% by weight and the double membrane layer contains the active ingredient in a concentration between 98% by weight and 2% by weight, respectively in relation to the total concentration of active ingredient, and the outer phase has no or almost no active ingredient.

Claims

1. A cosmetic composition for topical application, said composition comprising: a hydrophilic outer phase comprising water; at least one cosmetic active ingredient which is rice bran wax; and at least one carrier substance for the at least one cosmetic active ingredient; wherein: a) the at least one carrier substance forms a planar structure which comprises at least two lamellar double membrane layers, arranged one over another in the manner of a sandwich; b) between adjacent double membrane layers, aligned parallel to each other, a layer of an inner phase comprising water is arranged; c) the at least one cosmetic active ingredient is distributed in the at least two double membrane layers and in the layer of the inner phase such that the layer of the inner phase contains the at least one cosmetic active ingredient in a concentration range between 2% by weight and 98% by weight, and the at least two double membrane layers contain the at least one cosmetic active ingredient in a concentration between 98% by weight and 2% by weight, respectively, in relation to the total concentration of the at least one cosmetic active ingredient; d) the outer phase comprises the at least one cosmetic active ingredient in a concentration between 0% by weight and 2% by weight, in relation to the total concentration of the at least one cosmetic active ingredient; and e) the at least one carrier substance comprises hydrogenated phosphatidylcholine.

2. The composition according to claim 1, wherein the composition comprises the at least one cosmetic active ingredient in a concentration range between 0.1% by weight and 15% by weight, in relation to the composition ready for use.

3. The composition according to claim 1, wherein the at least two double membrane layers contain the at least one cosmetic active ingredient in a concentration of at least 70% by weight, in relation to the total concentration of the at least one cosmetic active ingredient.

4. The composition according to claim 3, wherein the at least two double membrane layers contain the at least one cosmetic active ingredient in a concentration range between 80% by weight and 90% by weight, in relation to the total concentration of the at least one cosmetic active ingredient.

5. The composition according to claim 1, wherein the composition further comprises a second cosmetic active ingredient which is a light protective filter selected from PABA and derivatives, octyl dimethyl PABA, homosalate, oxybenzone BEMT, p-methoxycinnamate, ethylhexyl triazone, octocrylene, benzophenone-3, benzophenone-4, benzophenone-9, Diethylamino hexyl benzoate, drometrizole trisiloxane, 4-methylbenzylidene camphor, 3-benzylidene camphor, octyl salicylate, methylene bis-benzotriazolyl tetramethylbutylphenol, bis-ethylhexyloxyphenol methoxyphenyl triazine, ethylhexyl methoxycinnamate, diethylhexyl butamido triazone, phenylbenzimidazole sulfonic acid, butyl methoxydibenzoylmethane, Diethylamino hydroxybenzoyl hexyl benzoate, disodium phenyl dibenzimidazole tetrasulfonate or terephthalylidene dicamphor sulfonic acid.

6. The composition according to claim 1, wherein the composition further comprises a second cosmetic active ingredient which is an antioxidant.

7. The composition according to claim 6, wherein the antioxidant is selected from vitamin A and/or vitamin C, tocopherols, carcinin, liponic acid, liposol maleates, carotenoids, lycopenes, colourless carotenoids, polyphenols, epicatechins, epigallocatechins, epigallocatechingallate, epicatechnin-3-gallate, caffeic acid, caffeic acid ester, rosmarinic acid, flavonoids, flavanols, flavanons, anthocyanidins, proanthocyanidins, resveratrol, silymarin, aspalathin, ellaginic acid, curcumin derivatives, dyhydroquercetin, N.D.G.A., rutin, tetrahydrocurcuminoid, tetrahydrodiferuloylmethane, tetrahydrodemethoxydiferuloylmethane, tetrahydrobisdemethoxydiferuloylmethane, glutathione, coenzyme q 10, L-carnosin, N-acetylcycsteine, phytic acid, furalglucytol, thioctic acid, EDT A, BHA, BHT, SOD, or 4-thiazolidinone kinetin, or a mixture thereof.

8. The composition according to claim 1, wherein the composition further comprises a soothing cosmetic ingredient which is selected from the group consisting of shea butter, a ceramide, cupuacu butter, squalane and a triglyceride.

9. The composition according to claim 1, wherein the at least one carrier substance is present in a concentration between 0.7% by weight and 10% by weight, in relation to the composition as ready for use.

10. The composition according to claim 1, wherein the composition further contains at least one alcohol.

11. The composition according to claim 10, wherein the at least one alcohol is selected from the group consisting of phenylethyl alcohol, pentylene glycol, caprylyl glycol, decylene glycol and glycerine.

12. The composition according to claim 1, wherein the composition further comprises an N-acyl ethanolamine in a concentration between 0.01% by weight and 10% by weight, in relation to the composition as ready for use.

13. The composition according to claim 12, wherein the acyl radical of the N-acyl ethanolamine is a C.sub.1-C.sub.24-acyl radical.

14. The composition according to claim 13, wherein the N-acyl ethanolamine is selected from the group consisting of N-acetyl ethanolamine, N-oleoyl ethanolamine, N-linolenoyl ethanolamine, N-cocoyl ethanolamine, and N-palmitoyl ethanolamine.

15. The composition according to claim 1, wherein the composition further comprises at least one preservative, thickener, and/or gelling agent.

16. The composition according to claim 15, wherein the thickener or gelling agent is a natural colloid, a natural hydrocolloid, a synthetic colloid or a synthetic hydrocolloid.

17. The composition according to claim 16, wherein the composition comprises respectively between: 0.5% by weight and 7% by weight hydrogenated phosphatidylcholine, 0.5% by weight and 10% by weight cupuacu butter, 0.5% by weight and 15% by weight shea butter, 0.001% by weight and 3% by weight ceramide, 0.1% by weight and 5% by weight of the colloid or hydrocolloid, 2% by weight and 42% by weight of oil or oil constituent, 0.01% by weight and 5% by weight of the at least one cosmetic active ingredient, 0% by weight and 10% by weight of other additives, and 5% by weight and 96% by weight water.

18. The composition according to claim 1, wherein the composition has a viscosity at 20 C. between 2.000 mPas and 40.000 mPas.

19. The composition according to claim 1, wherein the composition has a pH-value between 4.0 and 7.6.

20. The composition according to claim 1, wherein the composition further comprises a second cosmetic active ingredient which is selected from a light protective filter, an antioxidant, or a soothing cosmetic ingredient.

Description

(1) The inventive composition is explained below with the aid of four examples in connection with the drawings, in which:

(2) FIG. 1 shows a diagrammatic illustration of a first embodiment of the previously described particular structure;

(3) FIG. 2 shows a diagrammatic illustration of a second embodiment of the previously described particular structure; and

(4) FIG. 3 shows a diagrammatic illustration of a third embodiment of the previously described particular structure.

(5) In FIGS. 1 to 3, the same elements are provided with the same reference numbers.

(6) FIGS. 1 to 3 represent different embodiments of the structures as they occur in the inventive composition and are essential for the latter.

(7) All the structures shown diagrammatically in FIGS. 1 to 3 have in common a planar first double membrane layer 1 and a planar second double membrane layer 2, wherein the double membrane layers 1 and 2 enclose the planar layer of an inner phase 3 in the manner of a sandwich.

(8) Each double membrane layer 1 or respectively 2 consists of two layers A and B of the carrier substance, wherein within the two layers A or respectively B the individual molecules of the carrier substance are aligned so that the outer hydrophilic radicals 4 of the upper layer A of each double membrane layer 1 or respectively 2 are respectively aligned outwards to the outer hydrophilic phase which completely surrounds the respective structure, whereas the inner hydrophilic radicals 5 of the lower layer B point inwards to the layer of the inner phase 3. This has the result that within each layer A or respectively B the lipophilic radicals 6 of each double membrane layer 1 or respectively 2 are aligned to each other. Accordingly, in the structures shown in FIGS. 1 to 3, only the outer hydrophilic radicals 4 come in contact with the outer phase, whereas the inner hydrophilic radicals 5 of each double membrane layer 1 or respectively 2 come in contact exclusively with the layer of the inner phase 3.

(9) Reference number 7 designates respectively active ingredient molecules illustrated in dark print or respectively active ingredient aggregates illustrated in dark print, wherein the active ingredient molecules differ from the active ingredient aggregates in that active ingredient aggregates represent combinations of active ingredient molecules, which is abbreviated below as active ingredient 7.

(10) The diagrammatic illustrations according to FIGS. 1 to 3 differ from each other in that the active ingredient 7 is distributed differently between the layers 1 to 3.

(11) In FIG. 1, the predominant amount of active ingredient 7 is distributed in the double membrane layer 1 or respectively 2 and is embedded there between the hydrophobic radicals 6, whereas the layer of the inner phase 3 has a relatively small concentration of active ingredient 7. Such a composition which contains a predominant hydrophobic active ingredient in particular has such a structure.

(12) In FIG. 2 the predominant amount of active ingredient 7 is embedded into the layer of the inner phase 3, whereas the double membrane layer 1 or respectively 2 has a relatively small concentration of active ingredient 7, which is embedded between the hydrophobic radicals 6, preferably in the immediate vicinity of the hydrophilic radicals 4 and 5. Such a composition which contains a predominant hydrophilic active ingredient in particular has such a structure.

(13) FIG. 3 illustrates such a structure in which the inner phase 3 contains a relatively small concentration of active ingredient 7. The concern here is with the original active ingredient. Furthermore, FIG. 3 illustrates diagrammatically such active ingredients 8 in which likewise molecules or respectively aggregates can be concerned, which are anchored within the double membrane layer 1 or respectively 2 by means of lipophilic compounds which are illustrated diagrammatically in FIG. 3 as dark curved lines 9. In particular such a composition which contains predominantly a hydrophilic active ingredient has such a structure, wherein a portion of this active ingredient is transformed with the lipophilic compounds (anchor group) with the formation of intermolecular interactions between lipophilic compound and active ingredient, whereas the remaining portion contains a correspondingly non-transformed active ingredient 7. The extent of the transformation can be determined by coordination of the stoichiometric ratios of active ingredient and lipophilic compound. This possibility exists not only for hydrophilic active ingredients but also for amphiphilic active ingredients.

EXAMPLE A

Production of a Concentrate Containing Retinol as Active Ingredient

(14) A concentrate containing retinol as active ingredient was produced from the following ingredients:

(15) Ingredients of Phase 1:

(16) TABLE-US-00001 6% by weight phosphatidylcholine 3% by weight caprylic/capric triglyceride 3% by weight glycerine 5% by weight pentylene glycol

(17) Ingredient of Phase 2:

(18) TABLE-US-00002 10% by weight retinol

(19) Ingredient of Phase 3:

(20) TABLE-US-00003 73% by weight water

(21) The ingredients of Phase 1 were heated to 80 C. with uniform stirring. Then the ingredient of Phase 3 was heated to 75 C. At 80 C. the ingredient of Phase 2 was added to the ingredients of Phase 1 and were stirred uniformly together. Then the ingredients of Phase 3 were added to the ingredients of Phase 1 and 2 which had been stirred together, so that the ingredients of all phases which were thus mixed with each other have been homogenized at 20,000 r/min by means of Ultra Turrax. The pre-emulsion which was thus produced was microdispersed by means of a high pressure homogenizer under the following conditions: 2-5 cycles at 800 bar. After cooling of the micro-dispersed mixture with uniform stirring to 30 C., homogenization was carried out again for 2 minutes at 20,000 r/min by means of Ultra Turrax.

(22) In cosmetics, retinol is deemed to be an active ingredient which is difficult to stabilize, which is subject to a constant oxidative decomposition process. Classic stabilising methods such as the addition of antioxidants, encapsulating in liposomes or cyclodextrins again and again come up against their limits, because they either do not reach the desired active ingredient concentration or do not have the necessary stability.

(23) In a comparative test, surprisingly it was able to be established that the retinol stability was distinctly increased by the described composition.

(24) For this test, a liposomal formulation containing retinol in the concentration indicated above was compared with the previously described concentrate.

(25) For this purpose, the respective sample was exposed to a light irradiation (1.4 mW/cm2 over 20 minutes) as stress parameter. The irradiation took place in quartz glass chambers with a water-filled cover (company: Heraeus Quarzglas GmbH), which served to absorb the infrared energy. This was necessary, in order to prevent the vaporization of the solvent in the respective sample during the irradiation. The retinol concentration remaining after the irradiation was carried out by separation by means of high pressure liquid chromatography (RP-18 column, mobile phase consisting of a mixture methanol-n-hexane 72:78 (vol./vol.)) and subsequent detection of the UV absorption at 324, 292 and 276 nm. The irradiation was carried out for each sample three times, to thus guarantee the reproducibility.

(26) The liposomal formulation only allowed a 30% stabilization of the retinol, so that through the irradiation 70% by weight of the original retinol were decomposed, whereas the retinol concentration after the irradiation of the concentrate lay at 70%, so that hereby only 30% of the originally used active ingredient retinol was decomposed.

EXAMPLE B

Production of a Concentrate Containing Boswellia as Active Ingredient

(27) Ingredients of Phase 1:

(28) TABLE-US-00004 7.5% by weight hydrogenated phosphatidylcholine 3% by weight caprylic/capric triglyceride 3% by weight glycerine 5% by weight hexylene glycol 3% by weight meadow foam seed oil 5% by weight Boswellia serrata extract

(29) Ingredient of Phase 2:

(30) TABLE-US-00005 73.5% by weight water

(31) The ingredients of Phase 1 were heated to 85 C. with uniform stirring. Then the ingredients of Phase 2 were likewise heated to 85 C. and at this temperature were added to Phase 1 and hereafter the mixed phases were stirred uniformly and homogenized at 24,000 r/min by means of Ultra Turrax. The pre-emulsion which was produced was micro-dispersed for 4-6 cycles at 750 bar by means of a high pressure homogenizer. After cooling to 35 C. the micro-dispersion was homogenized again for 2 minutes at 20,000 r/min by means of Ultra Turrax. The concentrate which was thus produced was cooled with stirring to 30 C.

(32) Owing to its anti-inflammatory characteristics, Boswellia serrata extract is of great interest as an active ingredient for the cosmetic and pharmaceutical industry. Owing to its resin-like characteristics, however, Boswellia serrata extract is deemed to be a molecule which is difficult to stabilize, because it considerably impairs the emulsion formation and is therefore only used in small concentrations in cosmetic or pharmaceutical products.

(33) By a test which compares the previously described concentrate with the active ingredient named there in the concentration listed there with a conventional Boswellia serrata extract emulsion, which corresponded to the concentrate in its concentration of active ingredient, it was able to be established that only the concentrate provides a stable and highly concentrated form of presentation for the active ingredient.

(34) By macroscopic and microscopic analysis (microscope: Olympus CH2 Model CHT) it was demonstrated that the typical destabilization phenomena occurring after storage with the conventional emulsion did not occur with the concentrate. In particular, in contrast to the conventional emulsion, the concentrate did not show macroscopically any decomposition (phase separation) with subsequent distinctly detectable oil separation. Furthermore, both the concentrate and also the conventional emulsion were examined microscopically at a 400-times enlargement with regard to the crystalline structures contained therein and the droplet size growth. It was able to be established here that with the conventional emulsion within the first 3 days after production (storage at 232 C.) a distinct particle size growth and a morphological change in the lipid droplet form to amorphous, non-symmetrical structures occurred, which is judged among specialists as a sure sign of an incipient phase separation which is also able to be established macroscopically.

(35) In contrast to this, with the concentrate a change was not able to be established either macroscopically or microscopically, so that the concentrate remained stable and unchanged even in excess of months.

EXAMPLE C

Production of a Concentrate Containing Proline as Active Ingredient

(36) Ingredients of Phase 1:

(37) TABLE-US-00006 6% by weight hydrogenated phosphatidylcholine 7% by weight jojoba oil 3% by weight glycerine 5% by weight pentylene glycol 3% by weight Butyrospermum parkii

(38) Ingredient of Phase 2:

(39) TABLE-US-00007 15% by weight Proline

(40) Ingredient of Phase 3:

(41) TABLE-US-00008 61% by weight water

(42) The ingredients of Phase 1 were heated to 80 C. with uniform stirring. At 80 C. the ingredient of Phase 2 was added to the mixed Phase 1 and stirred uniformly. Hereafter the Phase 3, heated to 75 C. was added to the ingredients of Phases 1 and 2, which were mixed together, and this was homogenized at 20,000 r/min by means of Ultra Turrax. The pre-emulsion which was thus produced was micro-dispersed for 2-5 cycles at 800 bar by means of a high pressure homogenizer. After cooling to 30 C. with uniform stirring, the mixture which was thus produced was homogenized for 2 minutes at 20,000 r/min by means of Ultra Turrax.

(43) In this example the proline serves as model substance for an osmoprotectant.

(44) In a test which on the one hand comprises a conventional oil-in-water emulsion which contained the same concentration of proline and on the other hand the previously described concentrate, by way of comparison the proline concentration present in the upper layer of the skin was determined after application of the respective product.

(45) After application of the respective sample and after a 60-minute period of dwell had elapsed, 10 adhesive tape tear-offs were taken from the same skin area by the stripping method. For the comparative test, care was taken that skin areas of identical size were treated with identical quantities of the concentrate or respectively of the oil-in-water emulsion. The corresponding adhesive tape strips were extracted respectively with 1 ml methanol. The concentration of proline was determined by means of high pressure liquid chromatography (CROWNPAK CR (+) column, mobile phase consisting of a HCLO4 solution, pre-column derivatization with DABS-CL (CrestPak C18S column, mobile phase: 8 mM sodium dihydrogenphosphate dihydrate in H.sub.2O with 4% DMF, detection of the UV absorption at 280 nm), wherein all the values were established as a triple determination.

(46) As a result, it is to be recorded that the proline concentration determined in the skin after application of the concentrate was higher by 50% than the proline concentration which was measured after application of the oil-in-water emulsion.

EXAMPLE D

Production of a Concentrate Containing Palmitoyl Pentapeptide-3 as Active Ingredient

(47) Ingredients of Phase 1:

(48) TABLE-US-00009 8% by weight hydrogenated phosphatidylcholine 11% by weight isopropyl palmitate 3% by weight glycerine 10% by weight ethanol

(49) Ingredient of Phase 2:

(50) TABLE-US-00010 0.3% by weight palmitoyl pentapeptide-3

(51) Ingredient of Phase 3:

(52) TABLE-US-00011 67.7% by weight water

(53) The ingredients of Phase 1 were heated to 80 C. with uniform stirring. At 80 C. the ingredient of Phase 2 was added to Phase 1 and stirred uniformly. The ingredient of Phase 3, heated to 75 C. was added to the ingredients of Phases 1 and 2 and homogenized at 20,000 r/min by means of Ultra Turrax. The produced pre-emulsion was micro-dispersed for 2-5 cycles at 800 bar by means of a high pressure homogenizer and was then cooled with uniform stirring to 30 C. This was followed by a further homogenizing for 2 minutes at 20,000 r/min by means of Ultra Turrax.

(54) Palmitoyl pentapeptides-3 have been in the centre of dermatological/cosmetic interest for years. In a similar manner to copper peptides, palmitoyl pentapeptides stimulate the wound healing processes in the deeper layers of the skin by production of collagen and fibronectin. Thereby, skin ageing is actively counteracted and wound healing processes are actively assisted, with the effect frequently only occurring in periods of 4 to 6 weeks.

(55) According to the previously described method, the previously described concentrate was examined by comparison with a conventional formulation, wherein the previously described test conditions were applied. After this, it was able to be established that the penetration amount of palmitoyl pentapeptide-3 with the application of the concentrate was 40% higher compared with the conventional formulation.

(56) The concentrates produced according to examples A to D can be processed to a product ready for use by dilution in a ratio of between 5 to 50% by weight concentrate with 95 to 50% by weight additives, thus for example water, thickeners, hydrogels or further cosmetic active ingredients.

EXAMPLE E

Production of a Final Formulation with the Active Ingredient Hexapeptide-9

(57) Ingredients of Phase 1:

(58) TABLE-US-00012 2% by weight hydrogenated phosphatidylcholine 1% by weight hexapeptide-9 0.8% by weight Butyrospermum parkii 1.5% by weight caprylic/capric triglyceride 1% by weight squalane

(59) Ingredients of Phase 2:

(60) TABLE-US-00013 1% by weight glycerine 1.3% by weight pentylene glycol 19% by weight water

(61) Ingredients of Phase 3:

(62) TABLE-US-00014 25% by weight caprylic/capric triglyceride 0.10% by weight carbomer 0.10% by weight sodium carbomer 0.10% by weight xanthan gum

(63) Ingredients of Phase 4:

(64) TABLE-US-00015 3.5% by weight pentylene glycol 0.35% hydroxyethylcellulose ad 100.0% by weight water

(65) The ingredients of Phase 1 were heated to 85 C. with uniform stirring until all the active ingredients are present in dissolved form. Likewise, Phase 2 was heated to 85 C. with stirring in a separate vessel. Phase 2 was then added to Phase 1, stirred briefly and hereafter homogenized by means of Ultra Turrax at 24,000 r/min.

(66) The pre-emulsion resulting herefrom was micro-dispersed by means of a high pressure homogenizer in 5-7 cycles, pressure 600 bar. The produced dispersion was cooled to 30 C. with uniform stirring.

(67) Phase 3 and Phase 4 were heated in respectively separate vessels to 30 C. with uniform stirring. Phase 4 was then added to Phase 3 and then homogenized by Ultra Turrax (12,000 r/min). The produced dispersion was cooled to 30 C. with slight stirring. The high viscous dispersion from Phases 1 and 2 was then added. Hereafter, the mixture was homogenized at 30 C. by Ultra Turrax (12,000 r/min) until a uniform structure was present. The final formulation which was thus produced was able to be used directly.

EXAMPLE F

Production of a Final Formulation with the UVB Filter Octocrylene and the UVA Filter Butylmethoxydibenzoylmethane

(68) Ingredients of Phase 1:

(69) TABLE-US-00016 2.10% by weight hydrogenated phosphatidylcholine 3.00% by weight octocrylene 2.50% by weight butylmethoxydibenzoylmethane

(70) Ingredients of Phase 2:

(71) TABLE-US-00017 1.00% by weight glycerine 1.30% by weight pentylene glycol 18.00% by weight water 0.10% by weight caprylyl glycol

(72) Ingredients of Phase 3:

(73) TABLE-US-00018 22.00% by weight caprylic/capric triglyceride 0.10% by weight carbomer 0.10% by weight sodium carbomer 0.10% by weight xanthan gum

(74) Ingredients of Phase 4:

(75) TABLE-US-00019 3.50% by weight pentylene glycol 0.35% by weight hydroxyethylcellulose ad 100.0% by weight water

(76) The ingredients of Phase 1 were heated to 85 C. with uniform stirring until all the ingredients are present in dissolved form. Likewise, Phase 2 was heated in a separate vessel to 85 C. with stirring. Phase 2 was then added to Phase 1 and hereafter was stirred by means of Ultra Turrax at 24,000 r/min until a homogeneous mixture was produced. The pre-emulsion resulting from this was micro-dispersed by means of a high pressure homogenizer in 6-8 cycles, pressure 800 bar. The produced dispersion was cooled to 30 C. with uniform stirring.

(77) Phase 3 and Phase 4 were heated in a separate vessel to 30 C. with uniform stirring. Phase 4 was then added to Phase 3 and hereafter stirred by Ultra Turrax (12,000 r/min) until a homogenous mixture was produced. With slight stirring, the produced dispersion was cooled to 30 C. Then the high viscous dispersion from Phases 1 and 2 was added. The mixture was then homogenized at 30 C. by Ultra Turrax (12,000 r/min) until a uniform structure was present. The final formulation which was thus produced was able to be used directly.

EXAMPLE G

Production of a Final Formulation with the Active Ingredient Hypericin for the Treatment of Herpes

(78) Ingredients of Phase 1:

(79) TABLE-US-00020 1.50% by weight hydrogenated phosphatidylcholine 0.05% by weight hypericin 3.00% by weight Butyrospermum parkii 0.25% by weight squalane

(80) Ingredients of Phase 2:

(81) TABLE-US-00021 1.00% by weight glycerine 3.00% by weight ethanol 19.00% by weight water

(82) Ingredients of Phase 3:

(83) TABLE-US-00022 10.00% by weight Oleo europeae oil 14.00% by weight Butyrospermum parkii 0.10% by weight carbomer 0.10% by weight sodium carbomer

(84) Ingredients of Phase 4:

(85) TABLE-US-00023 10.00% by weight ethanol 8.00% by weight sorbitol 0.25% by weight hydroxyethylcellulose ad 100.0% by weight water

(86) Ingredients of Phase 5:

(87) TABLE-US-00024 0.20 aroma vanilla

(88) The ingredients of Phase 1 were heated to 85 C. with uniform stirring until all the ingredients were present in dissolved form. Likewise, Phase 2 was heated in a separate vessel to 85 C. with stirring. Hereafter, the homogenous Phase 2 was added to Phase 1, stirred briefly and thereafter homogenized by means of Ultra Turrax at 24,000 r/min. The pre-emulsion resulting herefrom was micro-dispersed by means of a high pressure homogenizer in 5-7 cycles, pressure 600 bar. The produced dispersion was cooled to 30 C. with uniform stirring.

(89) Phases 3 and 4 were heated respectively in separate vessels to 50 C. with uniform stirring. Phase 4 was then added to Phase 3 and hereafter homogenized by Ultra Turrax (12,000 r/min). With slight stirring, the produced dispersion was cooled to 30 C. Thereafter, Phase 5 was added to the mixture and again briefly homogenized by Ultra Turrax (10,000 r/min) until the aroma agent was worked in uniformly. The high viscous dispersion from Phases 1 and 2 was then added. Hereafter, the mixture was homogenized at 30 C. by Ultra Turrax (12.000 r/min) until a uniform structure was present. The final formulation which was thus produced was able to be used directly.

EXAMPLE H

Production of a Final Formulation with the Active Ingredient Panthenyl Triacetate for the Treatment of Complaints of Dry Nasal Mucosa

(90) Ingredients of Phase 1:

(91) TABLE-US-00025 1.50% by weight hydrogenated phosphatidylcholine 1.00% by weight panthenyl triacetate 0.80% by weight Butyrospermum parkii 1.50% by weight caprylic/capric triglyceride 0.20% by weight squalane

(92) Ingredients of Phase 2:

(93) TABLE-US-00026 1.00% by weight glycerine 1.30% by weight pentylene glycol 17.00% by weight water

(94) Ingredients of Phase 3:

(95) TABLE-US-00027 10.00% by weight caprylic/capric triglyceride 8.00% by weight Butyrospermum parkii 0.10% by weight carbomer 0.10% by weight sodium carbomer 0.10% by weight xanthan gum

(96) Ingredients of Phase 4:

(97) TABLE-US-00028 3.50% by weight pentylene glycol 0.30% by weight sodium hyaluronate ad 100.0% by weight water

(98) The ingredients of Phase 1 were heated to 85 C. with uniform stirring until all the active ingredients were present in dissolved form. Likewise, Phase 2 was heated in a separate vessel to 85 C. with stirring. Phase 2 was then added to Phase 1, stirred briefly and hereafter homogenized by means of Ultra Turrax at 24,000 r/min. The pre-emulsion resulting from this was micro-dispersed by means of a high pressure homogenizer in 2-4 cycles, pressure 700 bar. The produced dispersion was cooled to 30 C. with uniform stirring.

(99) Phases 3 and 4 were heated respectively in separate vessels to 50 C. with uniform stirring. Phase 4 was then added to Phase 3 and hereafter homogenized by Ultra Turrax (12,000 r/min). The produced dispersion was cooled to 30 C. with slight stirring. Thereafter, the high viscous dispersion from Phases 1 and 2 was added. The mixture was then homogenized at 30 C. by Ultra Turrax (12,000 r/min) until a uniform structure was present. The final formulation which was thus produced was able to be used directly.

EXAMPLE I

Production of a Concentrate with the Active Ingredient Octocrylene

(100) Ingredients of Phase 1:

(101) TABLE-US-00029 6.00% by weight hydrogenated phosphatidylcholine 20.00% by weight octocrylene 1.00% by weight squalane

(102) Ingredients of Phase 2:

(103) TABLE-US-00030 4.00% by weight glycerine 5.00% by weight pentylene glycol ad 100.0% by weight water

(104) The ingredients of Phase 1 were heated to 80 C. with uniform stirring until all the ingredients were present in dissolved form. Likewise, Phase 2 was heated to 80 C. in a separate vessel with stirring. Phase 2 was then added to Phase 1, stirred briefly and hereafter homogenized by means of Ultra Turrax at 15,000 r/min. The pre-emulsion resulting herefrom was micro-dispersed by means of a high pressure homogenizer in 5-6 cycles, pressure 800 bar. The produced dispersion is cooled to 30 C. with uniform stirring.

(105) The concentrate which is thus produced can be easily converted into a final formulation ready for use by corresponding dilution, preferably with water, a hydrocolloid and/or alcohols, wherein this final formulation is used as a light protection agent or respectively as a sun protection agent.

EXAMPLE J

Production of a Final Formulation with the Active Ingredient Octocrylene, to be Used as a Light Protection Agent

(106) Ingredients of Phase 1:

(107) TABLE-US-00031 1.50% by weight hydrogenated phosphatidylcholine 5.00% by weight octocrylene 0.25% by weight squalane

(108) Ingredients of Phase 2:

(109) TABLE-US-00032 1.00% by weight glycerine 1.25% by weight pentylene glycol 16.00% by weight water

(110) Ingredients of Phase 3:

(111) TABLE-US-00033 15.00% by weight C12-15 alkyl benzoate 8.00% by weight titanium dioxide 0.10% by weight carbomer 0.10% by weight sodium carbomer 0.10% by weight xanthan gum

(112) Ingredients of Phase 4:

(113) TABLE-US-00034 3.90% by weight pentylene glycol ad 100.0% by weight water

(114) The ingredients of Phase 1 were heated to 80 C. with uniform stirring until all the components were present in dissolved form. Likewise, Phase 2 was heated in a separate vessel to 80 C. with stirring. Phase 2 was then added to Phase 1, stirred briefly and hereafter homogenized by means of Ultra Turrax at 15,000 r/min. The pre-emulsion resulting herefrom was micro-dispersed by means of a high pressure homogenizer in 5-6 cycles, pressure 800 bar. The produced dispersion is cooled to 30 C. with uniform stirring.

(115) Phases 3 and 4 were heated respectively in separate vessels to 30 C. with uniform stirring. Phase 4 was then added to Phase 3 and hereafter homogenized by Ultra Turrax (10,000 r/min). The produced dispersion was cooled to 30 C. with slight stirring. The high viscous dispersion from Phases 1 and 2 was then added. Thereafter, the mixture was homogenized at 30 C. by Ultra Turrax (12,000 r/min) until a uniform structure was present. The final formulation which was thus produced was able to be used directly.

COMPARATIVE EXAMPLE A

(116) In order to be able to carry out a comparative determination of the light protection factor (LPF), a conventional composition was produced which had the same active ingredient in the same concentration as was previously described in Example J. The conventional composition here had the following ingredients:

(117) Ingredients of Phase 1:

(118) TABLE-US-00035 1.50% by weight PEG-20 stearate 5.00% by weight octocrylene 0.25% by weight squalane 1.00% by weight glycerine 15.00% by weight C12-15 alkyl benzoate 8.00% by weight titanium dioxide 0.10% by weight carbomer 0.10% by weight sodium carbomer

(119) Ingredients of Phase 2:

(120) TABLE-US-00036 0.10% by weight xanthan gum 4.15% by weight pentyleneglycol ad 100.0% by weight water

(121) The ingredients of Phase 1 were heated to 80 C. with uniform stirring until all active ingredients were present in dissolved form. Likewise, phase 2 was heated in a separate vessel to 80 C. with stirring. Phase 2 was then added to Phase 1, stirred briefly and hereafter homogenized by means of Ultra Turrax at 15,000 r/min. The produced dispersion was cooled to 30 C. with slight stirring. Thereafter, the mixture was homogenized at 30 C. by Ultra Turrax (15000 r/min) until a uniform structure was present.

EXAMPLE K

Production of a Final Formulation with the Active Ingredient Icaridin, for Use Against Ticks

(122) Ingredients of Phase 1:

(123) TABLE-US-00037 3.00% by weight hydrogenated phosphatidylcholine 10.00% by weight icaridin

(124) Ingredients of Phase 2;

(125) TABLE-US-00038 1.80% by weight pentylene glycol 19.00% by weight water

(126) Ingredients of Phase 3:

(127) TABLE-US-00039 5.00% by weight caprylic/capric triglyceride 0.10% by weight carbomer 0.10% by weight sodium carbomer 0.10% by weight dehydroxanthan gum

(128) Ingredients of Phase 4:

(129) TABLE-US-00040 3.50% by weight pentylene glycol ad 100.0% by weight water

(130) The ingredients of Phase 1 were heated to 80 C. with uniform stirring until all the ingredients were present in dissolved form. Likewise, Phase 2 was heated to 80 C. in a separate vessel with stirring. Phase 2 was then added to Phase 1, stirred briefly and hereafter homogenized by means of Ultra Turrax at 18,000 r/min. The pre-emulsion resulting herefrom was micro-dispersed by means of a high pressure homogenizer in 2-3 cycles, pressure 600 bar. The produced dispersion was cooled to 30 C. with uniform stirring.

(131) Phases 3 and 4 were heated to 30 C. respectively in separate vessels with uniform stirring. Phase 4 was then added to Phase 3 and homogenized by Ultra Turrax (12,000 r/min). The produced dispersion was cooled to 30 C. with slight stirring. Thereafter, the high viscous dispersion from Phases 1 and 2 was added. The mixture was then homogenized at 30 C. by Ultra Turrax (11,000 r/min) until a uniform structure was present. The final formulation which was thus produced was able to be used directly.

COMPARATIVE EXAMPLE B

(132) In order to be able to carry out a comparative determination of the effectiveness of the previously described composition according to Example K against ticks, a conventional composition was produced which, like Example K, had the same active ingredient in the same concentration.

(133) Ingredients of Phase 1:

(134) TABLE-US-00041 3.00% by weight polyglyceryl-3 polyricenoleate 10.00% by weight icaridin 5.00% by weight caprylic/capric triglyceride 0.10% by weight carbomer 0.10% by weight sodium carbomer 0.10% by weight dehydroxanthan gum

(135) Ingredients of Phase 2:

(136) TABLE-US-00042 5.00% by weight pentylene glycol ad 100.0% by weight water

(137) For the production of this conventional cream-like composition, the ingredients of Phase 1 were heated to 80 C. with uniform stirring until all the ingredients were present in dissolved form. Likewise, Phase 2 was heated to 80 C. in a separate vessel with stirring. Phase 2 was then added to Phase 1, stirred briefly and hereafter homogenized by means of Ultra Turrax at 18,000 r/min. The produced dispersion was cooled to 30 C. with slight stirring. The mixture was then homogenized at 30 C. by Ultra Turrax (12,000 r/min) until a uniform cream-like structure was present.

EXAMPLE L

Production of a Final Formulation with the Active Ingredient Permethrin, for Use Against Lice

(138) Ingredients of Phase 1:

(139) TABLE-US-00043 2.00% by weight hydrogenated phosphatidylcholine 0.40% by weight Permethrin

(140) Ingredients of Phase 2:

(141) TABLE-US-00044 1.80% by weight pentylene Glycol 19.00% by weight water

(142) Ingredients of Phase 3:

(143) TABLE-US-00045 5.00% by weight caprylic/capric triglyceride 0.06% by weight carbomer 0.06% by weight sodium carbomer 0.05% by weight dehydroxanthan gum

(144) Ingredients of Phase 4:

(145) TABLE-US-00046 3.50% by weight pentylene glycol ad 100.0% by weight water

(146) The ingredients of Phase 1 were heated to 80 C. with uniform stirring until all the active ingredients were present in dissolved form. Likewise, Phase 2 was heated to 80 C. in a separate vessel with stirring. Phase 2 was then added to Phase 1, stirred briefly and hereafter homogenized by means of Ultra Turrax at 9,000 r/min. The pre-emulsion resulting herefrom was micro-dispersed by means of a high pressure homogenizer in 3-5 cycles, pressure 800 bar. The produced dispersion was cooled to 30 C. with uniform stirring.

(147) Phases 3 and 4 were heated to 30 C. respectively in separate vessels with uniform stirring. Phase 4 was then added to Phase 3 and homogenized by Ultra Turrax (9,000 r/min). The produced dispersion was cooled to 30 C. with slight stirring. Thereafter, the high viscous dispersion from Phases 1 and 2 was added. Hereafter, the mixture was homogenized at 30 C. by Ultra Turrax (9,000 r/min) until a uniform structure was present. The final formulation which was thus produced was able to be used directly.

EXAMPLE M

Production of a Final Formulation with the Active Ingredient Vitamin K, for Use with Rosacea

(148) Ingredients of Phase 1:

(149) TABLE-US-00047 1.50% by weight hydrogenated phosphatidylcholine 5.00% by weight vitamin K 0.20% by weight squalane 0.10% by weight rice bran wax 1.00% by weight caprylic/capric triglyceride 0.25% by weight phenylethyl alcohol

(150) Ingredients of Phase 2:

(151) TABLE-US-00048 18.00% by weight water

(152) Ingredients of Phase 3:

(153) TABLE-US-00049 5.00% by weight caprylic/capric triglyceride 0.10% by weight carbomer 0.10% by weight sodium carbomer 0.20% by weight hydroethyl cellulose

(154) Ingredients of Phase 4:

(155) TABLE-US-00050 3.50% by weight pentylene glycol ad 100.0% by weight water

(156) The ingredients of Phase 1 were heated to 75 C. with uniform stirring until all the ingredients were present in dissolved form. Likewise, Phase 2 was heated to 75 C. in a separate vessel with stirring. Phase 2 was then added to Phase 1, stirred briefly and hereafter homogenized by means of Ultra Turrax at 15,000 r/min. The pre-emulsion resulting herefrom was micro-dispersed by means of a high pressure homogenizer in 3-4 cycles, pressure 800 bar. The produced dispersion was cooled to 30 C. with uniform stirring.

(157) Phases 3 and 4 were heated to 30 C. respectively in separate vessels with uniform stirring. Phase 4 was then added to Phase 3 and hereafter homogenized by Ultra Turrax (12,000 r/min). The produced dispersion was cooled to 30 C. with slight stirring. Thereafter, the high viscous dispersion from Phases 1 and 2 was added. The mixture was then homogenized at 30 C. by Ultra Turrax (10,000 r/min) until a uniform structure was present. The final formulation which was thus produced was able to be used directly.

Evidence of the Effectiveness of the Final Formulation Described in Example G in a Case of Herpes

(158) 10 subjects (6 female, 4 male) aged between 25 years and 55 years, who had all suffered for at least two years from irregularly occurring herpes infections, particularly in the region of the lips and beneath the nose, were treated with the final formulation according to Example G at the peak level of the herpes infection. All subjects complained on the one hand of an intense itching and on the other hand of pain.

(159) In a first series of tests, the subjects were treated with a conventional ointment which contained the active ingredient hypericin in the concentration corresponding to Example G. The number of daily applications of the conventional ointment was left to the subjects themselves.

(160) Before the start of the application, after two days, after four days and after eight days, the extent of the herpes attack and of the accessory symptoms connected therewith was determined and noted by subjective assessment. The following grading was used as a basis for this:

(161) 0=no detectable case of herpes

(162) 1=just still detectable case of herpes

(163) 2=slight case of herpes

(164) 3=medium case of herpes

(165) 4=intense case of herpes

(166) 5=very intense case of herpes

(167) Furthermore, the time up to healing of the acute case of herpes was determined in days, wherein at least a Grade 1 had to be given for this.

(168) The result of this first series of tests is reproduced in the following table.

(169) TABLE-US-00051 Conventional ointment containing hypericin Subject before after 2 after 4 after 8 healing No./Sex start days days days after days 1/m 5 5 4 3 20 2/m 5 4 3 2 17 3/m 5 5 4 3 24 4/m 4 4 3 2 14 5/f 4 4 3 2 8 6/f 3 2 3 2 7 7/f 5 5 4 2 10 8/f 4 4 3 2 7 9/f 5 4 3 1 5 10/f 5 4 4 3 21

(170) The previously selected subjects were then engaged for a second series of tests when they were suffering again from an acute case of herpes. The time varied here between the first series of tests and the second series of tests, depending on the subject, between three months and nine months.

(171) In the second series of tests, the subjects were treated with the composition specified in Example G, with it being left to the subjects themselves to determine the number of daily applications of the composition according to Example G.

(172) The evaluation of this second series of tests took place in an analogous manner to the evaluation of the first series of tests and is reproduced in the following table. It is to be noted here that the subject No. of the first series of tests is identical to the subject No. of the second series of tests.

Composition According to Example G

(173) TABLE-US-00052 Subject before after 2 after 4 after 8 Healing No./Sex start days days days after days 1/m 5 4 3 1 10 2/m 5 3 2 1 8 3/m 4 3 3 1 8 4/m 5 3 2 1 6 5/f 4 3 2 1 5 6/f 4 3 2 0 0 7/f 5 4 3 1 3 8/f 5 4 2 0 0 9/f 4 3 2 0 0 10/f 4 2 2 1 2

(174) The comparison of the previously reproduced two tables clearly proves the superiority of the composition according to Example G compared with the conventional ointment. In particular, all the subjects reported consistently that in particular already after a few applications the itching and the pain distinctly abated, which was not the case with the conventional ointment.

Determining the Light Protection Factor of the Composition According to Example J

(175) The COLIPA light protection factor test method was used to determine the light protection factor. This method is a laboratory method which requires an artificial ultraviolet (UV) light source with defined, known output. On carrying it out, a graduated series of delayed UV erythema reactions is induced on several small areas of the skin of selected subjects.

(176) The subjects must present themselves at the test laboratory at least twice: On the first occasion they are exposed to the required UV doses, on the second occasion the delay of erythema reactions brought about by sun protection products is assessed with an identical test set-up. By the gradual increase of the UV dose, different degrees of skin erythema (reddening as a result of a superficial vasodilation) are produced, which reach a maximum value approximately 24 hours after the UV exposure. The exposure time which brings about an erythema on unprotected skin type II and III according to Fitzpatrick is generally approximately two minutes. The lowest dose which produces a distinct area of erythema is the minimum erythema dose or MED. The MED for unprotected skin (MEDu; u stands for unprotected) and the MED after application of a sun protection agent (i.e. the MED for protected skin=MEDp; p stands for protected) are determined simultaneously on the same subject. The MEDu and the MEDp can be evaluated visually by trained evaluators or instrumentally with a colorimeter. Several preparations can be tested here simultaneously on the same subject. The light protection factor of the preparation is calculated for each subject on the basis of the ratio of MEDp to MEDu. A preparation must be tested on at least 10 subjects. The confidence limits for the average light protection factor are to lie +/20% within the mean value, i.e. when the mean light protection factor is 10, the calculated confidence limits should lie above 8 or respectively below 12. If this is not the case, tests must be carried out on further subjects until the statistical criteria are met or 20 subjects have been used. The mean light protection factor of a preparation is calculated from the results of all subjects.

(177) The COLIPA light protection factor test method furthermore describes a standardized method for the application and distribution of the sun protection agents onto the test surfaces, because this phase of the testing was identified as a substantial source of experimental errors. In all tests, in accordance with the expected light protection factor of the test formulations a standard preparation is to be used according to COLIPA with a correspondingly high or low light protection factor.

(178) An examination of the test area is carried out on the subjects from the lower line of the shoulder blades down to waist height. Evidence of sunburn, suntan, scars, skin lesions and irregular pigmentation is determined on the back of each subject. If, in the opinion of the examiner, one of the listed artefacts is present in a significant manner, the subject is excluded from the study. The examination was carried out on 20 subjects.

(179) Classification of Skin Types According to Fitzpatrick

(180) The skin types are classified as follows

(181) Skin type I tanning: never, sunburn: always

(182) Skin type II tanning: slight, sunburn: always

(183) Skin type III tanning: moderate, sunburn: rare

(184) As UV source in the Solar Light Company's 601-300 Multiport Simulator, the spectrum of a xenon arc lamp is displayed through special filters onto the erythemally effective range (COLIPA spectrum) and applied onto the skin. The simulator is equipped with 6 irradiation fields which can emit different irradiation doses simultaneously. Through an individual time- or output-controlled closure mechanism, different UV doses can be administered and thus a light graduation can be determined. The LPF is determined by measurement of a product field (e.g. sun cream) and an empty field (unprotected skin). The irradiation can be carried out by a rotatable ray output both sitting and lying.

(185) In order to establish the innate reactivity of each subject to UV radiation, a series of UV irradiations are carried out 24 hours before the actual examination. Each irradiation field is 1 cm in diameter. The time intervals are selected as a geometric series, wherein the irradiation duration is extended by 25% with each field. The irradiated areas are assessed 16-24 hours after UV exposure and the MEDu (MED of the unprotected skin) is determined. The MED (minimum erythema dose) serves as an indicator for the dose to be applied for the light protection factor examination (LPF examination). The MED is defined as the irradiation energy which is required in order to produce a weak, but clearly discernible reddening of the skin with sharp delimitation. The irradiation dose in this examination was detected chronologically.

(186) The LPF for the composition according to Example J was determined compared with the LPF of the composition according to Example A at distinct positions on the backs of the subjects (n=20). The determining of the positions was carried out as follows: Marking of the entire test area Marking of the individual test areas at 35 cm.sup.2, respectively for the previously mentioned two examples which are to be compared.

(187) The respective composition (Example J or Comparative Example A) is applied onto each test field in a quantity of 2 mg/cm.sup.20.02. After the application, an interval of approximately 15 min is waited as the action time before the UV irradiation.

(188) After the action time has elapsed, firstly an unprotected area on the subject's back is irradiated. Then the test is repeated on the areas treated with the respective composition.

(189) The same test is repeated on a second test area 2 h after application of the product. The test fields are treated with a series of UV irradiation units of different intensity. The actual exposure time is selected by means of the previously determined MED of the test person and of the assumed LPF of the product. More precisely, the MED is multiplied by the assumed LPF of the product; the exposure time results from this. A 25% geometric series is selected as UV dose. After completion of the irradiation, the position of the test fields is marked. Each subject is requested to cover the entire test area, to protect against further UV irradiation.

(190) The evaluation of the treated and irradiated test fields was carried out by trained personnel 20-24 hours after UV exposure. The individual and averaged LPF values for the composition according to Example J and the composition according to Comparative Example A are indicated in the following table.

(191) Example Sun

(192) TABLE-US-00053 Irradia- tion after action Mean value Standard examined sample time of of the LPF deviation Example J 15 min. 23.6 2.3 Example J 120 min. 21.2 4.6 Comparative Example A 15 min. 13.7 4.5 Comparative Example A 120 min. 9.8 5.9

(193) In connection with the measurement which is carried out, it is also to be mentioned that the high light protection factor of the composition according to Example J was even still present after an action time of 120 minutes, which was not the case with the composition according to Comparative Example A. It can be concluded from this that owing to the particular structure of the composition according to Example J, the latter is positioned in a stable manner in the stratum corneum, which was not the case with the composition according to Comparative Example A. Here, the LPF decreased drastically from 13.7 to 9.8.

(194) Evidence of the effectiveness of the final formulation described in Example K for the prevention of tick contamination In order to test the effectiveness of the composition according to Example K compared with the conventional composition according to Comparative Example B, a live narcotized domestic pig of the genus sus scrofa domestica (age 2 years) was shaved fully on its left side and respectively on its right side. The two sides of the pig were delimited from each other along the spine by a 3 cm wide double-sided adhesive tape, in order to thus prevent a migration of the ticks from one side of the pig to the other side of the pig. The remaining margins of the sides of the pig were likewise provided with this adhesive tape.

(195) After fixing the anaesthetized pig in position in an upright position, the composition according to Example K was applied onto one side of the pig (measurement area approximately 500 cm.sup.2) and the composition according to Comparative Example B was applied onto the other side of the pig (measurement area approximately 500 cm.sup.2) respectively in a concentration of 1 g/10 cm.sup.2 and was rubbed uniformly over the measurement areas. After an action time of 10 minutes, each side of the pig was colonized by a tick population of identical stage of development and of identical number of ticks (respectively 20 ticks).

(196) After a period of four hours after colonization, the number of ticks on each side of the pig was established. A differentiation was made here as to how many ticks had attached themselves firmly and how many ticks still colonized the respective side of the pig without a bite. In addition, the migrated ticks which were fixed in the adhesive strip were counted. In addition, an examination was carried out microscopically as to whether the ticks were still alive after four hours.

(197) The results of this investigation are reproduced in the following table:

(198) TABLE-US-00054 Composition Composition according to according to Comparative Example K Example B Initial tick number 20 20 Tick number without bite 6 1 Tick number with bite 8 16 Migrated ticks 6 3 Dead ticks (total) 16 8

(199) The comparison of the previously reproduced tables clearly proves the superiority of the composition according to Example K compared with the conventional composition according to Comparative Example B. In particular, the fact that only eight ticks have anchored themselves in the skin and that a substantially higher number of dead ticks were able to be found, prove that the composition according to Example K is highly effective.

(200) With regard to the hydrogenated phosphatidylcholines used in Examples A to M, it is to be recorded that these have a concentration of hydrogenated phosphatidylcholine of 933% by weight and that the acyl radicals consist of 85% by weight stearic acid and 14% palmitic acid.