Compositions for cosmetic, pharmaceutic or dietary applications

The present invention relates to a composition of vegetable extract and / or ingredients and / or active ingredients, carbohydrate and phospholipid, a process for the preparation of such a composition and the pharmaceutical, dietetic or cosmetic use of such a composition.

Plant raw materials play an increasingly important role in the preparation of pharmaceutical, dietetic and cosmetic applications. The demand for pure natural formulations is of increasing importance. Herbal raw materials, especially herbal extracts with active ingredients are not always stable and usually not easy to incorporate into a formulation.

In the <patcit id="pcit0001" dnum="US5387415A"><text>US 5,387,415</text></patcit> Aloe vera juice pellets are made by dropping the juice with collagen in liquid nitrogen at -196 ° C. The process is very labor intensive and leads to high energy consumption. A similar procedure is in<patcit id="pcit0002" dnum="US5401502A"><text>US 5,401,502</text></patcit> described.

<patcit id="pcit0003" dnum="US5783211A"><text>US 5,783,211</text></patcit> describes bisabolol nanoparticles, preemulsion with lecithin in a high-pressure homogenizer, then spray-dried with starch and maltodextrin. It always has to be worked with a strength matrix. The products are spray-dried. Many herbal extracts and their ingredients are very sensitive and can be decomposed or degraded during spray drying, which should be avoided.

<patcit id="pcit0004" dnum="US5180713A"><text>US 5,180,713</text></patcit> describes the preparation of pharmaceutical liposomes in organic solvents in the presence of cryoprotectants, such as sugars. It must be worked in organic solvents that are difficult to remove from the final product and are not desirable in natural products.

<patcit id="pcit0005" dnum="US6534087B"><text>US 6,534,087</text></patcit> describes foamed tablets of active ingredient; Lecithin and maltodextrin. From this, no metered powders or granules with stable properties can be produced.

<patcit id="pcit0006" dnum="US20040234673A"><text>US 20040234673</text></patcit> discloses a composition having an amorphous carbohydrate phase, a crystalline phase, and a third phase selected from one or more of flavors, volatiles, and materials that are sensitive to external agents, wherein the third phase is formed in the other two phases is dispersed by means of emulsifier. The extrusion of this composition takes place at high temperatures. By working at higher temperatures, the ingredients of plant extracts are decomposed and can not develop their desired activity.

In the patent applications <patcit id="pcit0007" dnum="EP209037A"><text>EP 209037</text></patcit>. <patcit id="pcit0008" dnum="EP209038A"><text>EP 209038</text></patcit>. <patcit id="pcit0009" dnum="EP275005A"><text>EP 275005</text></patcit>. <patcit id="pcit0010" dnum="EP275224A"><text>EP 275224</text></patcit>. <patcit id="pcit0011" dnum="EP283713A"><text>EP 283713</text></patcit>. <patcit id="pcit0012" dnum="EP300282A"><text>EP 300282</text></patcit>. <patcit id="pcit0013" dnum="EP304603A"><text>EP 304603</text></patcit>. <patcit id="pcit0014" dnum="EP441279A"><text>EP 441279</text></patcit>. <patcit id="pcit0015" dnum="EP464297A"><text>EP 464297</text></patcit>. <patcit id="pcit0016" dnum="EP1390008A"><text>EP 1390008</text></patcit>. <patcit id="pcit0017" dnum="EP1837030A"><text>EP 1837030</text></patcit>. <patcit id="pcit0018" dnum="EP1844785A"><text>EP 1844785</text></patcit> plant extracts are stabilized by complex formation of the active ingredients with phospholipids; this requires working in solvents such as methylene chloride or methanol. The procedure is very complex and requires the use of questionable solvents.

The problems of formulation and the limited stability in transport and storage of the compositions of said prior art are due to the selection of their components, in particular z. B. the quality of lecithins with Phosphatidylcholingehalten of less than 15%.

The present invention is therefore based on the object to provide a composition which has a high content of plant extract and / or ingredients and / or active ingredients, has high stability during transport and storage and can be processed easily and gently in formulations, a process for Preparation of such a composition and to provide suitable applications of such a composition.

The solution is carried out with compositions having the features of claim 1, a process for producing such a composition having the features of claim 6 and with applications having the features of claim 7.

The compositions of the invention contain 28-32% vegetable extract and / or herbal active ingredient, 60-70% maltodextrin and 2-8% phospholipid from phospholipid fractions having a phosphatidyl choline content of 40-80%. Preferred are compositions with 30% vegetable extract and / or vegetable active ingredient, 67% maltodextrin and 3% phospholipid from phospholipid fractions having a phosphatidyl choline content of 40-80%. The compositions make it possible to achieve high active ingredient contents in the formulations. The compositions are preservative and solvent-free and consist largely only of natural vegetable raw materials.

As a vegetable raw material extract of plants or plant parts, fruit concentrates, herbal extracts, vegetable oils and the like in question such as acai extract (Euterpe oleracea), acerola extract (Malpighia glabra), field horsetail (Equisetum arvense, horsetail), agaric extract (Agarius blazei murill), aloe (aloe vera, aloe barbadensis), apple extract (malus), artichoke leaf extract (cynara scolymus), artichoke flower extract (cynara edulis), arnica (Arnica montana), oyster extract, ostrea edulis), valerian root extract (valeriana officinalis), bearberry leaf extract (artostaphylos uva-ursi), bamboo extract (Bambus vulgaris, Bamboo), bitter melon extract (Momordica charantia), bitter orange extract (Citrus aurantium), nettle leaf extract (Urtica dioica), nettle root extract (Urtica dioica),Broccoli extract (Brassica oleracea), watercress (Rorippa nasturtium), stinging nettle extract (Coleus forskohlii), capsicum extract (Capsicum frutescens), Centella asiatica (Gotu kola), cinchona extract (Cinchona), cranberry extract (Vaccinium vitis-daea), curcuma extract (Curcuma longa), Damiana Extract (Tunera diffusa), Dragon Fruit Extract (Pitahaya), Echinacea Purpurea, Wheat Placenta Extract, Edelweiss Extract (Leotopodium alpinum), Ivy Extract (Hedera helix), Earth Root Thorn Extract (Tribulus terrestris), Garcinia Cambogia Extract (Garcinia Cambogia), Ginkgo Extract (Ginkgo biloba) , Ginseng extract (Panax ginseng), pomegranate extract (Punica granatum), grapefruit extract (Citrus paradisi), griffonia extract (Griffonia simplicifolia), green tea extract (Camellia sinensis), guarana extract (Paullinia cupana), cucumber extract (Cucumis sativus),Rosehip extract (Rosa canina), blueberry extract (Vaccinium myrtillus), hibiscus extract (Malvacea), mallow extract, honey extract, hops extract (Humulus), ginger extract (Zingiber officinale), Icelandic mosses (Ceteraria islandica), jojoba extract (Simmondsia chinensis), St. John's wort (St. Johns Wort, Hypericum Perforatum), coffee concentrate, cocoa bean extract (Theobroma cacao), cactus flower extract, chamomile flower extract (Matricaria recutita, Chamomile, Matricaria chamomila), carrot extract (Daucus carota), kiwi extract (Aperygidae), kudzu extract (Pueraria lobata), coconut milk extract, pumpkin seed extract (Curcurbita pepo), cornflower extract (Centaurea cyanus), lotus flower extract, dandelion root extract (Taraxacum officinale), macae extract (Lepidium peruvianum), magnolia blossom extract, mango extracts, milk thistle extract (Silybum marianum),Mariengold (Calendula officinaleis), Mate extract (Hex paraguariensis), Butcher's wort extract (Rugcus aculeatus), Seaweed extracts, Cranberry (Cranberry, Cranberry, Vaccinium macrocarpon), Moringa oleiferae extract, Musk mallow (Malva moschata), Evening primrose oil extract (Azadirachta indica), Nettle extract (Urticaceae) , Olive leaf extract (Olea europea), Orange extract (Hespridin), Orchid extract, Papaya extract (Carica papaya), Peppermint extracts, Carica papaya (Geissospermum), Pomeranie extract (Citrus aurantioum), Cranberry extract (Vaccinium vitas-ideea), Pygeum African extract (Prunus africana), Grapevine extracts, resveratrol extract (Polygonum cuspidatum), rooibos (Aspalasthus linnearis), rose petal extract, horse chestnut extract (Aesculus hippocastanum, Horse chestnut), rosemary (Rosmary, Rosemarinus officinalis),Red Clover Extract (Trifolium platense), Red Wine Extract (Vitis vinifera), Saw Palmetto Extract (Serenoa repens), Salad Extract (Lactuca sativa), Sandalwood Extract (Santalum rubrum), Sage (Sage, Salvia officinalis), Horsetail Extract (Equisetum), Yarrow Extract (Achillea millefolium), Black pepper extract (Piper nigrum), black tea extract, water lily extract (Nymphaea), white willow, (Willow Bark, Salix Alba), licorice (Glycyrrhiza), devil's claw root extract (Harpagophytum procumbens), thyme extract (Thymus vulgaris), tomato extract (Lycopersicum esculentum), grape seed extract ( Vitis vinifera), grape skin extract (Vitis vinifera), water cress (Rorippa amphibia), willow bark extract (Salix alba), frankincense extract (Artemisia absinthium), white tea extract, yam root extract (Dioscorea opposita), yohimbine extract (Pausinystalia yohimbe),Witch hazel (Hamamelis), cinnamon bark extract (Cinnamomum cassia Presl), lemon extract (Citrus), onion extract (Allium cepa).

In addition to the extracts also herbal active ingredients or ingredients can be used alone or in combination with the extracts. Suitable herbal active substances are, for example: glycyrrhizin, caffeine, proanthocianidine, hesperitin, rutin, luteolin, polyphenols, aspalatin, oleuropine, theobromine, bioflavanoids or combinations of glycyrrhizin and glycerica glabra extracts, caffeine and camellia sinesis or camellia alba or guarana (Paulinia cubana ) or Coffes arabica, Proanthocianidin and Vitis vinifera (grapevine), Hespiridin and Rutin and Citrus aurantii amara peel extract, Luteolin and Chamomilla reticulataq, Polyphenole and Camellia sinensis or Vaccinium macrocarpon (Cranberry), Caffeine / Theobromine and Hex paraguaiensis (Mate), Biovlavanoids and Green tea extract (Camellia sinensis), curcumin and Curcuma longa, epigallocatechin gallate,

As phospholipids are phospholipids and phospholipid fractions of vegetable raw materials such as soybeans, sunflower, oilseed rape, peanut, corn, lupins or cottonseed or Eigelbphospholipide with a phosphatidylcholine content of 40-80% or defined phospholipids such as di-acylphosphatidylcholine (such as. B. dimyristoyl, dipalmitoyl, Disteraoylphosphatidylcholin), hydrogenated phospholipids, hydrolyzed or modified phospholipids having a phosphatidylcholine content of 40-80% in question.

Lecithin is composed of neutralipids, glycolipids and phospholipids. The phospholipids are composed of, for example, phosphatidylcholine (PC), phosphatidylethanolamine (PE), phosphatidylinositol (PI), phosphatidylserine (PS), lysophosphatidylcholine (LPC), lysophosphatidylethanolamine (LPE), lysophosphatidylinositol (LPI), etc. (<nplcit id="ncit0001" npl-type="b"><text>A. Wendel Lecithin, Kirk-Othmer Encyclopedia of Chemical Technology, Fourth Edition, Volume 15; Willem van Nieuwenhuyzen, Fett / Lipid 99 (1997), No. 1, S10-14</text></nplcit>. <nplcit id="ncit0002" npl-type="s"><text>Willem van Nieuwenhuyzen, Eur. J. Lipid Sei. Technol. (2008), 472-486</text></nplcit>, Commercially available lecithin contains about 12-15% phosphatidylcholine. Deoiled lecithin, also called pure lecithin, contains 20-25% phosphatidylcholine. By fractionation with ethanol, phospholipid fractions can be produced with 30 to 100% phosphatidylcholine content. Phosphatidylcholine-enriched commercial products are, for example, phospholipids from soy, such as Lipoid S 20 (approximately 20-24% PC, 16-22% PE), Lipoid S45 (45% PC, 10-18% PE), Lipoid S75 (70% PC , 7-10% PE), Lipoid S80 (75% PC, 7% PE), Lipoid SIOO (&gt; 94% PC), Phospholipon 20 (approximately 20-24% PC, 16-22% PE), Phospholipon 50 ( about 45-50% PC), phospholipon 85G (&gt; 80% PC), phospholipon 9OG (&gt; 95% PC) or phospholipids from rapeseed, such as Lipoid R20 (about 20-24% PC, 16-22% PE) , Lipoid R75 (70% PC, 7-10% PE), Lipoid R45 (45% PC, 10-18% PE), Lipoid R75 (75% PC, 7% PE), Lipoid R80 (75% PC,

The carbohydrate used is maltodextrin.

The preparation of the compositions according to the invention is carried out by simultaneously or sequentially dissolved or dispersed in water at room temperature in water and homogenized in conventional devices, such as by Microfluidizer, 1 to 3 passes, homogenized, then filtered or sterile filtered, z. B. by 2-8 microns filter cartridges, and then gently at -30 ° C to +45 ° C freeze or vacuum dried. The dried product can be ground to the desired grain size with appropriate equipment at a hole diameter of 0.5-1.5 mm.

During redispersion, stable liposomal preparations can be prepared.

The dried composition is stable to transport and storage and can be easily incorporated into cosmetic, dietetic and pharmaceutical formulations. Advantages are the good solubility, the wettability of the active ingredient is improved, the dispersing behavior of the active ingredient is optimized, the stability of the active ingredient against environmental influences is improved, the smell and taste of the active ingredient is optimized. When processing the novel compositions in cosmetic, dietetic or pharmaceutical formulations optimum bioavailability is achieved. Formulations are, for example, orally, such as powder granules, tablets, capsules, and topical preparations such as creams, lotion, etc., with the addition of the usual auxiliaries.

Examples:

Example 1 (not according to the invention)

Aloe Vera 10 kg (10%) are mixed with 87 kg (87%) of maltodextrin and 3 kg (3%) of Lipoid P45 and dispersed in 100 kg of water and then homogenized twice using a Microfluidizer. The dispersion is then sterile filtered through a 0.2 micron filter cartridge under laminar flow, frozen at -30 ° C and dried in vacuo at -35 ° C to a maximum of +45 ° C.

After drying, the agglomerates are ground.

Example 2

<ul><li>White tea extract: 30%</li><li>Maltodextrin: 67%</li><li>Lipoid P 45: 3%</li></ul>

The preparation is carried out analogously to Example 1.

Example 3

<ul><li>Green tea extract: 30%</li><li>Maltodextrin: 67%</li><li>Lipoid P 45: 3%</li></ul>

The preparation is carried out analogously to Example 1.

Example 4

<ul><li>Hibiscus extract: 30%</li><li>Maltodextrin: 67%</li><li>Lipoid P 45: 3%</li></ul>

The preparation is carried out analogously to Example 1.

Example 5

<ul><li>Guarana extract: 30%</li><li>Maltodextrin: 67%</li><li>Lipoid P 45: 3%</li></ul>

The preparation is carried out analogously to Example 1.

Example 6

<ul><li>Citric acid: 15%</li><li>Tartaric acid: 10%</li><li>Lactic acid: 5%</li><li>Aerosil: 5%</li><li>Maltodextrin: 62%</li><li>Lipoid P45: 3%</li></ul>

The preparation is carried out analogously to Example 1.

Example 7 (not according to the invention)

<ul><li>White tea extract: 20%</li><li>Maltodextrin: 70%</li><li>Lipoid S20: 10%</li></ul>

The preparation is carried out analogously to Example 1.

Example 8 (not according to the invention)

<ul><li>Green tea extract (containing 1% caffeine and 5% polyphenols): 40%</li><li>Threhalose: 59%</li><li>Lipoid S75: 1%</li></ul>

The preparation is carried out analogously to Example 1.

Example 9 (not according to the invention)

<ul><li>Guarana extract: 20%</li><li>Glucose: 78%</li><li>Phospholiphone 80: 2%</li></ul>

The preparation is carried out analogously to Example 1.

Example 10 (not according to the invention)

<ul><li>White tea extract: 28%</li><li>Mannitol: 70%</li><li>Lipoid S80: 2%</li></ul>

The preparation is carried out analogously to Example 1.

Preference is given to cosmetic preparations.

Example 11

Preparation of a soft cream

<ul><li>Phase A: 40.0 g SLM 2005 (SLM 2005 = Lipoid SLM 20 base formulation consisting of hydrogenated soy lecithin, ethanol, glycerol and medium chain triglycerides).</li><li>Phase B: 82.8 g of distilled water, 0.2 g of Keltrol CGG-SFT (xanthan gum product with laminar-flow rheology for transparent solutions specially designed for use in cosmetic and other personal care products.) Dust-free, low-viscosity powder that is stable is over a wide pH range), 1.0 g Phospholipon 80H, 1.0 g Composition according to Example 1-5</li><li>Phase C: 36.0 g miglyol, 12.0 g jojoba oil, 2.0 g vitamin E acetate</li><li>Phase D: 12.0 g ethanol, 6.0 g glycerol, 6.0 g hydrolite, 1.0 g panthenol</li></ul>

Phase B is heated to 60-65 ° C until all ingredients are dissolved and then incorporated with stirring at 40 ° C to phase A, then stirred phase C and then thereafter phase D is added with stirring for about 1 minute on Ultra-Turax Homogenized at 40 ° C.

Example 12

Preparation of a soft cream

<ul><li>Phase A: 40.0 g SLM 2005</li><li>Phase B: 77.8 g distilled water, 0.2 g Keltrol CG-SFT, Phospholipon 80H</li><li>Phase C: 36.0 g miglyol, 12.0 g jojoba oil, 2.0 g tocopherol acetate</li><li>Phase D: 12.0 g of ethanol, 6.0 g of glycerol, 6.0 g of hydrolite, 1 g of panthenol</li><li>Phase E: 5.0 g of distilled water, 1.0 g of the composition according to Example 1-5.</li></ul>

Phase B is heated to 60-65 ° C until all components are dissolved and then incorporated with stirring at 40 ° C to Phase A; Thereafter, phase C is added with stirring and homogenized; Thereafter, the homogenized at 400 ° C, phase D is added and homogenized with stirring for about 1 minute on Turax at 40 ° C.

Thereafter, the phase E is added with cold stirring.

Example 13

Preparation of a lotion

<ul><li>Phase A: 20.0 g SLM 2005</li><li>Phase B: 107.6 g of distilled water, 0.4 g of Keltrol CGG-SFT = xanthan gum (see above), 3.0 g of Phospholipon 80H, 1.0 g of the composition of Example 1-5, 1.0 g of panthenol</li><li>Phase C: 30.0 g miglyol, 6.0 g jojoba oil, 2.0 g tocopherol acetate</li><li>Phase D: 14.0 g of ethanol, 106.0 g of glycerol, 6.0 g of hydrolites</li></ul>

Phase B is heated to 60-65 ° C until all components are dissolved and then incorporated with stirring at 40 ° C to Phase A; Thereafter, phase C is added and stirred homogeneously and then the phase D is added and homogenized with stirring for about 1 minute on Ultra-Turax at 40 ° C.

Example 14

Preparation of a lotion

<ul><li>Phase A: 20.0 g SLM 2005</li><li>Phase B: 97.6 g distilled water, 0.4 g Keltrol CGG-SFT, 3.0 g Phospholipon 80H = hydrogenated phospholipid with approx. 80% phosphatidyl choline, 1.0 g composition according to Example 1-5, 1.0 g panthenol</li><li>Phase C: 30.0 g miglyol = fatty acid ester, 6.0 g jojoba oil, 1.0 g tocopherol acetate, 14.0 g ethanol, 10.0 g glycerol, 6.0 g hydrolites,</li><li>Phase D: 10.0 g of distilled water, 1.0 g of the composition according to Example 1-5.</li></ul>

Phase B is heated to 60-65 ° C until all components are dissolved and then incorporated with stirring at 40 ° C to phase A, then phase C is added and stirred homogeneously and then added the phase D and stirring for about 1 minute Homogenized on Ultra-Turax at 40 ° C.

Example 15

cream

<ul><li>Phase A: 18.0 g Miglyol 812, 9.0 g Tegosoft DC, 10.0 g avocado oil, 6.0 g Lanette 18, 2.0 g Tegin M, 0.2 g stearic acid, 1.0 g tocopherol acetate</li><li>Phase B: 2.0 g TegoCare Cg 90; 6.0 g glycerin, 1.0 g panthenol, 0.4 g allatoin, 132.2 g water</li><li>Phase C: 1.0 g of the composition according to Example 1-5, 9.0 g of water</li><li>Phase D: 0.4 g preservative.</li></ul>

Phase A and B are each heated to 80 ° C. Phase B is incorporated in phase A with stirring and then posthumogenised for 1 minute with an Ultra-Turex. In the subsequent Kaltrühren phase C and D is added.