Compositions for cosmetic, pharmaceutic or dietary applications

Description

The present invention relates to a composition of plant extract and / or active ingredients and / or active substances, a carbohydrate and a phospholipid, a method for the preparation of such a composition, and the pharmaceutical, dietary or cosmetic use of such a composition.

[0002] Plant raw materials play an increasingly important role in a composition for pharmaceutical, dietary and cosmetic use. The demand for all-natural formulations is of increasing importance. Plant raw materials, in particular plant extracts with active ingredients, are not always stable and, as a rule, cannot be easily incorporated into the formulation.

[0003] In US 5,387,415 pellets with aloe vera juice are made, the collagen juice is added dropwise to liquid nitrogen at -196 ° C. This method is very laborious and results in a high energy consumption. A similar method is described in US 5,401,502.

[0004] US 5,783,211 describes nanoparticles of bisabolol, a pre-emulsion with lecithin in a high pressure homogenizer followed by spray drying together with starch and maltodextrin. It is always necessary to use a starch matrix there. The products are spray dried. Many herbal extracts and their ingredients are very sensitive and can degrade or decompose during spray drying, which should be avoided.

[0005] US 5,180,713 describes the preparation of pharmaceutical liposomes in organic solvents in the presence of cryoprotectants, e.g. sugars. It is necessary to use organic solvents that are difficult to remove from the final product and which are not desired in natural products. [0006] US 6,534,087 describes foamed active ingredient tablets; lecithins and maltodextrins. The described method cannot produce metered powders or granules with stable properties.

[0007] US 20040234673 discloses a composition with an amorphous carbohydrate phase, with a crystalline phase and a third phase, which is selected from one or more materials composed of flavors, volatile substances and substances that are sensitive to external influences, the 3 phase being is dispersed with an emulsifier in the other two phases. The extrusion of this composition is carried out at high temperatures. When treated at higher temperatures, the components of the plant extracts decompose and can no longer exhibit the desired activity.

[0008] In patent applications EP 209037, EP 209038, EP 275005, EP 275224, EP 283713, EP 300282, EP 304603, EP 441279, EP 464297, EP 1390008, EP 1837030, EP 1844785, plant extracts are stabilized by the formation of an active ingredient complex with phospholipids; for this it is necessary to use solvents such as methylene chloride or methanol. The treatment process is very complicated and requires the use of undesirable solvents.

[0009] The formulation problems and the limited transport and storage stability of the compositions of the cited art are due to the selection of their ingredients, in particular e.g. the quality of the lecithin with a phosphatidylcholine content below 15%.

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[0010] It is therefore an object of the present invention to provide a composition having a high proportion of plant extract and / or ingredients and / or active substances, showing high stability during transport and storage, and easy and gentle processing into formulations, to provide a method for the preparation of such a composition and suitable uses of such a composition.

[0011] The solution is obtained thanks to compositions with the features of claim 1, a method for the preparation of such a composition with the features of claim 6 and uses with the features of claim 7.

The compositions according to the invention contain 28-32% plant extract and / or plant active ingredient, 60-70% maltodextrin and 2-8% phospholipid from the phospholipid fraction with a phosphatidylcholine content of 40-80%. Preference is given to compositions with 30% plant extract and / or plant active ingredient, 67% maltodextrin and 3% phospholipid from the phospholipid fractions with a phosphatidylcholine content of 40-80%. The compositions make it possible to obtain a high concentration of the active ingredient in the formulations. The compositions are free of preservatives and solvents and consist mainly of only natural plant raw materials.

[0013] The plant raw material used is an extract of plants or parts of plants, fruit concentrates, herbal extracts, vegetable oils and the like, such as e.g. Acai extract (Euterpe oleracea), acerola extract (Malpighia glabra), horsetail (Equisetum arvense), Agaricus mushroom extract (Agarius Blazei Murill), aloe (Aloe vera, Aloe barbadensis), apple extract (Malus), extract artichoke leaves (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 (bamboo vulgaris), cucumber crack (Momordica charantia) extract, bitter orange extract (Citrus aurantium), nettle leaf extract (Urtica dioica), nettle root extract (Urtica dioica), broccoli extract (Brassica oleracea ), watercress (Rorippa nasturtium), brazilian urticaria extract (Coleus forskohlii), peppercorn extract (Capsicum frutescens), Centella asiatica (Gotu Kola), cinchona extract, cranberry extract (Vaccinium vitis-daea), turmeric extract (Curcuma longa), Damiana herb extract (Tunera diffusa), dragon fruit extract (Pitahaya), Echinacea purpurea, wheat placenta extract, edelweiss extract (Leotopodium alpinum ), ivy extract (Hedera helix), tribulus terrestris extract, Malabar tamarind extract (Garcinia Cambogia), ginkgo extract (Gingko biloba), ginseng extract (Panax ginseng), pomegranate fruit extract (Punica granatum), grapefruit extract (Citrus paradisi), black bean extract (Griffonia simplicifolia), green tea extract (Camellia sinensis), guarana extract (Paullinia cupana), cucumber extract (Cucumis sativus) , rose fruit extract (Rosa canina), blueberry extract (Vaccinium myrtillus), hibiscus extract (Malvacea), marshmallow extract, honey extracts, hops extract (Humulus), ginger extract (Zingiber officinale), Icelandic moss (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 (Cucurbita pepo), cornflower extract (Centaurea cyanus), lotus flower extract, dandelion root extract (Taraxacum officinale), poppy seed extract (Lepidium peruvianum), magnolia flower extract, mango extracts, milk thistle extract (Silybum marianum), calendula (Calendula Officinalis), mate extract (Hex, paraguariensis) barbed mouse (Rugcus aculeatus) extract, sea algae extracts, cranberry (Cranberry, Vaccinium macrocarpon),

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V15201PL00 / TS Moringa Oleifera extract, Musk mallow (Malva moschata), Evening primrose oil extract (Azadirachta indica), Nettle extract (Urticaceae), Olive tree leaf extract (Olea europea), Orange extract (Hesperidin), Extract orchid extract, papaya extract (Carica papaya), peppermint extracts, Carica papaya (Geissospermum), bitter orange extract (Citrus aurantioum), lingonberry extract (Vaccinium Vitas-idaea), Pygeum Afrikanum extract (Prunus africana), grapevine extracts, extracts of resveratrol (Polygonum cuspidatum), rooibos (Aspalasthus Linnearis), rose flower extract, horse chestnut extract (Aesculus hippocastanum, chestnut), rosemary (Rosus officinalis) , red clover extract (Trifolium platense), grapevine extract (Vitis vinifera), saw palmetto extract (Serenoa repens), lettuce 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), willow bark (Willow Bark, Salix alba), licorice (Glycyrrhiza), devil's claw root extract (Harpagophytum procumbens), thymus extract (Thymus vulgaris), tomato extract (Lycopersicum esculentum), grape seed extract (Vitis vinifera), grape skin extract (Vitis vinifera), turnip turnip (Rorippa amphibia), willow bark extract (Salix alba), mugwort extract (Artemisia absinthium), white tea extract, Chinese yam root (Dioscorea opposita), jochimba extract (Pausinystalia yohimbe), witch hazel (Hamamelis), cinnamon bark extract (Cinnamomum cassia, Presl), lemon extract (Citrus), onion extract (Allium cepa).

[0014] In addition to the extracts, it is also possible to use the herbal active substances or ingredients, alone or in combination with the extracts. As herbal active substances are used, e.g. glycyrrhizin, caffeine, proanthocyanidin, hesperetin, rutin, luteolin, polyphenols, aspalatin, oleuropin, theobromine, bioflavonoids or combinations of glycyrrhizin and extracts of Glycerica glabra, caffeine and Camellia sinensis or Camellia albaant, or guarana, and Vitis vinifera (grapevine), hesperidin and rutin and Citrus aurantii amara peel extract, luteolin and Chamomilla reticulataq, polyphenols and Camellia sinensis or Vaccinium macrocarpon (cranberry), caffeine / theobromine, and Hex paraguaiensis (mate), bioflavonoids and green tea extract (Camellia sinensis), curcumin and Curcuma longa, epigallocatechin gallate, hespicin, epigallocatechin, nebohedyin, epigallocatechin, epidhedyin, epicatin, epigallocatechin, asiaticoside, ellagotanin, chlorogenic acid, oleuropein, arbutin, betulin, esculin, silymarin, etc., especially puerarin isoflavone (with or as Pueraria lobata extract), oleuropein (with or as Olea europea leaf extract), luteolin (with or as Chamilla reticulate extract), baicalin (with or as Scutellaria baicalinensis root extract), chlorogenic acid (with or as an extract of Eucommia ulmoides / gutta-percha), apigenin ( with or as Citrus grandis peel extract), hesperidin (with or as Citrus aurantium amara peel extract), caffeine (from Paulinia cupana / guarana extract), aspalatin (with or as Aspalatus linnearis / rooibos extract), rutin (with or as extract of Sophora japonica), polyphenol, quinic acid (with or as extract of Vaccinium marcrocarpon / cranberry), ellagotanin (with or as extract of Punica granatum / pomegranate), asiaticoside (with or as extract of Centella asiatica) , proanthcyanidins (with or as extract of Vitis vinifera (proanthocyanidins)), rutin (with or as extract of Viola odorata), 18beta-glycyrrhetinic acid (with or as extract of Liquiritia), glycyrrhizin (with or as extract of Liquiritia), theanine , polyphenols (with or as Camellia / Thea sinensis extract), caffeoylquinic acid, caffeine, theobromine (with or as extract from Hex paraguaiens / mate).

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[0015] Phospholipids used are phospholipids or phospholipid fractions, derived from plant raw materials such as soybeans, sunflower seeds, rapeseed, peanuts, corn, lupins or cotton seeds, or egg yolk phospholipids with a phosphatidylcholine content of 40-80% or certain phospholipids such as diacylphosphatidylcholine (e.g. dimyristoyl-, dipalmitoyl-, disterooylphosphatidylcholine), hydrogenated phospholipids, hydrolysed or modified phospholipids with a phosphatidylcholine content of 40-80%.

Lecithin is composed of neutral fats, glycolipids and phospholipids. Phospholipids consist of e.g. phosphatidylcholine (PC), phosphatidylethanolamine (PE), phosphatidylinositol (PI), phosphatidylserine (PS), lysophosphatidylcholine (LPC), lysophosphatidylethanolamine (LPE), lysophosphatolamine (LPE), lysophosphatol, etc. -Othmer Encyclopedia of Chemical Technology, Fourth Edition, Volume 15; Willem van Nieuwenhuyzen, Fett / Lipid 99 (1997), No. 1, pp. 10-14, Willem van Nieuwenhuyzen, Eur. J. Lipid Sei. Technol. (2008), 472-486. Commercially available lecithin contains approximately 12-15% phosphatidylcholine.

Oil-free lecithin, also known as pure lecithin, contains 20-25% phosphatidylcholine. By fractionating from ethanol, phospholipid fractions with 30 to 100% phosphatidylcholine content can be produced. Commercially available products enriched in phosphatidylcholine are, for example, soybean phospholipids such as Lipoid S 20 (approx. 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 (> 94% PC), Phospholipon 20 (ca. 20-24% PC, 16-22% PE), Phospholipon 50 (approx. 45-50% PC), Phospholipon 85G (> 80% PC),

Phospholipon 9OG (> 95% PC) or rapeseed phospholipids such as Lipoid R20 (approx. 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, 7% PE), Lipoid R100 (> 94% PC) or rapeseed phospholipids such as Lipoid R20 (approx. 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, 7% PE), Lipoid R100 (> 94% PC) or soy phospholipids from non-GMO soybeans such as Lipoid P45 (45% PC, 10-18% PE ), Lipoid P75 (75% PC, 7% PE), Lipoid P100 (> 94% PC).

[0017] Maltodextrin is used as the carbohydrate.

The preparation of the compositions according to the invention is carried out in such a way that the ingredients are dissolved or dispersed simultaneously or sequentially at room temperature in water and homogenized in conventional homogenization devices, e.g. with a microfluidizer, in 1 to 3 cycles, followed by filtration or sterile filtration, e.g. with 2-8 μm candle filters, and then gently lyophilized or dried under vacuum at -30 ° C to + 45 ° C. The dried product may be ground using suitable equipment with an opening diameter of 0.5-1.5 mm to the desired particle size.

[0019] Stable liposome preparations can be prepared by redispersing.

[0020] The dried composition is stable during transport and storage, and can be easily incorporated into cosmetic, dietary and pharmaceutical preparations. Its advantages are good solubility, improved wettability of the active ingredient, optimized dispersion of the active ingredient, improved stability of the active ingredient with respect to environmental influences, optimized smell and taste of the active ingredient. When incorporating the new compositions into cosmetic, dietary or pharmaceutical preparations, optimal bioavailability is achieved. The formulations are e.g. oral such as powders, granules, tablets, capsules and are topical preparations such as creams, milks etc. with the addition of the usual excipients.

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Examples

Example 1 (not according to the invention)

[0021] Aloe Vera 10 kg (10%) is mixed with 87 kg (87%) maltodextrin and 3 kg (3%) Lipoid P45) and dispersed in 100 kg of water, then homogenized 2x with a microfluidizer. The dispersion is then sterile filtered through a 0.2 µm candle filter in a laminar flow, frozen at -30 ° C and vacuum dried at -35 ° C to at most + 45 ° C.

[0022] After drying, the agglomerates were milled.

Example 2

[0023]

White tea extract: 30%

Maltodextrin: 67%

Lipoid P 45: 3%

[0024] The preparation is analogous to Example 1.

Example 3

[0025]

Green tea extract: 30%

Maltodextrin: 67%

Lipoid P 45: 3%

[0026] The preparation is analogous to Example 1.

Example 4

[0027]

Hibiscus extract: 30%

Maltodextrin: 67%

Lipoid P 45: 3%

[0028] The preparation is analogous to Example 1.

Example 5

[0029]

Guarana extract: 30%

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Maltodextrin: 67%

Lipoid P 45: 3%

[0030] The preparation is analogous to Example 1.

Example 6

[0031]

Citric acid: 15%

Tartaric acid: 10%

Lactic acid: 5%

Aerosil: 5%

Maltodextrin: 62%

Lipoic P45: 3%

[0032] The preparation is analogous to Example 1.

Example 7 (not according to the invention)

[0033]

White tea extract: 20%

Maltodextrin: 70%

Lipoid S20: 10%

[0034] The preparation is analogous to Example 1.

Example 8: (not according to the invention)

[0035]

Green tea extract (with 1% caffeine and 5% polyphenols): 40%

Trehalose: 59%

Lipoid S75: 1%

[0036] The preparation is analogous to Example 1.

Example 9 (not according to the invention)

[0037]

Guarana extract: 20%

Glucose: 78%

Phospholipon 80: 2%

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[0038] The preparation is analogous to Example 1.

Example 10 (not according to the invention)

[0039]

White tea extract: 28%

Mannitol: 70%

Lipoid S80: 2%

[0040] The preparation is analogous to Example 1.

[0041] Cosmetic preparations are preferred.

Example 11

Producing a light cream

[0042]

Phase A: 40.0 g SLM 2005 (SLM 2005 = Lipoid SLM 20 base formulation consisting of hydrogenated soy lecithin, ethanol, glycerin and medium chain triglycerides).

Phase B: 82.8 g distilled water, 0.2 g Keltrol CGG-SFT (xanthan gum with laminar flow rheology for clear solutions that are primarily intended for use in cosmetic and other personal care products. which is stable over a wide range of pH values), 1.0 g of Phospholipon 80H, 1.0 g of the composition of Example 1-5

Phase C: 36.0 g of Miglyol, 12.0 g of Jojoba Oil, 2.0 g of Vitamin E Acetate

Phase D: 12.0g Ethanol, 6.0g Glycerin, 6.0g Hydrolite 1.0g Panthenol

[0043] Phase B is heated to 60-65 ° C until all ingredients are dissolved, then it is introduced into phase A while stirring at 40 ° C, then phase C is added with stirring, followed by phase D and for about 1 minute homogenizes with an Ultra-Turax at 40 ° C.

Example 12

Producing a light cream

[0044]

Phase A: 40.0 g SLM 2005

Phase B: 77.8g Distilled Water, 0.2g Keltrol CG SFT, Phospholipon 80H

Phase C: 36.0 g of Miglyol, 12.0 g of jojoba oil, 2.0 g of tocopherol acetate

Phase D: 12.0 g Ethanol, 6.0 g Glycerin, 6.0 g Hydrolite, 1 g Panthenol

Phase E: 5.0 g of distilled water, 1.0 g of the composition of Example 1-5.

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[0045] Phase B is heated to 60-65 ° C until the components are completely dissolved, then it is introduced into phase A while stirring at 40 ° C; phase C is then added with stirring and homogenized; then homogenized phase D is added at 400 ° C and homogenized by stirring for about 1 minute with a Turrax at 40 ° C.

[0046] Phase E is then added under cold stirring.

Example 13

Producing milk

[0047]

Phase A: 20.0 g SLM 2005

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 Phase C: 30.0 g of Miglyol, 6.0 g of jojoba oil, 2.0 g of tocopherol acetate

Phase D: 14.0 g of Ethanol, 106.0 g of Glycerin, 6.0 g of Hydrolite

[0048] Phase B is heated to 60-65 ° C until the components are completely dissolved, then, while stirring at 40 ° C, it is introduced into phase A; phase C is then added and mixed for homogenization, finally phase D is added and, with stirring for ca. 1 minute, it is homogenized with an Ultra-Turax at 40 ° C.

Example 14

Producing milk

[0049]

Phase A: 20.0 g SLM 2005

Phase B: 97.6 g of distilled water, 0.4 g of Keltrol CGG-SFT,

3.0 g Phospholipon 80H = hydrogenated phospholipid with approx. 80% ydylcholine phosphate , 1.0 g of the composition according to Example 1-5, 1.0 g panthenol

Phase C: 30.0 g of Miglyol ester = fatty acid ester, 6.0 g of jojoba oil, 1.0 g of tocopherol acetate, 14.0 g of ethanol, 10.0 g of glycerin, 6.0 g of Hydrolite,

Phase D: 10.0 g of distilled water, 1.0 g of the composition of Example 1-5.

[0050] Phase B is heated to 60-65 ° C until the components are completely dissolved, then it is introduced into phase A while stirring at 40 ° C, after which phase C is added and mixed for homogenization, and finally the phase is added. D, and, while stirring for ca. 1 minute, homogenized with an Ultra-Turax device at 40 ° C.

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Example 15

cream

[0051]

Phase A: 18.0 g of Miglyol 812, 9.0 g of Tegosoft DC, 10.0 g of Avocado Oil, 6.0 g of Lanette 18, 2.0 g of Tegin M, 0.2 g of Stearic Acid, 1.0 g tocopherol acetate

Phase B: 2.0 g TegoCare Cg 90; 6.0 g of glycerin, 1.0 g of panthenol, 0.4 g of allantoin, 132.2 g of water

Phase C: 1.0 g of the composition of Example 1-5, 9.0 g of water

Phase D: 0.4 g of preservative.

[0052] Phases A and B are heated to 80 ° C. Phase B is introduced into phase A with stirring and then homogenized for 1 minute using the Ultra-Turax. During the subsequent cold mixing, phases C and D are introduced while stirring.