Pharmaceutical or cosmetic composition for a main preparation

Abstract

The pharmaceutical or cosmetic composition comprises the following components: a) a dermatologically acceptable carrier substance, b) a first active substance, and c) a second active substance; wherein d) the first active substance comprises royal jelly; and e) the second active substance comprises retinol, retinol analogs or mixtures thereof.

Description

[0001] Pharmaceutical or cosmetic composition for a main preparation

[0002] The invention relates to a pharmaceutical or cosmetic composition according to the preamble of claim 1.

[0003] The invention is based on the object of creating a combination preparation which avoids the known disadvantages of retinol and retinoids in general and, on the other hand, has an improved effect against age-related changes in the skin.

[0004] The invention solves the problem with a pharmaceutical or cosmetic composition, in particular in the form of a skin preparation, which has the features according to claim 1.

[0005] The advantages achieved by the invention are essentially that, thanks to the composition according to the invention, which contains an additional active ingredient in the form of royal jelly, a surprising immediate effect against skin wrinkles and a demonstrable reduction in wrinkles with regular use.

[0006] By coordinating the active ingredients and their synergistic interaction, the spreading performance, adsorption, moisturizing effect and anti-aging effect are improved.

[0007] Definitions:

[0008] Antioxidants: Antioxidants offer protection against so-called "free radicals." For example, vitamins C and E and their derivatives protect sensitive ingredients in cosmetic products from atmospheric oxygen and free radicals, while also exerting their specific effects in the skin. In contrast, synthetic phenolic antioxidants, e.g., butylhydroxytoluene (INGI: BHT), are classified as pure excipients.

[0009] Additional complexing agents, e.g. based on ethylenediaminetetraacetic acid (INCI: EDTA), citric acid and phosphonic acid salts, can be combined with the actual antioxidants.

[0010] Black pearl extract: is an ingredient extracted from the black mother-of-pearl shells in Tahiti. Emulsifiers: are additives used to blend two immiscible liquids into a finely dispersed mixture, known as an emulsion, and to stabilize this mixture. Natural, membrane-forming substances such as ceramides and phosphatidylcholine represent an alternative to conventional emulsifiers. Similar to the skin's barrier layers, they form layered, lamellar structures in creams, have fewer side effects, and blend seamlessly into the skin's physiology.

[0011] Humectants

[0012] The compositions of the invention conveniently contain moisturizing adjuvants. Non-limiting examples of moisturizing agents that can be used with the compositions of the present invention include amino acids, chondroitin sulfate, diglycerin, erythritol, fructose, glucose, glycerin, glycerin polymers, glycol, 1,2,6-hexanetriol, honey, hyaluronic acid, hydrogenated honey, hydrogenated starch hydrolysate, inositol, lactitol, maltitol, maltose, mannitol, natural moisturizing factor, PEG-15 butanediol, polyglyceryl sorbitol, salts of pyrrolidonecarboxylic acid, potassium PCA, propylene glycol, sodium gluconate, sodium PCA, sorbitol, sucrose, trehalose, urea, and xylitol.

[0013] Royal jelly: is the food used by honeybees to raise their queens. It contains, in particular, royalactin. Glyceryl caprylate: is a particularly effective natural preservative.

[0014] Auxiliary ingredients for cosmetics:

[0015] Cosmetic products typically contain nourishing fatty substances as well as fat- and water-soluble active ingredients, along with numerous other ingredients, depending on their intended use. These can be summarized under the term "excipients" and have a variety of functions. Among other things, they enable the production of very different compositions of products such as creams, gels, pastes, lotions, solutions, varnishes, sticks, powders, and aerosols. They give these products their long-term physical stability for transport and storage, prevent contamination by mold, yeast, and bacteria, increase the chemical stability of sensitive active ingredients to atmospheric oxygen, and influence sensory impressions such as consistency, spreadability on the skin, smell (fragrance), and color. The most commonly used excipient is water (INGI: Aqua).Water is an important component in emulsions and, in conjunction with emulsifiers, serves to distribute nourishing fatty substances in droplets, thus significantly facilitating their application to the skin. Water also acts as a solvent for polar (hydrophilic) active ingredients and excipients. In conjunction with moisture-binding agents, the water content of the preparations leads not only to a temporary, but also to a longer-lasting, measurable increase in skin moisture. Other excipients include preservatives, emulsifiers, surfactants, oils, antioxidants, moisturizers, plasticizers, consistency regulators, chelating agents, stabilizers, fragrances, dyes, and pigments. After adding the dermatological or cosmetic active ingredients in the form of an emulsion, gel, or solution to the resulting preparation, the resulting mixture is stirred until a completely homogeneous mass or liquid is formed.

[0016] Lecithins: are phosphatidylcholines (phospholipids, which are esters of fatty acids, glycerol, phosphoric acid, and choline). Phospholipids are involved in the structure of the lipid bilayer of biomembranes (specifically, in the liposomal encapsulation of the active substances according to the invention).

[0017] Liposomes: Liposomes are small vesicles whose shell consists of a lipid bilayer, similar to a cell membrane. The membrane molecules are characterized by their amphiphilic nature; they possess a hydrophilic head and a hydrophobic tail. There are various known methods for producing liposomes. One such method is described in detail in the US patent application published under number US 2011 3T84Q6.

[0018] Medium-chain triglycerides: Triglycerides that contain medium-chain fatty acids, in particular caproic, caprylic, capric and lauric acid.

[0019] Pentylene glycol: is both a moisturizer and a preservative. It helps inhibit the growth of microorganisms on the skin. Because it is water-soluble, it acts as a solubilizer. Pentylene glycol can be produced from sugarcane bagasse and corn cobs.

[0020] Propylene glycol: is a moisturizer for the skin. In low concentrations, propylene glycol accumulates in the skin cells and binds water there. The water can then no longer escape from the skin. The skin is better hydrated, appears noticeably more radiant, and feels better. Retinol: Retinol, also known as vitamin A, is known for its anti-aging effects and is therefore used in skin care products. It stimulates cell renewal and supports the body's own collagen production. Retinol works in the uppermost layers of the skin and makes the skin smoother and more even-toned, as it can reduce pigmentation spots, smooth fine wrinkles, and shrink large pores. However, retinol certainly does have its disadvantages. The skin must be acclimated to the retinol relatively slowly and with intervals between treatments.

[0021] Retinol analogues: These are chemically different substances to retinol, but have similar effects, especially on the skin.

[0022] Further advantageous embodiments of the invention can be commented as follows:

[0023] In a preferred embodiment of the invention, the two active substances are dispersed in the carrier substance in the form of liposomes. This improves the bioavailability of the active ingredients. In a further embodiment, the two active ingredients are encapsulated and stabilized in liposomes with a size of 150 to 350 nm, preferably 200 to 250 nm, finely distributed in the carrier substance.

[0024] In another embodiment, the two active ingredients are encapsulated separately in the liposomes. Alternatively, the two active ingredients can also be mixed and encapsulated in the liposomes.

[0025] In a special embodiment, the liposome membranes contain lecithins or triglycerides. This results in a synergistic effect between the active ingredients and lecithin.

[0026] In another embodiment, the retinol analogue comes from extracts of cultured dedifferentiated plant cells.

[0027] The retinol analogue can advantageously be selected from the following group:

[0028] - Extract from the Babchi plant;

[0029] - Extract of Hypnea Musciformis;

[0030] - Extract of Sargassum Fifipendula;

[0031] - Algae oligosaccharides,

[0032] -> Xantophyllis, or mixtures thereof.

[0033] In another embodiment, the second active ingredient is Pistacia Lentiscus (Mastic) Gum or Chios mastic gum. In another embodiment, the proportion of royal jelly in the composition is at least 0.0015% by weight, preferably at least 0.0019% by weight.

[0034] In a further embodiment, the proportion of the second active substance in the composition is at least 0.03 wt.%, preferably at least 0.04 wt.%.

[0035] The composition can be in the form of creams, especially skin and eye creams; soaps, lotions, gels or serums.

[0036] In a further embodiment, the composition contains further active ingredients selected from the following group:

[0037] - Crithmum Maritimum, Especially Crithmum Maritimum Callus Culture Filtrate;

[0038] - Hyaluronic acids;

[0039] - Black Pearl Extract;

[0040] - Synthetic tripeptides with a molecular weight below 500 Da;

[0041] - Leaf extract of Plantage lanceolata;

[0042] - xanthan gum;

[0043] - Extract of the bacterium lodobacter ssp.:

[0044] - Tetradecy I -am in obutyroyl va lyl-ami nobutyric acid urea trifluoroacetate

[0045] - Acmella Oleracea extract;

[0046] - Leaf juice of the South African medicinal plant Bulbihe Frutescens:

[0047] - alpha-glucan;

[0048] - Phytosteryi rapeseed glycerides: and

[0049] - Japanese root extract.

[0050] In a specific embodiment, the composition has a pH value higher than 3.5, preferably higher than 4.0. The pH value is advantageously below 6.5, preferably below 6.0.

[0051] In a further embodiment, the ratio between the first active substance and the second active substance is in the range of 1:4 to 1:35, preferably in the range of 1:15 to 1:27,

[0052] The carrier substance of the composition can be water or an aqueous emulsion of excipients. The proportion of water in the composition is advantageously at least 49% by weight, preferably at least 52% by weight. The proportion of water in the composition is advantageously at most 70% by weight, preferably at most 64% by weight.

[0053] In a further embodiment, the composition additionally contains a moisturizer, preferably propylene glycol, pentylene glycol, a hyaluronic acid, glyceryl glucoside, aloe vera extract, or mixtures thereof. The proportion of the moisturizer in the composition is expediently at least 3% by weight, preferably at least 5% by weight.

[0054] In a further embodiment, the composition additionally comprises a preservative.

[0055] The composition is suitable for topical applications, especially for cosmetic purposes.

[0056] The composition can also be formulated as a concentrate for the production of a topical skin preparation and then advantageously has a higher concentration of the two active ingredients. The first active ingredient can then have a proportion of 0.05 to 1.0% by weight, preferably 0.1 to 0.5% by weight, and the second active ingredient can have a proportion of 1.5 to 3.4% by weight, preferably 2.0 to 2.7% by weight.

[0057] The carrier substance can be selected from the group consisting of liposomes, nanosomes, oil-in-water emulsions, and water-in-oil emulsions. Conveniently, the carrier substance can comprise glycerol, caprylic / capric acid triglycerides, phospholipids, or mixtures thereof.

[0058] The composition according to the invention is suitable for the treatment of signs of skin aging, especially wrinkles. It is also suitable for promoting the proliferation, protection, and revitalization of skin stem cells. The composition can also be used to treat intrinsic and extrinsic skin aging.

[0059] The invention and further developments of the invention are explained in more detail below using several exemplary embodiments. Example 1 (Base Mixture Concentrate for Use in Skin Serums)

[0060] Components wt%

[0061] Water 79.9

[0062] Caprin triglyceride 12.7

[0063] 1,2-pentanedi oil 2.7

[0064] Pistacia Lentiscus (Mastic)Gum 2.3

[0065] Lecithin 2.0

[0066] Glyceryl Caprylate 0.3

[0067] Royal jelly 0.1

[0068] Total 100.0

[0069] Example 2 (Base mixture / concentrate for use in skin creams)

[0070] Components wt%

[0071] Water 79.6

[0072] Gaprilic Triglyceride 12.6

[0073] 1,2-pentanediol 2,7

[0074] Pistacia Lentiscus (Mastic)Gum 2.3

[0075] Lecithin 2.0

[0076] G8 - €10 Glycerides 0.3

[0077] Royal jelly 0.5

[0078] Total 100.0

[0079] Example 3 (skin cream)

[0080] Components wt.»%

[0081] Water 62.1

[0082] Glycerin 5.5

[0083] Pentylene glycol 5.0 Propanediol 5.0

[0084] Coco-Caprylate 3:2

[0085] Dicaprylyl Carbonate 2.6

[0086] Sodium Hyaluronate 0.160

[0087] Crithmum Maritimum Callus Culture Filtrate 0.100

[0088] Pistacia Lentiscus (Mastic) Gum 0.040

[0089] Royal Jelly 0.002

[0090] Perfume (Fragrance) 0.500

[0091] Caprylic / Capric triglycerides 0.250

[0092] Lecithin 0.042

[0093] Glyceryl Caprylate 0.006

[0094] Rest (excipients / adjuvants) 15.5

[0095] Total 100.0

[0096] Example 4 (skin cream)

[0097] Components wt%

[0098] Water 52.3

[0099] Propanediol 5.0

[0100] Glycerin 4.8

[0101] Pentytene glycol 2.07

[0102] Caprylyl Caprylate / Caprate 2.0

[0103] Sodium Hyaluronate 0.100

[0104] Pistacia Lentiscus (Mastic) Gum 0.046

[0105] Royal Jelly 0.002

[0106] Perfume (Fragrance) 0.558

[0107] Caprylic Triglyceride 0.254

[0108] Lecithin 0.040

[0109] Rest (excipients / adjuvants) 32.83

[0110] Total 100.0 Example 5 (Skin Cream)

[0111] Components wt%

[0112] Water 52.10

[0113] Propanediol 6.24

[0114] Glycerin 4.87

[0115] Caprylic / Capric Triglycerides 4.25

[0116] Pentylene glycol 3.07

[0117] Pistacia Lentiscus (Mastic) Gum 0.462

[0118] Royal Jelly 0.002

[0119] Lecithin 0.040

[0120] Glyceryl Caprylate / 0.006

[0121] Rest (excipients / adjuvants) 28.96

[0122] Total 100.0

[0123] Although there are various embodiments of the present invention as described above, it should be understood that the various features can be used individually or in any combination.

[0124] This invention is therefore not simply limited to the above-mentioned, particularly preferred embodiments.

Claims

Patent claims 1. A pharmaceutical or cosmetic composition comprising the following components: a) a dermatologically suitable carrier substance, b) a first active substance, and c) a second active substance, characterized in that d) the first active substance comprises royal jelly; and e) the second active substance comprises retinol, retinol analogues or mixtures thereof.

2. Composition according to claim 1, characterized in that the two active substances are dispersed in the carrier substance in the form of liposomes.

3. Composition according to claim 2, characterized in that the two active ingredients are encapsulated and stabilized in liposomes finely distributed in the carrier substance and having a size of 150 to 350 nm, preferably 200 to 250 nm.

4. Composition according to claim 2 or 3, characterized in that the two active ingredients are encapsulated separately in the liposomes.

5. Composition according to claim 2 or 3, characterized in that the two active ingredients are mixed and encapsulated in the liposomes.

6. Composition according to one of claims 2 to 5, characterized in that the membranes of the liposomes contain lecithins or triglycerides.

7. Composition according to one of claims 1 to 6, characterized in that the retinol analogue is obtained from extracts of cultured dedifferentiated plant cells.

8. Composition according to one of claims 1 to 7, characterized in that the retinol analogue is selected from the following group: - Extract from the Babchi plant; - Extract of Hypnea Musciformis;, - Extract of Sargassum Filipendula; - Algae oligosaccharides, - Xantophyilis., or mixtures thereof.

9. Composition according to one of claims 1 to 7, characterized in that the second active ingredient is Pistacia Lentiscus (Mastic) Gum or Chios mastic gum.

10. Composition according to one of claims 1 to 9, characterized in that the proportion of royal jelly in the composition is at least 0.0015% by weight, preferably at least 0.0019% by weight.

11. Composition according to one of claims 1 to 10, characterized in that the proportion of the second active substance in the composition is at least 0.03% by weight, preferably at least 0.04% by weight.

12. Composition according to one of claims 1 to 11, characterized in that it is in the form of creams, in particular skin and eye creams; soaps, lotions, gels or serums.

13. Composition according to one of claims 1 to 12, characterized in that it contains further active ingredients selected from the following group: - Crithmum Maritimum, especially Crithmum Maritimum Callus Culture Filtrate' - Hyaluronic acids; - Black Pearl Extract; - Synthetic tripeptides with a molecular weight below 500 Da; - Leaf extract of Plantago lanceolata; - xanthan gum; - extract of the bacterium lodobacter ssp.; - Tetradecyl-aminobutyroylvaly l-aminbutyric acid urea trifluoroacetate - Acrilella Oteracea extract; - Leaf juice of the South African medicinal plant Bulbi ne Frutescens; - alpha-glucan; - Phytosteryl rapeseed glycerides; and - Japanese root extract, 14. Composition according to one of claims 1 to 13, characterized in that it has a pH higher than 3.5, preferably higher than 4.

0.

15. Composition according to one of claims 1 to 14, characterized in that it has a pH value of less than 6.5, preferably less than 6.0 16. Composition: according to one of claims 1 to 15, characterized in that the quantitative ratio between the first active substance and the second active substance is in the range from 1:4 to 1:35, preferably in the range from 1:15 to 1:

27.

17. Composition according to one of claims 1 to 16, characterized in that the carrier substance is water or an aqueous emulsion of excipients, 18. Composition according to one of claims 1 to 17, characterized in that the proportion of water in the composition is at least 49% by weight, preferably at least 52% by weight.

19. Composition according to one of claims 1 to 18, characterized in that the proportion of water in the composition is at most 70% by weight, preferably at most 64% by weight.

20. Composition according to one of claims 1 to 19, characterized in that it additionally contains a moisturizer, preferably propylene glycol, pentytene glycol, a hyaluronic acid, glyceryl glucoside, aloe vera extract or mixtures thereof.

21. Composition according to claim 20, characterized in that the proportion of the moisturizer in the composition is at least 3% by weight, preferably at least 5% by weight.

22. Composition according to one of claims 1 to 21, characterized in that it additionally comprises a preservative.

23. Composition according to any one of claims 1 to 22 for topical applications, in particular for cosmetic purposes.

24. Composition according to one of claims 1 to 22, characterized in that it is designed as a concentrate for the manufacture of a topical skin preparation.

25. Composition according to one of claims 1 to 24, characterized in that the carrier substance is selected from the group consisting of liposome, nanosome, oil-in-water emulsion and water-in-oil emulsion.

26. Composition according to one of claims 1 to 25, characterized in that the carrier substance comprises glycerol, caprylic / capric acid triglycerides and phospholipids.

28. Composition according to any one of claims 1 to 27 for the treatment of signs of aging of the skin, in particular wrinkles. ZS, composition according to any one of claims 1 to 27 for promoting the proliferation, protection and vitalization of skin stem cells.

30. Composition according to any one of claims 1 to 27 for the treatment of intrinsic and extrinsic skin aging.