Pharmaceutical or cosmetic composition for a primary preparation

By combining royal jelly and retinol analogs in a skin formulation and utilizing liposome dispersion technology, the problem of slow retinol application has been solved, achieving rapid wrinkle reduction and moisturizing effects, and improving skin aging issues.

CN122180499APending Publication Date: 2026-06-09M OPITZ AG
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Patent Information

Application Number
CN202380103890.6
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2023-11-10
Publication Date
2026-06-09

AI Technical Summary

Technical Problem

Existing retinol-based skin care products have issues with slow adaptation during use and require intermittent use, and have failed to effectively improve wrinkles and dryness caused by aging.

Method used

Using royal jelly and retinol analogues as active ingredients, they are dispersed in a carrier substance in the form of liposomes to work synergistically to enhance skin absorption and moisturizing effects. Antioxidants, emulsifiers and moisturizers are added to form a stable skin formulation.

Benefits of technology

It achieves the rapid wrinkle-reducing effect of retinol analogs, improves skin proliferation and moisturizing effects, and provides immediate and lasting skin improvement.

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Abstract

Pharmaceutical or cosmetic composition comprising the following components: a) a dermatologically suitable carrier material, 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, a retinol analogue or a mixture thereof.
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Description

[0001] This invention relates to a pharmaceutical or cosmetic composition according to the preamble of claim 1.

[0002] The basic objective of this invention is to create a combination formulation that generally avoids the known drawbacks of retinol and retinoids, and on the other hand has an improved effect on skin changes caused by aging.

[0003] The present invention achieves the proposed objective by having a pharmaceutical or cosmetic composition having the features described in claim 1, particularly in the form of a skin preparation.

[0004] The advantages achieved by this invention are essentially that, due to the composition according to the invention containing additional active substances in the form of royal jelly, it produces an unexpectedly immediate effect on skin wrinkles and a proven wrinkle-reducing effect with regular application.

[0005] By adapting the active substances and their synergistic interactions, the proliferation performance, absorption, humidification effect, and anti-aging effect have been improved.

[0006] definition:

[0007] Antioxidants: Antioxidants provide protection against so-called "free radicals." For example, vitamins C and E and their derivatives protect sensitive ingredients in cosmetic formulations from the effects of oxygen and free radicals in the air, while also playing their specific roles in the skin. In contrast, synthetic phenolic antioxidants such as butylated hydroxytoluene (INCI: BHT) are classified as pure adjuvants.

[0008] Additional complexing agents (such as those based on ethylenediaminetetraacetic acid (INCI: EDTA), citrate, and phosphonates) can be combined to form actual antioxidants.

[0009] Black pearl extract: A component extracted from the black mother shell of Tahitian pearls.

[0010] Emulsifiers are additives used to blend two immiscible liquids into a finely dispersed mixture (i.e., an emulsion) and stabilize it. An alternative to conventional emulsifiers is natural film-forming substances such as ceramides and phosphatidylcholine. Similar to the skin's barrier layer, they form a layered, sheet-like structure in creams, have fewer side effects, and can be seamlessly integrated into the skin's physiological activities.

[0011] Moisturizer

[0012] The compositions according to the invention preferably contain a humectant. Non-limiting examples of humectants that can be used with the compositions of the invention include amino acids, chondroitin sulfate, diglycerides, erythritol, fructose, glucose, glycerol, glycerol polymers, glycols, 1,2,6-hexanetriol, molasses, hyaluronic acid, hydrogenated molasses, hydrogenated starch hydrolysate, inositol, lactic acid alcohol, maltitol, maltose, mannitol, natural moisturizing factors, PEG-15-butanediol, polyglycerol sorbitol, pyrrolidone carboxylic acid salts, potassium PCA, propylene glycol, sodium glucuronate, sodium PCA, sorbitol, sucrose, trehalose, urea, and xylitol.

[0013] Royal jelly: the liquid food bees feed their queen bee. It contains, in particular, the main protein in royal jelly.

[0014] Caprylic / capric triglyceride: a particularly effective natural preservative and preservative agent.

[0015] Additives used in cosmetics:

[0016] Besides the fatty substances used in skincare and the active ingredients soluble in fats and water, cosmetic formulations generally contain a wide variety of other ingredients depending on their intended application. Cosmetic formulations can be summarized under the term "auxiliaries" and have a wide range of functions. Cosmetic formulations can be made into formulations with entirely different structures, such as creams, gels, ointments, lotions, solutions, coatings, sticks, powders, dusting powders, and aerosols. They impart long-term physical stability to these formulations for easy transport and storage, prevent contamination by molds, yeasts, and bacteria, improve the chemical stability of sensitive active ingredients against atmospheric oxygen, and influence sensory impressions such as consistency, distributability on the skin, odor (fragrance), and color. The most commonly used auxiliary is water (INCI: Aqua). Water is an important component of emulsions and, in association with emulsifiers, is used for the droplet-like distribution of fatty substances used in skincare, thus making them very easy to apply to the skin. Furthermore, water also acts as a solvent for polar (hydrophilic) active ingredients and auxiliary agents. Related to humectant active ingredients, the water content in the formulation leads not only to temporary but also to a long-term, measurable increase in skin moisture. Other adjuvants include preservatives, emulsifiers, surfactants, oils, antioxidants, humectants, plasticizers, consistency modifiers, chelating agents, stabilizers, fragrances, dyes, and pigments. After adding the dermatological or cosmetic active ingredient to the obtained preparation in the form of an emulsion, gel, or solution, the resulting mixture is stirred until a completely homogeneous substance or liquid is produced.

[0017] Lecithin: is phosphatidylcholine (phospholipid, an ester formed from fatty acids, glycerol, phosphoric acid, and choline). Phospholipids participate in the construction of the phospholipid bilayer of biological membranes (specifically, when the active substance according to the invention is encapsulated in phospholipid bodies).

[0018] Phospholipids: Phospholipids are small water vesicles whose outer shell consists of a phospholipid bilayer, similar to a cell membrane. The amphiphilic properties of the membrane molecules are unique; they possess a hydrophilic head and a hydrophobic tail. Various known methods exist for preparing phospholipids. Such methods are exemplarily described in detail in U.S. Patent Application No. US 2011 318406.

[0019] Medium-chain triglycerides: Triglycerides that contain medium-chain fatty acids (especially caproic acid, caprylic acid, capric acid, and lauric acid).

[0020] Pentylene glycol: It is both a moisturizer and a preservative. It helps inhibit the growth of microorganisms on the skin. Because it is water-soluble, it is used as a solubilizer. Pentylene glycol can be prepared from sugarcane bagasse and corn cobs.

[0021] Propylene glycol: This is a moisturizer used on the skin. At low concentrations, propylene glycol can accumulate in skin cells and form water there. The water can then no longer escape from the skin. The skin is better and more fully moisturized, appearing noticeably more radiant and feeling better to the touch.

[0022] Retinol: Also known as Vitamin A, retinol is known for its anti-aging properties and is therefore used in skincare products. It mimics cell renewal and assists in the production of collagen. Retinol works in the outermost layer of the skin, making it smoother and more even as it reduces age spots, smooths fine lines, and minimizes pores. However, retinol also has some drawbacks. The skin needs a relatively slow adaptation to retinol, and there needs to be an interval between uses.

[0023] Retinol analogues: These are substances that are chemically different from retinol but exhibit similar effects, especially on the skin.

[0024] Other advantageous designs of the present invention can be described as follows:

[0025] In a preferred embodiment of the invention, the two active substances are dispersed in the carrier material in the form of liposomes. This results in an improvement in the bioavailability of the active substances. In another embodiment, the two active substances are encapsulated in fine liposomes dispersed in the carrier material, having a size of 150 to 350 nm, preferably 200 to 250 nm, and stabilized.

[0026] In another embodiment, the two active substances are encapsulated separately in the liposomes. Alternatively, the two active substances may be encapsulated together in the liposomes.

[0027] In one particular embodiment, the membrane of the liposome comprises lecithin or triglycerides. Here, a synergistic effect occurs between the active substance and lecithin.

[0028] In another embodiment, the retinol analogue is derived from extracts of cultured, dedifferentiated plant cells.

[0029] The retinol analogues may advantageously be selected from the group consisting of:

[0030] - Psoralea corylifolia plant extract;

[0031] - Uncaria rhynchophylla extract;

[0032] - Sargassum fusiforme extract;

[0033] - Algal oligosaccharides;

[0034] - Lutein;

[0035] Or a mixture thereof.

[0036] In another embodiment, the second active substance is frankincense gum or Chios frankincense gum.

[0037] 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.

[0038] In another embodiment, the proportion of the second active substance in the composition is at least 0.03% by weight, preferably at least 0.04% by weight.

[0039] The composition may be in the form of creams, especially skin creams and eye creams, soaps, lotions, gels or serums.

[0040] In another embodiment, the composition comprises additional active material components selected from the group consisting of:

[0041] - Sea fennel, especially sea fennel callus culture filtrate;

[0042] - Hyaluronic acid;

[0043] - Black pearl extract;

[0044] - Synthetic tripeptides with a molecular weight of less than 500 Da;

[0045] - Leaf extract of Plantago longifolia;

[0046] - Xanthan gum;

[0047] - Extracts from Iodobacter ssp. bacteria;

[0048] - Tetradecyl-aminobutyrylvaline-aminobutyric acid urea trifluoroacetate;

[0049] - Globe amaranth extract;

[0050] - Leaf juice of the South African medicinal plant, celery;

[0051] - α-glucan;

[0052] - Phytosterol rapeseed glycerides; and

[0053] - Japanese root extract (Japanischer Wurzelextrakt).

[0054] In one particular embodiment, the composition has a pH value higher than 3.5, preferably higher than 4.0. The pH value is preferably lower than 6.5, more preferably lower than 6.0.

[0055] In another embodiment, the ratio of the first active substance to the second active substance is in the range of 1:4 to 1:35, particularly in the range of 1:15 to 1:27.

[0056] The carrier material of the composition can be water or an aqueous emulsion of additives. The water content in the composition is preferably at least 49% by weight, more preferably at least 52% by weight. The water content in the composition is preferably at most 70% by weight, more preferably at most 64% by weight.

[0057] In another embodiment, the composition further comprises a moisturizer, preferably propylene glycol, pentanediol, hyaluronic acid, glyceryl glucoside, aloe vera extract, or a mixture thereof. The proportion of the moisturizer in the composition is preferably at least 3% by weight, more preferably at least 5% by weight.

[0058] In another embodiment, the composition further includes a preservative.

[0059] The composition is suitable for topical application, especially for cosmetic purposes.

[0060] The composition can also be formulated as a concentrate for preparing topical skin formulations and thus preferably has a higher concentration of both active substances. The first active substance may then have a share of 0.05 to 1.0% by weight, preferably 0.1 to 0.5% by weight, and the second active substance may have a share of 1.5 to 3.4% by weight, preferably 2.0 to 2.7% by weight.

[0061] The carrier material can be selected from the group consisting of liposomes, nanocapsules, oil-in-water emulsions, and water-in-oil emulsions. Preferably, the carrier material may include glycerol, caprylic / capric triglyceride, phospholipids, or mixtures thereof.

[0062] The compositions according to the invention are suitable for treating skin aging phenomena, particularly wrinkles. The compositions are also suitable for promoting, protecting, and activating skin stem cells. The compositions can also be used to treat both endogenous and exogenous skin aging.

[0063] The invention and its improvements are explained in more detail below with the aid of several embodiments.

[0064] Example 1 (Concentrated base mixture for use in skin creams)

[0065]

[0066] Example 2 (Base mixture / concentrate for use in skin cream)

[0067]

[0068] Example 3 (Skin Cream)

[0069]

[0070] Example 4 (Skin Cream)

[0071]

[0072] Example 5 (Skin Cream)

[0073]

[0074] While various embodiments of the invention have been described above, these embodiments should be understood to mean that the various features can be used individually or in any combination.

[0075] Therefore, the present invention is not simply limited to the particularly preferred embodiments mentioned above.

Claims

1. A pharmaceutical or cosmetic composition comprising the following components: a) A suitable carrier substance in dermatology. b) The first active substance, and c) Second active substance, Its features are, d) The first active substance includes royal jelly; and e) The second active substance includes retinol, retinol analogues, or mixtures thereof.

2. The composition according to claim 1, characterized in that, These two active substances are dispersed in the carrier material in the form of liposomes.

3. The composition according to claim 2, characterized in that, Both active substances are encapsulated in fine liposomes, dispersed in the carrier material, having a size of 150 to 350 nm, preferably 200 to 250 nm, and stabilized.

4. The composition according to claim 2 or 3, characterized in that, These two active substances are encapsulated in the liposomes respectively.

5. The composition according to claim 2 or 3, characterized in that, These two active substances are encapsulated together in the liposomes.

6. The composition according to any one of claims 2 to 5, characterized in that, The membrane of the liposome contains lecithin or triglycerides.

7. The composition according to any one of claims 1 to 6, characterized in that, The retinol analogue was obtained from extracts of cultured, dedifferentiated plant cells.

8. The composition according to any one of claims 1 to 7, characterized in that, The retinol analogues are selected from the following group: - Psoralea corylifolia plant extract; - Uncaria rhynchophylla extract; - Sargassum fusiforme extract; - Algal oligosaccharides, - Lutein, Or a mixture thereof.

9. The composition according to any one of claims 1 to 7, characterized in that, The second active substance is frankincense gum or Chios frankincense gum.

10. The composition according to any one of claims 1 to 9, characterized in that, The composition contains at least 0.0015% by weight, preferably at least 0.0019% by weight of royal jelly.

11. The composition according to any 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. The composition according to any one of claims 1 to 11, characterized in that, The composition exists in the form of creams, especially skin creams and eye creams, soaps, lotions, gels or serums.

13. The composition according to any one of claims 1 to 12, characterized in that, The composition comprises an active substance component selected from the group consisting of: - Sea fennel, especially sea fennel callus culture filtrate; - Hyaluronic acid; - Black pearl extract; - Synthetic tripeptides with a molecular weight of less than 500 Da; - Leaf extract of Plantago longifolia; - Xanthan gum; - Extracts from Iodobacter ssp. bacteria; - Tetradecyl-aminobutyrylvaline-aminobutyric acid urea trifluoroacetate; - Globe amaranth extract; - Leaf juice of the South African medicinal plant, celery; - α-glucan; - Phytosterol rapeseed glycerides; and - Japanese root extract.

14. The composition according to any one of claims 1 to 13, characterized in that, The composition has a pH value higher than 3.5, preferably higher than 4.

0.

15. The composition according to any one of claims 1 to 14, characterized in that, The composition has a pH value below 6.5, preferably below 6.

0.

16. The composition according to any one of claims 1 to 15, characterized in that, The ratio of the first active substance to the second active substance is in the range of 1:4 to 1:35, particularly in the range of 1:15 to 1:

27.

17. The composition according to any one of claims 1 to 16, characterized in that, The carrier substance is an aqueous emulsion of water or additives.

18. The composition according to any one of claims 1 to 17, characterized in that, The water content in the composition is at least 49% by weight, preferably at least 52% by weight.

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

20. The composition according to any one of claims 1 to 19, characterized in that, The composition further comprises a moisturizer, preferably propylene glycol, pentylene glycol, hyaluronic acid, glyceryl glucoside, aloe extract, or a mixture thereof.

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

22. The composition according to any one of claims 1 to 21, characterized in that, The composition also contains a preservative.

23. The composition according to any one of claims 1 to 22, for topical application, especially for cosmetic purposes.

24. The composition according to any one of claims 1 to 22, characterized in that, The composition is formed into a concentrate for the preparation of topical skin formulations.

25. The composition according to any one of claims 1 to 24, characterized in that, The carrier material is selected from the group consisting of liposomes, nanocapsules, oil-in-water emulsions, and water-in-oil emulsions.

26. The composition according to any one of claims 1 to 25, characterized in that, The carrier substances include glycerol, caprylic / capric triglyceride, and phospholipids.

27. The composition according to any one of claims 1 to 27 is used to treat skin aging, especially skin wrinkles.

28. The composition according to any one of claims 1 to 27, for promoting the proliferation, protection and activation of skin stem cells.

29. The composition according to any one of claims 1 to 27, for treating endogenous and exogenous skin aging.

Citation Information

Patent Citations

  • Lecithin carrier vesicles and methods of making the same

    US20110318406A1