Spot-on formulation useful for cosmetology and dermatology

• US 20090010968A1
• Filed: 05/12/2005
• Published: 01/08/2009
• Est. Priority Date: 05/12/2004
• Status: Abandoned Application

• Current Assignee: Dermaconcept Jmc
• Original Assignee: Dermaconcept Jmc
• Inventors: Peyrot, Jacques, Allart, Jean-Claude, Marty, Jean-Paul, Lefevre, Jean-Marie
• Application Number:
  US11/596,334
• Publication Number:
  US 20090010968A1
• Time in Patent Office: Days
• US Class Current: 424/401
• CPC Class Codes: A61K 2800/28 Rubbing or scrubbing compositions; Peeling or abrasive compositions; Containing exfoliants
• CPC Class Codes: A61K 31/133 having hydroxy groups, e.g. sphingosine
• CPC Class Codes: A61K 31/20 having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
• CPC Class Codes: A61K 31/201 having one or two double bonds, e.g. oleic, linoleic acids
• CPC Class Codes: A61K 31/202 having three or more double bonds, e.g. linolenic eicosanoids, e.g. leukotrienes A61K31/557
• CPC Class Codes: A61K 31/203 Retinoic acids ; Salts thereof
• CPC Class Codes: A61K 31/355 Tocopherols, e.g. vitamin E
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 8/671 Vitamin A; Derivatives thereof, e.g. ester of vitamin A acid, ester of retinol, retinol, retinal
• CPC Class Codes: A61K 8/678 Tocopherol, i.e. vitamin E
• CPC Class Codes: A61K 9/08 Solutions composition of solutions A61K47/00
• CPC Class Codes: A61K 9/107 Emulsions ; Emulsion preconcentrates; Micelles composition of emulsions A61K47/00
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 17/08 Antiseborrheics
• CPC Class Codes: A61P 17/10 Anti-acne agents
• CPC Class Codes: A61P 17/14 for baldness or alopecia
• CPC Class Codes: A61Q 17/04 Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
• CPC Class Codes: A61Q 19/00 Preparations for care of the skin
• CPC Class Codes: A61Q 19/08 Anti-ageing preparations
• CPC Class Codes: A61Q 5/12 Preparations containing hair conditioners

Abstract

The invention relates to a novel formulation of use in cosmetology and in dermatology which uses the storage capacity of the sebaceous glands.

The formulation is of the spot-on type and comprises a lipophilic active principle chosen from vitamin A, vitamin E a lipophilic agent for combating free radicals, ceramides or sphingoid bases and steroid hormones, in combination with one or more unsaturated C₄-C₂₆ fatty acids and a liquid vehicle, having sebaceous tropism.

Application to the localized topical administration of lipophilic active principles.

Claims

1. A formulation of spot-on type for localized topical application, comprising a saturated emulsion or solution comprising a lipophilic active principle in a mixture of solvents comprising one or more unsaturated C₄-C₂₆ fatty acids and a polar liquid vehicle, having sebaceous tropism.

2. The formulation of spot-on type as claimed in claim 1, wherein the active principle is selected from the group consisting of vitamin A;

vitamin E;

an lipophilic agent for combating free radicals;

ceramides or sphingoid bases; and

steroid hormones.

3. The formulation of spot-on type as claimed in claim 2, wherein vitamin A is provided in natural form (retinol), in the form of its acid (retinoic acid) or also of retinyl acetate, of retinaldehyde, of β

-carotene or of retinyl palmitate;

vitamin E is provided in the pure form or in the form of an ester, such as tocopherol acetate, tocopherol linoleate or tocopherol succinate;

the lipophilic agent for combating free radicals is chosen from derivatives of α

-lipoic acid, andrographolides or lipophilic derivatives of vitamin C, such as ascorbyl palmitate and stearate;

the sphingoid base is chosen from sphingosine, sphinganine, phytosphingosine, tetracetylphytosphingosine, N-acetylphytosphingosine, phytosphingosine hydrochloride and phytosphingosine salicylate; and

the steroid hormones are chosen from estrogens, antiandrogens and progesterone.

4. The formulation of spot-on type as claimed in claim 1, wherein the unsaturated C₄-C₂₆ fatty acid is selected from the group consisting of sapienic acid, linolenic acid and linoleic acid.

5. The formulation of spot-on type as claimed in claim 4, wherein the unsaturated C₄-C₂₆ fatty acid is α

- or γ

-linoleic acid.

6. The formulation of spot-on type as claimed in claim 1, wherein it is provided in the form of a simple oily solution, of an emulsion or of an emulsion of quaternary type which are saturated with active principle.

7. The formulation of spot-on type as claimed in claim 1, wherein the formulation is provided in the form of an anhydrous simple oily solution saturated with active principle and in that the polar liquid vehicle comprises an organic solvent.

8. The formulation of spot-on type as claimed in claim 7, wherein the organic solvent is selected from the group consisting of acetone, ethyl acetate, methanol, ethanol, isopropanol, dimethylformamide, diethylene glycol, dichloromethane, 1,2-O-isopropylideneglycerol (Solketal) and diethylene glycol monoethyl ether (Transcutol).

9. The formulation of spot-on type as claimed in claim 1, for its use as dermatological composition in human medicine.

20. A method for the cosmetic treatment of the skin, comprising applying, to the affected areas of the skin, a formulation of spot-on type as claimed in claim 1.

10. The use of a lipophilic active principle aimed at the skin for the preparation of a formulation for localized topical application in man intended to be absorbed by the sebaceous glands and then gradually released in the sebaceous flow over the stratum corneum, according to the physiological rhythm for excretion of the sebaceous glands.

11. The use of a lipid active principle chosen from vitamin A, steroid hormones, ceramides or their precursors, such as sphingoid bases, and essential fatty acids for the preparation of a formulation of spot-on type intended to treat acne.

12. The use of a lipid active principle chosen from ceramides or their precursors, such as sphingoid bases, and steroid hormones for the preparation of a formulation of spot-on type intended to treat seborrhea.

13. The use of a lipid active principle chosen from ceramides or their precursors, such as a sphingoid base, and essential fatty acids for the preparation of a formulation of spot-on type intended to treat seborrheic dermatitis.

14. The use of a lipid active principle chosen from vitamin E, vitamin A and glycerol for the preparation of a formulation of spot-on type intended to treat a deficiency of sebum.

15. The use of a lipid active principle chosen from steroid hormones for the preparation of a formulation of spot-on type intended to treat Fox-Fordyce disease, androgenic alopecia or hirsutism.

16. The use of a lipid active principle chosen from ceramides or their precursors, such as a sphingoid base, for the preparation of a formulation of spot-on type intended to treat chronic folliculitis of the scalp.

17. The use of a lipid active principle chosen from essential fatty acids for the preparation of a formulation of spot-on type intended to treat ichthyosis of the scalp.

18. The use of a lipid active principle chosen from kojic acid esters, a licorice extract, steroid hormones, vitamin A, ceramides or their precursors, such as a sphingoid base, for the preparation of a formulation of spot-on type intended to treat actinic lentigo, pigment disorders relating to aging and hypermelanosis.

19. (canceled)