Compounds, Formulations and Methods for Reducing Skin Wrinkles, Creasing and Sagging

a technology of creasing and sagging, which is applied in the direction of biocide, synthetic polymeric active ingredients, drug compositions, etc., can solve the problems of common creasing and sagging, skin wrinkles, and general undesirable effects, and achieve the effects of reducing skin wrinkles, creasing and sagging, skin creasing or sagging, and promoting the effect of compounding in the amount effectiv

Inactive Publication Date: 2009-03-05
GALDERMA LAB LP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0005]The present inventors have developed topical skin formulations and methods for reducing skin wrinkles, creasing and sagging. Compositions of the invention comprise α2 adrenergic receptor agonists, which have a skin-tightening effect and ameliorate skin wrinkles, skin creas

Problems solved by technology

Skin wrinkles, creasing and sagging are common and generally undesir

Method used

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  • Compounds, Formulations and Methods for Reducing Skin Wrinkles, Creasing and Sagging
  • Compounds, Formulations and Methods for Reducing Skin Wrinkles, Creasing and Sagging
  • Compounds, Formulations and Methods for Reducing Skin Wrinkles, Creasing and Sagging

Examples

Experimental program
Comparison scheme
Effect test

example 1

Synthesis of (5-Bromo-quinoxalin-6-yl)-(4,5-dihydro-1H-imidazol-2-yl)-amine

[0069]To a stirred solution of 6-amino-5-bromoquinoxaline hydrobromide (10 g) in distilled water (150 ml) is added thiophosgene (3 ml). The solution is stirred for two hours at room temperature and the resultant precipitate is collected by filtration, washed with water, and dried to afford 5-bromo-6-isothiocyanato-quinoxaline.

[0070]The 5-bromo-6-isothiocyanato-quinoxaline (3.5 g.) is directly dissolved in benzene (400 ml) and added dropwise to a well-stirred solution of ethylene diamine (15 g.) in benzene (50 ml). During a period of about two hours, an oil separates as a lower layer. The upper benzene layer is poured off and the oil is washed with diethyl ether and then dissolved in methanol (500 ml). The methanolic solution is refluxed until hydrogen sulfide evolution ceases. The methanolic solution is concentrated in vacuo to a volume of approximately 100 ml upon which a yellow solid precipitates. The preci...

example 2

[0071]An aqueous solution topical formulation of the invention comprises (5-Bromo-quinoxalin-6-yl)-(4,5-dihydro-1H-imidazol-2-yl)-amine-L-tartrate (brimonidine tartrate) (0.15% w / w); Puriteg (0.005% w / w) (stabilized chlorine dioxide) as a preservative; and the inactive ingredients: boric acid; calcium chloride; magnesium chloride; potassium chloride; purified water; sodium borate; sodium carboxymethylcellulose; sodium chloride; with hydrochloric acid and / or sodium hydroxide to adjust the pH to 5.6 to 6.6. The osmolality is in the range of 250-350 mOsmol / kg.

example 3

[0072]An aqueous solution topical formulation comprises (5-Bromo-quinoxalin-6-yl)-(4,5-dihydro-1H-imidazol-2-yl)-amine-L-tartrate, (brimonidine tartrate) (0.15% w / w); benzalkonium chloride (0.005 wt. %) as a preservative; and the inactive ingredients: boric acid; calcium chloride; magnesium chloride; potassium chloride; purified water; sodium borate; sodium carboxymethylcellulose; sodium chloride; with hydrochloric acid and / or sodium hydroxide to adjust the pH to 5.6 to 6.6. The osmolality is in the range of 250-350 mOsmol / kg.

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Abstract

Methods, compounds, and topical formulations for reduction of skin sagging, creasing and/or wrinkling are disclosed. The methods comprise topically applying a composition comprising an α2 adrenergic receptor agonist. Amelioration of skin sagging, creasing and/or wrinkling begins within minutes after topical application of a disclosed composition. A single application can significantly reduce skin sagging, creasing and/or wrinkling for at least about 8 hours.

Description

[0001]The present teachings are directed to compounds and methods for treatment or prevention of skin wrinkles and sagging.BACKGROUND OF THE INVENTION[0002]Skin wrinkles, creasing and sagging are common and generally undesirable. Such skin conditions can result from many causes, such as aging.[0003]Many different treatments are used to reverse wrinkles, creasing or skin sagging. Examples of these treatments include injection of toxins such as botulinum toxin; injection of fillers such as collagen, fat, and hyaluronic acid, topical formulations of tretinoin, chemical peeling, dermabrasion, laser resurfacing, microdermabrasion, photorejuvenation, and plastic surgery such as face-lifts and forehead lifts. All of these procedures have associated side effects and / or cautions (see, e.g., the web site http: / / www.mayoclinic.com / health / wrinkle-treatment / SN00008)[0004]Thus, there remains a need for compositions and methods for reducing skin wrinkles, creasing and sagging.SUMMARY OF THE INVENT...

Claims

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Application Information

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IPC IPC(8): A61K31/498A61K31/4164A61K31/137A61P17/00A61Q19/08A61Q17/04A61K8/49A61K8/41
CPCA61K8/41A61K8/4946A61K31/74A61K45/06A61K2800/70A61Q19/00A61Q19/08A61Q17/04A61K8/494A61K2300/00A61P17/00A61P31/00
Inventor DEJOVIN, JACKDEJOVIN, ISABELLE JEAN
Owner GALDERMA LAB LP
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