Topically Bioavailable Acne and Rosacea Treatment Compositions

• US 20040156873A1
• Filed: 02/10/2003
• Published: 08/12/2004
• Est. Priority Date: 02/10/2003
• Status: Abandoned Application

• Current Assignee: Shyam K. Gupta
• Original Assignee: Shyam K. Gupta
• Inventors: GUPTA, SHYAM K.
• Application Number:
  US10/248,691
• Publication Number:
  US 20040156873A1
• Time in Patent Office: Days
• US Class Current: 424/401
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 2800/28 Rubbing or scrubbing compositions; Peeling or abrasive compositions; Containing exfoliants
• CPC Class Codes: A61K 2800/522 Antioxidants; Radical scavengers
• CPC Class Codes: A61K 2800/75 Anti-irritant
• CPC Class Codes: A61K 31/205 Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
• CPC Class Codes: A61K 31/60 Salicylic acid; Derivatives thereof
• CPC Class Codes: A61K 31/7008 Compounds having an amino group directly attached to a carbon atom of the saccharide radical, e.g. D-galactosamine, ranimustine
• CPC Class Codes: A61K 31/728 Hyaluronic acid
• CPC Class Codes: A61K 8/0212 Face masks
• CPC Class Codes: A61K 8/35 Ketones, e.g. benzophenone
• CPC Class Codes: A61K 8/63 Steroids; Derivatives thereof
• CPC Class Codes: A61K 8/64 Proteins; Peptides; Derivatives or degradation products thereof
• CPC Class Codes: A61K 8/673 Vitamin B group
• CPC Class Codes: A61K 8/675 Vitamin B3 or vitamin B3 active, e.g. nicotinamide, nicotinic acid, nicotinyl aldehyde tocopheryl nicotinate A61K8/678
• CPC Class Codes: A61K 8/676 Ascorbic acid, i.e. vitamin C
• CPC Class Codes: A61K 8/736 Chitin; Chitosan; Derivatives thereof
• CPC Class Codes: A61K 8/9722 Chlorophycota or Chlorophyta [green algae], e.g. Chlorella
• CPC Class Codes: A61K 8/9767 Pinaceae [Pine family], e.g. pine or cedar
• CPC Class Codes: A61K 8/9789 Magnoliopsida [dicotyledons]
• CPC Class Codes: A61K 8/9794 Liliopsida [monocotyledons]
• CPC Class Codes: A61Q 19/00 : Preparations for care of the skin

Abstract

The present invention relates to acne and rosacea compositions by a six-prong synergistic combination treatment strategy that includes (1) control of excess sebum production, (2) control of undesirable bacteria or mites, (3) control of inflammation, (4) enhanced desquamation of follicular infundibulum cells, (5) reduction of irritation from anti-acne or rosacea compositions themselves, and (6) enhancement of the topical bioavailability of anti-acne and rosacea compositions. This is achieved by a synergistic combination of commonly utilized topical anti-acne and rosacea ingredients with a topical bioavailability enhancement composition, which results in enhanced anti-acne and rosacea action from such ingredients. Moreover, additional inclusion of an anti-inflammatory composition, and also a vascular micro-circulation enhancement composition, further results in synergistic superior anti-acne and rosacea benefits from such compositions. The present invention discloses additional surprising synergistic combinations for the control of acne and rosacea that are suitable for a variety of delivery systems and packaging forms.

Claims

1. A topical acne and rosacea treatment composition comprising:

(i) at least one acne and rosacea beneficial cosmetic or drug composition, and

(ii) at least one topical bioavailability enhancing antioxidant composition, and

(iii) at least one composition to improve micro-circulation, and

(iv) a cosmetically or pharmaceutically acceptable delivery system.

2. A composition according to claim 1 wherein,

(i) from about 0.0001% to about 40% of at least one acne and rosacea beneficial cosmetic or drug composition, and

(ii) from about 0.0001% to about 10% of at least one topical bioavailability enhancing antioxidant composition, and,

(iii) from about 0.0001% to about 10% of at least one composition to improve micro-circulation, and

(iv) from about 1% to about 99% of a cosmetically or pharmaceutically acceptable delivery system.

3. A composition according to claim 1 wherein topical acne or rosacea beneficial cosmetic or drug composition is selected from Salicylic acid, niacinamide salicylate, niacinamide ascorbate, niacinamide folate, niacinamide lipoate, niacinamide lactate, niacinamide glycolate, niacinamide mandalate, niacinamide malate, niacinamide hydroxycitrate, niacinamide hydroxytetronate, niacinamide aleurate, niacinamide petroselinate, niacinamide pantothenate, niacinamide adenosine monophosphate (AMP), niacinamide diphosphate (ADP), niacinamide adenosine triphosphate (ATP), niacinamide hydroquinone carboxylate, allantoin lactate, allantoin glycolate, allantoin mandelate, allantoin malate, allantoin ascorbate, allantoin phytate, allantoin citrate, allantoin hydroxy citrate, allantoin aleurate, allantoin salicylate, allantoin hyaluronate, glucosamine lactate, glucosamine glycolate, glucosamine malate, glucosamine mandelate, glucosamine ascorbate, glucosamine phytate, glucosamine citrate, glucosamine hydroxy citrate, glucosamine aleurate, glucosamine salicylate, glucosamine hyaluronate, creatine lactate, creatine glycolate, creatine malate, creatine mandelate, creatine ascorbate, creatine phytate, creatine citrate, creatine hydroxy citrate, creatine aleurate, creatine salicylate, creatine hyaluronate, niacinamide lactate, niacinamide glycolate, niacinamide malate, niacinamide mandelate, niacinamide ascorbate, niacinamide phytate, niacinamide citrate, niacinamide hydroxy citrate, niacinamide aleurate, niacinamide salicylate, niacinamide hyaluronate, pyridoxine lactate, pyridoxine glycolate, pyridoxine malate, pyridoxine mandelate, pyridoxine ascorbate, pyridoxine phytate, pyridoxine citrate, pyridoxine hydroxy citrate, pyridoxine aleurate, pyridoxine salicylate, pyridoxine hyaluronate, chitosan lactate, chitosan glycolate, chitosan malate, chitosan mandelate, chitosan ascorbate, chitosan phytate, chitosan citrate, chitosan hydroxy citrate, chitosan aleurate, chitosan salicylate, chitosan hyaluronate, azelaic acid, niacinamide azelate, pyridoxine azelate, chitosan azelate, glucosamine azelate, retinoic acid, niacinamide retinoate, pyridoxine retinoate, chitosan retinoate, glucosamine retinoate, Benzyl Alcohol, Dehydroacetic Acid, Phenoxyethanol, Ethylhexyl glycerin, Usnic acid, or combinations thereof.

4. A composition according to claim 1 wherein the topical bioavailability enhancing antioxidant composition is selected from Ascorbic acid, Ascorbic acid derivatives, Glucosamine ascorbate, Arginine ascorbate, Lysine ascorbate, Glutathione ascorbate, Nicotinamide ascorbate, Niacin ascorbate, Allantoin ascorbate, Creatine ascorbate, Creatinine ascorbate, Chondroitin ascorbate, Chitosan ascorbate, DNA Ascorbate, Carnosine ascorbate, Vitamin E, various Vitamin E derivatives, Tocotrienol, Rutin, Quercetin, Hesperedin (Citrus sinensis), Diosmin (Citrus sinensis), Mangiferin (Mangifera indica), Mangostin (Garcinia mangostana), Cyanidin (Vaccinium myrtillus), Astaxanthin (Haematococcus algae), Lutein (Tagetes patula), Lycopene (Lycopersicum esculentum), Resveratrol (Polygonum cuspidatum), Tetrahydrocurcumin (Curcuma longa), Rosmarinic acid (Rosmarinus officinalis), Hypericin (Hypericum perforatum), Ellagic acid (Punica granatum), Chlorogenic acid (Vaccinium vulgaris), Oleuropein (Olea europaea), α

-Lipoic acid, Niacinamide lipoate, Glutathione, Andrographolide (Andrographis paniculata), Carnosine, Niacinamide, Potentilla erecta extract, Polyphenols, Grapeseed extract, Pycnogenol (Pine Bark extract), pyridoxine, and combinations thereof.

5. A Composition According to claim 1 wherein the blood micro-circulation improvement composition is selected from Horse Chestnut Extract (Aesculus hippocastanum extract)), Esculin, Escin, Yohimbine, Capsicum Oleoresin, Capsaicin, Niacin, Niacin Esters, Methyl Nicotinate, Benzyl Nicotinate, Ruscogenins (Butchers Broom extract;

Ruscus aculeatus extract), Diosgenin (Trigonella foenumgraecum, Fenugreek), Emblica extract (Phyllanthus emblica extract), Asiaticoside (Centella asiatica extract), Boswellia Extract (Boswellia serrata), Ginger Root Extract (Zingiber Officianalis), Piperine, Vitamin K, Melilot (Melilotus officinalis extract), Glycyrrhetinic acid, Ursolic acid, Sericoside (Terminalia sericea extract), Darutoside (Siegesbeckia orientalis extract), Amni visnaga extract, extract of Red Vine (Vitis Vinifera) leaves, apigenin, phytosan, luteolin, and combinations thereof.

6. A composition according to claim 1 wherein cosmetically or pharmaceutically acceptable delivery system or carrier base can optionally include additional skin beneficial ingredients selected from skin cleansers, surfactants (cationic, anionic, non-ionic, amphoteric, and zwitterionic), skin and hair conditioning agents, vitamins, hormones, minerals, plant extracts, anti-inflammatory agents, concentrates of plant extracts, emollients, moisturizers, skin protectants, humectants, silicones, skin soothing ingredients, analgesics, skin penetration enhancers, solubilizers, moisturizers, emollients, anesthetics, colorants, perfumes, preservatives, seeds, broken seed nut shells, silica, clays, beads, luffa particles, polyethylene balls, mica, pH adjusters, processing aids, and combinations thereof.

7. A composition according to claim 1 wherein a cosmetically acceptable delivery system or a carrier base can be selected in the form of a lotion, cream, gel, spray, thin liquid, body splash, mask, serum, solid cosmetic stick, lip balm, shampoo, liquid soap, bar soap, bath oil, cologne, hair conditioner, salve, collodion, impregnated patch, impregnated strip, skin surface implant, and any other such cosmetically or pharmaceutically acceptable topical delivery forms.

8. The compositions according to claim 7 wherein the cosmetically or pharmaceutically acceptable delivery system can be traditional water and oil emulsions, suspensions, colloids, microemulsions, clear solutions, suspensions of nanoparticles, emulsions of nanoparticles, powders, or anhydrous compositions.