Patent application title:

Topical vasodilator composition

Publication number:

-

Publication date:
Application number:

16/158,363

Filed date:

2018-10-12

βœ… Patent granted

Patent number:

US 10,478,466 B1

Grant date:

2019-11-19

PCT filing:

-

PCT publication:

-

Examiner:

Nannette Holloman

Agent:

Hall Estill Law Firm

Adjusted expiration:

2038-10-12

Smart Summary: A new skin treatment has been developed to help reduce bruises. It contains Arnica oil, which is known for its healing properties, along with a special herb called notoginseng that may improve blood flow. The composition also includes various silicone compounds to help with skin absorption. This combination aims to strengthen blood vessels and speed up the healing of bruises. Overall, the goal is to provide a more effective solution for treating skin contusions. πŸš€ TL;DR

Abstract:

A topical composition comprising from about 0.05% to about 10.0% by weight of Arnica oil, from about 5.0% to about 20.0% by weight of a notoginseng herb comprising dammarane-type ginsenosides, from about 0.05% to about 10% by weight of a compound comprising cyclopentasiloxane, dimethicone crosspolymer, dimethicone/vinyl dimethicone crosspolymer, dimethiconol, and a cosmetically acceptable aqueous carrier.

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Classification:

A61K36/258 »  CPC main

Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines; Magnoliophyta (angiosperms); Magnoliopsida (dicotyledons); Araliaceae (Ginseng family), e.g. ivy, aralia, schefflera or tetrapanax Panax (ginseng)

A61K9/0014 »  CPC further

Medicinal preparations characterised by special physical form; Galenical forms characterised by the site of application Skin, i.e. galenical aspects of topical compositions

A61K9/06 »  CPC further

Medicinal preparations characterised by special physical form Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels

A61K47/10 »  CPC further

Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient; Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers

A61K47/18 »  CPC further

Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient; Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids

A61K47/22 »  CPC further

Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient; Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones

A61K47/34 »  CPC further

Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient; Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers

A61K47/44 »  CPC further

Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient Oils, fats or waxes according to two or more groups of -; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin

A61P9/08 »  CPC further

Drugs for disorders of the cardiovascular system Vasodilators for multiple indications

A61K9/00 IPC

Medicinal preparations characterised by special physical form

Description

RELATED APPLICATIONS

This application is a continuation-in-part of U.S. patent application Ser. No. 15/043,940, filed on Feb. 15, 2016 which in turn claims priority to U.S. Provisional Patent Application No. 62/116,152 filed Feb. 13, 2015, the contents of which are hereby incorporated by reference.

FIELD OF THE INVENTION

The present invention relates to a topical skin treatment composition for the treatment of bruises.

BACKGROUND

A bruise, also known as a contusion, is a common skin injury that results from the breakage of tiny blood vessels leaking under the skin. Blood from damaged blood vessels beneath the skin collects near the surface of the skin to appear as what we recognize as a black and blue mark. This mark is from skin discoloration by red blood cells and their contents. Generally, there are limited treatments for contusions to the skin. Vascular dilators may be administered in an amount sufficient to improve blood supply to the skin. Without wishing to be bound by theory, vascular dilators are also believed to strengthen blood vessels. Bruise creams generally are available to consumers, which typically include at least Arnica oil either alone or in combination with Witch Hazel or Menthol. However, there is little evidence found that Arnica containing products actually reduce the duration of contusions. See Alonso D., Lazarus M. C., Baumann L; β€œEffects of topical arnica gel on post-laser treatment bruises” Dermatol Surg. 2002 Aug. 28(8):686-8.

A need continues to exist for a treatment that reduces the duration of contusions of the skin.

SUMMARY OF THE INVENTION

The present invention is directed to a topical composition comprising from about 0.05% to about 10.0% by weight of Arnica oil, from about 5.0% to about 20.0% by weight of a Panax herb comprising dammarane-type ginsenoside, and a cosmetically acceptable aqueous carrier.

DETAILED DESCRIPTION

The topical composition of the present invention comprises from about 0.05% to about 10.0% of Arnica oil. The composition also comprises from about 5.0% to about 20.0% of a Panax herb comprising dammarane-type ginsenoside. The topical composition is available in a cosmetically acceptable aqueous carrier.

The topical composition of the present invention comprises from about 0.05% to about 10.0%, preferably from about 0.5% to about 8%, more preferably from about 1.0% to about 5.0% by weight of the composition of Arnica oil. Arnica Oil or Arnica montana extract is a species containing helenalin, which is a sesquiterpene lactone possessing anti-inflammatory properties especially beneficial against bruising. Arnica montana extract stimulates activity of white blood cells, thus causing reduction of bruising and swelling. It assists the healing process by facilitating transport of blood and fluid accumulated in the injured area through a dilating action of subcutaneous blood capillaries. It accelerates the healing of damaged tissues by encouraging immune cell function and shortens the recovery time after the surgery or injury.

The topical composition of the present invention also comprises from about 5.0% to about 25.0%, preferably from about 8% to about 12%, more preferably from about 6.0% to about 10%, by weight of the composition of a Panax herb comprising dammarane-type ginsenosides. In preferred embodiments of the topical composition of the present invention the Panax herb comprising dammarane-type ginsenosides is selected from the group consisting of Panax ginseng, Panax quinquefolius, Panax vietnamensis, and Panax notoginseng and mixtures thereof. In a more preferable embodiment of the topical composition the Panax herb comprises Panax notoginseng.

In an alternate embodiment, the topical composition of the present invention also comprises from about 20.0% to about 30.0%, preferably from about 22.0% to about 28.0%, more preferably from about 24.0% to about 26.0%, by weight of the composition of a Panax herb comprising dammarane-type ginsenosides. In preferred embodiments of the topical composition of the present invention the Panax herb comprising dammarane-type ginsenosides is selected from the group consisting of Panax ginseng, Panax quinquefolius, Panax vietnamensis, and Panax notoginseng and mixtures thereof. In a more preferable embodiment of the topical composition the Panax herb comprises Panax notoginseng.

Panax ginsenosides are hemostatic perennial herbs predominantly grown in China and Japan and are known for their ability to invigorate the body and build blood. They are often used for treatment of blood related diseases and conditions, including blood stasis, angina, coronary heart disease. They are used to treat adrenal glands and conditions related to make sex hormones and prostate cancer.

A Panax ginsenoside composition may be produced by the process described in U.S. Pat. No. 6,500,468 B1, issued to Zeng et al. on Dec. 31, 2002.

The topical composition of the present invention further comprises a cosmetically acceptable aqueous carrier. The carrier comprises from about 70% to about 99.45% by weight of the composition. The carrier may be in the form of an ointment, cream, lotion, gel, paste, solution, or other such carriers known in the art. The carrier may contain liposomes, micelles, and/or microspheres. Carriers useful in this invention include any such materials known in the art that are nontoxic and do not interact with other components of the composition in a deleterious manner.

A preferred embodiment of the topical composition of the present invention comprises a carrier that is an ointment. Ointments, as is well known in the art, are semisolid preparations based on petrolatum or petrolatum derivatives. The specific ointment base to be used is one that will provide for optimum delivery of the composition and will provide other desirable characteristics, for example emoliency. Ointment bases may also contain vegetable oils, fats obtained from animals or polyethylene glycols.

Another preferred embodiment of the topical composition comprises a carrier that is a cream. Creams are viscous liquids or semisolid emulsions, either oil-in-water or water-in-oil. Cream bases contain an oil phase, an emulsifier, and an aqueous phase. The oil phase generally comprises petrolatum and a fatty alcohol such as cetyl or stearyl alcohol. The aqueous phase usually exceeds the oil phase in volume and may contain a humectant. The emulsifier is generally a nonionic, anionic, cationic or amphoteric surfactant.

Another preferred embodiment of the topical composition comprises a carrier that is a gel. Gels are semi-solid suspension-type systems. Single-phase gels contain organic macromolecules distributed substantially uniformly throughout the carrier liquid, which is typically aqueous, but also, preferably, contains an alcohol and, optionally, an oil. Preferred gelling agents are crosslinked acrylic acid polymers, such as the β€œcarbomer” family of polymers. E.g. carboxypolyalkylenes. Also preferred are hydrophilic polymers such as polyethylene oxides, polyoxyethylene-polyoxypropylene copolymers, and polyvinylalcohol; cellulosic polymers, such as hydroxypropyl cellulose, hydroxyethyl cellulose, hydroxypropyl methylcellulose and methylcellulose; gums such as tragacanth and xanthan gum, sodium alginate; and gelatin. In order to prepare a uniform gel, dispersing agents such as alcohol or glycerin can be added, or the gelling agent can be dispersed by trituration, mechanical mixing, or stirring, or combination thereof.

Another preferred embodiment of the topical composition comprises a carrier that is a lotion. Lotions are preparations to be applied to the skin surface without friction and are typically liquid or semiliquid preparation in which solid particles, including the active agents are present in a water or alcohol base. Lotions are usually suspensions of solids and preferably comprise a liquid oily emulsion of the oil-in-water type. It is generally necessary that the insoluble matter in a lotion be finely divided. Lotions typically contain suspending agents to produce better dispersion as well as compounds useful for localizing and holding the active agent in contact with the skin, e.g., methylcellulose, sodium carboxymethylcellulose, or the like.

An additional preferred embodiment of the topical composition of the present invention comprises a carrier that is a paste. Pastes are semisolid dosage forms in which the active agent is suspended in a suitable base. Depending on the nature of the base, pastes are divided between fatty pastes or those made from a single-phase aqueous gels. The base in a fatty paste is generally petrolatum, hydrophilic petrolatum, or the like. The pastes made from single-phase aqueous gels generally incorporate carboxymethylcellulose or the like as a base.

Formulations for the topical compositions may also be prepared with liposomes, micelles, and microspheres. Liposomes are microscopic vesicles having a lipid wall comprising a lipid bilayer, and can be used for topical delivery of the present composition as well. Liposomal preparations for use in this invention include cationic, anionic and neutral preparations.

Micelles are known as comprised of surfactant molecules arranged so that their polar headgroups form an outer spherical shell, while their hydrophobic hydrocarbon chains are oriented towards the center of the sphere forming a core. Micelles form in aqueous solution containing surfactant at a high enough concentration so that micelles naturally result. Surfactants useful for forming micelles include, but are not limited to, potassium laurate, sodium octane sulfonate, sodium decane sulfonate, sodium lauryl sulfate, docusate sodium, decyltrimethylammonium bromide, dodecyltrimethylammonium bromide, tetradecyltrimethylammonium bromide, dodecyl ammonium chloride, polyoxyl 12 dodecyl ether, and nonoxynol 30. Micelle formulations can be used in conjunction with the present invention either by incorporation into the reservoir of a topical delivery system, or into a formulation to be applied to the body surface.

Microspheres may also be used for topical administration of the composition of the present invention. Similarly, like liposomes and micelles, microspheres essentially encapsulate a composition to be applied on the skin. Microspheres are generally formed from synthetic or naturally occurring biocompatible polymers, but may also be comprised of charged lipids such as phospholipids.

The carrier in any form of topical delivery should be biologically and chemically inert, non-toxic, non-irritating and not interacting with components of the composition. Additionally, a carrier should provide for deep penetration of the composition into the skin.

The topical composition of this invention is a homeopathic composition comprising naturally derived ingredients, which can be used safely at the same time as conventional medicines, promoting accelerated time of recovery after surgery or skin injury, and guarding against staining of skin, swelling and pain.

Methods of Useβ€”The topical composition of the present invention are preferably applied topically to the desired area of the skin in an amount sufficient to provide effective delivery of the Arnica oil and Panax ginsenoside.

Method of Manufactureβ€”The topical compositions of the present invention may be prepared by any known or otherwise effective techniques, suitable for making the desired composition.

EXAMPLE

The following example further describes and demonstrates the embodiments of the present invention within the scope of the invention. The example is given solely for the purpose of illustration and is not to be considered as limitations of the present invention, as many variations thereof are possible without departing from the spirit and scope of the invention. All exemplified amounts are concentrations by weight of the Each exemplified example promotes improved healing and dissipation of contusions of the skin, as measured by the discoloration of the skin at the site of the contusion, through at least vasodilatation of the region afflicted by the contusion, when the composition is topical applied to the region of the skin presenting the contusion.

Example 1

Water 71.42%
Glycerin  3.00%
Arnica Oil  2.00%
Potassium Cetyl Phosphate  0.75%
Glyceryl Stearate Citrate  3.00%
Caprylic/Capric Triglyderides  4.25%
Shea Butter  2.00%
Ceteareth 20  2.00%
Cetearyl Alcohol  4.17%
Panax Notoginseng  5.00%
MSM  0.75%
Dimethicone 200 Fluid  0.50%
Phytonadione (Vitamin K)  0.25%
Camellia Sinensis (Green  0.01%
Tea) Leaf Extract
Vitamin E  0.10%
Germall  0.80%

Example 2

Water 58.35%
Glycerin  2.60%
Arnica Oil  1.72%
Potassium Cetyl Phosphate  0.65%
Glyceryl Stearate Citrate  2.60%
Caprylic/Capric Triglyderides  3.65%
Shea Butter  1.72%
Ceteareth 20  1.72%
Cetearyl Alcohol  3.58%
Panax Notoginseng 21.00%
MSM  0.75%
Dimethicone 200 Fluid  0.50%
Phytonadione (Vitamin K)  0.25%
Camellia Sinensis (Green  0.01%
Tea) Leaf Extract
Vitamin E  0.10%
Germall  0.80%

Example 3

Water (or) Aqua 60.44%
Dimethyl Sulfone  1.50%
Carbomer  0.50%
Caprylic/Capric Triglycerides  2.50%
Glyceryl Stearate Citrate  3.00%
Arnica Montana Flower Oil  7.00%
Cetearyl Alcohol  3.25%
Glyceryl Stearate (and) PEG 100  1.50%
Stearate
Glyceryl Stearate (and) Behenyl  0.50%
Alcohol (and)
Palmitic Acid (and) Stearic Acid (and)
Lecithin
(and) Lauryl Alcohol (and)
Myristyl Alcohol (and) Cetyl Alcohol
Butyrospermum Parkii (Shea Butter)  0.10%
Dimethicone  4.00%
Cyclopentasiloxane  1.50%
Cyclopentasiloxane (and)  7.00%
Dimethicone Crosspolymer
(and) Dimethicone/Vinyl
Dimethicone Crosspolymer
(and) Dimethiconol
Notoginseng Powder  5.00%
Phytonadione (Vitamin K1)  0.25%
Camellia Sinensis (Green Tea) Leaf  0.01%
Extract
Tocopheryl Acetate  0.10%
Potassium Hydroxide  0.35%
Hydroxyacetophenone  0.50%
1,2-Hexanediol (and) Caprylyl Glycol  1.00%

The dimensions and values disclosed herein are not to be understood as being strictly limited to the exact numerical values recited. Instead, unless otherwise specified, each such dimension is intended to mean both the recited value and a functionally equivalent range surrounding that value. For example, a dimension disclosed as β€œ40 mm” is intended to mean β€œabout 40 mm.”

All documents cited in the Detailed Description of the Invention are, in relevant part, incorporated herein by reference; the citation of any document is not to be construed as an admission that it is prior art with respect to the present invention.

While particular embodiments of the present invention have been illustrated and described, it would be obvious to those skilled in the art that various other changes and modifications can be made without departing from the spirit and scope of the invention. It is therefore intended to cover in the appended claims all such changes and modifications that are within the scope of this invention.

Claims

What is claimed is:

1. A topical composition comprising:

(a) from about 0.05% to about 10.0% by weight of Arnica oil;

(b) from about 5.0% to about 20.0% by weight of a notoginseng herb comprising dammarane-type ginseno sides;

(c) from about 0.05% to about 10% by weight of a compound comprising cyclopentasiloxane, dimethicone crosspolymer, dimethicone/vinyl dimethicone crosspolymer, and dimethiconol;

(d) from about 0.05% to about 5.0% by weight cetearyl alcohol;

(e) from about 0.75% to about 0.85% by weight of a compound formed from diazolidinyl urea (β€œDU”) and iodopropynyl butylcarbamate (β€œIPBC”), wherein the ratio of DU to IPBC is substantially 99% to 1% by weight;

(f) about 0.05% to about 2.5% by weight of dimethyl sulfone;

(g) about 0.25% weight of phytonadione; and

a cosmetically acceptable aqueous carrier, wherein upon a topical application of the composition to a skin contusion region, such application promotes vasodilatation in the region and dissipation of the contusion, wherein the notoginseng herb comprising dammarane-type ginsenosides is selected from the group consisting of, Panax quinquefolius, Panax vietnamensis, and Panax notoginseng and mixtures thereof.

2. The topical composition according to claim 1, in which the cetearyl alcohol comprising from about 1.05% to about 4.0% by weight cetearyl alcohol.

3. The topical composition according to claim 1, further comprising from about 0.05% to about 8.0% by weight dimethicone.

4. The topical composition according to claim 3, further comprising from about 0.01% to about 2.5% by weight of cyclopentasiloxane.

5. The topical composition according to claim 1, further comprising from about 0.01% to about 2.5% by weight of cyclopentasiloxane.

6. The topical composition according to claim 5, further comprising from about 2.75% to about 3.25% by weight of glycerin.

7. The topical composition according to claim 1, further comprising about 0.10% by weight of vitamin E.

8. The topical composition according to claim 1, in which the cosmetically acceptable aqueous carrier is in the form of an ointment.

9. The topical composition according to claim 1, in which the cosmetically acceptable aqueous carrier is in the form of a cream.

10. The topical composition according to claim 1, in which the cosmetically acceptable aqueous carrier is in the form of a gel.

11. The topical composition according to claim 1, in which the cosmetically acceptable aqueous carrier is in the form of a lotion.

12. The topical composition according to claim 1, in which the cosmetically acceptable aqueous carrier is in the form of a paste.

13. The topical composition according to claim 1, further comprising liposomes, and/or micelles, and/or microspheres, wherein the liposomal preparation include cationic, and/or anionic, and/or neutral preparations.

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