Pharm/Biotech
Resources

Outsourcing Guide

Cont. Education

Software/Reports

Training Courses

Web Seminars

Jobs

Buyer's Guide

Home Page

Pharm Patents /
Licensing

Pharm News

Federal Register

Pharm Stocks

FDA Links

FDA Warning Letters

FDA Doc/cGMP

Pharm/Biotech Events

Consultants

Advertiser Info

Newsletter Subscription

Web Links

Suggestions

Site Map
 

 

 

 


Title:  Topically applied creatine containing composition

United States Patent:  6,730,331

Issued:  May 4, 2004

Inventors:  Stoll; David M. (9735 Wilshire Blvd., Suite 418, Beverly Hills, CA 90212)

Appl. No.:  136931

Filed:  April 30, 2002

Abstract

The present invention is a stable topical creatine application suitable for absorption directly through the skin into the underlying muscle without traveling through the blood system for the purpose of increasing muscle energy. It is created by combining creatine with phosphoric acid in a cosmetically elegant vehicle suitable for topical use. Chondroitin sulfate and glucosamine can also be added. Topical creatine avoids the side effects of oral creatine supplements.

SUMMARY OF THE INVENTION

The present invention is a topical application of creatine in a vehicle suitable for absorption directly through the skin into the underlying muscle without traveling through the blood system. The topical application includes ingredients with the functions of solvent, carrier for creatine, pH adjuster, amino acid, energy producer, skin conditioning agent, aromatic, skin smoothing agent, skin toning agent, buffer agent, preservative, and colorant.

Embodiments of the present invention could take the form of any of the following; a liquid, a gel, a cream, an ointment, a paste, a powder, a shampoo, a lotion, a patch, or a spray. The invention can also be impregnated into clothing such as hosiery or sportswear. Then when a person exercises their sweat leaches the creatine compound out of the clothing and into their skin. In addition, other ingredients such as amino acids, vitamins, minerals, carbohydrates, liposomes or penetration enhancers may be added.

Another embodiment of this invention includes the addition of glucosamine sulfate and chondroitin for patients who have evidence of osteoarthritis and other causes of pain ruled out.

DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENT

The preferred embodiment of the invention is a spray with the following formulation:

 Concentration Ingredient               Function
 25-30%        Water                    solvent
 45-50%        Ethanol                  solvent
 2-5%          Ethoxydiglycol           Carrier for creatine
 2-5%          Triethanolamine          pH adjuster (neutralizer)
 0.5-2%        Creatine monohydrate     Amino acid energy
 0.10-0.5%     Ginseng extract          Energy producer
 0.10-0.5%     Dimethicone copolyol     Skin conditioning agent
 0.05-0.5%     Lavender oil             aromatic
 0.05-0.5%     Bergamont oil            aromatic
 0.05-0.25%    Sage extract             Skin smoothing agent
 0.05-0.25%    Elder flower             Skin smoothing agent
 0.05-0.25%    Chamomile                Skin smoothing agent
 0.05-0.25%    Witch hazel extract      Skin toning agent
 0.10-0.5%     Phosphoric acid          Buffer agent
 0.10-0.5%     Phenoxyethanol           preservative
 0.05-0.25%    Methylparaben            preservative
 0.05-0.25%    Propylparaben            preservative
 0.05-0.25%    Butylparaben             preservative
 0.05-0.25%    Ethylparaben             preservative
 0.01-0.1%     Food Drug and Cosmetic Act colorant
               (FD & C) blue #1
 0.01-0.1%     FD & C red #40           colorant

The preferred method of preparing the creatine spray includes the following steps. Blending deionized water with phosphoric acid and creatine to create a clear and uniform slurry. Blending a neutralizer with deionized water, dimethicone copolyol, ginseng and a combination ofherbal extracts to achieve a skin soothing conditioner. Combining the slurry with the conditioner to create a stable creatine solution of pH 7.8. Blending ethanol and ethoxydiglycol into the stable creatine solution to form a fast drying, quickly absorbing stable creatine solution. This method of preparation is a novel way of putting creatine in solution without allowing conversion of creatine to creatinine. Testing has shown this method keeps the creatine viable in the liquid solvent for at least 6 months.

A novel discovery of the current invention relates to its absorption. Ingredients such as corticosteroids or sun screens when applied over large skin surfaces are absorbed into the systemic circulation and exhibit demonstrable plasma levels of those respective ingredients. As a small molecular weight (134) molecule, creatine should be rapidly absorbed into the systemic circulation, especially upon being applied over the entire skin surface of the body. However, studies demonstrate that no creatine was detected in the plasma of the volunteers 1 hour after application of the above formulation on the entire skin surface. This indicates that the easily absorbed creatine is being incorporated directly into the muscle without having to pass through the blood circulation. This affords easy bioavailability of the creatine to muscles. The topically applied creatine is absorbed and acts directly on the target organ similar to methylsalicylate in arthritis creams and aminophylline in thigh creams.

The alternate embodiment includes 0.25-3% chondroitin sulfate, or 0.25-3% glucosamine, or 0.25-3% chondroitin sulfate and 0.25-3% glucosamine.

EXPERIMENTS

A. Several volunteers had their blood drawn to determine baseline levels of creatine, serum glutamate oxalacetate transaminase (SGOT), serum glutamate pyruvate transaminase (SGPT) and bilirubin. The volunteers then applied the creatine 1% spray described herein, all over their entire skin surface. One hour later, their blood was again tested for plasma levels of creatine, SGOT, SGPT and bilirubin. The results were as follows:

  Baseline values 1 hour after application of creatine 1% spray
                           Volunteer 1:
        Creatine 0.5                      0.5
        SGOT 25                          23
        SGPT 13                          15
        Bilirubin 0.5                     0.5
                           Volunteer 2:
        Creatine 0.8                      0.8
        SGOT 18                          18
        SGPT 15                          16
        Bilirubin 0.5                     0.5
                           Volunteer 3:
        Creatine 0.5                      0.5
        SGOT 25                          22
        SGPT 23                          24
        Bilirubin 0.4                     0.4


All 3 volunteers used the creatine spray for 2 weeks before exercising and reported that they felt an increase in muscle energy by the end of the 2-week period.

B. A study was conducted on the invention at Alabama A&M University. There were seven participants. Three participants used placebo and four used the invention. Each applied the spray to their skin daily before working out. After two weeks they evaluated the product. The three who used placebo had no side effects and no good effects. Of the four who used the invention, none had any side effects and three felt that they experienced some increase in energy.

The topically applied creatine containing composition has been described with reference to a particular embodiment. Other modifications and enhancements can be made without departing from the spirit and scope of the claims that follow.

Claim 1 of 4 Claims

What is claimed is:

1. A muscle stimulant spray comprising:

                25-30%             Water
                45-50%             Ethanol
                2-5%               Ethoxydiglycol
                2-5%               Triethanolamine
               0.5-2%              Creatine monohydrate
              0.10-0.5%            Ginseng extract
              0.10-0.5%            Dimethicone copolyol
              0.05-0.5%            Lavender oil
              0.05-0.5%            Bergamont oil
              0.05-0.25%           Sage extract
              0.05-0.25%           Elder flower
              0.05-0.25%           Chamomile
              0.05-0.25%           Witch hazel extract
              0.10-0.5%            Phosphoric acid
              0.10-0.5%            Phenoxyethanol
              0.05-0.25%           Methylparaben
              0.05-0.25%           Propylparaben
              0.05-0.25%           Butylparaben
              0.05-0.25%           Ethylparaben
              0.01-0.1%            FD&C blue #1
              0.01-0.1%            FD&C red #40.



____________________________________________
If you want to learn more about this patent, please go directly to the U.S. Patent and Trademark Office Web site to access the full patent.

 

 

[ Outsourcing Guide ] [ Cont. Education ] [ Software/Reports ] [ Training Courses ]
[ Web Seminars ] [ Jobs ] [ Consultants ] [ Buyer's Guide ] [ Advertiser Info ]

[ Home ] [ Pharm Patents / Licensing ] [ Pharm News ] [ Federal Register ]
[ Pharm Stocks ] [ FDA Links ] [ FDA Warning Letters ] [ FDA Doc/cGMP ]
[ Pharm/Biotech Events ] [ Newsletter Subscription ] [ Web Links ] [ Suggestions ]
[ Site Map ]