WO2002022120A1 - Analgesique et sa methode d'utilisation - Google Patents

Analgesique et sa methode d'utilisation Download PDF

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Publication number
WO2002022120A1
WO2002022120A1 PCT/US2001/026027 US0126027W WO0222120A1 WO 2002022120 A1 WO2002022120 A1 WO 2002022120A1 US 0126027 W US0126027 W US 0126027W WO 0222120 A1 WO0222120 A1 WO 0222120A1
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WIPO (PCT)
Prior art keywords
extract
group
agent
combinations
composition
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PCT/US2001/026027
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English (en)
Inventor
Teresa Leigh Barr
Stephen D. Holt
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Medical Merchandising, Inc.
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Publication date
Priority claimed from US09/662,962 external-priority patent/US6348501B1/en
Priority claimed from US09/800,245 external-priority patent/US6653352B2/en
Application filed by Medical Merchandising, Inc. filed Critical Medical Merchandising, Inc.
Priority to AU2001290552A priority Critical patent/AU2001290552A1/en
Publication of WO2002022120A1 publication Critical patent/WO2002022120A1/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A—HUMAN NECESSITIES
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    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
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    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
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Definitions

  • Arthritis is a common chronic problem, which occurs below the surface of the skin. Millions of people and animal have the condition. Various topical creams and ointments are sold for treatment of arthritis; however, most utilize an anesthetic, such as lidocaine, benzocaine or other numbing agent for the skin surface.
  • an anesthetic such as lidocaine, benzocaine or other numbing agent for the skin surface.
  • Capsaicin is also effective to relieve the various musculoskeletal pains, itching, neuropathic pains, dysesthesias caused by shingles, post herpetic neuralgia, post mastectomy pain, and peripheral neuropathies. It is further commonly prescribed to reduce the pain of neuropathies produced by diabetes (burning pain, discomfort, often at night) and other diseases that are neuropathic in origin including the discomfort and odd sensations of shingles (post herpetic neuralgia, which can be extremely painful), as well as dysesthesias that can occur with thoracotomies and post surgical scars. Unfortunately, although capsaicin is often the most effective agent available, the active ingredient is a potent skin irritant, producing a burning, uncomfortable sensation to the skin.
  • the burning side effect has also discouraged the use of capsaicin to treat other types of discomfort, such as pruritus or itching.
  • Pruritus or itching can be caused by many stimuli, such as poison ivy, hemorrhoids, or athlete's foot.
  • the unpleasant side effects of capsaicin have discouraged its use to treat such types of discomfort.
  • the burning that occurs when the skin is exposed to sunlight that has been treated with capsaicin or exposed to water has discouraged the use of capsaicin.
  • a capsaicin based pain reliever which does not irritate the skin or cause a burning discomfort even when exposed to water and sunlight, would be extremely desirable and acceptable to patients and people in general who are experiencing the types of pain or discomfort outlined above.
  • Prior attempts to produce such an invention can be seen in U.S. Patent No. 5,134,166 and
  • U.S. Patent No. 4,997,853 that use anesthetics in association with capsaicin, effectively numbing sites.
  • the present invention does not attempt to numb the site, and instead permit continued use of a hand or foot, with sensory input, rather than simply stopping all sensory input to the area while warming with capsaicin.
  • the present invention was developed to provide a lotion, which has as the three critical ingredients, capsaicin, plus an anesthetic and an analgesic.
  • composition overcomes other obstacles of known capsaicin creams in that the amounts used enable the warming relief of the peppers in combination with the coolness of the anaesthetic, yet enable the user to still feel objects they touch due to the use of an analgesic as a critical component rather than large amounts of analgesics.
  • the present invention has been developed which does not rely on topical anesthetics, such as lidocaine (Entry 5310, p.786 Merck Index, Tenth Edition 1983) and benzocaine (ethyl aminobenzoate, Entry 3710, p.546 Merck Index, Tenth Edition, 1983) into formulations containing capsaicin, and then applying such formulations for the initial period of treatment to eliminate the painful burning from the application of capsaicin, allowing the patient to continue therapy while being able to feel through the skin onto which the lotion is applied.
  • Arthritis is a common chronic problem, which occurs below the surface of the skin. Millions of people and animal have the condition.
  • Various topical creams and ointments are sold for treatment of arthritis; however, most utilize an anesthetic, such as lidocaine, benzocaine or other numbing agent for the skin surface.
  • the present invention relates to a method of treating arthritis using a lotion composition therefore in which capsaicin is used as the principle therapeutic agent along with an analgesic and an anaesthetic in a lotion.
  • An object of the present invention is to provide a lotion, which is easily applied, easy to absorb into the skin, and provides ability to feel objects.
  • composition comprising a carrier, capsaicin, an encapsulation agent, an ester of amino acid and a light-diffusing compound.
  • a method for treating a victim of pain or discomfort comprises applying the above-described composition topically to the skin of the victim near an area affected by the pain or discomfort.
  • a method for making a composition useful for topical application to treat pain or discomfort is carried out by mixing a carrier to form an aqueous solution, adding an encapsulation agent to reduce burning of the capsaicin, adding an amount of esters of amino acids and finally adding a light refractive element having an ability to stop secondary burning effect by the capsaicin due to the suns rays.
  • the resulting aqueous solution preferably has a cream-like viscosity.
  • Capsaicin is trans-8-methyl-N-vanillyl-5 nonenamide, a naturally occurring alkyl vanillylamide, a type of capsaicinoid. It is found in high concentration in fruit of plants of the Capsicum genus.
  • the genus capsicum is a member of a large tropical family Solanaceae.
  • Capsicum annum Capsicum Chinese and Capsicum frutescens are closely related.
  • Capsicum frutescens is also known as Cayenne Pepper, chili Pepper, Pimento Tabasco Pepper and Tabasco-sauce pepper. The chili pepper, red pepper and paprika all are species of Capsicum. All hot peppers contain capsaicinoids.
  • Capsaicinoids are natural materials, which produce a burning sensation in the mouth.
  • Capsicum has recently been officially defined in the US Pharmacopia 23 where it is defined as the dried ripe fruit of Capsicum frutescens Linne or Capsicum annum Linne.
  • capsaicinoids There are two main capsaicinoids, capsaicin and dihydrocapsaicin and three minor capsaicinoids, nordihydrocapsaicin, homocapsaicin andhomodihydrocapsaicin. All capsaicinoids are considered usable within the scope of this invention.
  • Capsicum is the dry powder obtained by grinding up the fruits of these plants.
  • Capsicum oleoresin or capsaicin oleoresin
  • Capsaicin a white crystalline material, is obtained from the liquid concentrate.
  • Capsaicin (N-Vanillyl-8-methyl-6-(E)-noneamide) is the most pungent of the capsaicinoids. It is very soluble in fats, oils and alcohols. Capsicum also contains a red coloring matter, oleic acid, palmitic acid and stearic acid. Capsicum frutescens extract can be obtained from Bio-Botanica, Inc. of Hauppauge, New York and appears as a viscous fluid, having a sallow yellow color, a caustic and pungent aroma, and is soluble in ethanol. Capsicum is a powerful local stimulant. It is strongly rubefacient acting without vesication.
  • the lotion of the invention comprises capsaicin as a first active ingredient.
  • the lotion will contain in the range of about 0.00125% to about 1.0% by weight of capsaicin.
  • Compositions containing more than about 1.0% by weight of capsaicin will provide a therapeutic effect, with up to 62.0% by weight capsaicin, except that the burning side effect will increase in proportion to the increase percentage of capsaicin.
  • Compositions containing 0.025% to 20.0% by weight of capsaicin could be used.
  • Compositions of 0.025 to 2.0% by weight are considered usable as well.
  • compositions containing in the range of 0.025% to 0.25% by weight of capsaicin are preferred because they are narrowly encompassed within current FDA guidelines regarding capsaicin use.
  • the FDA guidelines were developed at a time when there was not an effective method for relieving the discomfort generated by capsaicin.
  • the present invention provides a method to increase the amount of capsaicin that can be administered comfortably.
  • capsaicin is mixed with a carrier fluid.
  • the carrier fluid is water-based and forms an aqueous solution containing the ingredients.
  • the carrier may be a fluid, such as an oil based carrier, a fat based carrier, a fatty alcohol based carrier or a combination of these carriers. Deionized water also can be used as the carrier for the present invention.
  • the composition also may comprise an analgesic as a second active ingredient.
  • Additional irritant can be added to the capsaicin and carrier.
  • Histidines such as a histamine dihydrochloride, are considered usable in the scope of the present invention to create vasodilation, and act as a second irritant. It is possible to add more than one histidine to achieve the analgesic reaction.
  • any one of the following histidines, or combinations thereof, are considered usable in this invention: L-histidines, histamine dihydrochloride, DL-histidine, D-histidine hydrochloride monohydrate, L- histidine hydrochloride monohydrate, L-histidine methyl ester dihydrochloride, L-histidinol dihydrochloride, histamine phosphate.
  • Adding the second irritant produces an analgesic effect and does not numb the site, like an anesthetic or depress cutaneous sensory receptors. Instead, it has a topical counter-irritant effect by stimulating cutaneous sensory receptors, see, Federal Register, Vol. 48, No. 27, Tuesday February 8, 1983, pages 5367 et. seq.
  • amine and caine type local anesthetics such as benzocaine and lidocaine, act differently as anesthetics not producing an analgesic effect which is achieved by adding an additional irritant, such as a histamine hydrochloride or most preferably a histamine dihydrochloride.
  • the novel lotion of the present invention also uses an encapsulation agent, suitable examples of which include colloidal oatmeal, hydrogenated lecithin, dipotassium glycyrrhizinate. Similar encapsulation agents, or even combinations of these agents, have been found to be effective.
  • the encapsulation agent is colloidal oatmeal.
  • the colloidal oatmeal has intrinsic SFP, natural sunscreen capability.
  • the colloidal oatmeal encapsulates the capsaicin to reduce the inflammation effect the capsaicin has on the skin, while still enabling the capsaicin to work effectively.
  • colloidal oatmeal typically, up to about 3.0 wt. % colloidal oatmeal is used in this invention, although any amount between about 2.0 wt. % and up to about 10.0 wt. % can be used.
  • the colloidal oatmeal works within the scope of this invention because it contains hydrophilic colloids. These colloids help to provide a protective barrier on the skin to control inflammation.
  • histidines such as L-histidines, are present in colloid oatmeal. Histidines can be present in the oats in weight percents of up to about 3.0% of the total amino acids in the oats. The invention has found that using the colloidal oats synergistically enhance the histamine dichlorohydride effect, when histamine dichlorohydride is used.
  • the unique formulation is a topically (externally) applied formulation which has three simultaneous effects, analgesic, anesthetic and antipruritic effects, by (1) depressing cutaneous sensory receptors to relieve pain and (2) stimulating cutaneous sensory receptors using a topical counter irritant. It is the combination of analgesic and anesthetic effects, which make this invention unique.
  • the composition of the present invention also may comprise other additives.
  • the lotion may contain a coagulating agent, suitable examples of which include xanthum gum, myristal myristate, polyethylene glycols (PEG's) and other stearates for coagulation of the compound.
  • the composition also may comprise a transdermal activator.
  • "Lavender flower oil” or lavender oil, and a “bergaptene-free” bergamot oil or bergamot extract can be beneficial in that the lavender is an active transdermal activator which causes the formula to penetrate the skin; rather than remaining on the surface of the skin.
  • Lavender oil and bergamot extract also are beneficial in that both provide muscle relaxant characteristics.
  • the bergamot oil also provides help with acne, fevers, herpes, and diabetic neuropathy. Between about 1.0 and 2.0 wt. % of lavender oil is needed for transdermal activation, but between about 0.5 and about 5.0 wt % can be used.
  • the composition also may comprise a suspension agent.
  • a suspension agent is alkyl benzoate.
  • Alkyl benzoate is considered usable within the scope of the present invention, and helps to suspend the particle size of the colloidal oatmeal and titanium dioxide.
  • the lotion also can include any of the following components: Arnica montana, Hypericum perforarum (known as St.
  • Citric acid to adjust the pH of the compound
  • amino acid esters such as lauryl menthyl esters
  • propylene glycol with methyl and propyl parabens as preservatives
  • a chelating agent to keep the product from separating, such as edetatedisodium, triethanolamine hydrochloride which acts as a reagent, other preservatives and Benzoin derivatives.
  • Still other components considered usable in the present invention are phenoxy ethanol, ethyl paraben, and butyl paraben as preservatives, or in the preservative system.
  • Other ingredients, such as inositol, methyl paraben, propyl paraben, hydroxy ethyl cellulose can be used therein, for formulations which are gels rather than creams.
  • Carbomer 940 can be used to make the formula into a gel rather than a cream.
  • the present invention also may comprise menthol or an ester of an amino acid from which menthol can be obtained.
  • menthol or an ester of an amino acid from which menthol can be obtained.
  • the addition of menthol to the lotion of the present invention will provide the lotion with fast acting and long acting effects.
  • Suitable esters of amino acids include for example menthyl and lauryl esters of amino acids and combinations thereof.
  • a preferred ester of amino acid is menthyl lauryl pidolate.
  • the uses of the invention are contemplated for post perpetic neuralgia, and scar conditions after surgery, such as for treating the scars from a mastectomy. Also, the present invention is considered usably for victims of neuropathy, such as diabetes with neuropathy.
  • a victim of pain or discomfort is treated by applying the above-described composition topically to the skin of the victim near an area affected by the pain or discomfort.
  • the types of pain or discomfort to which the invention may be applied include those discussed in the background of the invention.
  • the inventive composition is applied to the selected area, such as a joint, and rubbed in.
  • the amount of lotion applied is not critical. Generally, it should be applied in an amount, which is sufficient to wet the area of application. Usually, the amount used will be in the range of from about 0.3 to about 3.0 ccs.
  • the application of the composition can be repeated as required to control the discomfort.
  • the preferred composition of the invention When the preferred composition of the invention is applied, it provides near immediate relief from the itching caused by poison ivy or hemorrhoids, without a burning sensation. The relief lasts for several hours. It is surprising that a capsaicin-based composition would be useful for the treatment of such discomfort.
  • additional compounds can be added to the formulation. These components can be methyl sulphonyl methane, sodium bicarbonate, calamine, allantoin, kaolin, and combinations thereof.
  • the treatment should be repeated several times per day, such as in the range of 2 to 8 times per day, preferably 3-5 times per day, and continued for several days.
  • most patients do not experience the burning discomfort heretofore known as a very common side effect of topical capsaicin application.
  • this formulation also as a spray using propellants, such as butyl propellants.
  • Propellant for the spray on composition contemplated as usable herein can be selected from the group butane, propane, isobutane, and combinations thereof.
  • a foam version of the formulation, additionally using a propellant and a surfactant is considered within the scope of the present invention.
  • a preferred surfactant is a member of the group of amine oxides. The most preferred surfactant is alkyl dimethyl amine oxide.
  • capsaicin is distributed according to known techniques in various pharmaceutically acceptable carriers to form a lotion.
  • Some of these carriers contain volatile diluents such as alcohol and may contain various emulsifying and suspending agents.
  • the present invention also may involve the use of an analgesic and an anesthetic in combination to produce a warm sensation on the patient's skin without the usual burning side effects of traditional capsaicin ointments or gels.
  • the invention also applies to a method for making the lotion comprising, the steps of mixing the preferred ingredients, heating the mixture to 60°C, adding the acetyl alcohol, the glycerol monostearate, the myristal myristate, the polysorbates and the titanium dioxide, then, one at a time, adding to the heated materials, benzyl alcohol, colloidal oatmeal, and lavender oil. While maintaining the temperature, the xanthum gum is dissolved into the propylene glycol, water and Uniphen P-23. The blended ingredients should then be removed from heat and the capsaicin should be dissolved into the benzyl alcohol the mixture is cooled to 40°C, the capsaicin is blended into the mixture forming the lotion.
  • this invention relates to a composition of matter useful for treating bodily pains and discomforts. In another aspect, this invention relates to a method for treating bodily pains and discomforts. In yet another aspect, this invention relates to formulating a pain and discomfort reliever.
  • capsaicinoids There are two main capsaicinoids, capsaicin and dihydrocapsaicin and three minor capsaicinoids, nordihydrocapsaicin, homocapsaicin and homodihydrocapsaicin. All capsaicinoids are considered usable within the scope of this invention.
  • the composition of the invention comprises capsaicin as a first active ingredient and at least one second active ingredient acting as an analgesic to reduce the sensation of capsaicin induced skin irritation.
  • the ingredients are contained in a carrier fluid.
  • the genus capsicum is a member of a large tropical family Solanaceae. There are numerous species, of which Capsicum annum, Capsicum Chinese and Capsicum frutescens are closely related. Capsicum frutescens is also known as Cayenne Pepper, chili Pepper, Pimento Tabasco Pepper and Tabasco-sauce pepper.
  • Capsicum is a powerful local stimulant. It is strongly rubefacient acting without vesication.
  • the dipotassium glycyrrhizinate is prepared from finely cut licorice root extracted with water. Ethanol is then added to this extract and the precipitate is separated after sedimentation. Inorganic acid is added to the filtrate, and the precipitating sediment is filtered. After neutralization with water, it is dissolved in a potassium hydroxide solution and evaporated until dry. The residue is recrystallized in media such as acetic acid or ethanol to obtain monopotassium glycyrrhizinate. The product is faintly yellow without an order and sweet in taste. Typically this product can be acquired from Barnet Products Corp. of Englewood Cliffs, New Jersey.
  • Hydrogenated lecithin is available from Barnet Products Corporation, as well. It is an emulsifier and stabilizer for solutions. In addition, it is used to reduce inflammation on the skin.
  • the unique lecithin will synergistically react with the dipotassium glycyrrhizinate to enhance the effect of the dipotassium glycyrrhizinate on encapsulation of the capsaicin. Additionally, the lecithin is used to reduce irritation that differs from inflammation. Inflamed skin is red and hot, irritated skin is itchy without necessarily being inflamed and red.
  • Esters of amino acids are next added to the formulation.
  • Esters of amino acid usable in the scope of this invention are preferably menthyl and lauryl esters of amino acids.
  • the esters of amino acid are menthyl lauryl pidolate.
  • This ester is comprised of menthyl as well as pidolic acid and lauric alcohol.
  • This component has no odor.
  • 0.1 - 1.0 wt. % is used in this compound in order to create the necessary analgesic effect.
  • the active element in this component is menthol that acts as an analgesic. It is considered within the scope of the present invention to use enough menthyl lauryl pidolate to attain between 0.1 and 16 wt % menthol in the formulation.
  • the unique formulation is a topically (externally) applied formulation which has three simultaneous effects, analgesic, anesthetic and antipruritic effects, by (1) depressing cutaneous sensory receptors to relieve pain and (2) stimulating cutaneous sensory receptors using a topical counter irritant. It is the combination of analgesic and anesthetic which make this invention unique.
  • Light scattering compounds can be any compound which has the ability to scatter light, such as by using particles having a diameter up to about 100 microns and more preferably between 30-60 microns.
  • Titanium dioxide is considered the best light scattering element for the present invention. Titanium dioxides usable within the scope of the present invention are preferably fine particle or pigmentary titanium dioxides available from Solaveil, of Durham, England. Any of the Solaviel TiO 2 products for cosmetic use can be used. All will reflects ultraviolet and provide broad UVB light protection, effectively scattering the light rays.
  • the TiO 2 can provide a complete block of sunlight, and when mixed with the colloidal oatmeal, the light waves can be refracted and the skin protected from burning from the light.
  • octyl dodecyl neopentanoate can be used for light scattering. Bernell Chemical sells these compounds.
  • Zinc oxide can be used as light scattering component, which also has the advantage of being anti-itch, or anti-pruritic effect.
  • benzophenones methoxycinnamate, para amino benzoic acid and combinations thereof can be used. It is also within the scope of the present invention, to add component onto the surface of the titanium dioxide to further enhance the effect of the titanium dioxide.
  • aluminum stearate and aluminum oxide can be additionally used with the titanium dioxide for light scattering.
  • the titanium dioxide, with or without the aluminum are typically dispersed in caprylic/capric triglyceride, causing this component to contain approximately 50% by weight of solids. It should be noted that other additives may be used in the present invention such as myristal myristate and other stearates for coagulation of the compound.
  • Xanthum gum can be added to the invention to provide a higher density compound, and act as a thickening agent.
  • Other elements such as licorice extract, glyceryl polymethacrylate and hydroxypropyl cellulose can be used in various formulations of the basic invention.
  • a suspension agent can be added to the formula of the present invention. Alkyl benzoate is considered usable within the scope of the present invention.
  • Deionized water is an excellent aqueous carrier for the present invention.
  • the present invention is fast acting and long acting due to the menthol present in the compositions.
  • the uses of the invention are contemplated for post perpetic neuralgia, and scar conditions after surgery, such as for treating the scars from a mastectomy.
  • the present invention is considered usably for victims of neuropathy, such as diabetes with neuropathy.
  • a victim of pain or discomfort is treated by applying the above-described composition topically to the skin of the victim near an area affected by the pain or discomfort.
  • the types of pain or discomfort to which the invention may be applied include those discussed in the background of the invention.
  • the inventive composition preferably in ointment or cream form, is applied to the selected area, such as a joint, and rubbed in.
  • the amount applied is not critical. Generally, it should be applied in an amount that is sufficient to wet the area of application. Usually, the amount used will be in the range of from about 0.3 to about 3 ccs.
  • the application of the composition can be repeated as required to control the discomfort.
  • the preferred composition of the invention When the preferred composition of the invention is applied, it provides near immediate relief from the itching caused by poison ivy or hemorrhoids, without a burning sensation. The relief lasts for several hours. It is surprising that a capsaicin-based composition would be useful for the treatment of such discomfort.
  • additional compounds can be added to the formulation. These components can be methyl sulphonyl methane, sodium bicarbonate, calamine, allantoin, kaolin, and combinations thereof.
  • the treatment should be repeated several times per day, such as in the range of 2 to 8 times per day, preferably 3-5 times per day, and continued for several days.
  • most patients do not experience the burning discomfort heretofore known as a very common side effect of topical capsaicin application.
  • this formulation for a gel, a cream, an opaque cream, a spray using propellants, such as butyl propellants, and a liquid or lotion, such as a roll on.
  • propellants such as butyl propellants
  • a liquid or lotion such as a roll on.
  • Propellant for the spray on composition contemplated as usable herein can be selected from the group butane, propane, isobutane, and combinations thereof.
  • a foam version of the formulation, additionally using a propellant and a surfactant is considered within the scope of the present invention.
  • a preferred surfactant is a member of the group of amine oxides. The most preferred surfactant is alkyl dimethyl amine oxide.
  • the resulting cream composition made in accordance with one embodiment of the invention contains the following ingredients.
  • the resulting gel composition made in accordance with one embodiment of the invention contains the following ingredients.
  • the resulting roll on/lotion composition made in accordance with one embodiment of the invention contains the following ingredients.
  • composition made in accordance with one embodiment of the invention contains the following ingredients.
  • the resulting day time formula composition made in accordance with one embodiment of the invention contains the following ingredients.
  • the resulting night time formula composition made in accordance with one embodiment of the invention contains the following ingredients.
  • the invention relates to a composition
  • a composition comprising: a topical carrier; a transdermal component selected from the group comprising peppermint extract, ester, ginger extract, horseradish extract, yarrow extract, chamomile extract, rosemary extract, methylsulfonylmethane, benzyl alcohol, benzoic acid and combinations thereof; a capsicum extract; an encapsulation agent selected from the group comprising gums and resins and their derivatives; a solubility agent; a viscosity adjusting agent; and an analgesic agent.
  • the viscosity adjusting agent is a member of the group comprising magnesium chloride, citric acid, sodium chloride, and combinations thereof
  • the analgesic agent is selected from the group histamine dihydrochloride, glucasomine, white willow bark, ibuprofen, salicylamide, salicylic acid and salsalate and combinations thereof.
  • the encapsulation agent is preferably selected from the group consisting of xanthum gum, gellan gum, arabica gum, acacia gum, gum tragacanth, guar gum, dammar resin, elemi resin, sandarac resin, polyvinyl acetate, polyester, amide, carboxymethyl cellulose, carboxymethyl hydroxyethyl cellulose, carboxypolymethylene and combinations thereof.
  • the composition can further comprise a skin and tissue emollient.
  • the most preferred topical carrier is selected from the group comprising: aqueous carriers, oil based carriers, fat based carriers, and fatty alcohol based carriers, water or combinations thereof.
  • the preferred ester is an alkyl ester.
  • the analgesic agent is a member of the group comprising histamine hydrochloride and methylnicotinate.
  • the preferred histamine is histamine hydrochloride is a dihydrochloride.
  • the analgesic agent has a weight percent in the range of about 0.025% up to about 0.1%.
  • the capsicum extract is in the range of 0.01 to 20.0 % by weight.
  • the composition can additionally comprise a light scattering element selected from the group: titanium dioxide, zinc oxide, and benzophenones, methoxy cinnamate, para amino benzoic acid, octyl, dodecyl, neopentanoate, aluminum stearate with titanium dioxide, aluminum oxide with titanium dioxide, and combinations thereof.
  • a light scattering element selected from the group: titanium dioxide, zinc oxide, and benzophenones, methoxy cinnamate, para amino benzoic acid, octyl, dodecyl, neopentanoate, aluminum stearate with titanium dioxide, aluminum oxide with titanium dioxide, and combinations thereof.
  • the invention can also comprise an anti-itch agent, which is a member of the group: methyl sulphonyl methane, sodium bicarbonate, calamine, allantoin, kaolin, and combinations thereof.
  • an anti-itch agent which is a member of the group: methyl sulphonyl methane, sodium bicarbonate, calamine, allantoin, kaolin, and combinations thereof.
  • the invention also includes a. patch for treating arthritis and neurological pains consisting of an elastomeric adhesive unit on which is disposed a formulation comprising an effective amount to treat arthritis and neurological pains comprising: a topical carrier; a transdermal component selected from the group comprising peppermint extract, ester, ginger extract, horseradish extract, yarrow extract, chamomile extract, rosemary extract, methylsulfonylmethane, benzyl alcohol, benzoic acid and combinations thereof; a capsicum extract; an encapsulation agent selected from the group comprising gums and resins and their derivatives; a solubility agent; a viscosity adjusting agent; and an analgesic agent.
  • a topical carrier a transdermal component selected from the group comprising peppermint extract, ester, ginger extract, horseradish extract, yarrow extract, chamomile extract, rosemary extract, methylsulfonylmethane, benzyl alcohol, benzoic acid and combinations thereof
  • the invention also applies a gel comprising: topical carrier; a transdermal component selected from the group comprising peppermint extract, ester, ginger extract, horseradish extract, yarrow extract, chamomile extract, rosemary extract, methylsulfonylmethane, benzyl alcohol, benzoic acid and combinations thereof; a capsicum extract; an encapsulation agent selected from the group comprising gums and resins and their derivatives; a solubility agent; a viscosity adjusting agent; and an analgesic agent.
  • the invention includes a sunscreen comprising, a topical carrier; a transdermal component selected from the group comprising peppermint extract, ester, ginger extract, horseradish extract, yarrow exfract, chamomile extract, rosemary extract, methylsulfonylmethane, benzyl alcohol, benzoic acid and combinations thereof; a capsicum extract; an encapsulation agent selected from the group comprising gums and resins and their derivatives; a solubility agent; a viscosity adjusting agent; and an analgesic agent; and a light scattering element having a particle size up to 100 nm.
  • a cream for treating pruritis comprising a topical carrier; a transdermal component selected from the group comprising peppermint extract, ester, ginger extract, horseradish extract, yarrow extract, chamomile extract, rosemary extract, methylsulfonylmethane, benzyl alcohol, benzoic acid and combinations thereof; a capsicum extract; an encapsulation agent selected from the group comprising gums and resins and their derivatives; a solubility agent; a viscosity adjusting agent; and an analgesic agent.
  • the transdermal component is used in amounts from about 0.01 to about to 33.0%, more preferably from about 0.5% to about 9.0%.
  • the invention also relates to a hemorrhoid cream comprising an effective amount to treat hemorrhoids comprising: a topical carrier; a transdermal component selected from the group comprising peppermint extract, ester, ginger extract, horseradish extract, yarrow extract, chamomile extract, rosemary extract, methylsulfonylmethane, benzyl alcohol, benzoic acid and combinations thereof; a capsicum extract; an encapsulation agent selected from the group comprising gums and resins and their derivatives; a solubility agent; a viscosity adjusting agent; and an analgesic agent.
  • the invention relates to a lotion comprising: a topical carrier; a transdermal component selected from the group comprising peppermint extract, ester, ginger extract, horseradish extract, yarrow extract, chamomile extract, rosemary extract, methylsulfonylmethane, benzyl alcohol, benzoic acid and combinations thereof; a capsicum extract; an encapsulation agent selected from the group comprising gums and resins and their derivatives; a solubility agent; a viscosity adjusting agent; an analgesic agent.; and an emulsifying agent.
  • the emulsifying agent is preferably glyceryl monostearate and polysorbate.
  • the invention also relates to a spray on formulation
  • a spray on formulation comprising: a propellant; a transdermal component selected from the group comprising peppermint extract, ester, ginger extract, horseradish extract, yarrow extract, chamomile extract, rosemary extract, methylsulfonylmethane, benzyl alcohol, benzoic acid and combinations thereof; a capsicum extract; an encapsulation agent selected from the group comprising gums and resins and their derivatives; a solubility agent; a viscosity adjusting agent; and an analgesic agent.
  • the propellant can be a butane, propane, isobutane, and combinations thereof.
  • the invention also pertains to a foam formulation comprising: a surfactant comprising an amine oxides; a propellant; a transdermal component selected from the group comprising peppermint extract, ester, ginger extract, horseradish extract, yarrow extract, chamomile extract, rosemary extract, methylsulfonylmethane, benzyl alcohol, benzoic acid and combinations thereof; a capsicum extract; an encapsulation agent selected from the group comprising gums and resins and their derivatives; a solubility agent; a viscosity adjusting agent; and an analgesic agent.
  • the most preferred surfactant is amine oxide is alkyl dimethyl amine oxide.
  • the invention also relates to a method for treating a victim of a discomfort comprising the step of applying a composition containing capsicum extract wherein said compositions further comprise a topical carrier, a transdermal component selected from the group comprising peppermint extract, ester, ginger extract, horseradish extract, yarrow extract, chamomile extract, rosemary extract, methylsulfonylmethane, benzyl alcohol, benzoic acid and combinations thereof, wherein the topical carrier comprises a member selected from the group comprising water, aqueous carriers, oil based carriers, fat based carriers, and fatty alcohol based carrier and combinations thereof, an encapsulation agent selected from the group comprising gums and resins and their derivatives, a solubility agent, a viscosity agent comprising a member of the group: magnesium chloride, citric acid, sodium chloride and combinations thereof, and an analgesic agent selected from the group: histamine dihydrochloride, glucasomine, white willow bark, ibu
  • the inventive method also works for victims that suffer from the discomfort caused by arthritis, hemorrhoids and pruritus.
  • the invention also relates to a daytime ingestible pain-relieving composition for human use comprising: a capsicum extract; an colloidal oatmeal encapsulation agent; an analgesic agent selected from the group histamine dihydrochloride, glucasomine, white willow bark, ibuprofen, salicylamide, salicylic acid and salsalate and combinations thereof, a pain-relieving component; a stimulant; an endurance enhancer, a mental alertness component, a stomach buffering agent, and a joint support supplement.
  • the preferred pain reliever is ibuprofen
  • the preferred stimulant is caffeine
  • the preferred joint support supplement is selected from the group comprising Boswellin, glucosamine, Chondroitin and methylsulfonylmethane.
  • the preferred endurance enhancer is ginseng.
  • the preferred mental alertness component is ginko biloba.
  • the most preferred stomach-buffering agents are either stevia or glycyrrhizinate.
  • the invention also relates to a nighttime ingestable pain-relieving composition for human use comprising: a capsicum extract; a colloidal oatmeal encapsulation agent; an analgesic agent selected from the group histamine dihydrochloride, glucosamine, white willow bark, ibuprofen, salicylamide, salicylic acid and salsalate and combinations thereof; a pain-relieving component; a sleep agent; a joint support supplement, and stomach buffering agent.
  • the pain-relieving component is ibuprofen, acetaminophen, salicylamide and combinations thereof
  • the preferred sleep agent is melatonin, kava kava, valerian root, passion flower, hops and diphenhydramine hydrochloride and combinations thereof.
  • the joint support supplement boswellin, glucosamine, chondroitin or methylsulfonylmethane.
  • the stomach buffering agent selected from the group stevia and glycyrrhizinate.

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Abstract

L'invention concerne une composition renfermant des extraits de capsicum et d'autres ingrédients permettant de neutraliser les sensations gênantes résultant de l'application d'extraits de capsicum sur la peau. Cette composition est destinée au traitement de différents types de douleurs, y compris les douleurs provoquées par l'arthrite, les neuropathies, la cicatrisation post-opératoire, les hémorroïdes douloureuses et pruriantes, et les prurits, et n'induit pas d'effets secondaires gênants normalement associées à l'application topique d'extraits de capsicum.
PCT/US2001/026027 2000-09-15 2001-09-14 Analgesique et sa methode d'utilisation WO2002022120A1 (fr)

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US09/662,962 US6348501B1 (en) 1999-09-29 2000-09-15 Lotion compositions utilizing capsaicin
US09/800,245 US6653352B2 (en) 1999-09-29 2001-03-06 Pain reliever and method of use
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Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007148307A1 (fr) * 2006-06-23 2007-12-27 The Procter & Gamble Company Compositions et trousses comprenant de la mélatonine et un constituant chondroprotecteur
WO2009047826A2 (fr) * 2007-10-11 2009-04-16 Tuttofarmaco S.R.L. Composition pharmaceutique renfermant du sucralfate et de la mésalazine
WO2010034019A1 (fr) * 2008-09-22 2010-03-25 Biochemics, Inc. Administration transdermique de médicaments employant un osmolyte et un agent vasoactif
GB2514417A (en) * 2013-05-24 2014-11-26 Susan Jane Branch Topical composition
US9278233B2 (en) 2008-12-04 2016-03-08 Biochemics, Inc. Methods and compositions for tattoo removal

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US4681897A (en) * 1984-01-16 1987-07-21 The Procter & Gamble Company Pharmaceutical products providing enhanced analgesia

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US4681897A (en) * 1984-01-16 1987-07-21 The Procter & Gamble Company Pharmaceutical products providing enhanced analgesia
US4812446A (en) * 1984-01-16 1989-03-14 The Procter & Gamble Company Pharmaceutical products providing enhanced analgesia

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007148307A1 (fr) * 2006-06-23 2007-12-27 The Procter & Gamble Company Compositions et trousses comprenant de la mélatonine et un constituant chondroprotecteur
WO2009047826A2 (fr) * 2007-10-11 2009-04-16 Tuttofarmaco S.R.L. Composition pharmaceutique renfermant du sucralfate et de la mésalazine
WO2009047826A3 (fr) * 2007-10-11 2009-09-11 Tuttofarmaco S.R.L. Composition pharmaceutique renfermant du sucralfate et de la mésalazine
WO2010034019A1 (fr) * 2008-09-22 2010-03-25 Biochemics, Inc. Administration transdermique de médicaments employant un osmolyte et un agent vasoactif
US9566256B2 (en) 2008-09-22 2017-02-14 Biochemics, Inc. Transdermal drug delivery using an osmolyte and vasoactive agent
US10537536B2 (en) 2008-09-22 2020-01-21 Biochemics, Inc. Transdermal drug delivery using an osmolyte and vasoactive agent
US10751309B2 (en) 2008-09-22 2020-08-25 Biochemics, Inc. Transdermal drug delivery using an osmolyte and vasoactive agent
US9278233B2 (en) 2008-12-04 2016-03-08 Biochemics, Inc. Methods and compositions for tattoo removal
US10322077B2 (en) 2008-12-04 2019-06-18 Biochemics, Inc. Methods and compositions for tattoo removal
GB2514417A (en) * 2013-05-24 2014-11-26 Susan Jane Branch Topical composition

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