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WO2009114812A1 - Compositions anti-transpirantes contenant un sel de cuivre et leurs procédés d’utilisation - Google Patents

Compositions anti-transpirantes contenant un sel de cuivre et leurs procédés d’utilisation Download PDF

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Publication number
WO2009114812A1
WO2009114812A1 PCT/US2009/037169 US2009037169W WO2009114812A1 WO 2009114812 A1 WO2009114812 A1 WO 2009114812A1 US 2009037169 W US2009037169 W US 2009037169W WO 2009114812 A1 WO2009114812 A1 WO 2009114812A1
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WIPO (PCT)
Prior art keywords
composition
salt
copper
copper salt
total volume
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/US2009/037169
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English (en)
Inventor
Ernest Bloom
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Individual
Original Assignee
Individual
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Filing date
Publication date
Priority claimed from US12/402,497 external-priority patent/US20090257970A1/en
Application filed by Individual filed Critical Individual
Priority to EP09719053A priority Critical patent/EP2252252A1/fr
Priority to CA2717536A priority patent/CA2717536A1/fr
Publication of WO2009114812A1 publication Critical patent/WO2009114812A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A61K8/368—Carboxylic acids; Salts or anhydrides thereof with carboxyl groups directly bound to carbon atoms of aromatic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/42—Amides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q15/00—Anti-perspirants or body deodorants

Definitions

  • compositions relate to a ⁇ tiperspirant compositions, and more particularly to antiperspirant compositions containing a copper salt and a penetration enhancer. Certain compositions further include an aluminum or zirconium salt.
  • Antiperspirant compositions based on aluminum and zirconium are well known.
  • Shin et al. U.S. Pat. No. 4,774,079
  • Parekh et al. U.S. Pat. No. 6,902,724
  • Carrillo et al. U.S. Pat. No. 6,991,781
  • the mechanism of antiperspirants, such as these involves the formation of aluminum or zirconium hydroxide precipitates, which plug the sweat ducts and block sweat from reaching the skin surface.
  • salicylic acid has been used in certain antiperspirant formulations, For instance, a salicylic acid gel base has been used as a vehicle for aluminum chloride hexahydrate in the treatment of hyperhidrosis, as described in A. Benohanian et al., Intern ⁇ tion ⁇ lJoum ⁇ l of Dermatology, 37, 701-703 (1998), the entire disclosure of which is hereby incorporated by reference. Salicylic acid has also been used in antiperspirant compositions based on aluminum and zirconium (see, e.g., Motley et al., U.S. Pat. No, 5,516,511). Despite these advances, more effective topical antiperspirant compositions are needed, particularly for those patients suffering from excessive perspiration, and for those patients who do not respond well to available conventional therapies.
  • compositions including a copper salt and a penetration enhancer. Certain compositions further include a salt of aluminum or zirconium, or a mixture thereof.
  • the copper salt can be a copper(II) salt.
  • the copper salt can be copper chloride or copper chloride dihydrate.
  • the copper salt may be dissolved in the composition.
  • the copper salt can be included in the composition in an amount from about 0.1% to about 25% by weight of the total volume of the composition.
  • the copper salt may be included in the composition in an amount from about 1% to about 16% by weight, of the total volume of the composition, e.g. about 2%, about 4%, about 8%, or about 15%.
  • the penetration enhancer may be included in an amount from about 0.1 % to about 50% by weight, of the total volume of the composition.
  • the penetration enhancer may be included in an amount from about 1% to about 20%, e.g. from about 1% to about 10%, e.g. about 4%.
  • the composition may include water.
  • water may be included in an amount from about 0.4% to about 10% by volume, of the total volume of the composition.
  • the composition may include an alcohol, e.g. a straight-chain, branched, or cyclic alcohol having from about 1 to about 8 carbon atoms.
  • the alcohol may be ethyl alcohol.
  • the alcohol may be present in an amount from about 0.1% to about 50% by volume, of the total volume of the solution, e.g. from about 1% to about 40%, e.g. about 20%.
  • the composition may also include an organic carrier.
  • the organic carrier maybe selected from the group consisting of straight-chain, branched, and cyclic alcohols, polyols (including diols and glycols), esters, and carbonates having from about 1 to about 6 carbon atoms, and combinations thereof.
  • the organic carrier can be propylene glycol.
  • the composition may include an aluminum salt, a zirconium salt, or a mixture thereof.
  • the aluminum or zirconium salt may be a hydrate.
  • the composition may include aluminum trichloride hexahydrate.
  • the aluminum or zirconium salt may be included in an amount from about 0.1% to about 25% by weight of the total volume of the composition.
  • the aluminum or zirconium salt may be included in an amount from about 1% to about 10%, e.g. about 4%.
  • Implementations include methods for reducing or preventing perspiration and for treating hyperhidrosis. Implementations also include methods for treating or preventing undesirable odors associated with human sweat glands and skin. Certain methods comprise applying an effective amount of a composition containing a copper salt and a penetration enhancer to the skin of a human subject, In some methods, the composition may also include an aluminum or zirconium salt (or a mixture thereof). Other methods include first applying an effective amount of a composition containing a copper salt and a penetration enhancer followed by applying an effective amount of a composition containing an aluminum or zirconium salt (or a mixture thereof). In some methods, die subject may suffer from social sweating associated with normal daily activities. In composition containing an aluminum or zirconium salt (or a mixture thereof). In some methods, the subject may suffer from exercise-induced sweating.
  • compositions can combine in an additive or synergistic manner the effects of copper with the effects of the penetration enhancer.
  • the effects of copper may also be additive or synergistic with the effects of aluminum or zirconium.
  • the compositions may be effective in reducing perspiration and in treating excessive perspiration or hyperhidrosis, particularly with, but not limited to, subjects not responding well to other treatments.
  • the compositions may reduce perspiration for an extended time after application so that application may be necessary only a few times per week, or month, to achieve and maintain the desired degree of reduced perspiration.
  • the compositions may be effective for treating the axillae, hands, feet, lower back, groin, and other areas.
  • antiperspirant compositions comprising a copper salt and a penetration enhancer.
  • concentrations are initial concentrations, Le, those at the time the composition is made (e.g. shortly after the constituent is added to the composition). It is understood, Md within the scope of this invention, that concentrations of certain constituents at later times may be different than the initial concentrations (e.g. due to evaporation).
  • copper salt includes copper ions in the form of or derived from one or more copper salts, including copper salt hydrates.
  • the copper salts used herein are chiefly salts or salt hydrates of copper(II).
  • Examples of copper salts useful herein include, without limitation, chlorides, bromides, iodides, sulfates, nitrates, cyanides, acetates, acetylacetates, oxalates, carbonates, formates, oleates, and maleates, or hydrates thereof, (for example, but not limited to, co ⁇ er(II) chloride dihydrate (CuCl 2 (H 2 O) 2 ) and copper(II) sulfate pentahydrate (Cu(SO 3 )(H 2 O) 5 )).
  • inorganic and organic salts may also be used, such as those found in S.M. Berge et al, J. Phanna Sci., 66(1), 1-19 (1977), and Remington: The Science and Practice ofPhamiacy, R. Hendrickson, ed., 21st edition, Lippincott, Williams & Willdns, Philadelphia, PA (2005) at p. 732 S Table 38-5.
  • the antiperspirant effect of the copper salts described herein is chiefly due to the therapeutic inhibition of cell metabolic activity by the metal or metal ion.
  • Target cells of this inhibition include cells that are part of, and related to, the sweat glands and associated structures.
  • This proposed mechanism is different from the conventional mechanism of aluminum and zirconium salts.
  • a significant portion of the inhibitory biological action of copper is thought to come from its redox properties. Copper can catalyze the production of very reactive radical ions such as the hydroxyl radical. An increase in free radicals of this type is known as oxidative stress, and is an active area of research In a variety of diseases where copper may play an important role.
  • oxidative stress can inhibit cell growth or cause cell death, as reported, for example, by L.M. Gaetke and CK. Chow, Toxicology, 189(1-2), 147-63 (2003); and G. Filomeni et al, J. Biol. Chem., 282(16), 12010-21 (2007).
  • Copper may interfere with other vital cellular functions, including highly energy-dependant membrane pumping functions, which occur in sweat glands. It is therefore thought that copper (e.g. Cu(II) and Cu(I)) may damage, disrupt, or even cause apoptosis or cell death of some the sweat gland cells, thereby reducing or eliminating sweat production.
  • penetration enhancer means an agent which enables or increases entrance of substances primarily into the lumen of the sweat gland duct.
  • a penetration enhancer may also increase percutaneous absorption through the epidermis, to the dermis, and into the bloodstream.
  • Penetration enhancers of the disclosed compositions include salicylic acid and urea.
  • Other penetration enhancers, such as dimethylsulfoxide (DMSO) may also be used.
  • Suitable penetration enhancers such as those listed in Remington (2006), at page 959 ⁇ see Table 47-9), may also be used, including surfactants such as sodium lauryl sulfate, sodium laurate, sodium dodecylsulfate, polyoxyetfaylene-20-cetylether, and polyoxyethylene-9-lauryl ether, bile salts and derivatives such as sodium glycocholate, fatty acids and derivatives such as oleic acid and caprylic acid, and other agents such as citric acid, EDTA, decylrnethyl sulfoxide, glycerol, azone, and cyclodextrin.
  • surfactants such as sodium lauryl sulfate, sodium laurate, sodium dodecylsulfate, polyoxyetfaylene-20-cetylether, and polyoxyethylene-9-lauryl ether
  • bile salts and derivatives such as sodium glycocholate
  • fatty acids and derivatives
  • salicylic acid and urea may act as penetration enhancers of the active antiperspirant ingredient.
  • Salicylic acid is a keratolytic agent, causing cells of the epidermis to slough off, and causing keratin-lined skin pores and ducts to remain more open.
  • Salicylic acid is known in the treatment of eczema, keratosis pilaris, psoriasis, and related skin conditions.
  • salicylic acid may enhance biological access or absorption of the active antiperspirant ingredient, as disclosed in A, Benohanian et al., above, by improving access to and/or maintaining enhanced opening (patency) of the sweat gland ducts. It is thought that urea may have a similar effect since urea is also a widely used keratolytic agent for treating the skin conditions mentioned above. Salicylic acid may also have other beneficial properties, such as promoting normal skin (non-perspiration related) hydration levels, as also disclosed in A. Benohanian et al., above.
  • a suitable organic carrier will have certain desirable properties including the ability to (i) dissolve or disperse the copper salt and the penetration enhancer; (ii) enable a stable, homogeneous composition to be formed; (iii) dry soon after being applied to the skin; and (iv) leave little to no residue after drying.
  • Suitable organic carriers may also be selected for viscosity, lubricity, and other properties.
  • Suitable organic carriers used herein include straight-chain, branched, and cyclic alcohols, polyols (including diols and glycols), esters, and carbonates having from about 1 to about 6 carbon atoms.
  • Examples include, without limitation, methanol, ethanol, n-propanol, isopropanol, n ⁇ butanol, 2- methoxyethanol, 2-ethoxyethanol, ethylene glycol, 1,2-pro ⁇ ylene glycol, diethylene glycol, isopropanol, isobutanol, diethylene glycol monoethylether, 1,3-butylene glycol, 2,3-butylene glycol, dipropylene glycol, and 2,4-dihydroxy-2-raethylpentane.
  • suitable organic carriers including excipients and colloidal systems
  • certain organic carriers may also act as penetration enhancers.
  • water, an alcohol, or both water and an alcohol may be added to the composition to alter the solubility, viscosity, lubricity, and other properties of the composition.
  • Suitable alcohols include straight-chain, branched, and cyclic alcohols having from about 1 to about 8 carbon atoms.
  • Exemplary alcohols include, without limitation, methanol, ethanol, isopropanol, n-propanol, n-butanol, isobutanol, tert-butyl alcohol, 1-hexanol, l-octanol s and cyclohexanol.
  • Other suitable alcohols may also be used.
  • compositions comprising a copper salt and a penetration enhancer also include an aluminum salt, a zirconium salt (which include hydrates thereof) or a mixture thereof.
  • aluminum trichloride hexahydrate AlCl 3 (HsO) S
  • AlCl 3 (HsO) S aluminum trichloride hexahydrate
  • compositions of a copper salt with an aluminum and/or zirconium salt also include one or more substituents listed above, including an organic carrier, water, and an alcohol.
  • methods of reducing or preventing perspiration, of treating hyperhidrosis, and of treating or preventing undesirable odors associated with human sweat glands and skin include applying to the skin of a human an effective amount of a composition comprising a copper salt and a penetration enhancer.
  • a method of reducing or preventing perspiration, of treating hyperliidrosis, or of treating or preventing undesirable odors associated with human sweat glands and skin include first applying a composition comprising a copper salt and a penetration enhancer followed by applying a composition comprising an aluminum or zirconium salt (or a combination thereof).
  • the subject may suffer from social sweating associated with normal daily activities.
  • the subject may suffer from exercise-induced sweating.
  • compositions described herein will typically be administered locally and topically at the desired location, for example, but not limited to, the axillae, hands, feet, and groin areas.
  • the compositions may be administered by direct application or with a suitable skin applicator.
  • the composition may also be administered via or as part of any other suitable vehicle, applicator, or deodorant or antiperspirant formulation, including, without limitation, a dropper (e.g. an eye-dropper or pipette), a sponge-top type applicator, a spray, aerosol, roll-on, stick, gel, lotion, cream, salve, or powder.
  • a human female subject was identified as suffering from social sweating associated with various daily activities. She also had underirable axiiaary odor(s) in day- to-day social situations. Approximately 1 -3mls of Solution 2 of Example 1 was applied at each treatment to the axillae of the subject, either directly or using an applicator. The subject treated herself at bedtime. Within two successive daily bedtime applications, sweat production and any associated malodor had markedly decreased. Once achieved, this antiperspirant effect could be maintained by similar reapplications approximately once per week.
  • a human female subject was identified as suffering from exercise-induced sweating. Approximately l-3mls of Solution 3 of Example 1 was applied at each treatment to the feet of the subject, either directly or using an applicator. The subject treated herself at bedtime. Within two successive daily bedtime applications, sweat production markedly decreased. Once achieved, this antiperspirant effect could be maintained by similar reapplications approximately two to three times per week.
  • a human male subject was identified as suffering from exercise-induced sweating. Approximately l-3mls of Solution 3 of Example 1 was applied at each treatment to the hands of the subject, either directly or using an applicator. The subject treated himself at bedtime. Within two successive daily bedtime applications, sweat production markedly decreased. Once achieved, this antiperspirant effect could be maintained by similar reapplications approximately two to three times per week.
  • Example 6 Treatment of the Lower Back
  • a human male subject was identified as suffering from exercise-induced sweating. Approximately ImI of Solution 2 of Example 1 was applied at each treatment to the lower back of a human male subject, either directly or using an applicator. The subject treated himself nightly. Two or three such applications resulted in approximately 80-90% reduction in sweating, as measured by a comparison of the total amount of sweat absorbed by a cloth. The measurements were made immediately following defined regimens of exercise. The baseline was determined by comparing the data from the pre- and post-treatment periods. This significant antiperspirant effect could be maintained by similar reapplications approximately once or twice per week.
  • Solutions 5, 6 and 7 were prepared in accordance with Example 1, with the substitution or addition OfAlCIa(HjO) C where indicated.
  • Percentage of water is the percentage of water added in addition to water added from the metal salt hydrate.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Cosmetics (AREA)

Abstract

La présente invention concerne des compositions anti-transpirantes contenant un sel de cuivre et un activateur de pénétration. L’activateur de pénétration peut être l’acide salicylique ou l’urée. Outre le sel de cuivre, la composition peut également comporter un sel d’aluminium ou de zirconium. L’invention concerne également des procédés d’utilisation des compositions. Des modes de réalisation peuvent être utiles dans le traitement de la transpiration, de l’hyperhidrose, et des odeurs indésirables associées des aisselles, des mains, des pieds, du bas du dos, de l’aine, et d’autres régions corporelles.
PCT/US2009/037169 2008-03-14 2009-03-13 Compositions anti-transpirantes contenant un sel de cuivre et leurs procédés d’utilisation Ceased WO2009114812A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP09719053A EP2252252A1 (fr) 2008-03-14 2009-03-13 Compositions anti-transpirantes contenant un sel de cuivre et leurs procédés d utilisation
CA2717536A CA2717536A1 (fr) 2008-03-14 2009-03-13 Compositions anti-transpirantes contenant un sel de cuivre et leurs procedes d'utilisation

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US6949708P 2008-03-14 2008-03-14
US61/069,497 2008-03-14
US12/402,497 2009-03-12
US12/402,497 US20090257970A1 (en) 2008-03-14 2009-03-12 Antiperspirant compositions containing a copper salt and a penetration enhancer and methods of using the same

Publications (1)

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WO2009114812A1 true WO2009114812A1 (fr) 2009-09-17

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EP (1) EP2252252A1 (fr)
CA (1) CA2717536A1 (fr)
WO (1) WO2009114812A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016060626A1 (fr) * 2014-10-16 2016-04-21 Geli̇şi̇m Maki̇na-Madenci̇li̇k-Mühendi̇sli̇k Ti̇c. Ve San. Ltd. Şti̇. Procédés et compositions pour prévenir et traiter l'hyperhidrose

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030007939A1 (en) * 1998-07-31 2003-01-09 Howard Murad Pharmaceutical compositions and methods for managing dermatological conditions
US20040062681A1 (en) * 2002-09-30 2004-04-01 Winston Anthony E. Pseudo-plastic or thixotropic liquid deodorant product for ostomy pouches
US20070110687A1 (en) * 2005-11-16 2007-05-17 Jairajh Mattai Antiperspirant Compositions

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030007939A1 (en) * 1998-07-31 2003-01-09 Howard Murad Pharmaceutical compositions and methods for managing dermatological conditions
US20040062681A1 (en) * 2002-09-30 2004-04-01 Winston Anthony E. Pseudo-plastic or thixotropic liquid deodorant product for ostomy pouches
US20070110687A1 (en) * 2005-11-16 2007-05-17 Jairajh Mattai Antiperspirant Compositions

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016060626A1 (fr) * 2014-10-16 2016-04-21 Geli̇şi̇m Maki̇na-Madenci̇li̇k-Mühendi̇sli̇k Ti̇c. Ve San. Ltd. Şti̇. Procédés et compositions pour prévenir et traiter l'hyperhidrose

Also Published As

Publication number Publication date
CA2717536A1 (fr) 2009-09-17
EP2252252A1 (fr) 2010-11-24

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