US3265571A - Thixotropic acne vulgaris composition - Google Patents

Thixotropic acne vulgaris composition Download PDF

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Publication number
US3265571A
US3265571A US446709A US44670965A US3265571A US 3265571 A US3265571 A US 3265571A US 446709 A US446709 A US 446709A US 44670965 A US44670965 A US 44670965A US 3265571 A US3265571 A US 3265571A
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US
United States
Prior art keywords
acne
skin
composition
thixotropic
salicylic acid
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.)
Expired - Lifetime
Application number
US446709A
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English (en)
Inventor
Joseph Z Krezanoski
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Barnes Hind Pharmaceuticals Inc
Original Assignee
Barnes Hind Pharmaceuticals Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Barnes Hind Pharmaceuticals Inc filed Critical Barnes Hind Pharmaceuticals Inc
Priority to US446709A priority Critical patent/US3265571A/en
Priority to GB25737/65A priority patent/GB1038608A/en
Priority to DK401865AA priority patent/DK108264C/da
Priority to SE10366/65A priority patent/SE347157B/xx
Priority to DE1617320A priority patent/DE1617320C3/de
Application granted granted Critical
Publication of US3265571A publication Critical patent/US3265571A/en
Anticipated expiration legal-status Critical
Expired - Lifetime 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
    • A61K8/30—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
    • A61K8/34—Alcohols
    • A61K8/347—Phenols
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/06—Aluminium, calcium or magnesium; Compounds thereof, e.g. clay
    • A61K33/08—Oxides; Hydroxides
    • 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
    • A61K8/23—Sulfur; Selenium; Tellurium; Compounds thereof
    • 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
    • A61K8/26—Aluminium; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/008—Preparations for oily skin

Definitions

  • This invention relates to an improved therapeutic composition, and more particularly to a composition wherein sodium thiosulfate is combined with fibrous boehmite for topical application.
  • a formulation particularly adapted for" treatment of tinea versicolor is provided.
  • a formulation containing hydnocortisone for the treatment of the inflammatory types of acne and acne rosacea is provided.
  • Another embodiment of the invention provides a formulation for those skin maladies associated with hyperplasia of the infected sebaceous gland, such as acne vulgaris and seborrheic dermatitis.
  • Burows solution phenolated calamine lotion, sulphur lotion, calcium-zinc oxide and sulphur lotion as well as salicylic acid and resorcinol incorporated in a variety of oleaginous and/or hydroalcoholic vehicles.
  • These preparations in general provide for two major actions: (a) the kerotolytic (peeling) effect; and (b) the antibacterial effect.
  • the pH of many preparations presently employed is usually in the alkaline region and may be as high as 10. It is well known that vehicles having an alkaline pH may often contribute significantly to the irritated condition already prevailing in a highly exacerbating stage of acne vulgaris.
  • alcohol vehicles containing 60% or more of alcohol are employed as vehicles for salicylic acid, resorcinol, and some antibacterial agents which could otherwise not be properly and adequately dispersed for dermatological use. Alcohol could increase the irritating effect also where the skin is already highly inflamed and, further, upon the evaporation of alcohol, the crystalline residue may irritate the skin.
  • a novel Patented August 9, 1966 ice formulation for the treatment of acne vulgaris is provided.
  • Formulations are also provided for the treatment of tinea versicolor and for the treatment of inflammatory types of acne and acne rosacea.
  • One object of this invention is to provide an effective therapeutic agent for the treatment of acne vulgaris.
  • Another object of this invention is to provide a treatment agent for skin maladies associated with hyperplasia of the infected sebaceous gland such as acne vulgaris and seborrheic dermatitis as well as tinea versicolor and acne and acne rosacea which is of a thixotropic nature. This physical characteristic greatly enhances the dispersion stability of the formulations.
  • a further object of the invention is to provide a formulation wherein all of the ingredients are in solution and/ or colloidal dispersion and which is therefore free from large granular or crystalline materials.
  • Still another object of this invention is to provide a therapeutic agent low in alcohol content for the treatment of skin maladies associated with hyperplasia of the infected sebaceous gland.
  • a still further object of the invention is to provide a treatment agent for skin maladies associated with hyperplasia of the infected sebaceous gland as well as tinea versicolor and acne and acne rosacea which is nonoily and which has a substantially physiological pH.
  • Another object of this invention is to provide a method of forming a stable therapeutically active dermatological preparation containing resorcinol ancl/ or salicylic acid wherein the active ingredients are in solution and/ or colloidal dispersion and wherein the preparation is thixotropic, is free of oil and-contains little alcohol.
  • a still further object of the invention is to provide a preparation of sodium thi-osulfate which is stable in storage but which releases nascent sulfur when used on the ski-n.
  • an effective therapeutic agent for the treatment of skin maladies associated with hyperplasia of the infected sebaceous gland can be provided by preparing an aqueous lotion or cream which combines fibrous boehmite, sodium thiosulfate, salicylic acid, and resorcinol in a small amount of alcohol.
  • chelating agents may advantageously be employed in the composition as well as cooling and perfuming agents such as menthol and camphor.
  • fibrous boehmite in all of the disclosed formula-tions is to act as a dispersing and thickening agent for the mixture.
  • the fibrous boehmite forms a gel matrix so that the other ingredients are held in suspension and/ or solution in a thixotropic mixture. If one attempted to form the mixture without the fibrous boehmite, or if one attempts to substitute conventional aluminum hydroxide gel, the components deposit out as crystals.
  • fibrous boehmite we have been able to maintain all of the active ingredients in solution or colloidal dispersion. Formulations prepared two years ago have shown no sign of forming solid deposits.
  • the sodium thiosulfate, salicylic acid and resorcinol are not only effective therapeutic agents but the sodium thiosulfate stabilizes the salicylic acid and the resorcinol.
  • the sodium thiosulfate is adsorbed onto the aluminum fibrils of the boehmite lattice and released as nascent sulfur when the lotion is rubbed into the skin.
  • the fibrous boehmite comprises boehmite which is stabilized with about 9% of acetic acid, the balance of D the composition being substantially entirely aluminum oxide.
  • the fibrous boehmite which is employed is fully described in United States Patent 2,915,475, so it will not be further described here.
  • the fibrous boehmite may be employed in concentrations of from 0.5 to in the composition.
  • the sodium thiosulfate can be employed in concentrations of from 0.5 to 30%, and preferably from 0.5 to and the salicylic acid and resorcinol can be employed in concentrations of from 0.1 to 5%, if used. If menthol and camphor are used, they can each be employed in concentrations of from 0.01 to 1%.
  • the amount of alcohol which is used can vary from 10 to and either ethyl or isopropyl alcohol or a mixture of isopropyl alcohol and propylene glycol can be employed.
  • a chelating agent it is preferred to use disodium ethylene diamine tetracetic acid in a concentration of about 0.1% to 0.5% although other chelating agents well known to those skilled in the art may be employed.
  • the disodium ethylene diamine tetracetic acid is sometimes hereinafter referred to as sodium EDTA.
  • Percent Fibrous boehmite 3 Sodium thiosulfate a- 8 Salicylic acid 2 Resoreinol 2 Menthol 0.1 Camphor 0.1 Isopropyl alcohol 25 Disodium EDTA 0.1
  • a formulation which has been found highly efiicacious in the treatment of tinea versicolor is as follows:
  • the fibrous boehmite is first dispersed in 50 ml. of water.
  • the sodium thiosulfate is dissolved separately in an additional 16 ml. of water and added to the dispersed fibrous boehmite.
  • the salicylic acid, resorcinol (if used), hydrocortisone (if used), menthol and camphor are dissolved in isopropyl alcohol or a mixture of isopropyl alcohol and propylene glycol and added gradually to the dispersion with vigorous agitation.
  • the pH may now be adjusted, if necessary, by the addition of an alkali such as sodium hydroxide.
  • the fibrous boehmite employed in this formulation is in the form of a polymer stabilized with acetic acid. Pursuant to application of the composition to the skin, small amounts of aluminum ion are released to provide for an astringent protein precipitating activity desirable in acne therapy. The aluminum ion also precipitates and inactivates the short chain fatty acids known to be generated and produced by the microbial flora often residing in active comedones as described by John S. Strauss and Albert M. Kligman, Arch. Derm., 82, 779-790 (1960). It has been shown by Strauss et al. that the short chain fatty acids abounding in acne lesions are in a major way contributory to the inflammation encountered in acne lesions.
  • the basic formulations presented above are compatible with aluminum chloride and aluminum potassium sulfate and these latter salts can be added in concentrations ranging from 0.5% to 5.0% to increase the activity ascribed to the aluminum ion.
  • hydrogen ions are necessary for the decomposition of the thiosulfate ion.
  • the hydrogen ions are generated at the acne lesion site as short chain fatty acids according to Strauss sulfate in these formulations, we have selective deposition of sulfur in situ (at the precise site of dermal affliction, the acne lesion) in an active colloidal form, not possible by ordinary topical application of native sulphur dispersions in ordinary vehicles now commonly employed with some measure of benefit.
  • sulphur dioxide is another by-product of the reaction, and that it is dissipated. Some measurable transient antibacterial activity may be ascribed to sulphur dioxide.
  • the other end-product is water. It maybe noted from the above equation that hydrogen ions are actually dissipated, thus reducing the hyperacidity associated with comedones, a beneficial effect.
  • the normal pH of the aqueous fraction of sweat on the skin has been shown to be between 4.0 and 6.5. In these formulations, it has been possible to adjust to a pH of 5.5 or in the range of 5 to 6 which is entirely compatible with normal physiological skin conditions.
  • the product is translucent, and when applied to the skin, dries to form a practically crystal-clear film which is substanti-ative to the skin.
  • the substantiativity of the formulation comes about by virtue of a net positive charge and the extremely large surface area associated with the stabilized fibrous boehmite particles.
  • a thixotropic composition for treating skin maladies associated with hyperplasia of the infected sebaceous gland comprising an aqueous mixture having a physiological pH and containing Percent Fibrous boehmite 0.5 to 10 Sodium thiosulfate 0.5 to 15 Resorcinol 0.1 to 5 Salicylic acid 0.1 to 5 and Alcohol 10 to 25 all percentages being by Weight.
  • composition of claim 1 which also contains from about 0.1 to 1.0% of menthol and from about 0.1 to 1.0% camphor.
  • a thixotropic composition for treating skin maladies associated with hyperplasia of the infected sebaceous gland comprising an aqueous mixture having a physiological pH and containing Percent Fibrous boehmite 3 Sodium thiosulfate 8 Salicylic acid 2 Resorcinol 2 Menthol 0.1 Camphor 0.1 Isopropyl alcohol 25 and Disodium ethylene diamine tetracetic acid 0.1
  • thixotropic composition for treating skin maladies comprlsmg an aqueous mixture having a physiological pH and containing Percent Fibrous boehmite 0.5 to 10 Sodium thiosulfate 0.5 to 30 Alcohol 10 to 25 all percentages being by weight.
  • a thixotropic composition for treating skin maladies Percent comprising an aqueous mixture having a physiological pH Sodium EDTA 0.25 and containing Colloid-a1 alumina 4.0
  • Salicylic acid U.S.P 1.0 Isopropyl alcohol, N.F 25.0
  • a thixotropic composition for treating skin maladies JULIAN S. LEVHT Primary Examiner. comprising an aqueous mixture having a physiological pH i and o tai i VERA C. CLARKE, Asszstant Examiner.

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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)
  • Epidemiology (AREA)
  • Inorganic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Birds (AREA)
  • Dermatology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Cosmetics (AREA)
US446709A 1965-04-08 1965-04-08 Thixotropic acne vulgaris composition Expired - Lifetime US3265571A (en)

Priority Applications (5)

Application Number Priority Date Filing Date Title
US446709A US3265571A (en) 1965-04-08 1965-04-08 Thixotropic acne vulgaris composition
GB25737/65A GB1038608A (en) 1965-04-08 1965-06-17 New compositions for use in acne and like conditions
DK401865AA DK108264C (da) 1965-04-08 1965-08-05 Kosmetisk middel.
SE10366/65A SE347157B (enrdf_load_html_response) 1965-04-08 1965-08-06
DE1617320A DE1617320C3 (de) 1965-04-08 1966-04-06 Hautbehandlungsmittel

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US446709A US3265571A (en) 1965-04-08 1965-04-08 Thixotropic acne vulgaris composition

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US3265571A true US3265571A (en) 1966-08-09

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US446709A Expired - Lifetime US3265571A (en) 1965-04-08 1965-04-08 Thixotropic acne vulgaris composition

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US (1) US3265571A (enrdf_load_html_response)
DE (1) DE1617320C3 (enrdf_load_html_response)
DK (1) DK108264C (enrdf_load_html_response)
GB (1) GB1038608A (enrdf_load_html_response)
SE (1) SE347157B (enrdf_load_html_response)

Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4005191A (en) * 1974-06-04 1977-01-25 Clark Mary G Topical ointment composition
US4237112A (en) * 1979-05-25 1980-12-02 Johnson Products Co., Inc. Medicated hair and scalp conditioner
US4318907A (en) * 1978-04-04 1982-03-09 Westwood Pharmaceuticals, Inc. Method for treating acne vulgaris and compositions useful for that purpose
US4608370A (en) * 1985-03-04 1986-08-26 Aronsohn Richard B Skin formulation
US5510109A (en) * 1990-11-28 1996-04-23 Matsushita Electric Industrial Co., Ltd. Antibacterial and antifungal composition
US5874463A (en) * 1994-10-24 1999-02-23 Ancira; Margaret Hydroxy-kojic acid skin peel
EP1151742A3 (fr) * 2000-05-04 2002-11-06 L'oreal Utilisation de fibres dans une composition de soin ou de maquillage pour matifier la peau
US6869611B1 (en) 1996-02-08 2005-03-22 Douglas E. Kligman Composition and method of effecting superficial chemical skin peels
FR2886852A1 (fr) * 2005-06-10 2006-12-15 Galderma Sa Composition a base d'une avermectine et d'hydrocortisone notamment pour le traitement de la rosacee
US20090110645A1 (en) * 2007-10-25 2009-04-30 Ecolab, Inc. Use of metal astringents for the treatment and prevention of hairy heel warts
WO2018114232A1 (en) 2016-12-21 2018-06-28 Unilever N.V. Use of chelating agents for improving color stability of resorcinol

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1113005A (en) * 1977-12-06 1981-11-24 Pierluigi Vanoni Excipient composition for creams
JPS6253925A (ja) * 1985-09-02 1987-03-09 Toyoji Ishimoto 無刺激性皮膚真菌症治療剤の組成物およびその製造法
DE19624568A1 (de) * 1996-06-20 1998-05-14 Hans Lufen Mittel zur topischen Behandlung von Hauterkrankungen

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
None *

Cited By (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4005191A (en) * 1974-06-04 1977-01-25 Clark Mary G Topical ointment composition
US4318907A (en) * 1978-04-04 1982-03-09 Westwood Pharmaceuticals, Inc. Method for treating acne vulgaris and compositions useful for that purpose
US4237112A (en) * 1979-05-25 1980-12-02 Johnson Products Co., Inc. Medicated hair and scalp conditioner
US4608370A (en) * 1985-03-04 1986-08-26 Aronsohn Richard B Skin formulation
US5510109A (en) * 1990-11-28 1996-04-23 Matsushita Electric Industrial Co., Ltd. Antibacterial and antifungal composition
US6710076B2 (en) 1994-10-24 2004-03-23 Physician's Choice Of Arizona, Inc. Hydroxy-kojic acid skin peel
US5874463A (en) * 1994-10-24 1999-02-23 Ancira; Margaret Hydroxy-kojic acid skin peel
US6300369B1 (en) 1994-10-24 2001-10-09 Margaret Ancira Hydroxy-kojic acid skin peel
US6869611B1 (en) 1996-02-08 2005-03-22 Douglas E. Kligman Composition and method of effecting superficial chemical skin peels
EP1151742A3 (fr) * 2000-05-04 2002-11-06 L'oreal Utilisation de fibres dans une composition de soin ou de maquillage pour matifier la peau
US20110178049A1 (en) * 2005-06-10 2011-07-21 Galderma S.A. Avermectin/hydrocortisone compositions for treating afflictions of the skin. e.g., rosacea
FR2886852A1 (fr) * 2005-06-10 2006-12-15 Galderma Sa Composition a base d'une avermectine et d'hydrocortisone notamment pour le traitement de la rosacee
WO2006131651A3 (fr) * 2005-06-10 2007-09-13 Galderma Sa Composition a base d'une avermectine et d’ηydrocortisone notamment pour le traitement de la rosacée
US20090163455A1 (en) * 2005-06-10 2009-06-25 Galderma S.A. Avermectin/hydrocortisone compositions for treating afflictions of the skin, e.g., rosacea
US20090110645A1 (en) * 2007-10-25 2009-04-30 Ecolab, Inc. Use of metal astringents for the treatment and prevention of hairy heel warts
US8703104B2 (en) 2007-10-25 2014-04-22 Ecolab Usa Inc Use of metal astringents for the treatment of hairy heel warts
WO2018114232A1 (en) 2016-12-21 2018-06-28 Unilever N.V. Use of chelating agents for improving color stability of resorcinol
EP3558224B1 (en) 2016-12-21 2020-04-29 Unilever N.V. Use of chelating agents for improving color stability of resorcinol
US11478411B2 (en) 2016-12-21 2022-10-25 Conopco, Inc. Use of chelating agents for improving color stability of resorcinol

Also Published As

Publication number Publication date
DK108264C (da) 1967-10-30
DE1617320C3 (de) 1979-01-25
GB1038608A (en) 1966-08-10
SE347157B (enrdf_load_html_response) 1972-07-31
DE1617320A1 (de) 1971-02-18
DE1617320B2 (de) 1978-05-24

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