EP0133437A1 - Onguent pour les soins de la peau contenant des vitamines - Google Patents

Onguent pour les soins de la peau contenant des vitamines

Info

Publication number
EP0133437A1
EP0133437A1 EP84900801A EP84900801A EP0133437A1 EP 0133437 A1 EP0133437 A1 EP 0133437A1 EP 84900801 A EP84900801 A EP 84900801A EP 84900801 A EP84900801 A EP 84900801A EP 0133437 A1 EP0133437 A1 EP 0133437A1
Authority
EP
European Patent Office
Prior art keywords
vitamin
ointment
zinc
emollient
oil
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.)
Withdrawn
Application number
EP84900801A
Other languages
German (de)
English (en)
Inventor
Gerald L. Bilton
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.)
ADVANCED DRUG TECHNOLOGY Corp
Original Assignee
ADVANCED DRUG TECHNOLOGY Corp
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 ADVANCED DRUG TECHNOLOGY Corp filed Critical ADVANCED DRUG TECHNOLOGY Corp
Publication of EP0133437A1 publication Critical patent/EP0133437A1/fr
Withdrawn legal-status Critical Current

Links

Classifications

    • 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
    • A61K31/59—Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/88—Liliopsida (monocotyledons)
    • A61K36/886—Aloeaceae (Aloe family), e.g. aloe vera

Definitions

  • Vitamins A and D and their derivatives have been used to alleviate the symptoms of skin rashes such as diaper rash and acne, and petroleum jelly-based ointments containing these vitamins are commercially available.
  • an ointment which combines and optimizes the skin-conditioning and wound-healing properties of the oil-soluble vitamins has not heretofore been available.
  • compositions of the present invention which are oil-based ointments comprising a carrier mixture of both a penetrating and non-penetrating (barrier) emollient oil, and a polyhydric alcohol emollient; a mixture of vitamins E, A, and D, a vitamin A-activating amount of a zinc salt, an aloe extract and an organic astringent.
  • the emollients, vitamins, zinc salts, aloin and astringent function together to moisturize and protect normal skin, as well as to alleviate the symptoms of skin diseases and to promote the healing of wounds and burns when the ointment is applied topically.
  • the ointments of the present invention comprise a mixture of three oil-soluble vitamins, vitamins E, A, and D, which are employed to promote the general healing of wounds such as cuts and scratches, and to reduce the severity of proliferative or eruptive skin diseases or disorders such as acne, psoriasis, impetigo, eczema, diaper rash, poison ivy, ulcers, sunburn or blisters and the like.
  • Vitamin E will comprise the majority of the vitamin mixture, due to its efficacy as a wound-healer and its low toxicity, preferably comprising over 95% of the vitamin mixture, most preferably over 98% of the mixture.
  • Vitamins A and D will preferably comprise less than about 2% of the vitamin mixture, most preferably less than 1%, e.g., about 0.03-0.15%.
  • vitamin A as used in the context of this invention is intended to include all of the biologically-active forms and analogs of this vitamin, including vitamin A 1 (retinol), vitamin A 2 (dehydroretinol), retinoic acid (tretinoin), 13-cis-retinoic acid, vitamin A acetate and vitamin A palmitate .
  • Vitamin A is necessary for the normal growth of most cells of the body and especially for normal growth and proliferation of the different types of epithetial cells.
  • Vitamin A is lacking, the epithelial structures of the body tend to become stratified and keratinized. Therefore, vitamin A deficiency manifests itself by scaliness of the skin and accompanying acne.
  • Topical retinoic acid has been employed to effectively treat acne, due to its comedolytic action. Topical retinoic acid causes variable acanthosis, parakeratosis, disruption and thinning of the stratum corneum, erythema and increased skin permeability.
  • Retinoic acid has been proposed for the treatment of variants of acne such as those induced by steroids, sunlight, and environmental pollutants such as tars and chlorinated hydrocarbons. See, J.W. Melski, et al., New England J. Med., 382, 503 (1980). Recently, 13-cis-retinoic acid has been demonstrated to be an effective treatment for cystic and conglobulate acne.
  • Vitamin A will preferably be employed as vitamin A 1 , vitamin A acetate, vitamin A palmitate or mixtures thereof in an amount from about 0.025-0.1% by weight of the ointment.
  • vitamin E as used in the context of the present invention is intended to include any of the biologically-active members of the vitamin E group, including d- or d1-alpha-tocopherol; d- or d1-alpha-tocopherol acetate or d- or d1-alpha tocopheryl acid succinate. Vitamin E is thought to aid wound healing by promoting tissue elasticity and continuity, thus reducing scarring. The use of topical vitamin E has also been proposed for the alleviation of pressure sores and ulcers (i.e., bedsores). Vitamin E is also believed to function as an antioxidant, thus stabilizing the vitamin A which is present. Vitamin E has been proposed to be necessary for the effective absorption, transport and stroage of vitamin A. See, S.R. Ames, Amer. J. Clin. Nutr., 22, 934 (1969). Vitamin E will preferably comprise about 4-19% by weight of the present ointments, most preferably from about 9-17%.
  • vitamin D as used in the context of the present invention is intended to include the biologically-active vitamin D compounds or metabolites such as vitamin D 2 , vitamin D 3 , or 1,25- dihydroxycholecalciferol. Vitamin D mediates intestinal calcium absorption, bone calcium metabolism and muscle activity. Vitamin D has also been proposed as a facilitator of wound-healing via reducing scarring and increasing tissue elasticity. Vitamin D, preferably Vitamin D 3 , will preferably comprise from about 0.001 to 0.1% by weight, most preferably from about 0.005 to 0.05% by weight of the ointments of the present invention. However, the vitamin D may be entirely eliminated from this formulation, if desired.
  • Vitamin C may also be added to this ointment, particularly vitamin C in the form of its palmitate. Vitamin C tends to promote healing and facilitate tissue oxygen transfer.
  • the ointments of the present inveniton are also formulated to comprise an organic or inorganic zinc salt.
  • Useful zinc salts will include zinc acetate, zinc sulfate, zinc orotate, zinc oxide, zinc stearate, zinc carbonate, and mixtures thereof. Such salts function as skin cleansers and astringents, and have been employed topically to treat eczema, impetigo, psoriasis and varicose ulcers.
  • Zinc salts have also been proposed to increase the level of retinol-binding protein, and thus to effect the activation and utilization of retinol.
  • zinc salts and vitamin A have been used together to treat acne. See, G. Michaelsson, et al., Arch.
  • Zinc has also been proposed as an aid to the healing of surgical wounds. See, R.I. Henkin, New England J. Med., 291, 675 (1974).
  • zinc salt an amount of zinc salt equal to about 1-10% by weight of the ointment is preferred, greater amounts of zinc salts may be employed, e.g., up to about 50% by weight of the ointment, where it is desired to enhance the cosmetic effects of the zinc salt and wherein the zinc salt or salts are selected to minimize local irritation due to the astringency of the salts.
  • zinc salts mercury, magnesium and selenium salts, primarily the oxides may be used, preferably in amounts from 0.01 to 10% by weight of the ointment.
  • the ointments of the present invention will also include about 0.01-10% by weight of an aloe extract, preferably from about 0.02-2.0% by weight of the extract, which is preferably incorporated as an aloe concentrate, e.g., aloe vera or aloe perryi concentrate.
  • an aloe extract refers to the inspissated juice of the aloe plant as well as to its dried concentrates which contain aloe-emodin, aloin or other active anthraquinone principles. Apart from their moisturizing properties, such extracts have been used to reduce thermal burn and sunburn inflammation and to enhance the healing of burns and wounds.
  • the ointments of the present invention will also comprise 0.05-5.0%, preferably 0.1-2.0% by weight of an organic astringent agent such as witch hazel extract, gallstannic acid, tannin, digallic acid, and the like. These compounds act to inhibit the pathological transcapillary movement of plasma protein, thus reducing inflammation, edema and exudation.
  • an organic astringent agent such as witch hazel extract, gallstannic acid, tannin, digallic acid, and the like.
  • the ointments of the present invention also comprise minor but effective amounts of antibacterial preservatives, such as about 0.025-1-5%, preferably 0.05-0.5% of a mixture of (C 1 -C 4 )-lower alkyl-4-hydroxybenzoates.
  • the above-described active ingredients are formulated so as to comprise about 5-40% by weight of the present ointments and are carried to and absorbed by the skin surface in admixture with about 60-95% of a carrier mixture of emollients.
  • the emollient mixture will comprise a major portion, e.g. 35-75%, or 45-55% of a non-penetrating barrier-type emollient oil.
  • a non-penetrating barrier-type emollient oil e.g. 35-75%, or 45-55%.
  • emollients are petrolatum, heavy mineral oils, paraffin wax, beeswax, and silicones, e.g., polysiloxanes. These oils rehydrate the skin by blocking the escape of skin moisture, lubricate the skin, and protect the skin from environmental irritants.
  • the emollient mixture will also include about 5-35% or preferably, 10-25% of a penetrating emollient oil, which effectuates the absorption of the active ingredients beyond the epidermal stratum.
  • a penetrating emollient oil include phytosterols, C 20 - fatty acid coral (sea whip) extracts, and vegetable oils such as peanut, evening primrose, sunflower, sesame and safflower oils; and animal oils such as sperm oil and cod liver oil.
  • a preferred class of penetrating emollient oils is the polyoxyethylene lanolin derivatives or the polyoxyethylene sorbitol/lanolin derivatives, which are described by G. Barnett in Cosmetics-Science and Technology, E.
  • Useful compounds of this type are formed by the condensation of about 10-80 moles of ethylene oxide per mole of lanolin or by the linking of sorbitol and lanolin with a polyoxyethylene chain containing 10-80 moles of ethylene oxide.
  • such compounds are commercially available from ICI Americas, Wilmington, Delaware as Atlas ® G-1790 (20 moles of ethylene oxide/mole of lanolin), Atlas ® G-1441 (40 moles of ethylene oxide linking sorbitol and lanolin) and Atlas ® G-1471 (75 moles of ethylene oxide linking sorbitol and lanolin).
  • the emollient oil mixtures of the present invention will also include about 2-20%, preferably about 5-15% of a polyhydric alcohol emollient, e.g., a C 2 -C 5 alkanol having 2-4 hydroxyl groups such as glycerol, sorbitol, propylene glycol and the like.
  • a polyhydric alcohol emollient e.g., a C 2 -C 5 alkanol having 2-4 hydroxyl groups such as glycerol, sorbitol, propylene glycol and the like.
  • preferred wound-healing emollient ointments will have about 5-35% of a mixture of active ingredients including 4-19% vitamin E, 0.025-0.1% vitamin A, 0.005-0.05% vitamin D 3 , 1-10% of zinc oxide, 0.1-2% of powdered witch hazel extract, and 0.02-2% of aloe vera concentrate dispersed in about 65-95% of a carrier mixture comprising about 45-55% petrolatum, 10-25% ethoxylated lanolin, 5-15% glycerin and 0.05-0.5% of antimicrobial preservatives.
  • the ointments are typically prepared by preparing a stirred melt of the emollient oils and the polyhydric alcohol emollient, stirring in a homogeneous mixture of the zinc salt, the organic astringent, the aloe vera concentrate and the preservative, and then adding a mixture of the vitamins.
  • stirred ointment begins to solidify it is transferred to an ointment filler and tubed, i.e., into metallized plastic tubes.
  • a melt of 8615g of petrolatum, 3089g of ethoxylated lanolin and 2040g of glycerin was prepared in a stainless steel tub.
  • a mixture of 2465g vitamin E (1,100 I.U./g), 13.3g vitamin A (1.5 x 10 6 I.U./g) and 2.0g vitamin D 3 (1 x 10 6 I.U./g) was prepared and stirred for 5 minutes. The vitamin mixture was added with stirring to the remainder of the ingredients. The homogeneous mixture was stirred until solidification began, then transferred to a Colton ointment filler and filled into one-ounce tubes under 30 lbs. pressure.
  • the ointment of this invention has been used in the treatment of acne and of superficial wounds and bruises and has been reported as effective in providing symptomatic relief in such applications.
  • the recommended mode of application is to cover the affected area with a thin layer of the ointment and optionally, to cover the wound with a sterile gauze.
  • the ointment may be delivered by a depot technique, such as a skin patch containing a reservoir of the ointment for slow continuous release to and through the skin surface.
  • the ointment is applied to the skin, which is then subjected to an ultrasound treatment by techniques well known in the art. While certain representative embodiments of the invention have been described herein for purposes of illustration, it will be apparent to those skilled in the art that modifications therein may be made without departing from the spirit and scope of the invention.

Landscapes

  • Health & Medical Sciences (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Mycology (AREA)
  • Microbiology (AREA)
  • Medical Informatics (AREA)
  • Botany (AREA)
  • Biotechnology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Cosmetics (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Un onguent à base d'huile utile pour soigner les blessures et pour soulager les affections de la peau contient les vitamines A, D et E, un sel de zinc, un extrait d'aloès et un astringent organique additionné à un mélange de porteurs oléagineux émollient.
EP84900801A 1983-01-21 1984-01-18 Onguent pour les soins de la peau contenant des vitamines Withdrawn EP0133437A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US46000783A 1983-01-21 1983-01-21
US460007 1999-12-13

Publications (1)

Publication Number Publication Date
EP0133437A1 true EP0133437A1 (fr) 1985-02-27

Family

ID=23827040

Family Applications (1)

Application Number Title Priority Date Filing Date
EP84900801A Withdrawn EP0133437A1 (fr) 1983-01-21 1984-01-18 Onguent pour les soins de la peau contenant des vitamines

Country Status (3)

Country Link
EP (1) EP0133437A1 (fr)
CA (1) CA1243951A (fr)
WO (1) WO1984002845A1 (fr)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5541220A (en) * 1984-03-07 1996-07-30 Ismail; Roshdy Agents for the treatment and protection of the skin
DE3507791A1 (de) * 1984-03-07 1985-09-26 Roshdy Ismail Mittel zum schutz der haut
US5624675A (en) * 1989-06-06 1997-04-29 Kelly; Patrick D. Genital lubricants containing zinc salts to reduce risk of HIV infection
US5254538A (en) * 1989-10-04 1993-10-19 Trustees Of Boston University Method of treating periodontal disease
EP0494995A4 (en) * 1989-10-04 1993-03-17 Trustees Of Boston University Method of accelerating wound and ulcer healing and treating periodontal disease
JPH06505959A (ja) * 1990-05-07 1994-07-07 ボッコー　バリー　アイ 安定な脱臭油及びその医薬組成物の方法及び製剤
GB9109733D0 (en) * 1991-05-07 1991-06-26 Unilever Plc Cosmetic composition
SE9200199L (sv) * 1992-01-24 1993-07-25 Rune Soeremark Farmaceutisk komposition och dess anvaendning
IT1256170B (it) * 1992-11-03 1995-11-29 Medicazione per patologie cutanee
FR2717079B1 (fr) * 1994-03-11 1996-04-12 Oreal Composition contenant un oxyde de métal non photocatalytique et du tocophérol, son utilisation dans le domaine cosmétique et/ou dermatologique et procédés la mettant en Óoeuvre.
EP0711558A1 (fr) * 1994-10-21 1996-05-15 Unilever Plc Des compositions pour application topique sur la peau, les cheveux et les argles
US5869061A (en) * 1996-06-04 1999-02-09 Brugh; Bettie Sue Protective hand lotion of aloe vera gel and vitamin E gel
US5753637A (en) * 1996-10-09 1998-05-19 Ideal Ideas, Inc. Method of treating acne conditions
US5910312A (en) * 1996-10-09 1999-06-08 Ideal Ideas, Inc. Acne treatment composition with vasoconstrictor
WO1998053806A1 (fr) * 1997-05-26 1998-12-03 New Vision Co., Ltd. Compositions medicinales a administration topique renfermant les vitamines d et les vitamines k
US6552009B2 (en) 1998-07-16 2003-04-22 Gentrix Llc Compositions and methods of treating abnormal cell proliferation
US20010002396A1 (en) * 1998-07-16 2001-05-31 Charles Achkar Compositions and methods of treating skin conditions
US6497893B1 (en) 1999-06-30 2002-12-24 Kimberly-Clark Worldwide, Inc. Silk protein treatment composition and treated substrate for transfer to skin
CO5150167A1 (es) * 1998-12-04 2002-04-29 Johnson & Johnson Consumer Composiciones para el cuidado de la piel, que contienen sales de cinc y retinoides
US6506394B1 (en) 1999-06-30 2003-01-14 Kimberly-Clark Worldwide, Inc. Delivery of a botanical extract to a treated substrate for transfer to skin
WO2001000156A1 (fr) * 1999-06-30 2001-01-04 Kimberly-Clark Worldwide, Inc. Administration d"un agent benefique pour la peau sur un substrat traite
US6500443B1 (en) 1999-06-30 2002-12-31 Kimberly-Clark Worldwide, Inc. Delivery of a sacrificial substrate to inhibit protease permeation into skin
US7262224B2 (en) * 1999-11-30 2007-08-28 Hanna Isul Skin Therapy, Inc. Cosmetic rejuvenating and healing product, method of its manufacture and uses thereof
US6503524B1 (en) 2000-06-16 2003-01-07 Kimberly-Clark Worldwide, Inc. Delivery of a skin health benefit agent to a treated substrate for transfer to skin
GB2374804B (en) * 2001-04-26 2004-03-31 Subhas Chandra Bhairo Skin treatment cream
WO2003092703A1 (fr) * 2002-04-30 2003-11-13 Hisamitsu Pharmaceutical Co., Inc. Procedes et compositions pour inhiber l'irritation au moyen d'un disaccharide et d'ions metalliques
US20050019379A1 (en) 2003-07-22 2005-01-27 Kimberly-Clark Worldwide, Inc. Wipe and methods for improving skin health
US20200100997A1 (en) * 2017-02-06 2020-04-02 3Skin As Sunscreen Composition
US11147761B2 (en) * 2018-01-12 2021-10-19 Nicole Akmenkalns Topical supplement composition and method of use

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US3878197A (en) * 1972-12-13 1975-04-15 Ray H Maret Process for preparing extracts of aloe vera
US4154823A (en) * 1976-06-10 1979-05-15 Schutt Steven R Skin treatment compositions and methods of using same
US4214000A (en) * 1978-10-30 1980-07-22 Johnson & Johnson Zinc salt of all-trans-retinoic acid for the treatment of acne
US4224319A (en) * 1979-07-31 1980-09-23 Ernest Marcadet Antiseptic composition for topical application to the skin

Non-Patent Citations (1)

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Also Published As

Publication number Publication date
CA1243951A (fr) 1988-11-01
WO1984002845A1 (fr) 1984-08-02

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Inventor name: BILTON, GERALD, L.