EP1206282A1 - Polymeres filmogenes, procedes d'utilisation, et leurs dispositifs et applications - Google Patents

Polymeres filmogenes, procedes d'utilisation, et leurs dispositifs et applications

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Publication number
EP1206282A1
EP1206282A1 EP00918503A EP00918503A EP1206282A1 EP 1206282 A1 EP1206282 A1 EP 1206282A1 EP 00918503 A EP00918503 A EP 00918503A EP 00918503 A EP00918503 A EP 00918503A EP 1206282 A1 EP1206282 A1 EP 1206282A1
Authority
EP
European Patent Office
Prior art keywords
composition according
agent
skin
composition
polyvinyl alcohol
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
EP00918503A
Other languages
German (de)
English (en)
Inventor
Spiros Fotinos
Ekaterini Tsardaka
George Koborozos
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.)
Lavipharm SA
Original Assignee
Lavipharm SA
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 Lavipharm SA filed Critical Lavipharm SA
Publication of EP1206282A1 publication Critical patent/EP1206282A1/fr
Ceased legal-status Critical Current

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Classifications

    • 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
    • A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • 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
    • 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
    • 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
    • A61K8/43—Guanidines
    • 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
    • A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives 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
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/494—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
    • 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
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4973—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
    • 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
    • A61K8/64—Proteins; Peptides; Derivatives or degradation products thereof
    • A61K8/65—Collagen; Gelatin; Keratin; Derivatives or degradation products 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
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67—Vitamins
    • A61K8/678—Tocopherol, i.e. vitamin E
    • 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
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/81—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
    • A61K8/8129—Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by an alcohol, ether, aldehydo, ketonic, acetal or ketal radical; Compositions of hydrolysed polymers or esters of unsaturated alcohols with saturated carboxylic acids; Compositions of derivatives of such polymers, e.g. polyvinylmethylether
    • 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
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9789—Magnoliopsida [dicotyledons]
    • 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
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9794—Liliopsida [monocotyledons]
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7015—Drug-containing film-forming compositions, e.g. spray-on
    • 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

Definitions

  • a method for delivering an active agent to the skin of a subject including the steps of combining a polymer, and an active ingredient, adding an alcohol to the mixture to form a composition, and applying the composition to the skin of the subject for delivery of the active agent to the
  • the formulation of the invention includes a film- forming material wherein the film is formed upon application of the formulation to a selected site of the human body
  • the specific formulation can form a film when applied to the skin
  • the composition can be manufactured as a commercial product in an appropriate device/apparatus for application of the composition to the skin of the subject
  • the amount of the composition that is delivered by the device to the skin can contain an effective amount of the one or more of the active substances in the composition
  • the composition may also include a beneficially acting agent that possesses multifunctional properties such as glycerol, lanolin, vaseline, and the like
  • the film is formed directly on the site of application after the composition is sprayed or otherwise applied, and when dry the gel forms a film on the skin
  • an active agent can be any of a variety of wound healing agents.
  • An embodiment of the formulation contains a polymer, for example, a polyvinyl alcohol (PVA), for example, a mixture of polyvinyl alcohol A and polyvinyl alcohol B (DuPont, Wilmington, DE).
  • PVA polyvinyl alcohol
  • Other biocompatible polymers which are biologically inert polymers include cellulose, carboxymethyl cellulose, PVP/polyvinyl propylene, polyurethane, ethylene vinyl acetate, or copolymers thereof (U.S. Patent No. 5,925,372).
  • a preferred polymer is a polyvinyl alcohol, which confers sufficient viscosity to the composition so that it can form a film, which upon evaporation and concentration of the solvent can form a film that adheres to the skin.
  • an "active ingredient” or agent is a substance that presents specific properties used for the treatment of a particular condition
  • active agents can be pharmaceutical agents, cosmetics, or wound healing agents
  • a "beneficially acting agent” is used mainly in a cosmetic formulation and are not considered to be directed to the treatment of a particular condition, but possesses multifunctional properties that can contribute to the improvement of a condition
  • glycerol glycerin
  • An embodiment of the formulation contains an active ingredient or agent, more particularly, an solution or mixture of one or more pharmaceutical, wound healing, and/or cosmetic active ingredients, and can include additional materials such as ethanol, propylene glycol, butylene glycol, and/or other components
  • the active pharmaceutical ingredients can include an anti-infective, for example, an anti-viral agent, an anti-bacterial agent, an anti-fungal agent, or an anti-parasitical agent
  • An antibacterial agent such as chlorhexidine digluconate, or T ⁇ closan (an antiseptic agent, Irgasan DP 300,
  • the active ingredient can optionally be formulated in an alcohol solvent, more particularly a lower alkyl alcohol (lower alkanol), for example, methanol. /j-propanol, 7-propanol, more preferably ethanol, or an alcohol solution or suspension, preferably an ethanol solution or suspension Active ingredients such as salicylic acid, sodium disulfite, and dl- ⁇ -tocopherol can be prepared in the alcohol
  • a formulation can be prepared using only two mixtures or solutions in which the active ingredient m an alcohol solvent is referred to as "B" (see Tables 3, 5, and 6)
  • a single solution can be used, for example an aqueous solution, in which case a designation for the solution or mixture is not given (see Table 7).
  • a controlled dosage of an embodiment of the invention which is a composition can be assisted with an adhesive patch which is a border for a non-patch portion, the non-patch portion having a specific area, for delivery to that specific area of skin.
  • the patch can be of any shape, for example round or rectangular, and the proportion of the border to the non-patch interior is selected by one of skill in the art of design of adhesive patches, to remain in place for a limited period of time following application by any of the devices above.
  • the non-patch interior may have an area of one to 5 sq. cm, or 0.2 to one sq.
  • the patch is attached to the skin or mucosa of the particular location of skin to be treated, and the composition is applied to the non-patch portion of exposed skin, for example, by spraying or spreading, the patch can be removed when the composition has dried to form a film, or can remain in place
  • Skin shall mean all of an mtact epidermis, a tissue exposed by surgery, a mucosal surface such as an epidermal surface in an oral or vaginal cavity or on a glans penis, and a wound tissue created by abrasion, burn, incision, or a projectile Cleansing of wounds using a spray has been shown (U S Patent No 5,059,187), however the spray being delivered as shown in this art was not shown also to form a film
  • “Mucosa” shall mean the moist epithelial tissues, including for example, the oral or vaginal cavities and glans penis
  • the preparation of the gel comprises mixing the ingredients designated as B with those designated as A, as so designated in the Tables, under a condition of continuous agitation To this mixture the ingredients designated as C are added
  • the preparation is maintained in a sealed container for a period of time, for example, for approximately 6-18 hours, for example, for 12 hours, to allow for removal of the air bubbles Air bubbles can form and rise to the upper surface of the liquid under conditions of ambient pressure and temperature Removal of air bubbles from the liquid can be accelerated by application of decreased atmospheric pressure or increased temperature, under conditions of pressure and temperature that are compatible with maintenance of the activity and stability of the composition
  • compositions of the present invention are useful for delivery of one or more of a pharmaceutical agent, for example, an anaesthetic agent, an anti- inflammatory agent such as a glucocorticosteroid and a non-steroidal an ti-infl ammatory agent (NSAED), or for delivery of one or more of a cosmetic agent, or for delivery of a combination of two or more pharmaceutical and/or cosmetic agents
  • a pharmaceutical agent for example, an anaesthetic agent, an anti- inflammatory agent such as a glucocorticosteroid and a non-steroidal an ti-infl ammatory agent (NSAED)
  • NSAED non-steroidal an ti-infl ammatory agent
  • an anaesthetic agent examples include Suprane® (desflurane, Ohmeda), Versed® (midazolam hydrochlo ⁇ de, Roche), Duronest® (etidocaine hydrochlo ⁇ de, Astra), Naropin® (ropivacaine hydrochlo ⁇ de, Nesacaine® (chloroprocaine hydrochloride), and Xylocaine® (lidocaine hydrochloride).
  • Base forms of the anaesthetic agents can be incorporated into a composition, for example, lidocaine base in Example 1 1 herein.
  • glucocorticosteroid agent examples include Celestone® (betamethasone sodium, Schering), Cortone® acetate (cortisone acetate, Merck), Decadron®
  • a cosmetic agent can include, for example, an anti-irritant such as: -bisabolol, camomile extract, tea tree (Melaleuca alternifolia) oil, green tea (Camellia sinensis) extract, aloe (Aloe vera) extract (NOVA; see Examples 1-6), licorice (Glycerrhiza glabra) extract, glycyrrhetinic acid, witch hazel (Hamamelis virginiana) extract, and glycerol.
  • an anti-irritant such as: -bisabolol, camomile extract, tea tree (Melaleuca alternifolia) oil, green tea (Camellia sinensis) extract, aloe (Aloe vera) extract (NOVA; see Examples 1-6), licorice (Glycerrhiza glabra) extract, glycyrrhetinic acid, witch hazel (Hamamelis virginiana) extract, and glycerol.
  • Green tea and other plant material extracts can be obtained, for example, in solution with propylene glycol and water, for example, Optivegetol Green Tea PI 08 Hydro, Gattefosse (France); Optivegetol Cinnamon (Cinnamomum cassia) PI 10 Hydro, Gattefosse; and Optivegetol Guarana (Paullinia cupana) PI 07 Hydro, Gattefosse.
  • Optivegetol green tea hydroglycollic extract possesses anti-inflammatory and anti-irritant properties.
  • antioxidant agent examples include propyl gallate, sodium bisulfite, ascorbic acid (vitamin C) and ascorbic acid esters, butylated hydroxytoluene (BHT), butylated hydroxyanisole (BHA), vitamin E, and cysteine.
  • a vitamin examples include: vitamin A, vitamin A palmitate, ⁇ -carotene, ascorbic acid (vitamin C). ascorbyl palmitate, tocopherol (vitamin E), tocopheryl acetate (vitamin E acetate), vitamin K, and vitamin F (glyceryl linoleate and glyceryl linolenate).
  • Examples of a skin-conditioning ingredient include: extract of any of aloe (for example, Aloe vera), Camellia sinensis (green tea), camomile, cucumber, corn flower, orange peel, dog rose hip; marine extracts such as those from seaweed, kelp, and algae; rice bran oil, wheat germ oil, avocado oil and almond oil; an -hydroxy acid (AHA) such as glycolic acid, lactic acid, malic acid, and citric acid; a ⁇ -hydroxyl acid such as salicylic acid, a polymeric hydroxylic acid, and a ketoacid; and a ⁇ -glucan, panthenol, an anthocyanidin. a phytic acid, and an amino acid such as glycine, proline, lysine and leucine.
  • aloe for example, Aloe vera
  • Camellia sinensis green tea
  • camomile cucumber
  • corn flower orange peel
  • dog rose hip marine extracts
  • marine extracts such as those from seaweed
  • a cosmetic active agent known in the art may be incorporated in the film forming compositions for improving skin appearance.
  • These agents can be any of anti-hyperpigmentation, anti-blotching, anti- aging, eye contour, slimming, anti-cellulite, soothing/sunburn, anti-irritating, skin firming and lifting, anti-elastase and anti-collagenase substances, free radical scavengers, seboregulators, hydratives, vitamins, AHA products, anti-oxidants and minerals.
  • Anti-hyperpigmentation agents typically used for counterbalancing this condition can include tyrosinase inhibitors such as peptide mixtures and plant extracts, fermentation products, and antioxidants such as hydroquinone (see Examples 7-8), kojic acid (see Example 9), ascorbic acid derivatives, synthetic or natural derivatives of hydroquinone and hydroquinone precursors. Gatuline whitening obtained by fermentation of kojic and lactic acids, is a tyrosinase inhibitor.
  • anti-hyper pigmentation agents are Melawhite of Pentharm Ltd., Basel, Switzerland; BiowhiteTM of Coletica, France; Etioline of Sederma, France; Arbossa of Kelesima, Italy; Gatuline whitening of Gattefosse, France; Ascorbocilan C of Exsymol, Monaco; and Kojic acid of Alps Pharm., Japan.
  • Seboregulators include hpoamino acids of natural origin such as capryloyl glycine, oxidative enzyme mixtures, and mixtures of hydrolyzed yeast proteins and vitamins and related compounds
  • seboregulators are Asebiol® BT of Laboratoires Serobiiquess. France, Lipacide C8G of Seppic, France, Sebomine/SB 12 of Sederma, France, and Biome ⁇ s of Biopole, Belgium
  • AHA specific products can be mono-, di-, t ⁇ -hydroxy acids of natural origin, which may further be linked to polysaccharides or proteins
  • AHA specific products are Glycacid® and Protacid® of Coletica, France; Multifruit® BSC of Brooks Industries Inc., USA; Amidroxy of Alban Mulle Int., France; and AHA extracts of Phytochim, France.
  • compositions of embodiments herein include Crolastine 30 which contributes to elasticity of the skin, Hygrocomplex ARO which is a moisturizing agent, Crodalan (Croda, England), and Biopure 100 which is a preservative (see Table 1).
  • Each formulation can be sprayed upon the skin by any of the methods known in the art, for example, delivering a measured dose using a spray container (see U.S. Patent Nos. 5,618,515 and 5,769,283) as an atomizer attached to a reservoir, or for example, a pump inserted into the aqueous solution such that removal of a restraining cap enables use of first and second fingers to stabilize the vessel containing the reservoir while pushing with the thumb causes delivery of the measured dose.
  • a spray container see U.S. Patent Nos. 5,618,515 and 5,769,283
  • a pump inserted into the aqueous solution such that removal of a restraining cap enables use of first and second fingers to stabilize the vessel containing the reservoir while pushing with the thumb causes delivery of the measured dose.
  • Use of an atomizer does not require pressurization of an additional gas component.
  • the geometry of the relationship of the pump and the reservoir containing the gel can be of standard description, for example, a separate sque
  • Mixture or solution A can comprise polyvinyl alcohol A in a range from 5 to 10% amount, on a wet basis, with respect to the total composition. This component is preferably present at less than 20%, more particularly 1-10%, more particularly from 6 to 8%, more preferably from 6.9 to 7.5%, on a wet basis, with respect to the total composition.
  • Polyvinyl alcohol B is present at less than 20%, more particularly 1-10%, more particularly from 3.5 to 6.0%, preferably from 4.0 to 5.0%, more preferably from 4.5 to 4.8%, on a wet basis, with respect to the total composition.
  • the ratio of polyvinyl alcohol A:polyvinyl alcohol B ratio is about 3:2.
  • Solution or mixture A generally comprises 50 to 60% of the total composition, preferably 52 to 59% of the composition, on a wet basis, with respect to the total composition
  • Examples 1-32 Formulations of active components in film forming polymers
  • the cosmetic formulations of Examples 1-6 are shown in Table 1, and formulations containing anti-pigmentation agents are shown in Examples 7-9 in Table
  • Examples 7-9 are formulations of the invention having anti- pigmentation agents.
  • Examples 7 and 8 contain hydroquinone, which can be applied topically as a depigmenter agent (Merck Index. Tenth Ed., 1983, Rahway, NJ)
  • the formulation for Example 9 contains anti-pigmentation agents MelfadeTM, GATULINE® whitening. Kojic acid, and BiowhiteTM.
  • the methods and compositions that are gel forming polymers are particularly suitable for application to a limited surface area of skin such as an age spot.
  • the invention in another embodiment is a formulation containing a local anesthetic (Example 11, Table 4), for example, the anesthetic lidocaine.
  • the invention provides a formulation containing an anti-histaminic agent, hydroxyzine (Examples 12-15, Table 5).
  • the methods and compositions of the invention are suitable to treatment of limited areas of skin having an inflammation or irritation, such as an allergic contact dermatitis, or a reaction to an insect bite, by application of a film-forming gel having a water soluble polymer and containing an active agent such as an anesthetic or antihistamine.
  • An anti-acne agent can combine one or more of each of an anti-irritant, antibacterial agent, and a keratolytic agent such as salicylic acid (Examples 20-22, Table 7). Additional formulations (Examples 23-29) are shown in Table 8, the formulations having an anti-bacterial agent such as chlorhexidine, triclosan, or both.
  • Crolast ⁇ n 30 is a hydrolyzed elastin, contributing to elasticity of the skin hygrocomplex ARO, a mixture of specific ammo acids, forms a natural moisturizing factor
  • Opt ⁇ vegetol a hydroglycolic extract of green tea leaves, has free radical scavenging, antioxidant, and vitamin P properties (Gattefosse, France)
  • ⁇ Crodalan is a multi-functional surface active emollient (Croda. England)
  • 2 GATULINE® whitening is a tyrosinase inhibitor containing a traction obtained by fermentation (kojic acid and lactic acid), licorice extract, and TRANSCUTOL® (Gattefosse. France) is a tyrosinase inhibitor (Coletica, France) " Oxynex 2004 is an antioxidant mixture used in pharmaceuticals, containing 20% butyl hydroxy toluene, ⁇ Q9c ascorbic acid, and 10% citric acid in glyceryl stearate and propylene glycol (E Merck, Germany)
  • Hydrolyzed collagen is a collagen extract used as a skin conditioning agent (Croda, Inc ) : Germal II is diazo dinyl urea preservative (ELTON. Greece) ⁇ MEM-EARL is a tissue culture medium (Sigma, St. Louis, MO).
  • each formulation was applied exclusively at the site of an inflamed area (the acne-related inflammation) of the face, and remained in place overnight. Application was repeated on each of subsequent nights, until complete healing was observed.
  • the results in the following tables are given as the percentage of subjects cured as a function of time, expressed as the number of nights of use.
  • the effectiveness of each of the formulations was evaluated using the following criteria increase in dryness of the inflamed area, reduction of erythema, and reduction of edema
  • Tables 10-12 show that each of the formulations of Examples 28-31, when applied using the methods of the invention to form a gel to deliver the active agents to the skin of the subject, was effective as an anti-acne agent, by the three criteria of increasing the dryness, reducing erythema (redness), and reducing edema (swelling), within four nights of use. Some of these formulations successfully met one or two of the criteria after only two to three nights of use.
  • the formulation of Example 28 eliminated inflammation and edema after two nights, and provided a dry area after three nights of use.
  • the formulation of Example 33 eliminated edema after one night, produced dry skin after two nights, and reduced inflammation after the fourth night of use.
  • Example 34 Evaluation of the formulations using a depletion analysis
  • Formulations herein were evaluated for capacity to release active substances as a function of time after topical application to human skin. To determine the rate and extent of release of an active component of compositions of the formulations, a patch depletion analysis was performed. Among formulations of embodiments of the invention herein, those of Examples 24, 25, and 31 were tested.

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Abstract

L'invention concerne des compositions et des procédés servant à apporter des principes actifs à la peau du sujet. Ces compositions sont constituées d'un polymère, d'un principe actif et d'un alcool et peuvent être appliquées au moyen d'un applicateur à bille ou à tampon, d'un pulvérisateur à aérosol ou à gouttelettes et par formation d'un film en contact avec la peau.
EP00918503A 1999-08-19 2000-03-29 Polymeres filmogenes, procedes d'utilisation, et leurs dispositifs et applications Ceased EP1206282A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US14975199P 1999-08-19 1999-08-19
US149751P 1999-08-19
PCT/US2000/008428 WO2001013955A1 (fr) 1999-08-19 2000-03-29 Polymeres filmogenes, procedes d'utilisation, et leurs dispositifs et applications

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EP1206282A1 true EP1206282A1 (fr) 2002-05-22

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EP00918503A Ceased EP1206282A1 (fr) 1999-08-19 2000-03-29 Polymeres filmogenes, procedes d'utilisation, et leurs dispositifs et applications

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EP (1) EP1206282A1 (fr)
AU (1) AU3930200A (fr)
ES (1) ES2199094T1 (fr)
WO (1) WO2001013955A1 (fr)

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Publication number Priority date Publication date Assignee Title
US7083781B2 (en) 1999-08-19 2006-08-01 Lavipharm S.A. Film forming polymers, methods of use, and devices and applications thereof
CN1856293B (zh) * 2003-09-23 2010-12-15 奥里金生物医学股份有限公司 多酚的无水局部用制剂
DE10352368A1 (de) * 2003-11-10 2005-06-09 Beiersdorf Ag Verwendung von Licochalkon A zur Behandlung von Insektenstichen
BR112012024289A2 (pt) 2010-03-26 2017-07-18 Galderma Res & Dev "método para fornecer um tratamento seguro e efetivo do eritema e composição de gel tópica"
GB201112657D0 (en) * 2011-07-22 2011-09-07 Lowe Nicholas J Compositions for treatment of skin disorders
CA2850273A1 (fr) 2011-10-19 2013-04-25 Galderma S.A. Methode permettant de reduire les rougeurs du visage associees a l'utilisation systemique d'inhibiteurs de phosphodiesterases de type 5
US8697753B1 (en) 2013-02-07 2014-04-15 Polichem Sa Method of treating onychomycosis
KR101439036B1 (ko) * 2013-06-20 2014-09-05 주식회사 행복한에코 녹차를 함유한 시트 필름 및 그 제조방법
CN103446052B (zh) * 2013-09-09 2015-03-04 马北峰 一种用于治疗人体轻微外伤的气雾剂

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DE1617282A1 (de) * 1965-11-30 1975-02-06 Astra Pharma Prod Vorrichtung zur lokalanaesthetisierung durch oertliche aufbringung und verfahren zur herstellung dieser vorrichtung
JPS57209215A (en) * 1981-06-19 1982-12-22 Mitsubishi Chem Ind Ltd Antiphlogistic composition
ATE151227T1 (de) * 1993-04-15 1997-04-15 Ecolab Inc Iod schutzmittel zum eintauchen der zitzen
BR9810062A (pt) * 1997-06-20 2002-01-02 Mary Kay Inc Composição cosmética contendo um agente alvejante, bem como uso de uma fonte de água em combinação com a mesma

Non-Patent Citations (1)

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Title
See references of WO0113955A1 *

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WO2001013955A1 (fr) 2001-03-01
ES2199094T1 (es) 2004-02-16

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