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WO1994026234A1 - Compositions d'emulsions eau-dans-l'huile - Google Patents

Compositions d'emulsions eau-dans-l'huile Download PDF

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Publication number
WO1994026234A1
WO1994026234A1 PCT/US1994/005077 US9405077W WO9426234A1 WO 1994026234 A1 WO1994026234 A1 WO 1994026234A1 US 9405077 W US9405077 W US 9405077W WO 9426234 A1 WO9426234 A1 WO 9426234A1
Authority
WO
WIPO (PCT)
Prior art keywords
weight percent
composition
oil
emulsion
water
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/US1994/005077
Other languages
English (en)
Inventor
Seang H. Yiv
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.)
Ibah Inc
Original Assignee
Ibah 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 Ibah Inc filed Critical Ibah Inc
Priority to AU68277/94A priority Critical patent/AU6827794A/en
Publication of WO1994026234A1 publication Critical patent/WO1994026234A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/001Preparations for care of the lips
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04Dispersions; Emulsions
    • A61K8/06Emulsions
    • A61K8/064Water-in-oil emulsions, e.g. Water-in-silicone emulsions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04Dispersions; Emulsions
    • A61K8/06Emulsions
    • A61K8/068Microemulsions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/39Derivatives containing from 2 to 10 oxyalkylene groups
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60Sugars; Derivatives thereof
    • A61K8/602Glycosides, e.g. rutin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/63Steroids; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/107Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q1/00Make-up preparations; Body powders; Preparations for removing make-up
    • A61Q1/02Preparations containing skin colorants, e.g. pigments
    • A61Q1/04Preparations containing skin colorants, e.g. pigments for lips

Definitions

  • the present invention relates to water-in-oil emulsion systems having a petrolatum base. More specifically, the emulsion systems contain a blend of petrolatum and waxes and are used as lip balm formulations.
  • Lip balm products are commonly used by individuals who suffer from dry or chapped lips.
  • the conditions for causing chapped lips varies widely, and common factors include exposure of the lips to wind, sun, or dry humidity environments.
  • Treatment for chapped lips commonly requires application of petrolatum-based lip balm compositions.
  • these petrolatum compositions are characterized as being short lasting and require repeated applications for extended protection against chapped lips.
  • Certain lip balms are formulated with lipophilic active agents which are solubilized in the lipophilic base constituents of the lip balms.
  • the lip balm should provide the requisite occlusivity effects and also be smooth upon application. It is a further need to provide a lip balm composition which is capable of containing a hydrophilic active agent in solubilized form.
  • the present invention provides both water-in-oil (w/o) emulsion compositions containing petrolatum and methods for using the compositions.
  • the emulsions can be formulated with either a solubilized hydrophilic or lipophilic, or both, biologically, and preferably therapeutically, active material.
  • the emulsion compositions are preferably employed as lip-balm compositions; however, the compositions can also be used for the treatment of topical indications.
  • the emulsion compositions have been found to produce superior lip balms which are characterized by providing protection to the lips for a longer period of time than petrolatum based compositions that are not emulsion systems.
  • the w/o emulsion compositions of the present invention contain up to about 5 weight percent water, from about 25 to about 85 weight percent petrolatum, from about 0.1 to about 10 weight percent of a surfactant component, the surfactant component being present in an amount sufficient to form a w/o emulsion, and from about 15 to about 40 weight percent of a wax component.
  • the emulsion also preferably contains an oil and a humectant.
  • Emulsions are defined as compositions which contain water (or aqueous phase) , a lipid (referred to as "oil") phase, and a surfactant mixture such that the aqueous phase is a discontinuous phase within the continuous lipid phase.
  • the emulsion is a microemulsion and the particle size of the aqueous phase is below about 200 nanometers, preferably from about 10 to about 150 nanometers, more preferably from about 25 to about 100 nanometers.
  • the w/o microemulsion compositions can be recognized by such simple tests as (1) visual observation - presence of a transparent stable system; (2) dye solubilization - a water soluble dye will remain in its original form in a w/o microemulsion; (3) conductivity analysis - w/o microemulsions do not conduct electricity well.
  • the emulsion compositions of the present invention display superior qualities for use as lip balm formulations and are retained on the lips for an extended period of time.
  • the water content of the w/o emulsion composition is up to about 5 weight percent, preferably from about 0.1 to about 3 weight percent, and more preferably from about 0.25 to about 2 weight percent.
  • the w/o emulsion compositions of the present invention preferably also contain one or more humectants that can improve the retention of the water of the emulsion.
  • Humectants include glycerin, propylene glycol, polyethylene glycol, gelatin, collagen, methyl glucose ethoxylates and propoxylates.
  • the preferred amount of the humectant is from about 0.1 to about 10, more preferably from about 0.3 to about 5, weight percent of the emulsion.
  • the preferred humectant is GLUCAM ® E-20, or methyl glucose propoxylate-20.
  • the lipophilic phase of the w/o emulsion compositions comprises from about 90 to about 99 weight percent, preferably from about 93 to about 99 weight percent, of the w/o emulsion composition.
  • the lipophilic phase contains a combination of petrolatum, wax, and optionally an oil, such as lanolin oil and C 9 . 83 triglycerides, or mixtures thereof .
  • Petrolatum refers to a purified mixture of semisolid hydrocarbons obtained from petroleum, and is generally of USP grade, and the petrolatum is preferably white petrolatum.
  • the petrolatum can be generally described as a yellowish to light amber or white, semisolid, unctuous mass having a density of from about 0.820-0.865, a melting point of from about 38-54°C, and a refractive index of about 1.460-1.474.
  • the petrolatum is present in an amount from about 25 to about 85 weight percent, preferably from about 60 to about 85 weight percent, of the w/o emulsion.
  • the wax component of the lipophilic phase of the w/o emulsions is preferably pharmaceutically acceptable for topical and/or mucosal administrations.
  • suitable waxes include C 20 . 80 , preferably C 40 . 60 synthetic or natural waxes.
  • Waxes which can be employed in the w/o emulsions are those waxes listed in Cosmetic, Toiletry and Fragrance Association Cosmetic Ingredient Handbook, Washington, DC (1988) , which is incorporated herein in its entirety and include such compounds as beeswax, ozokerite, bayberry wax, carnauba, hydrogenated jojoba wax, japan wax, montan wax, synthetic waxes, and mixtures thereof.
  • the preferred waxes to be incorporated in the w/o emulsion are beeswax, ozokerite, and mixtures thereof.
  • the wax is present from about 15 to about 40, more preferably from about 20 to about 35, weight percent of the w/o emulsion composition.
  • the wax component can also be presented into the emulsion composition as a blend together with the petrolatum component of the lipophilic phase.
  • the w/o emulsions of the present invention can also include a pharmaceutically-acceptable natural or synthetic oil as part of the lipophilic phase.
  • the oil is preferably a Cg_ 83 triglyceride, C 7 . 55 diester of propylene glycol, or a mixture thereof.
  • Commercially available oils which are acceptable for use in the w/o emulsions of the present invention include the Captex series, manufactured by
  • the oil component can be present in the w/o emulsions in an amount from 1 to about 50 weight percent, preferably from 1 to about 10 weight percent.
  • Lanolin preferably in its oil form, is a preferred component of the lip balm formulation and is present in the emulsion in an amount of from about 0.05 to about 10, preferably from about 0.1 to about 5, weight percent.
  • Lanolin is generally known as the purified, fat-like substance from the wool of sheep.
  • Lanolin oil is the liquid fraction of lanolin obtained by physical extraction from whole lanolin, and both of these compositions have emolient properties beneficial to the skin.
  • Commercially available lanolin and derivatives include pharmaceutical lanolin USP, Fluilan Lanolin oil, manufactured by Croda Inc., Edison, NJ, Anhydrous Lanolin USP AAA and Lanogene Lanolin oil manufactured by Amerchol, Edison, NJ.
  • a surfactant or a mixture of surfactants, the surfactant component is incorporated into the mixture of the aqueous and lipophilic phases in order to prepare the resulting emulsion.
  • Surfactants which may be employed in the w/o emulsions include both ionic surfactants, i.e., cationic, anionic or zwitterionic, and non-ionic surfactants, or mixtures thereof.
  • the surfactant component is present in the emulsion in an amount of from about 0.1 to about 10, preferably from about 0.2 to about 5, weight percent of the w/o emulsion composition.
  • Suitable cationic surfactants include, among others, cetyldimethylethylammonium bromide, cetylpyridinium chloride and other salts of these surfactants .
  • Anionic surfactants include, among others, fatty acids and salts thereof, cholic acids and derivatives thereof, diesters of tartaric acid, phospholipids, monoesters of lactic acid, and sulfanates.
  • Zwitterionics include such phospholipids as lecithin, phosphatidylethanolamine, and sphingomyelins.
  • Nonionic surfactants include such surfactants as methyl glucoside derivatives, polyglycerol esters, preferably decaglycerol mono, di/trioleate, triglycerol monooleate, monoglycerides and ethoxylated derivatives thereof.
  • a preferred nonionic surfactant is Glucate SS manufactured by Amerchol in Edison, NJ.
  • Glucate SS is a sesquiester of stearic acid and methyl glucoside.
  • the w/o emulsions of the present invention can also be formulated to include both hydrophilic and lipophilic biologically active agents, preferably in solublized form when admixed with the emulsion composition.
  • the active agent is preferably also therapeutically active when given in an effective dosage.
  • the incorporation of the active agent is advantageous when the w/o emulsion is used as either a lip balm or as a treatment for topical indications such as a cold sore, i.e., mouth sore, composition.
  • the w/o emulsions can also be formulated with minor amounts of flavorants to improve the taste. Examples include fruit flavorants such as cherry, grape, and orange, and other flavorants such as menthol .
  • the w/o emulsions of this invention can readily be prepared by simply mixing together with mild agitation the selected components in the desired ratios at room temperature or at slightly elevated temperatures. No high-energy mixing is necessary to prepare the microemulsions.
  • the ingredients do not have to be added in any particular order; however, it is preferred to first prepare an aqueous and a lipophilic mixture and then combine these two mixtures to form the w/o emulsions.
  • a lip balm having an increased hardness is desired due to its perceived ease of application. It has been found that the hardness can be increased by first admixing all of the ingredients, without the addition of the water, and this mixture is brought to a temperature of between 60-75°C, preferably about 70°C. The water is then admixed with the other ingredients at that temperature. The composition is poured into appropriate lip balm containers at a temperature of from about 70-80°C, and allowed to cool to about 22°C in the containers.
  • the resultant hardness of the lip balms is preferably below about 4 mm, more preferably below about 3.7 mm, and even more preferably below about 3.5 mm.
  • the invention will now be illustrated by, but is not limited in scope to, the following examples. Examples
  • w/o emulsion compositions were, for convenience, prepared without the presence of an active agent. It is understood, however, that either a hydrophilic or lipophilic biologically and/or therapeutically active agent could be incorporated into the w/o emulsion composition.
  • the physical characteristics of the emulsions can be tested including such properties as viscosity, conductance, and refractive indices.
  • a water-in-oil emulsion was prepared by first placing about 34 g of Pureco 110, 3.5 g Glucate SS, 0.5 g Lanolin oil, 2 g GLUCAM ® E-20, 260 g white petrolatum, and 111 g of bees wax into a 600 ml beaker. The beaker was covered and the mixture was heated to about 75°C wherein all of the components were in a molten state. The mixture was stirred until a clear homogeneous solution was obtained. To this mixture was added 1.5 g sterile water, 0.4 g cherry flavor and 0.07 g of 0.18% wt . menthol in glycerin with continuous mixing.
  • the flowable liquid was poured into lip balm tubes and allowed to cool and solidify.
  • the lip balm formulation was found to have long lasting characteristics when placed on the lips and worn over an extended period of time.
  • the lip balm had the following weight composition:
  • Example 3 The same procedure as set forth in Example 1 was used, except that the white petrolatum was replaced by using Ultima Petrolatum, which contains ozokerite wax, and the resulting lip balm formulation was found to be long lasting.
  • Example 3 The same procedure as set forth in Example 1 was used, except that the white petrolatum was replaced by using Ultima Petrolatum, which contains ozokerite wax, and the resulting lip balm formulation was found to be long lasting.
  • Example 2 The same procedure as set forth in Example 2 was used, except that the composition of the w/o emulsion was varied as set forth in the following table.

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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)
  • Chemical & Material Sciences (AREA)
  • Birds (AREA)
  • Dispersion Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dermatology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Emergency Medicine (AREA)
  • Medicinal Preparation (AREA)

Abstract

Emulsions eau-dans-l'huile présentant une base de pétrolatum et dotées de qualités supérieures en ce qui concerne leur utilisation comme compositions de baume pour les lèvres. Ces émulsions contiennent de l'eau en une teneur ne dépassant pas environ 5 % en poids, et sont de préférence formulées sous forme de micro-émulsions. Ces compositions contiennent de préférence également une cire, une huile, ainsi qu'un constituant humidifiant.
PCT/US1994/005077 1993-05-06 1994-05-06 Compositions d'emulsions eau-dans-l'huile Ceased WO1994026234A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU68277/94A AU6827794A (en) 1993-05-06 1994-05-06 Water-in-oil emulsion compositions

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US5855693A 1993-05-06 1993-05-06
US08/058,556 1993-05-06

Publications (1)

Publication Number Publication Date
WO1994026234A1 true WO1994026234A1 (fr) 1994-11-24

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Application Number Title Priority Date Filing Date
PCT/US1994/005077 Ceased WO1994026234A1 (fr) 1993-05-06 1994-05-06 Compositions d'emulsions eau-dans-l'huile

Country Status (2)

Country Link
AU (1) AU6827794A (fr)
WO (1) WO1994026234A1 (fr)

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0763354A4 (fr) * 1995-03-31 1999-12-22 Shiseido Co Ltd Composition d'un melange huile/eau
EP1306074A1 (fr) * 2001-10-25 2003-05-02 L'oreal Composition topique solide
EP1247514A3 (fr) * 2001-04-03 2003-12-17 Faber-Castell AG Liquide pour le soin et le maquillage des lèvres
DE10226990A1 (de) * 2002-06-18 2004-03-18 Sanguibiotech Ag Topisch applizierbare Mikro-Emulsionen mit binärer Phasen- und Wirkstoffdifferenzierbarkeit, deren Herstellung und deren Verwendung, insbesondere zur Versorgung der Haut mit bioverfügbarem Sauerstoff
WO2005046627A3 (fr) * 2003-11-07 2005-08-04 Oreal Composition de maquillage ou de soin de levres comprenant une microemulsion huile-dans-eau et un actif hydrophile
WO2008141906A1 (fr) * 2007-05-17 2008-11-27 Unilever Plc Composition de baume à lèvres
EP1506774B1 (fr) * 2002-05-22 2011-08-24 Nihon Pharmaceutical Co., Ltd. Inhibiteur du peristaltisme de muscles lisses
US8460641B2 (en) 2004-08-31 2013-06-11 Stiefel Research Australia Pty Ltd Microemulsion process and composition
WO2013171056A3 (fr) * 2012-05-14 2014-06-26 Beiersdorf Ag Baume à lèvres aromatisé
WO2015152422A1 (fr) * 2014-04-01 2015-10-08 L'oreal Composition sous la forme de nano- ou de micro-émulsion

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4226889A (en) * 1978-12-19 1980-10-07 Dragoco, Inc. Cosmetic stick composition
US4880621A (en) * 1981-02-27 1989-11-14 Societe Anonyme Dite: L'oreal Cosmetic composition for the treatment of the hair and skin comprising a powder of flowers or flower tops and a cohesion agent
US5108737A (en) * 1991-06-28 1992-04-28 Elizabeth Arden Co., Division Of Conopco, Inc. Colored cosmetic sticks

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4226889A (en) * 1978-12-19 1980-10-07 Dragoco, Inc. Cosmetic stick composition
US4880621A (en) * 1981-02-27 1989-11-14 Societe Anonyme Dite: L'oreal Cosmetic composition for the treatment of the hair and skin comprising a powder of flowers or flower tops and a cohesion agent
US5108737A (en) * 1991-06-28 1992-04-28 Elizabeth Arden Co., Division Of Conopco, Inc. Colored cosmetic sticks

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0763354A4 (fr) * 1995-03-31 1999-12-22 Shiseido Co Ltd Composition d'un melange huile/eau
EP1247514A3 (fr) * 2001-04-03 2003-12-17 Faber-Castell AG Liquide pour le soin et le maquillage des lèvres
EP1306074A1 (fr) * 2001-10-25 2003-05-02 L'oreal Composition topique solide
FR2831433A1 (fr) * 2001-10-25 2003-05-02 Oreal Composition topique solide
US7090860B2 (en) 2001-10-25 2006-08-15 L'oreal Topical composition
EP1506774B1 (fr) * 2002-05-22 2011-08-24 Nihon Pharmaceutical Co., Ltd. Inhibiteur du peristaltisme de muscles lisses
DE10226990A1 (de) * 2002-06-18 2004-03-18 Sanguibiotech Ag Topisch applizierbare Mikro-Emulsionen mit binärer Phasen- und Wirkstoffdifferenzierbarkeit, deren Herstellung und deren Verwendung, insbesondere zur Versorgung der Haut mit bioverfügbarem Sauerstoff
WO2005046627A3 (fr) * 2003-11-07 2005-08-04 Oreal Composition de maquillage ou de soin de levres comprenant une microemulsion huile-dans-eau et un actif hydrophile
US8460641B2 (en) 2004-08-31 2013-06-11 Stiefel Research Australia Pty Ltd Microemulsion process and composition
WO2008141906A1 (fr) * 2007-05-17 2008-11-27 Unilever Plc Composition de baume à lèvres
WO2013171056A3 (fr) * 2012-05-14 2014-06-26 Beiersdorf Ag Baume à lèvres aromatisé
WO2015152422A1 (fr) * 2014-04-01 2015-10-08 L'oreal Composition sous la forme de nano- ou de micro-émulsion

Also Published As

Publication number Publication date
AU6827794A (en) 1994-12-12

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