WO1991004730A1 - Composition and methods for the stabilization of materials dispersed onto applicators - Google Patents

Composition and methods for the stabilization of materials dispersed onto applicators Download PDF

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Publication number
WO1991004730A1
WO1991004730A1 PCT/US1990/005622 US9005622W WO9104730A1 WO 1991004730 A1 WO1991004730 A1 WO 1991004730A1 US 9005622 W US9005622 W US 9005622W WO 9104730 A1 WO9104730 A1 WO 9104730A1
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WO
WIPO (PCT)
Prior art keywords
weight
composition
applicator
compoεition
adjuvant
Prior art date
Application number
PCT/US1990/005622
Other languages
French (fr)
Inventor
Raymond S. Niedbala
Original Assignee
Solarcare Incorporated
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 Solarcare Incorporated filed Critical Solarcare Incorporated
Publication of WO1991004730A1 publication Critical patent/WO1991004730A1/en

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Classifications

    • 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
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A61K47/186—Quaternary ammonium compounds, e.g. benzalkonium chloride or cetrimide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/0208—Tissues; Wipes; Patches
    • 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
    • A61K8/73—Polysaccharides
    • A61K8/731—Cellulose; Quaternized cellulose derivatives
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • A61Q17/04—Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/74—Biological properties of particular ingredients
    • A61K2800/75—Anti-irritant

Definitions

  • the present invention relates to composi- tion ⁇ and methods which facilitate the topical administration of active ingredients.
  • topical administra ⁇ tion of active ingredients is employed to deliver the active ingredient at or immediately beneath the point of application.
  • sunscreens are useful in blocking the harmful effects of the sun and anti-inflammatory agents can relieve the dis ⁇ comfort caused by various irritants, such as poison ivy.
  • a large number of active ingredients are applied to the skin, although topical application may also be used for treating the eyes, the nose, the throat, the ears, the hair, the nails, the teeth, etc.
  • topical administration is an effective and convenient means to locally apply active ingredients.
  • active ingredients for topical application are applied in emulsion, oint- ment, gel, solution, or powder form.
  • emulsion, oint- ment, gel, solution, or powder form offers particular advantages in the bioavail- ability, stability and efficacy of the drug, medi ⁇ cinal or other active ingredient.
  • a conventional method for the topical application of such materials is through the use of applicators comprising, e.g., non-woven fiber sheets composed of cellulose fibers, synthetic fibers or combinations thereof.
  • applicators comprising, e.g., non-woven fiber sheets composed of cellulose fibers, synthetic fibers or combinations thereof.
  • the above- indicated emulsions, solutions, etc. are added to the applicator material, which is then packaged for storage and sale and ultimately applied by the user.
  • the applicator materials themselves may be prepared in a number of ways in order to allow flexibility in the shape, thickness, softness and absorbency thereof. Accordingly, such applicators have found a wide range of use in the topical application of certain materials.
  • U.S. Patent No. 4,383,986 discloses a hemorrhoidal composition dispersed onto an applicator.
  • the composition itself contains hydrocortisone and dimethylisosorbide, alcohol, witch hazel, amphoteric surfactants and a bacteric- ide.
  • U.S. Patent 3,103,682 discloses the application of suntanning oils or creams with an absorbent pad, such as a plastic sponge.
  • U.S. Patent No. 4,413,032 discloses a non-woven fabric covering for cellulose materials.
  • Ammonium salt cationic surfactants are used as wet- ting agents in the manufacture of the non-woven fabric.
  • the ammonium salt cationic surfactants are coated onto synthetic fibers during manufacture, and are capable of being chemisorbed onto cellu ⁇ lose fibers.
  • An improvement in the rate at which liquid can be absorbed into the cellulose material and the blocking of the return of liquid onto the cellulose is disclosed.
  • 4,753,843 discloses an integral non- woven web useful as a wipe or to protect objects from liquid contact, which comprises a center layer of hydrophobic thermoplastic fibers and an outer layer of thermoplastic fibers rendered hydrophilic through the addition of a non-ionic surfactant.
  • U.S. Patent 4,073,852 discloses a process for the manufacture of non-woven materials which are more absorbent at the center than at the edges thereof. Products produced by this process are useful as disposable diapers and the like.
  • U.S. Patent No. 3,795,624 discloses an applicator which is impregnated with a cosmetic formula. This formula allows for the removal of cosmetics, depositing a moisturizing film therefor. The moisturizing film may be removed by water.
  • the cosmetic formula of this patent comprises an anhy ⁇ drous composition consisting essentially of a non- ionic surfactant of several classes in an accep ⁇ table cosmetic vehicle.
  • Japanese Patent No. 57- 209008 discloses a cotton cleaner useful for removing cosmetics.
  • the cotton applicator itself is impregnated with a solution containing a ⁇ ynthe- tic rubber latex and a surfactant.
  • a physiologically compatible composi ⁇ tion suitable for topical application with a cellu ⁇ lose-containing fabric applicator comprising about 0.01% to about 10% by weight of a non-irritating ionic surfactant blocking agent for blocking bind- ing sites in the cellulose-containing fabric; about 0.05% to about 30% by weight of an active ingredi ⁇ ent for topical application by the applicator; and about 5 to about 95% by weight of a vehicle for dispersing the blocking agent and the active ingre- dominant in the applicator fabric.
  • a method for the preparation of an applicator comprising the compo ⁇ sition according to the present invention is also disclosed. Detailed Description of the invention
  • the present inventor has found that the use of ionic surfactants as part of a physiolog ⁇ ically compatible composition containing active ingredients suitable for topical application, increases the efficacy and stability of the active ingredients when dispersed in the applicator mate ⁇ rial.
  • the ionic surfactant blocking agents prefer ⁇ entially bind to the binding sites on the cellu- lose-containing applicator material, thereby increasing the amount of active ingredient avail ⁇ able for topical removal from the applicator upon the application of pressure to the applicator.
  • the present compositions comprise about 0.01% to about 10 wt.% of a non-irritating ionic surfactant blocking agent for blocking binding sites in a cellulose containing fabric; about 0.05% to about 30 wt.% of an active ingredient suitable for topical application by the applicator; and about 5 to about 95 wt. % of a vehicle for dispers ⁇ ing the ionic surfactant and the active ingredient in the applicator fabric.
  • the present compositions comprise an ionic surfactant in amount of about 0.1 to about 5 weight %; an active ingre-ist in an amount of about 0.1 to about 30 weight %; and a vehicle in an amount of about 10 to about 95% weight %.
  • the present compositions should have a specific gravity of about 0.8 to about 1.1, and preferably about 0.95 to about 1.05. When the com ⁇ positions are within these ranges, they are low enough in viscosity to disperse well on the appli ⁇ cator. That is, when the compositions have a spe ⁇ cific gravity of about 1.0, they have a flow similar to water, a low viscosity, and thus dis ⁇ perse well on the applicator material.
  • Ionic surfactants appropriate for use in the present invention are materials capable of binding to the above-noted binding sites on the cellulose-containing fabric applicator, thereby blocking the binding sites on the applicator and rendering them unavailable to bind the active ingredient.
  • appropriate ionic surfac- tants will provide a physiologically compatible final composition, i.e., one which will be non- irritating when applied by the end-user.
  • quaternized hydroxyethyl cellulose derivatives such as those derivatized with alkyl fatty quaternary groups, e.g., laurdi- monium hydroxyethylcellulose, cocodimonium hydroxy- ethylcellulose, steardimonium hydroxyethylcellu- lose); quaternary ammonium compounds (e.g., ben- zalkonium chloride, cetalkonium chloride, hydroxy- propyl bis-stearyldimoniu chloride, PPG-40 dieth- ylmoniu chloride, oleamidopropyl dimethyl-2,3- dihydroxypropyl ammonium chloride, stearalkonium chloride, hydroxy bis-oleyldimonium chloride, cocamidopropyl dimonium chloride, lauramidopropyl dihydroxy propyldimonium chloride, lauramidopropyl dihydroxy propyldimonium chloride, lauramido
  • ionic surfactant blocking agents used in a particular composition according to the present invention is variable, and will be dependent upon the properties desired in the final product. For example, in most cases, the external phase of the final composition will contain the ionic surfactant. Therefore, if one desires an oil-in-water solution, one would choose a water- soluble surfactant. In contrast, when a water-in- oil emulsion is intended, one would choose an oil- soluble ionic surfactant. Examples of water- soluble surfactants are quaternary ammonium sulfate compounds, amine oxide compounds and alkyl sul ⁇ fates.
  • oil-soluble surfactants are quaternary ammonium compounds, such as PPG-40 diethylmonium chloride, mink amidopropyl ethyl ⁇ dimonium ethosulfate and wheat germ amidopropyl ethyldimonium ethosulfate.
  • the particular ionic surfactant chosen must be soluble in the chosen vehicle.
  • the ionic surfactants useful in the present compositions may be either cationic or anionic. Generally, however, anionic surfactants are more irritating when administered topically than cationic surfactants. Therefore, the use of cationic surfactants is preferred in the present compositions.
  • the sur- factants that allows them to bind to the applicator material (specifically, to the binding sites dis ⁇ cussed above) causing the desired blocking action on the binding sites. Also, due to the ionic nature of these compounds, they will bind to the keratin or homey layer of the dermis to which they are applied, thereby softening the skin. For example, because these compounds are also usually long-chain fatty alkyls, they exhibit skin soft ⁇ ening effects, or film-forming qualities. These compounds may also act as emulsifiers, due to their long-chain structure.
  • active ingredients which may be used in the present invention, there are any of various drugs, edicinals or any other materials which will provide a desired physiological or pharmacological effect when applied topically by the end-user.
  • topical application is understood to mean application to a human or animal body to provide delivery of an active ingredient at or immediately beneath the point of application.
  • Appropriate active ingredients will provide the desired physiological and/or pharmaceutical response when topically applied by the applicator, while further providing a physiologically accep- table final composition.
  • Active ingredients useful in the present compositions include, e.g., topical anti-microbial agents, topical anti-fungal agents, sunscreens, analgesic agents, anti-inflammatory agents and anti-acne agents.
  • sunscreens useful in the present compositions include e.g.,para-amino ben- zoates (PABA derivatives) , salicylates, cinnamates, benzophenones, and other agents known to be useful as sunscreens.
  • Topical anti-fungal agents which may be used in the present compositions include, e.g., haloprogin, iodochlorhydroxyquin, miconazole nitrate, ketoconazole, nystatin, tolnaftate, bifon- azole, clotrimizole, econazole, undecylenic acid and salts thereof, such as calcium undecylenate, copper undecylenate and zinc undecylenate.
  • Topical anti-microbial agents which may be used in the present compositions include, e.g., neomycin sul ⁇ fate, poly ixin B sulfate, gramicidin, and bacitra- cin.
  • Topical analgesic agents useful in the pres ⁇ ent composition include, e.g., piroxicam, benzo- caine, camphor, methyl ⁇ alicylate, phenol and benzydamine.
  • Useful anti-inflammatory agents include, e.g., the hydrocortisones.
  • Useful anti- acne drugs for the present composition include, e.g., benzoyl peroxide.
  • Other active ingredients useful in the present invention will be evident to those skilled in the art based upon the present disclosure.
  • Vehicles which may be used to form the dispersion ⁇ , solution ⁇ , emulsions and/or suspen- sions of the present invention include, e.g., water, alcohols and oils.
  • the type of vehicle used in a particular composition pursuant to the present invention is highly variable. The choice of vehi- - li ⁇
  • te ⁇ will be apparent to one skilled in the art based upon the ingredients of the compo ⁇ ition and the propertie ⁇ desired in the final product.
  • the vehicle used must also provide a final composition which is physiologically acceptable.
  • Oils useful as vehicles in the present compositions include, e.g., petroleum oils (such as mineral oil), palm kernel oil, apricot kernel oil, jojoba oil, almond oil, grape seed oil, sesame oil, wheat germ oil, avocado oil, fish oil and mink oil.
  • Appropriate alcohols useful as vehicles in the present compositions include, e.g., ethanol, stearyl alcohol, propylene glycol, isopropanol and mixtures thereof.
  • Other vehicles useful in the present invention will be evident to one skilled in the art based upon the present disclosure.
  • adjuvants are useful in the pres ⁇ ent compositions in order to obtain final products desirable to the end user, to facilitate the prepa- ration of the compositions, to achieve final prod ⁇ ucts preferred by the consumer, etc.
  • Adjuvants which may be used in the present compositions include, e.g., surfactants, solvents, preserva ⁇ tives, skin conditioners and oils.
  • Surfactants which may be used as adju ⁇ vants in the present compositions include those of the non-ionic type.
  • the auxiliary non-ionic sur- factant ⁇ are useful for emulsifying the active ingredient prior to dispersing the liquid on the applicator.
  • Such surfactants may be prepared by, e.g., polymerizing ethylene oxide in a hydrophobic (oil soluble) base. Generally, as the number of ether linkages in such a compound increase, water solubility also increase ⁇ .
  • Typical hydrophobic bases which may be used to prepare such surfactants are, e.g., stearyl alcohol, oleyl alcohol, lauryl alcohol, cetearyl alcohol, and cetyl alcohol.
  • the non-ionic surfactants useful in the present compo ⁇ sition include, e.g., polyethylene glycol, poly- oxyethylene fatty acid esters, including poly- oxyethylene sorbitan fatty acid esters (e.g.
  • poly- sorbate 20, 40, 60, 80 and 85 poly- sorbate 20, 40, 60, 80 and 85
  • sorbitan fatty acid esters e.g., sorbitan laurate, sorbitan palmitate, sorbitan stearate, sorbitan tristearate, ⁇ orbitan oleate and sorbitan ⁇ e ⁇ quioleate
  • mono- and di-glycerol e ⁇ ter ⁇ e.g., glyceroleate, glycerol stearate and propylene glycol stearate
  • Preservatives useful in the present com ⁇ positions include, e.g., orthophenylphenols, cis- l-(3-chloroallyl)-3,5,7-tri-aza-l-azonia adamantane chloride, ethanol, dimethylol dimethyl hydantoin, benzethonium chloride, 3-phenyl-l-propanol, chloro- i ⁇ othiazoleinone, glycerol onolaurin, isopropyl parabens, monomethyloldimethyl hydantoin, methyl, ethyl, propyl and butyl parabens, phenethyl alco ⁇ hol, phenylmecuric compounds, sodium sulfite, glu- taraldehyde and benzyl alcohol.
  • orthophenylphenols cis- l-(3-chloroallyl)-3,5,7-tri-aza-l-azonia a
  • compositions may further con ⁇ tain skin conditioners, such as humectants or emol- lient ⁇ as adjuvants, to provide a product which is more desirable to the end-user.
  • skin conditioners such as humectants or emol- lient ⁇ as adjuvants
  • humec ⁇ tants are material ⁇ which condition the skin by maintaining a high water content thereon, thu ⁇ increa ⁇ ing the softness of the skin.
  • humectants include glycerin, glycol compounds, such as propylene glycol or ethylene glycol, sorbi- tol, lactic acid, sodium lactate, microcrystalline cellulose and collagen.
  • Emollients render the skin softer and more pliable through the provision of a barrier layer and their penetration into the sur- face layers of the skin.
  • Emollients useful in the present composition ⁇ include all of the non-ionic (i.e., hydrophobic) surfactants discussed above, cetyl alcohol, glyceryl monostearate, propylene glycol, stearyl alcohol, palmitic acid and i ⁇ o- stearic acid. Film-formers, such as dimethicone and cyclomethicone, as well as lanolin and oils, such as mineral oil and mink oil, are also useful as emollients in the present invention. Other adjuvants useful in the present invention will be evident to those skilled in the art based upon the present disclosure.
  • the adjuvants are present in the present compositions in an amount by weight of about 0.1% to about 30%.
  • the adjuvants are pres ⁇ ent in an amount of about 1.0% to about 25% by weight.
  • the pre ⁇ ent compositions may be formu ⁇ lated in solution, disper ⁇ ion, ⁇ uspension, and/or emulsion form, as deemed necessary by one skilled in the art, based upon the characteristics of the individual ingredients used and the desired results.
  • the present compositions may be prepared by any of the various methods of emulsification, disper ⁇ ion or mixture known to one skilled in the art and is not limited.
  • the present compo ⁇ ition Prior to addition to the applicator material, the present compo ⁇ ition may have to be stirred or heated in order to ensure homogeneity. Stirring and/or heating of the pres ⁇ ent composition may not be neces ⁇ ary, depending upon the formulation used and the specific gravity of the composition.
  • compositions are disper ⁇ ed in a cellulo ⁇ e-containing fabric applicator and made ready for topical application of the active ingredient.
  • the ionic surfactant blocking agents of the compo ⁇ itions of the present invention will act to block the binding site ⁇ pre ⁇ ent on the applicator material.
  • the present composition ⁇ may be applied directly to the cel- lulo ⁇ e-containing fabric applicator ⁇ and then packaged, e.g., for ⁇ ale to the final consumer.
  • the composition may be applied to the cellulose- containing fabric applicators in any appropriate manner known to one skilled in the art, e.g., by spraying the compo ⁇ ition onto the applicator, dipping the applicator into the compo ⁇ ition, etc.
  • the end-user or consumer may then conveniently u ⁇ e the present applicator by merely applying the applicator delivery surface directly to the area of the body for which administration of the active ingredient is desired.
  • the active ingredient will thereby be expressed from the applicator and topi- cally applied to the desired area. Once applied thusly, the active ingredient can provide the de ⁇ ired effect ⁇ at or directly beneath the ⁇ ite of application.
  • any type of cellulose-containing fabric material may be used as the applicator of the present invention.
  • the applicators may be in any form, including, e.g., swabs, pads, etc.
  • the spe ⁇ cific form is not limited and appropriate forms will be evident to one skilled in the art based on the present disclosure.
  • Examples of cellulose and cellulose-containing blends which may be used in the present invention include, e.g., grade numbers 800-897 produced by the Fort Howard Paper Co., Green Bay, Wisconsin and blends produced by The Scott Paper Co., Philadelphia, Pennsylvania such as those sold under the product names HIGHLOFT and DURATEX.
  • the cellulose-containing fabric applicators are of the non-woven type.
  • Other applicators useful in the present invention will be evident to those skilled in the art based upon the present disclosure.
  • the applicator containing the composition may then be sealed in vapor and/or moisture resi ⁇ tant container ⁇ (such as polyester, polyethylene or foil, alone or laminated together to form a desirable barrier).
  • the present applicator may be prepared as follows. The applicator is placed into a preformed package, such as an envelope which is ⁇ ealed on three sides. The liquid composition of the present invention is then added to the applicator and the package is sealed.
  • the applicator may be prepared by any other suitable manner known to those skilled in the art, so long as the cellulose-containing fabric applicator is saturated with the composition and the applicator is sealed within a protective pack ⁇ age.
  • the amount of the composition of the present invention applied to the applicator is variable and may be determined based upon the size and absorbency of the applicator. However, generally, enough liquid should be applied to cover or saturate 100% of the applicator. For example, in order to saturate a 7 x 7-3/4 inch applicator, about 5 to 15 grams of the present composition should be applied thereto. However, the amount of composition added to the fabric applicator is vari- able and the appropriate amount will be evident to one skilled in the art based on the present disclo ⁇ sure.
  • the cellulose-containing fabric applica ⁇ tor itself needs no special treatment during pro- duction, other than to be cut to the desired size and shape. Once cut in the appropriate manner, the applicator should be in condition to have the pres ⁇ ent composition applied thereto in the manner dis- cu ⁇ ed above.
  • the pre ⁇ ent invention will now be further illu ⁇ trated by reference to the following, speci- fic, non-limiting example ⁇ .
  • Example 1 To 7.Og of a 5.0% ⁇ olution of octyl dimethyl PABA in ethanol, l.Og of each of the following ionic surfactants (2) to (9) was added with stirring. 7 grams of each solution was then applied to a 7 x 7 inch piece of cellulose- containing applicator material Grade No. 814, manufactured by the Fort Howard Paper Co. , and sealed. The applicators were incubated for 30 days, opened and the liquid expressed. The liquids expre ⁇ ed from each applicator were then analyzed after diluting to a concentration of 1:1,000,000 in propanol. The ab ⁇ orbance of the active ingredient in each sample was measured spectrophotometrically.
  • Example 2 The composition of Example 2 was prepared as follows: All amounts are in percent by weight. Part A and Part B were individually heated to 70 * C. Once heated in thi ⁇ manner. Part A wa ⁇ then added to Part B with mixing. This mixture was then cooled until it reached a temperature of 50*C. When the mixture of Parts A and B reached 50 * C, Part C was added thereto.
  • Parts A, B and C were then allowed to cool until reaching a temperature of 30*C.
  • Parts D and E and F were added simultaneously thereto, with mixing.
  • Mixing was continued until the composition reached room temperature.
  • the compo ⁇ ition wa ⁇ then applied to a cellulose- containing fabric applicator as in Example 1 and allowed to ⁇ tand at room temperature.
  • Quaterium 26 (mink amidopropyl dimethy1-2-hydroxyethyl ammonium chloride) 5.0 PART F
  • Example 2 ha ⁇ main ⁇ tained it ⁇ ⁇ tability at room temperature for at least six months (i.e., ha ⁇ remained emulsified, the active ingredient ⁇ have not decompo ⁇ ed, etc.)
  • thi ⁇ compo ⁇ ition provides for the enhanced topical application of the active ingre ⁇ washers: oxybenzone, octyl methoxycinnamate and octyl salicylate; while further providing a smooth feel to the ⁇ kin.

Abstract

A physiologically compatible composition suitable for topical application with a cellulose-containing fabric applicator comprises about 0.01 % to about 10 % by weight of a non-irritating ionic surfactant blocking agent for blocking binding sites in the cellulose-containing fabric; about 0.05 % to about 30 % by weight of an active ingredient for topical application by the applicator; and about 5 % to about 95 % by weight of a vehicle for dispersing the blocking agent and the active ingredient in the fabric applicator.

Description

COMPOSITION AND METHODS FOR THE STABILIZATION OF MATERIALS
DISPERSED ONTO APPLICATORS
Reference to Related Applications
This application is related to PCT Published Application No. WO89/10738, published November 16, 1989, having a filing date of May 9, 1988 for "Sunscreen
Composition and Application System", the disclosure of which is incorporated herein by reference.
Field of the Invention The present invention relates to composi- tionε and methods which facilitate the topical administration of active ingredients.
Background of the Invention There are numerous drugs, edicinals and other active ingredients which offer various bene- fits when applied topically to the human or animal body to provide desired physiological effects to an isolated part of the body. The topical administra¬ tion of active ingredients is employed to deliver the active ingredient at or immediately beneath the point of application. For example, sunscreens are useful in blocking the harmful effects of the sun and anti-inflammatory agents can relieve the dis¬ comfort caused by various irritants, such as poison ivy. A large number of active ingredients are applied to the skin, although topical application may also be used for treating the eyes, the nose, the throat, the ears, the hair, the nails, the teeth, etc. Although enough active ingredient may be absorbed into the systemic circulation to cause systemic effects, absorption from topical adminis¬ tration is usually too erratic to be used for sys- temic therapy. However, topical administration is an effective and convenient means to locally apply active ingredients.
Conventionally, active ingredients for topical application are applied in emulsion, oint- ment, gel, solution, or powder form. Each of these forms offers particular advantages in the bioavail- ability, stability and efficacy of the drug, medi¬ cinal or other active ingredient.
A conventional method for the topical application of such materials is through the use of applicators comprising, e.g., non-woven fiber sheets composed of cellulose fibers, synthetic fibers or combinations thereof. The above- indicated emulsions, solutions, etc., are added to the applicator material, which is then packaged for storage and sale and ultimately applied by the user. The applicator materials themselves may be prepared in a number of ways in order to allow flexibility in the shape, thickness, softness and absorbency thereof. Accordingly, such applicators have found a wide range of use in the topical application of certain materials.
The use of applicators to topically apply drugs, medicinals and other active agents, has been addressed in, e.g., U.S. Patent No. 4,383,986 which discloses a hemorrhoidal composition dispersed onto an applicator. The composition itself contains hydrocortisone and dimethylisosorbide, alcohol, witch hazel, amphoteric surfactants and a bacteric- ide. Likewise, U.S. Patent 3,103,682 discloses the application of suntanning oils or creams with an absorbent pad, such as a plastic sponge.
In efforts to improve the application of ingredients, most of the work in the applicator area has focused on methods of manufacture or methods for embodying particular functionalities onto the applicator material itself. For example, U.S. No. Patent 4,723,954 discloses a process for increasing the water repellency of non-woven fabric which combines specific layers of cellulose and synthetic fibers.
U.S. Patent No. 4,413,032 discloses a non-woven fabric covering for cellulose materials. Ammonium salt cationic surfactants are used as wet- ting agents in the manufacture of the non-woven fabric. The ammonium salt cationic surfactants are coated onto synthetic fibers during manufacture, and are capable of being chemisorbed onto cellu¬ lose fibers. An improvement in the rate at which liquid can be absorbed into the cellulose material and the blocking of the return of liquid onto the cellulose is disclosed. However, there is no dis¬ closure of the use of such surfactants in composi¬ tions containing active ingredients which are suit- able for topical application, as the surfactants used would be too irritating for topical use. U.S. Patent No. 4,753,843 discloses an integral non- woven web useful as a wipe or to protect objects from liquid contact, which comprises a center layer of hydrophobic thermoplastic fibers and an outer layer of thermoplastic fibers rendered hydrophilic through the addition of a non-ionic surfactant.
U.S. Patent 4,073,852 discloses a process for the manufacture of non-woven materials which are more absorbent at the center than at the edges thereof. Products produced by this process are useful as disposable diapers and the like.
U.S. Patent No. 3,795,624 discloses an applicator which is impregnated with a cosmetic formula. This formula allows for the removal of cosmetics, depositing a moisturizing film therefor. The moisturizing film may be removed by water. The cosmetic formula of this patent comprises an anhy¬ drous composition consisting essentially of a non- ionic surfactant of several classes in an accep¬ table cosmetic vehicle. Japanese Patent No. 57- 209008 discloses a cotton cleaner useful for removing cosmetics. The cotton applicator itself is impregnated with a solution containing a εynthe- tic rubber latex and a surfactant.
However, in spite of such attempts, dis¬ persions of fluids containing drugs, medicinals or other active ingredients placed onto an applicator (e.g., a non-woven fabric) often demonstrate insta- bility, which is reflected in a loss of availabil¬ ity of the drug from the dispersion. The mechanism for such loss has been found to be the binding of the drug to the applicator material itself, i.e., the binding of the drug to the fabric. Such bind- ing may be attributed to the functional groups (usually hydroxyl groups) which are particularly abundant in cellulose materials and act as binding sites. Drugs contained in such liquid compositions may also bind or adsorb onto hydrophobic regions of the applicator material.
In an attempt to address these problems caused by the binding sites on such applicators, a process has been disclosed for binding and soft¬ ening towel material using ionic compounds (see, Hughes and Koch, Soap and Chemical Specialties, pp 109-112, December 1965). These compounds, such as distearyl dimethyl ammonium chloride and 2-hepto- decyl-l-methyl-1-(2'stearoyla ido-ethyl)-imida- zolium methyl sulfate, are discussed as being useful for binding to and softening fabrics. How¬ ever, the ionic compounds of this reference would not be useful for the topical application of drugs, medicinals, and other active ingredients, due to their potential for irritancy when applied to the skin.
Therefore, in view of the deficiencies of known compositions and methods as described above, it can be seen that it would be desirable to have a composition which, when dispersed in an applicator, will allow for the greater efficacy and availa¬ bility of the drug, while not causing irritation to the skin upon topical application.
Summary of the nvention According to the present invention, there is provided a physiologically compatible composi¬ tion suitable for topical application with a cellu¬ lose-containing fabric applicator comprising about 0.01% to about 10% by weight of a non-irritating ionic surfactant blocking agent for blocking bind- ing sites in the cellulose-containing fabric; about 0.05% to about 30% by weight of an active ingredi¬ ent for topical application by the applicator; and about 5 to about 95% by weight of a vehicle for dispersing the blocking agent and the active ingre- dient in the applicator fabric. A method for the preparation of an applicator comprising the compo¬ sition according to the present invention is also disclosed. Detailed Description of the invention
The present inventor has found that the use of ionic surfactants as part of a physiolog¬ ically compatible composition containing active ingredients suitable for topical application, increases the efficacy and stability of the active ingredients when dispersed in the applicator mate¬ rial. The ionic surfactant blocking agents prefer¬ entially bind to the binding sites on the cellu- lose-containing applicator material, thereby increasing the amount of active ingredient avail¬ able for topical removal from the applicator upon the application of pressure to the applicator.
The present compositions comprise about 0.01% to about 10 wt.% of a non-irritating ionic surfactant blocking agent for blocking binding sites in a cellulose containing fabric; about 0.05% to about 30 wt.% of an active ingredient suitable for topical application by the applicator; and about 5 to about 95 wt. % of a vehicle for dispers¬ ing the ionic surfactant and the active ingredient in the applicator fabric. Preferably, the present compositions comprise an ionic surfactant in amount of about 0.1 to about 5 weight %; an active ingre- dient in an amount of about 0.1 to about 30 weight %; and a vehicle in an amount of about 10 to about 95% weight %.
The present compositions should have a specific gravity of about 0.8 to about 1.1, and preferably about 0.95 to about 1.05. When the com¬ positions are within these ranges, they are low enough in viscosity to disperse well on the appli¬ cator. That is, when the compositions have a spe¬ cific gravity of about 1.0, they have a flow similar to water, a low viscosity, and thus dis¬ perse well on the applicator material.
Ionic surfactants appropriate for use in the present invention are materials capable of binding to the above-noted binding sites on the cellulose-containing fabric applicator, thereby blocking the binding sites on the applicator and rendering them unavailable to bind the active ingredient. Moreover, appropriate ionic surfac- tants will provide a physiologically compatible final composition, i.e., one which will be non- irritating when applied by the end-user.
As the ionic surfactant blocking agents of the present compositions, the following types of compounds may be used: quaternized hydroxyethyl cellulose derivatives (such as those derivatized with alkyl fatty quaternary groups, e.g., laurdi- monium hydroxyethylcellulose, cocodimonium hydroxy- ethylcellulose, steardimonium hydroxyethylcellu- lose); quaternary ammonium compounds (e.g., ben- zalkonium chloride, cetalkonium chloride, hydroxy- propyl bis-stearyldimoniu chloride, PPG-40 dieth- ylmoniu chloride, oleamidopropyl dimethyl-2,3- dihydroxypropyl ammonium chloride, stearalkonium chloride, hydroxy bis-oleyldimonium chloride, cocamidopropyl dimonium chloride, lauramidopropyl dihydroxy propyldimonium chloride, dimethyl benzyl ammonium chloride, mink amidopropyl ethyldimonium ethosulfate, mink amidopropyl dimethyl-2-hydroxy- ethyl ammonium chloride and wheat germ amidopropyl- ethyl-aimonium ethosulfate) ; quarternary ammonium εulfaτ.e compounds (e.g., soya ethyl ammonium etho¬ sulfate, rincinoleic acid ammonium ethosulfate, isostearylamido propyl ethyldimonium ethosulfate, bis-amidopropyl-N,N-dimethyl-N-ethyl ammonium ethylsulfate, and soya dimethyl ethyl ammonium sulfate}; amine oxide compounds (e.g., lauramine oxide, myristamine oxide, oleamine oxide, steara- mine oxide, potassium dihydroxyethyl cocamine oxide phosphate, palmitamine oxide, cocamidopropyl amine oxide and cocamidopropylamine) ; alkyl sulfates (e.g., TEA-lauryl sulfate, sodium lauryl sulfate, sodium olefin sulfonate, and sodium dodecylbenzene sulfonate) ; and polyvinylpyrrolidone and long chain alpha-olefins (e.g., butylated polyvinylpyrroli¬ done, and polyvinylpyrrolidone-eicosene copolymer) . Other suitable ionic surfactants for use in the present invention will be evident to those skilled in the art based upon the present disclosure. The choice of ionic surfactant blocking agents used in a particular composition according to the present invention is variable, and will be dependent upon the properties desired in the final product. For example, in most cases, the external phase of the final composition will contain the ionic surfactant. Therefore, if one desires an oil-in-water solution, one would choose a water- soluble surfactant. In contrast, when a water-in- oil emulsion is intended, one would choose an oil- soluble ionic surfactant. Examples of water- soluble surfactants are quaternary ammonium sulfate compounds, amine oxide compounds and alkyl sul¬ fates. Examples of oil-soluble surfactants are quaternary ammonium compounds, such as PPG-40 diethylmonium chloride, mink amidopropyl ethyl¬ dimonium ethosulfate and wheat germ amidopropyl ethyldimonium ethosulfate. Moreover, when the present compositions are to be solutions, the particular ionic surfactant chosen must be soluble in the chosen vehicle. As can be seen from the ionic surfactants set forth above, the ionic surfactants useful in the present compositions may be either cationic or anionic. Generally, however, anionic surfactants are more irritating when administered topically than cationic surfactants. Therefore, the use of cationic surfactants is preferred in the present compositions.
It is the ionic character of the sur- factants that allows them to bind to the applicator material (specifically, to the binding sites dis¬ cussed above) causing the desired blocking action on the binding sites. Also, due to the ionic nature of these compounds, they will bind to the keratin or homey layer of the dermis to which they are applied, thereby softening the skin. For example, because these compounds are also usually long-chain fatty alkyls, they exhibit skin soft¬ ening effects, or film-forming qualities. These compounds may also act as emulsifiers, due to their long-chain structure.
As active ingredients which may be used in the present invention, there are any of various drugs, edicinals or any other materials which will provide a desired physiological or pharmacological effect when applied topically by the end-user. As set forth above, topical application is understood to mean application to a human or animal body to provide delivery of an active ingredient at or immediately beneath the point of application. Appropriate active ingredients will provide the desired physiological and/or pharmaceutical response when topically applied by the applicator, while further providing a physiologically accep- table final composition. Active ingredients useful in the present compositions include, e.g., topical anti-microbial agents, topical anti-fungal agents, sunscreens, analgesic agents, anti-inflammatory agents and anti-acne agents.
Examples of sunscreens useful in the present compositions include e.g.,para-amino ben- zoates (PABA derivatives) , salicylates, cinnamates, benzophenones, and other agents known to be useful as sunscreens. Topical anti-fungal agents which may be used in the present compositions include, e.g., haloprogin, iodochlorhydroxyquin, miconazole nitrate, ketoconazole, nystatin, tolnaftate, bifon- azole, clotrimizole, econazole, undecylenic acid and salts thereof, such as calcium undecylenate, copper undecylenate and zinc undecylenate. Topical anti-microbial agents which may be used in the present compositions include, e.g., neomycin sul¬ fate, poly ixin B sulfate, gramicidin, and bacitra- cin. Topical analgesic agents useful in the pres¬ ent composition include, e.g., piroxicam, benzo- caine, camphor, methyl εalicylate, phenol and benzydamine. Useful anti-inflammatory agents include, e.g., the hydrocortisones. Useful anti- acne drugs for the present composition include, e.g., benzoyl peroxide. Other active ingredients useful in the present invention will be evident to those skilled in the art based upon the present disclosure. Vehicles which may be used to form the dispersionε, solutionε, emulsions and/or suspen- sions of the present invention include, e.g., water, alcohols and oils. The type of vehicle used in a particular composition pursuant to the present invention is highly variable. The choice of vehi- - li ¬
te ε will be apparent to one skilled in the art based upon the ingredients of the compoεition and the propertieε desired in the final product. The vehicle used must also provide a final composition which is physiologically acceptable.
Oils useful as vehicles in the present compositions include, e.g., petroleum oils (such as mineral oil), palm kernel oil, apricot kernel oil, jojoba oil, almond oil, grape seed oil, sesame oil, wheat germ oil, avocado oil, fish oil and mink oil. Appropriate alcohols useful as vehicles in the present compositions include, e.g., ethanol, stearyl alcohol, propylene glycol, isopropanol and mixtures thereof. Other vehicles useful in the present invention will be evident to one skilled in the art based upon the present disclosure.
Certain adjuvants are useful in the pres¬ ent compositions in order to obtain final products desirable to the end user, to facilitate the prepa- ration of the compositions, to achieve final prod¬ ucts preferred by the consumer, etc. Adjuvants which may be used in the present compositions include, e.g., surfactants, solvents, preserva¬ tives, skin conditioners and oils. Surfactants which may be used as adju¬ vants in the present compositions include those of the non-ionic type. The auxiliary non-ionic sur- factantε are useful for emulsifying the active ingredient prior to dispersing the liquid on the applicator. Such surfactants may be prepared by, e.g., polymerizing ethylene oxide in a hydrophobic (oil soluble) base. Generally, as the number of ether linkages in such a compound increase, water solubility also increaseε. Typical hydrophobic bases which may be used to prepare such surfactants are, e.g., stearyl alcohol, oleyl alcohol, lauryl alcohol, cetearyl alcohol, and cetyl alcohol. The non-ionic surfactants useful in the present compo¬ sition include, e.g., polyethylene glycol, poly- oxyethylene fatty acid esters, including poly- oxyethylene sorbitan fatty acid esters (e.g. , poly- sorbate 20, 40, 60, 80 and 85), sorbitan fatty acid esters (e.g., sorbitan laurate, sorbitan palmitate, sorbitan stearate, sorbitan tristearate, εorbitan oleate and sorbitan εeεquioleate) , and mono- and di-glycerol eεterε (e.g., glyceroleate, glycerol stearate and propylene glycol stearate) .
Preservatives useful in the present com¬ positions include, e.g., orthophenylphenols, cis- l-(3-chloroallyl)-3,5,7-tri-aza-l-azonia adamantane chloride, ethanol, dimethylol dimethyl hydantoin, benzethonium chloride, 3-phenyl-l-propanol, chloro- iεothiazoleinone, glycerol onolaurin, isopropyl parabens, monomethyloldimethyl hydantoin, methyl, ethyl, propyl and butyl parabens, phenethyl alco¬ hol, phenylmecuric compounds, sodium sulfite, glu- taraldehyde and benzyl alcohol.
The present compositions may further con¬ tain skin conditioners, such as humectants or emol- lientε as adjuvants, to provide a product which is more desirable to the end-user. Generally, humec¬ tants are materialε which condition the skin by maintaining a high water content thereon, thuε increaεing the softness of the skin. Examples of such humectants include glycerin, glycol compounds, such as propylene glycol or ethylene glycol, sorbi- tol, lactic acid, sodium lactate, microcrystalline cellulose and collagen. Emollients render the skin softer and more pliable through the provision of a barrier layer and their penetration into the sur- face layers of the skin. Emollients useful in the present compositionε include all of the non-ionic (i.e., hydrophobic) surfactants discussed above, cetyl alcohol, glyceryl monostearate, propylene glycol, stearyl alcohol, palmitic acid and iεo- stearic acid. Film-formers, such as dimethicone and cyclomethicone, as well as lanolin and oils, such as mineral oil and mink oil, are also useful as emollients in the present invention. Other adjuvants useful in the present invention will be evident to those skilled in the art based upon the present disclosure.
The adjuvants are present in the present compositions in an amount by weight of about 0.1% to about 30%. Preferably, the adjuvants are pres¬ ent in an amount of about 1.0% to about 25% by weight.
The preεent compositions may be formu¬ lated in solution, disperεion, εuspension, and/or emulsion form, as deemed necessary by one skilled in the art, based upon the characteristics of the individual ingredients used and the desired results.
The present compositions may be prepared by any of the various methods of emulsification, disperεion or mixture known to one skilled in the art and is not limited. Prior to addition to the applicator material, the present compoεition may have to be stirred or heated in order to ensure homogeneity. Stirring and/or heating of the pres¬ ent composition may not be necesεary, depending upon the formulation used and the specific gravity of the composition.
Once the compositions are prepared, they are disperεed in a celluloεe-containing fabric applicator and made ready for topical application of the active ingredient. The ionic surfactant blocking agents of the compoεitions of the present invention will act to block the binding siteε preεent on the applicator material. The present compositionε may be applied directly to the cel- luloεe-containing fabric applicatorε and then packaged, e.g., for εale to the final consumer. The composition may be applied to the cellulose- containing fabric applicators in any appropriate manner known to one skilled in the art, e.g., by spraying the compoεition onto the applicator, dipping the applicator into the compoεition, etc. The end-user or consumer may then conveniently uεe the present applicator by merely applying the applicator delivery surface directly to the area of the body for which administration of the active ingredient is desired. The active ingredient will thereby be expressed from the applicator and topi- cally applied to the desired area. Once applied thusly, the active ingredient can provide the deεired effectε at or directly beneath the εite of application.
Any type of cellulose-containing fabric material may be used as the applicator of the present invention. The applicators may be in any form, including, e.g., swabs, pads, etc. The spe¬ cific form is not limited and appropriate forms will be evident to one skilled in the art based on the present disclosure. Examples of cellulose and cellulose-containing blends which may be used in the present invention include, e.g., grade numbers 800-897 produced by the Fort Howard Paper Co., Green Bay, Wisconsin and blends produced by The Scott Paper Co., Philadelphia, Pennsylvania such as those sold under the product names HIGHLOFT and DURATEX. Preferably, the cellulose-containing fabric applicators are of the non-woven type. Other applicators useful in the present invention will be evident to those skilled in the art based upon the present disclosure.
Once the present compositions are absorbed in the cellulose-containing fabric appli¬ cator material, the applicator containing the composition may then be sealed in vapor and/or moisture resiεtant containerε (such as polyester, polyethylene or foil, alone or laminated together to form a desirable barrier). For example, the present applicator may be prepared as follows. The applicator is placed into a preformed package, such as an envelope which is εealed on three sides. The liquid composition of the present invention is then added to the applicator and the package is sealed. However, the applicator may be prepared by any other suitable manner known to those skilled in the art, so long as the cellulose-containing fabric applicator is saturated with the composition and the applicator is sealed within a protective pack¬ age. Generally, the amount of the composition of the present invention applied to the applicator is variable and may be determined based upon the size and absorbency of the applicator. However, generally, enough liquid should be applied to cover or saturate 100% of the applicator. For example, in order to saturate a 7 x 7-3/4 inch applicator, about 5 to 15 grams of the present composition should be applied thereto. However, the amount of composition added to the fabric applicator is vari- able and the appropriate amount will be evident to one skilled in the art based on the present disclo¬ sure.
The cellulose-containing fabric applica¬ tor itself needs no special treatment during pro- duction, other than to be cut to the desired size and shape. Once cut in the appropriate manner, the applicator should be in condition to have the pres¬ ent composition applied thereto in the manner dis- cuεεed above. The preεent invention will now be further illuεtrated by reference to the following, speci- fic, non-limiting exampleε.
Examples
Example 1 To 7.Og of a 5.0% εolution of octyl dimethyl PABA in ethanol, l.Og of each of the following ionic surfactants (2) to (9) was added with stirring. 7 grams of each solution was then applied to a 7 x 7 inch piece of cellulose- containing applicator material Grade No. 814, manufactured by the Fort Howard Paper Co. , and sealed. The applicators were incubated for 30 days, opened and the liquid expressed. The liquids expreεεed from each applicator were then analyzed after diluting to a concentration of 1:1,000,000 in propanol. The abεorbance of the active ingredient in each sample was measured spectrophotometrically. The percent difference between the amount of octyl dimethyl PABA present in the liquid (i.e., its absorbance) before it was diεperεed on the appli¬ cator and after it was expresεed from the applica¬ tor was calculated. The results are shown below. Ionic Surfactant Liquid Applicator %Diff.
(1) Control 0.213 0.183 - 9.4 (no surfactant)
(2) Hydroxypropyl- 0.204 0.249 +18 bis-oleyl di- monium chloride
(3) Isoεtearyl amido 0.230 0.251 + 8.1 propyl ethyldi¬ monium ethosulfate (4) Cocamidopropyl 0.217 0.237 + 8.4 dihydroxypropyl dimonium chloride
(5) Oleamidopropyl 0.216 0.224 + 3.6 dimethyl 2,3-dihy- droxypropyl ammon¬ ium chloride
(6) Lauramidopropyl 0.219 0.272 +19.5 dihydroxypropyl dimonium chloride (7) Bis-amidoprop- 0.209 0.205 - 2.0 yl- ,N-dimethyl- N-ethyl ammonium ethyl sulfate
(8) Dimethyl benzyl 0.221 0.245 + 9.8 ammonium chloride
(9) Soya dimethyl 0.228 0.245 + 7.0 ethyl ammonium ethosulfate
The example set forth above demonstrates that the amount of active ingredient (i.e., octyl dimethyl PABA) present in the liquid composition of the instant invention after expression from the cellulose-containing applicator, is generally much higher than that of the control. Accordingly, it can be seen that the compositions of the present invention allow for greater availability of an active ingredient from such a fabric applicator. Example 2 The composition of Example 2 was prepared as follows: All amounts are in percent by weight. Part A and Part B were individually heated to 70*C. Once heated in thiε manner. Part A waε then added to Part B with mixing. This mixture was then cooled until it reached a temperature of 50*C. When the mixture of Parts A and B reached 50*C, Part C was added thereto. The mixture of Parts A, B and C was then allowed to cool until reaching a temperature of 30*C. When the mixture reached 30°C, Parts D and E and F were added simultaneously thereto, with mixing. Mixing was continued until the composition reached room temperature. The compoεition waε then applied to a cellulose- containing fabric applicator as in Example 1 and allowed to εtand at room temperature.
Ingredientε %(w/w )
PART A Purified water qε 49.8
Carbomer 934(0.3% εolution) 7.0
PART B
Polyoxyethylene 21 εtearyl ether 1.8
Glyceryl stearate 1.0 Polowax NF 1.2
Stearyl alcohol 0.8
Dimethicone 2.0
PART C
PEG 15 cocoamine 0.1 PART D
SDA 40 (specially denatured alcohol #40) 7.0
Oxybenzone 5.0
Octyl methoxycinnamate 7.5 Octyl salicylate 5.0
Cyclomethicone 2.0 PART E
Quaterium 26 (mink amidopropyl dimethy1-2-hydroxyethyl ammonium chloride) 5.0 PART F
DMDM Hydantoin 0.1
The compoεition of Example 2 haε main¬ tained itε εtability at room temperature for at least six months (i.e., haε remained emulsified, the active ingredientε have not decompoεed, etc.) Moreover, thiε compoεition provides for the enhanced topical application of the active ingre¬ dients: oxybenzone, octyl methoxycinnamate and octyl salicylate; while further providing a smooth feel to the εkin.
The present invention may be embodied in other specific forms without departing from the spirit or eεεential attributeε thereof and, accord¬ ingly, reference should be made to the appended claims, rather than to the foregoing εpecification as indicating the scope of the invention.

Claims

Claims
1. A physiologically compatible composi¬ tion suitable for topical application with a cellu¬ lose-containing fabric applicator, comprising about 0.01% to about 10% by weight of a non-irritating ionic surfactant blocking agent for blocking bind¬ ing siteε in the celluloεe-containing fabric; about 0.05% to about 30% by weight of an active ingredi¬ ent for topical application by εaid applicator; and about 5% to about 95% by weight of a vehicle for diεperεing εaid blocking agent and active ingre¬ dient in εaid fabric applicator.
2. A compoεition aε in claim 1, further comprising about 0.1% to about 30% by weight of a physiologically compatible adjuvant for enhancing said topical application.
3. A compoεition aε in claim 2, wherein εaid adjuvant is selected from the group consiεting of emollientε and humectantε.
4. A compoεition as in claim 1, further comprising about 0.1% to about 30% by weight of a physiologically compatible adjuvant for facilitating the preparation of said composition.
5. A composition as in claim 4, wherein said adjuvant is selected from the group consiεting of εurfactantε, oils, solventε and preservatives.
6. A composition as in claim 1, wherein said ionic surfactant iε εelected from the group conεiεting of quaternized hydroxyethyl celluloεe derivatives, quaternary ammonium compounds, quater¬ nary ammonium sulfate compoundε, amine oxide com¬ pounds, alkyl sulfates, polyvinylpyrrolidoneε and long chain alpha-olefinε.
7. A compoεition as in claim 1, wherein said active ingredient is selected from the group consiεting of sunscreenε, anti-inflammatory agentε, anti-fungal agentε, anti-microbial agentε and anal- geεic agentε.
8. A compoεition as in claim 1, having a εpecific gravity of about 0.8 to about 1.1.
9. A compoεition aε in claim 8, having a εpecific gravity of about 0.95 to about 1.05.
10. A composition as in claim 1, wherein said ionic surfactant is preεent in an amount of from about 0.1% to about 5% by weight.
11. A composition as in claim 1, wherein said active ingredient is preεent in an amount of from about 0.1% to about 30% by weight.
12. A compoεition aε in claim 2, wherein εaid adjuvant iε preεent in an amount of from about 1.0% to about 25% by weight.
13. A composition as in claim 4, wherein said adjuvant is present in an amount of from about
1.0% to about 25% by weight.
14. A composition as in claim 1, wherein said vehicle is present in an amount of from about 10% to about 95% by weight.
15. A method for blocking the binding sites on a cellulose-containing fabric applicator material comprising diεpersing on said applicator material a composition comprising about 0.01% to about 10% by weight of an ionic surfactant; about 0.05% to about 30% by weight of an active ingre¬ dient; and about 5% to about 95% by weight of vehicle.
16. A physiologically compatible composi¬ tion 'suitable for topical application with a non- woven cellulose-containing fabric applicator. compriεing eibout 0.01% to about 10% by weight of lauramidopropyl dihydroxypropyl dimonium chloride; about 0.05% to about 30% by weight of octyl dimethyl PABA; and about 5% to about 95% by weight of ethanol.
PCT/US1990/005622 1989-10-06 1990-10-03 Composition and methods for the stabilization of materials dispersed onto applicators WO1991004730A1 (en)

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0613675A1 (en) * 1993-03-05 1994-09-07 JOHNSON & JOHNSON CONSUMER PRODUCTS, INC. Cosmetic applicator useful for cleansing, moisturizing and protecting the skin from diaper rash
WO1995031189A1 (en) * 1994-05-17 1995-11-23 Bioglan Laboratories Ltd. A medicated wipe

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4383986A (en) * 1981-08-17 1983-05-17 Ortho Pharmaceutical Corporation Hemorrhoidal compositions
US4559157A (en) * 1983-04-21 1985-12-17 Creative Products Resource Associates, Ltd. Cosmetic applicator useful for skin moisturizing

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4383986A (en) * 1981-08-17 1983-05-17 Ortho Pharmaceutical Corporation Hemorrhoidal compositions
US4559157A (en) * 1983-04-21 1985-12-17 Creative Products Resource Associates, Ltd. Cosmetic applicator useful for skin moisturizing

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0613675A1 (en) * 1993-03-05 1994-09-07 JOHNSON & JOHNSON CONSUMER PRODUCTS, INC. Cosmetic applicator useful for cleansing, moisturizing and protecting the skin from diaper rash
WO1995031189A1 (en) * 1994-05-17 1995-11-23 Bioglan Laboratories Ltd. A medicated wipe

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