WO1997010802A1 - Formulations a usage local et systemes d'administration - Google Patents

Formulations a usage local et systemes d'administration Download PDF

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Publication number
WO1997010802A1
WO1997010802A1 PCT/US1996/015596 US9615596W WO9710802A1 WO 1997010802 A1 WO1997010802 A1 WO 1997010802A1 US 9615596 W US9615596 W US 9615596W WO 9710802 A1 WO9710802 A1 WO 9710802A1
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WO
WIPO (PCT)
Prior art keywords
formulation
agent
sodium lauryl
hydrogen peroxide
foam
Prior art date
Application number
PCT/US1996/015596
Other languages
English (en)
Inventor
David D. Mundschenk
Original Assignee
Phylomed Corporation
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 Phylomed Corporation filed Critical Phylomed Corporation
Priority to EP96936055A priority Critical patent/EP0862407A4/fr
Priority to US09/043,433 priority patent/US7060253B1/en
Publication of WO1997010802A1 publication Critical patent/WO1997010802A1/fr

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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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/14—Alkali metal chlorides; Alkaline earth metal chlorides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/40—Peroxides
    • 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
    • A61K8/04—Dispersions; Emulsions
    • A61K8/046—Aerosols; Foams
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/22—Peroxides; Oxygen; Ozone
    • 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
    • A61K8/965—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution of inanimate origin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
    • 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
    • A61Q17/005—Antimicrobial preparations
    • 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

Definitions

  • the present invention relates to topical and other hygiene formulations, and to aerosol devices useful for the delivery of such formulations in the form of lathers and foams.
  • the invention relates to formulations useful in the oral cavity, such as dentifrices containing hydrogen peroxide.
  • the invention relates to the pharmacological use of surfactants such as anionic surfactants, and in particular sodium lauryl sulfate.
  • the invention relates to topical and other hygiene formulations containing natural sea water.
  • Formulations such as cosmetics and pharmaceuticals can be dispensed in a wide variety of vehicles and forms, including powders, capsules, liquids, aerosols, and the like.
  • the delivery of formulations by the aerosol route is generally considered to take one of three forms: (1) the use of "space sprays", such as spray insecticides and air fresheners, which produce very fine sprays capable of evaporating rapidly or floating in the air; (2) the use of sprays such as hair sprays and deodorants, that are intended for continuous film formation; and (3) the use of aerated foams, such as shaving creams, which are produced by the rapid expansion of a propellant through an emulsion.
  • space sprays such as spray insecticides and air fresheners, which produce very fine sprays capable of evaporating rapidly or floating in the air
  • sprays such as hair sprays and deodorants
  • aerated foams such as shaving creams, which are produced by the rapid expansion of a propellant through an emulsion.
  • Aerosols for oral and nasal therapy are generally said to incorporate medicaments as solids suspended in a propellant. More recent advances in valve and propellant technology are said to provide improved delivery to the throat and nasal areas.
  • Formulations delivered in aerosol form by the use of such devices can often include the use of surfactants. For instance, surfactants are commonly used in nebulizer vehicles to decrease surface tension and thus affect particle size (Mintzer, above, p. 206).
  • SLS sodium lauryl sulfate
  • SLS itself was present in over 500 oral solid dosage forms approved by the FDA, as well as in 11 oral liquid dosage forms, 38 topical creams, lotions, ointments, medicates sponges or shampoos, and 28 dentrifices.
  • the rinses described in both patents rely on the detersive effect of oral surfactants.
  • the '708 patent describes the use of SLS as one such oral surfactant, and further describes its function as a "potentiator" for other ingredients.
  • patients were instructed to use one tablespoon of various rinses.
  • Such rinse products which are commercially available under the brand name "Plax" are typically swirled in the mouth in order to produce a weak foaming action.
  • Natural sea water for instance, has long been thought to provide certain desirable, including healing, qualities. See, for instance, Richard Russel, A Dissertation on the use of Sea Water in the Diseases of the Glands: Particularly the Scurvy. Jaundice. King's Evil. Leprosy and the Glandular Consumption.
  • Hydrogen peroxide functions as a weak antibacterial agent, a wound cleanser and a deodorant. It also serves a mechanical effect of effervescence and resultant removal of tissue and other debris.
  • hydrogen peroxide When used as an oral topical, however, hydrogen peroxide is typically administered in the form of a concentrate, solution, or gel.
  • the product is used for cleansing minor wounds, or minor gum inflammation resulting from dental procedures, orthodontic applications, denture irritations, accidental injury and other mouth and gum irritations (e.g., canker sores).
  • Such beneficial uses of hydrogen peroxide include its use as an oral germicide, cleansing agent and hemostat. It is considered a useful disinfectant for mucous membranes because of its low toxicity. See, e.g., Zinner. D.D., et. al.; Controlled Study of the Clinical Effectiveness of A New Oxygen Gel on Plaque. Oral Debris and Gingival inflammation, Pharmacol. Ther. Dent.. October 1970,
  • SLS and hydrogen peroxide have, on occasion, been used together in formulations for the oral cavity. See, for instance, U.S. Patent No. 5,104,644 and 5,174,990 (mouthrinse), 5,084,268 and 5,208,010 (tooth whitening dentifrice).
  • the present invention provides a system useful for delivering chemical agent-containing formulations in the form of foams or sprays.
  • the invention provides a system for delivering a chemical agent- containing formulation in the form of a foam or spray, the system comprising an aerosol dispenser containing a formulation comprising the chemical agent in the form of a solution or stable suspension and an aqueous solution of an anionic surface active agent as a delivery agent.
  • the invention provides a system for delivering a foam or spray such as a disinfecting foam or spray, the system comprising an aerosol dispenser containing a deliverable (e.g., foamable or sprayable) formulation comprising lauryl sulfate, and preferably sodium lauryl sulfate, as a delivery agent.
  • a deliverable e.g., foamable or sprayable
  • the system is used to deliver a cleansing, antiseptic, or disinfecting foam comprising hydrogen peroxide as the active agent.
  • a cleansing, antiseptic, or disinfecting foam comprising hydrogen peroxide as the active agent.
  • Such a system is particularly well suited for the delivery of hydrogen peroxide to the oral cavity, i.e., as a dental or oral formulation.
  • Applicant has found that the delivery of hydrogen peroxide to the oral cavity in the form of a foam or spray improves the effervescence of the formulation and, in turn, improves the removal of tissue and other debris.
  • the formulation is particularly well suited to suspend and remove food particles and other debris, and then itself be rinsed away quickly. It does not appear that hydrogen peroxide has previously been effectively used for such purposes in the form of a foam or spray in the manner described herein, particularly in a manner suitable for commercial application.
  • the system of the present invention is capable of producing rapid detergent action in order to instantly provide voluminous quantities of microbubbles from relatively small initial volumes of formulation.
  • This detergent action greatly facilitates the effectiveness of the formulation as an oral rinse.
  • the system of the present invention can rapidly provide a volume of bubbles from about 2 grams of formulation that is as great or greater than the volume obtained by swirling up to an ounce (e.g., about 25-30 grams) of a product like Plax in the mouth for 30 seconds, as recommended by the manufacturer.
  • Formulations of the present invention having hydrogen peroxide have also been found to be particularly effective antifungal agents. To the best of
  • hydrogen peroxide has not heretofore been approved or applied as an antifungal agent, and particularly not in the form of a foam or spray, or a composition delivered by an aerosol dispenser.
  • the present invention provides a method of delivering a formulation in the form of a organoleptically acceptable foam or spray, the preferred method comprising the steps of: (1) providing a formulation comprising a chemical agent to be delivered and sodium lauryl sulfate as a delivery agent, within an aerosol dispenser, and (2) delivering the formulation in the form of a foam or spray by activation of the dispenser.
  • the invention provides purified sea water compositions suitable for use in preparing formulations described herein. It appears that sea water has not heretofore been prepared in a form suitable for use in commercial cosmetic formulations.
  • the present invention provides a system for delivering a wide variety of chemical agents in the form of an efficacious foam.
  • chemical agents in the form of an efficacious foam.
  • the following words and terms shall have the meanings ascribed to them:
  • system will refer to an aerosol dispenser containing a formulation
  • formulation will refer to a solution, e.g., as a single phase liquid or stable dispersion, which is capable of being delivered from an aerosol dispenser in the form of a foam or spray;
  • chemical agent in turn, will refer to the active agent or other agent to be delivered in the form of a foam
  • “foam”, and inflections thereof, when used as a verb shall refer to the ability of a formulation to form a foam when dispensed from an aerosol dispenser, and when used as a noun shall mean a liquid-film matrix with a mass of gas bubbles in it;
  • “spray”, and inflections thereof, when used as a verb shall refer to the ability of a formulation to form a spray when dispensed from an aerosol dispenser, and when used as a noun shall mean a liquid moving in a mass of dispersed droplets, e.g., a fine jet of liquid discharged from a pressurized container, "delivery agent” shall refer to one or more ingredients in a formulation that functions to cause or facilitate either the foaming or spraying of the formulation when dispensed from an aerosol dispenser; and
  • dental formulation shall refer to any formulation useful in or on the mouth or gums (such as dentifrice, mouthwash, gargle, dental liquid), or other nasopharyngeal application.
  • Preferred foams of the present invention are substantially stable, yet can be readily broken upon agitation.
  • the foam is substantially stable after it is formed, so long as it is not agitated.
  • An example of such a foam is one that can be dispensed into the palm of the hand and there remain for at least 30 seconds, and preferably for on the order of minutes, without collapsing. Once agitated however, for instance by rubbing the palms together, the foam is readily broken and in fact essentially disappears within a second or two.
  • Preferred foams are similar in appearance and consistency to the suds obtained by the agitation of dishwashing liquids, that is, they are comprised of small bubbles.
  • Dispensers suitable for use in the system of the present invention are typically those that are capable of creating and dispensing a formulation in the form of a foam or spray in an aerosol manner through the use of a relatively low boiling liquid propellant such as butane and propane.
  • aerosol will refer herein to the delivery of a foam or spray in a manner that employs a hydrocarbon or other suitable propellant, as further explained herein.
  • Aerosol dispensers are distinct from “propellantless” dispensers, the latter type being narrowly defined as those that avoid the use of a pressurized gas to achieve rapid expansion of a propellant through an emulsion.
  • Propellantless dispensers are those that rely on the use of compressed air, for instance obtained by squeezing a bottle, as opposed to piston-type or spring-loaded dispensers.
  • a system of the present invention further comprises a dispenser, i.e., a container useful for holding one or more propellants, a valve, and an actuator.
  • a dispenser i.e., a container useful for holding one or more propellants, a valve, and an actuator.
  • Suitable aerosol dispensers provide an optimal combination of such properties as ease of use, capacity, inertness, safety and cost.
  • suitable dispensers include those prepared of glass, plastic, metal or a combination of such materials. Glass containers must be carefully selected to provide an optimal level of pressure safety and impact resistance. Plastics may be employed to coat glass containers for improved safety, or to coat metal containers to improve corrosion resistance and enhance formulation stability.
  • the propellant supplies the necessary pressure within an aerosol system to expel the formulation from the container and, in combination with other components, to convert the formulation into the desired foam.
  • Propellants may be broadly classified as liquified or compressed gases having vapor pressures generally exceeding atmospheric.
  • Propellants within this definition include various hydrocarbons, especially fluoro-chloro- derivatives of methane and ethane, low molecular weight hydrocarbons such as the propanes, butanes and pentanes, and compressed gases such as carbon dioxide, nitrogen and nitrous oxide.
  • Preferred propellants suitable for use in the system of the present invention provide an optimal combination of such properties as compatibility and cost.
  • preferred propellants include, but are not limited to, butane, dichlorodifluoromethane, dichlorotetrafluoroethane, isobutane, propane, trichloromonofluoromethane, and mixtures thereof.
  • Suitable propellants are commercially available from a number of sources, for instance, those identified as "Aeropres 46 (A-46)", a mixture of propane and isobutane available from Aeropres Corporation, Shreveport LA.
  • Aeropres 46 A-466
  • the primary function of the valve is to regulate the flow of the formulation and propellant from the container.
  • the characteristics of the delivered foam, including the accuracy and reproducibility of the delivery, should be optimized. Plastic, rubber, aluminum and stainless steel valves are particularly preferred.
  • An actuator is a fitting attached to an aerosol valve stem which, when depressed or moved, opens the valve to permit a foam or spray to issue from the container, and directs the foam or spray containing the formulation to the desired area.
  • the actuator usually indicates the direction in which the formulation is dispensed and protects the hands or fingers from the refrigerant effects of the propellant.
  • Actuators can incorporate an orifice of any suitable size and shape.
  • a system of the present invention comprises a delivery agent, preferably selected from the class of surface active agents known as anionic detergents.
  • Suitable anionic delivery agents include sodium cocomonoglyceride sulfonate, sodium lauryl sarcosinate, sodium dodecyl benzenesulfonate, and miscellaneous other surfactants such as dioctyl sodium sulfosuccinate, sodium lauryl sulfoacetate, sulfolaurate, and the 2-hydroxyalkyl sulfates. See, e.g., "Surfactants in Oral Hygiene Products", pp. 299-347 in Surfactants in Cosmetics.
  • a particularly preferred delivery agent is SLS.
  • SLS is itself classified as an emulsifying, wetting, and/or solubilizing agent.
  • SLS is actually a mixture of sodium alkyl sulfates, primarily sodium lauryl sulfate containing not more than a total of 8% of sodium sulfate and sodium chloride.
  • SLS is a long-chain fatty alcohol sulfate, and commercially available forms of SLS involve a mixture of long-chain saturated alkyl alcohols.
  • Oral grades of SLS are generally made from naturally occurring fats and oils, mostly from coconut fatty acids, or the like.
  • Some products are virtually all dodecyl derivative, while others contain mixtures of dodecyl, tetradecyl, and higher derivatives, depending on the degree of fractionation of the original fatty acids.
  • Such surface active agents including SLS, are preferably present in the formulation at a final concentration of between about 0.05% and about 5% , and more preferably between about 0.1 % and about 1 % , by weight, based on the weight of the chemical agent formulation.
  • Formulations containing less than about 0.5% SLS tend to have poor foaming characteristics, while those containing greater than about 5% SLS tend to impart unpleasant taste or other undesirable characteristics to the formulation.
  • the formulation delivered using a system of the present invention preferably comprises a chemical agent.
  • Suitable chemical agents include any compound, solution or molecule that is desired to be delivered as a foam or spray to the body, including any cavity of the body.
  • Examples of chemical agents that can be delivered to the body in the form of a foam or spray include topical analgesics, anesthetics, antibacterials, antibiotics, antifungal agents, anti- inflammatory agents (such as salicylates and steroids), antineoplastics, antiparasitics, antipruritics, antiviral agents, biologicals, contraceptives, dental preparations, deodorants, enzymes and digestants, germicides, hemorrhoidal preparations, hormones, minerals, vaginal preparations, and the like.
  • the system of the present invention is used for the preparation of foams for the application of abradants, antiacne preparations, antibacterials and/or antifungals, antidermatitis preparations, as well as antiherpes, anti-inflammatory, antiperspiration, antipuritics, antipsoriasis, antiseborrhea, or astringent agents, coal tar, depigmenting agents, detergents, emollients, fungicides, keratolytics, moisturizers, pediculicides, photosensitizers, scabicides, skin bleaches, skin protectants, cleansers, steroids, sulfur and salicylic acid, sun screens, vesicants, wart therapeutic agents, wound dressings, and the like.
  • Particularly preferred is a formulation that contains both hydrogen peroxide (as an anti-infective agent) and glycerin, aloe or other ingredient (as a skin or tissue protectant).
  • hydrogen peroxide as an anti-infective agent
  • glycerin aloe or other ingredient
  • the combination of hydrogen peroxide and glycerin has been used as effective local therapy for the treatment of pharyngitis, laryngitis, thrush, gingival infection and necrotizing ulcerative gingivitis.
  • the combination being non-toxic, has been found to be effective as a wide spectrum antibacterial and, as described herein, as an antifungal agent.
  • the combination When used for treating oral bacterial infections, the combination provides relief from symptoms and serves as an adjunct to systemic therapy. It also relieves pain associated with these conditions, thereby enabling the patient to maintain or resume normal oral intake.
  • the combination cleanses the tissue of debris, soothes irritated tissues and aids in restoring good oral hygiene. Patient acceptance has been good. See, for instance, Williams, J.C; Topical Therapy in Infections of the Mouth and Pharynx, Med Times. 91:332-334 (1963).
  • Glycerin is quite effective in protecting the skin and buccal membranes of the mouth and oral cavity. FDA monographs, for instance, define glycerin as an "Active Skin Protectant" for use on skin, lips, and the oral cavity.
  • hydrogen peroxide for instance at a concentration of between about 1 % and about 3% by weight, based on the weight of the formulation, is useful as a weak antibacterial agent, a wound cleanser (including suppurating ulcers and local infections), and a deodorant.
  • hydrogen peroxide is useful for the removal of debris (by virtue of its effervescence) and in the treatment of pharyngitis and Vincent's stomatitis.
  • Hydrogen peroxide is also useful as a disinfectant for cuts, burns, and the like, as well as for surfaces such as operating tables and instruments.
  • Foams of the present invention provide a convenient, stable form of hydrogen peroxide, capable of providing a time release phenomenon upon breakdown of the foam structure.
  • Another preferred chemical agent is natural sea water.
  • natural sea water can be stabilized to allow it to be formulated into a product for topical application, e.g. , incorporated as a "chemical agent" in a formulation of the present invention.
  • natural sea water can be collected from any suitable source, preferably a well that provides a constant and convenient source.
  • the water is then aerated and passed sequentially through a sequential series of pre-filters, e.g., gravel, sand, and finally activated carbon.
  • the water is finally passed through a suitable sub-micron (preferably 0.2 micron or less) filter.
  • a suitable sub-micron preferably 0.2 micron or less
  • one or more preservatives are added to the sub- micron filtered sea water in order to further lengthen its storage stability and preserve its utility.
  • suitable preservatives will be well within the skill of those in the cosmetics arts, given the present disclosure.
  • Preferred preservatives for sea water include those of the paraben series, and particularly methyl paraben and/or propyl paraben, which can be added to achieve final concentrations in the range of about 0.05% to about 0.5%, and preferably between about 0.1% and about 0.3%.
  • Phenonip preservative is described as a mixture of p-hydroxybenzoate esters
  • sea water When prepared and used in the manner described herein, sea water provides a number of unexpected and desirable properties.
  • a chemical agent in a delivery formulation of the present invention it is preferably used at a final concentration of between about 1 % and about 10% by weight, and preferably between about 3% and about 5% by weight of the concentrate used to prepare the final formulation. It can serve, for instance, as a replacement for added salts in a formulation.
  • purified, stable sea water provides a useful thickening effect on foams. Those skilled in the art will appreciate the manner in which this effect can be controlled and used to one's advantage.
  • Systems of the present invention can be prepared in any suitable manner, using techniques and equipment within the skill of those in the art. See, e.g., D. Klein, "Toothpastes", Chapter 14, pp. 511-532 in Pharmaceutical Dosage Forms - Disperse Systems. Marcel Dekker, Inc. 1989, the disclosure of which is incorporated herein by reference.
  • a preferred system as identified above can be prepared as follows: (1) the desired ingredients are selected, based upon their known properties;
  • Formulations can be provided in either of two forms, either as a homogeneous prefabricated formulation that is already contained within an aerosol dispenser, or as a formulation that can optionally be modified (e.g., diluted) for use and added to an aerosol dispenser.
  • the final system can be prepared by any suitable means, including by either of two common approaches.
  • the formulation generally cooled to below 0 degrees C
  • the refrigerated propellant are measured into open containers (usually chilled).
  • the valve-actuator assembly is then crimped onto the container to form a pressure-tight seal.
  • sufficient volatilization of propellant occurs to displace air from the container.
  • the "pressure fill” approach the formulation is placed in the container and either the propellant is forced under pressure through the valve orifice after the valve is sealed, or the propellant is allowed to flow under the valve cap and then the valve assembly is sealed ("under the cap” filling). In both of these "pressure fill” cases, provisions must be made for the evacuation of air by means of vacuum or displacement with a small amount of propellant.
  • GRAS general recognized as safe
  • the dispenser can be filled and packaged using techniques within the skill of those in the art. For instance, a typical filling ratio is 60% product to 40% compressed air, according to FDA regulations. Special filling heads are used to fill and pressurize the system. Examples of suitable chemical agents (and their intended use) include the following (percentages are provided on a weight basis, based on the weight of the final formulation):
  • oils such as perfume oils, particularly in formulations in which the sodium lauryl sulfate serves the additional purpose of holding such oils in solution or stable suspension;
  • - aloe vera e.g., between about 0.1 and 10 g/100 ml formulation, and preferably between about 0.3 and 1 g/100 ml
  • - sodium chloride e.g., at physiological concentrations, generally about
  • Suitable solvents for use in preparing a chemical agent solution of the present invention are those that provide an optimal combination of such properties as: the ability to solubilize the desired chemical agent; compatibility with the system; and suitability for topical use.
  • An example of a particularly preferred solvent is purified water.
  • other adjuvants such as fluoride, buffering agents, stabilizers and preservatives, foaming agents, antioxidants, flavorings, colors, viscosity modifiers, therapeutic additives, humectants, and binding agents can be used as well.
  • the system of the present invention is stable in storage, e.g., it can be stored one or more years without noticeable effect on its desired properties. It is preferably stored in a closed container and at room temperature.
  • the system of the present invention provides a unique and desirable combination of such properties as ease of use, aesthetic appearance, formulation stability, uniform distribution of active ingredients, ease of spreading and penetration, and release and availability of medication on contact with dermatomucosal surfaces.
  • the system is well-suited for the delivery of formulations that have not previously been delivered in the form of foams, for instance, for the delivery of hydrogen peroxide to the oral cavity.
  • foams When used for cleansing minor wounds or irritations of the mouth or gums, a small amount of the foam or spray is dispensed and applied to the affected area. It is allowed to remain in place for about 1 minute, and then expectorated.
  • the foam or spray can be used up to 4 times daily (after meals and at bedtime) or as directed by a dentist of physician. Children younger than 12 years of age should be supervised by an adult in the use of the foam, and for children younger than 2 years of age, a dentist or physician should be consulted prior to use.
  • the system is particularly well suited for the delivery of formulations that are not generally delivered in the form of foams, including for the delivery of dentifrices, including dental liquids, mouthwashes, oral lavages and gargles that contain hydrogen peroxide.
  • formulations that are not generally delivered in the form of foams, including for the delivery of dentifrices, including dental liquids, mouthwashes, oral lavages and gargles that contain hydrogen peroxide.
  • the sodium lauryl sulfate was used as a delivery agent and hydrogen peroxide as a cleansing or antiseptic agent.
  • the ingredients were mixed in a variety of relative concentrations and a dispenser was filled with the formulation.
  • the system was used by actuating the valve in order to generate a foam from the nozzle. At optimal concentrations of ingredients a foam rapidly appeared in direct response to the pressure applied to the valve.
  • the foam was a stable one, in that it remains on the skin with little visible shrinkage, yet it easily collapsed when rubbed between the fingers or palms.
  • the system is useful for a wide variety of applications, and particularly for applications in which the use of hydrogen peroxide is indicated and where the use of liquid hydrogen peroxide is inconvenient or ineffective.
  • the concentrate was prepared having the ingredients provided below:
  • sea water was filtered and preserved with (0.2%) methyl paraben in the manner described above, and used with deionized water in the ratio of 1 part sea water to 14 parts deionized water in order to provide an isosmotic formulation.
  • sea water and deionized water can be used at any suitable ratio, and preferably between the ratio of about 1 part sea water to 2 parts deionized water, and the ratio of about 1 part sea water to 30 parts deionized water.
  • the sodium lauryl sulfate was used as a delivery agent and the natural sea water was used for its purported healing effects.
  • the ingredients were mixed in a variety of relative concentrations and dispensers were filled with the formulations using conventional techniques. The system was used by actuating the valve in order to generate a foam from the nozzle. At optimal concentrations of ingredients a foam rapidly appeared in direct response to the pressure applied to the valve. The foam was a stable one in that it with little visible shrinkage, yet it when rubbed between the fingers or palms.
  • the system is useful for a wide variety of applications, and particularly for applications in which the use of sea water is indicated and where the use of fresh sea water is inconvenient or ineffective.
  • Propellant A-46 25 g The concentrate was prepared in the order, and having the ingredients, provided below:
  • Glycerin skin conditioning agent, humectant
  • TEA lauryl sulfate (40.0%) (surfactant, emulsifying 1.8 agent) 3.
  • Mineral oil (skin conditioning agent, emollient) 0.9
  • Shea butter biological additive, skin conditioning 0.9 agent
  • Polysorbate-60 polyoxyethylene sorbitan 0.3 monostearate (Tween 60) - surfactant, emulsifying agent
  • the ingredients were mixed in a variety of relative concentrations and a 2.5 ounce can dispenser was filled with the formulations.
  • the system was used by actuating the valve in order to generate a foam from the nozzle. At optimal concentrations of ingredients a foam rapidly appeared in direct response to the pressure applied to the container.
  • the foam is formulated to be useful as a skin covering, to be rubbed over the entire hands to form a protective film - not unlike the protection afforded by a glove.
  • Concentrate IV was prepared having the same ingredients and concentrations as set forth above with respect to Concentrate HI, although omitting the sunprotecting agents and using instead a total volume of 70% (rather than 62%) deionized water. Concentrate IV was used to fill 4.5 ounce can dispensers.
  • the foamed formulation could be used by spreading it over the hands to provide a protective "glove-like" covering.

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  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
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Abstract

L'invention se rapporte à un système d'administration d'un agent chimique se présentant sous la forme d'une mousse, qui, selon un mode de réalisation préféré, consiste à utiliser un distributeur aérosol afin d'administrer une formulation contenant à la fois un agent anionique actif en surface tel que le sulfate laurique de sodium comme agent d'administration, et un agent chimique tel que le peroxyde d'hydrogène comme agent chimique désinfectant ou de l'eau de mer naturelle.
PCT/US1996/015596 1995-09-22 1996-09-20 Formulations a usage local et systemes d'administration WO1997010802A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP96936055A EP0862407A4 (fr) 1995-09-22 1996-09-20 Formulations a usage local et systemes d'administration
US09/043,433 US7060253B1 (en) 1996-09-20 1996-09-20 Topical formulations and delivery systems

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US416795P 1995-09-22 1995-09-22
US60/004,167 1995-09-22

Publications (1)

Publication Number Publication Date
WO1997010802A1 true WO1997010802A1 (fr) 1997-03-27

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1996/015596 WO1997010802A1 (fr) 1995-09-22 1996-09-20 Formulations a usage local et systemes d'administration

Country Status (3)

Country Link
EP (1) EP0862407A4 (fr)
CA (1) CA2232677A1 (fr)
WO (1) WO1997010802A1 (fr)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999017739A1 (fr) * 1997-10-02 1999-04-15 Omc Holdings, Llc Compositions aerosol comprenant un onguent
EP1074245A2 (fr) * 1999-08-06 2001-02-07 Sam Schwartz Composition avec des sels minéraux pour un traitement thérapeutique
GB2380231A (en) * 2001-09-26 2003-04-02 Reckitt Benckiser Nv Corrosion inhibitors for tin plated aerosol canisters
FR2838643A1 (fr) * 2002-04-23 2003-10-24 Farmaceutici S R L Composition d'une pate dentifrice blanchissante non abrasive
EP1435229A1 (fr) * 2002-12-30 2004-07-07 Farmaceutici S.R.L. Composition dermatologique pour des produits dermatologiques à usage topique et produits dermatologiques ainsi préparés
US20110104079A1 (en) * 2005-12-28 2011-05-05 Marcia Snyder Foamable alcoholic composition
US20140335026A1 (en) * 2013-05-07 2014-11-13 Michael Florman Method of Cleaning an Oral Appliance

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3976223A (en) * 1972-02-02 1976-08-24 Carter-Wallace, Inc. Aerosol package
US5084268A (en) * 1991-06-17 1992-01-28 Dental Concepts, Inc. Tooth whitening dentifrice
US5104644A (en) * 1990-02-07 1992-04-14 7-L Corporation Mouthrinse composition

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR1520945A (fr) * 1967-04-25 1968-04-12 Curtis Helene Ind Inc Base pour émulsion contenant de l'eau oxygénée

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3976223A (en) * 1972-02-02 1976-08-24 Carter-Wallace, Inc. Aerosol package
US5104644A (en) * 1990-02-07 1992-04-14 7-L Corporation Mouthrinse composition
US5084268A (en) * 1991-06-17 1992-01-28 Dental Concepts, Inc. Tooth whitening dentifrice

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of EP0862407A4 *

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999017739A1 (fr) * 1997-10-02 1999-04-15 Omc Holdings, Llc Compositions aerosol comprenant un onguent
EP1074245A2 (fr) * 1999-08-06 2001-02-07 Sam Schwartz Composition avec des sels minéraux pour un traitement thérapeutique
EP1074245A3 (fr) * 1999-08-06 2001-05-30 Sam Schwartz Composition avec des sels minéraux pour un traitement thérapeutique
GB2380231A (en) * 2001-09-26 2003-04-02 Reckitt Benckiser Nv Corrosion inhibitors for tin plated aerosol canisters
FR2838643A1 (fr) * 2002-04-23 2003-10-24 Farmaceutici S R L Composition d'une pate dentifrice blanchissante non abrasive
EP1435229A1 (fr) * 2002-12-30 2004-07-07 Farmaceutici S.R.L. Composition dermatologique pour des produits dermatologiques à usage topique et produits dermatologiques ainsi préparés
US20110104079A1 (en) * 2005-12-28 2011-05-05 Marcia Snyder Foamable alcoholic composition
US20140335026A1 (en) * 2013-05-07 2014-11-13 Michael Florman Method of Cleaning an Oral Appliance
US9561161B2 (en) * 2013-05-07 2017-02-07 Michael Florman Method of cleaning an oral appliance
US9901522B2 (en) 2013-05-07 2018-02-27 Eversmile Method of cleaning an oral appliance

Also Published As

Publication number Publication date
CA2232677A1 (fr) 1997-03-27
EP0862407A1 (fr) 1998-09-09
EP0862407A4 (fr) 1999-03-03

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