A quick and easy system and method for delivering a composition to a nasal membrane is presented. The applicator assembly includes a sleeve member which encases a swab having a portion that contacts a gelled composition. The sleeve member is manually severed to expose the applicator and the composition. The gelled composition contained on the applicator is applied to the nasal membrane.

Description of the Invention

SUMMARY OF THE INVENTION

The present invention is generally directed to a method and system for applying a composition to a nasal membrane.

In accordance with one embodiment of the present invention, the system includes an applicator and a composition with a viscosity sufficient to maintain contact with the nasal membrane for a suitable period of time while still allowing efficient migration of a substance across the composition for delivery of the substance to the nasal membrane. In accordance with various aspects of this embodiment, the applicator includes a swab connected to a handle or stick. In accordance with various other aspects of the invention, the composition includes one or more active ingredients such as moisturizers, decongestants, and homeopathic agents. In accordance with yet additional aspects of this embodiment, the system includes a container for enclosing the applicator and the composition.

In accordance with another embodiment of the present invention, the system includes an applicator and a composition with a viscosity greater than about 1500 centipoise. In accordance with various aspects of this embodiment, the applicator includes a swab connected to a handle or stick. In accordance with various other aspects of the invention, the composition includes one or more active ingredients such as moisturizers, decongestants, and homeopathic agents. In accordance with yet additional aspects of this embodiment, the system includes a container for enclosing the applicator and the composition.

In accordance with yet another embodiment of the present invention, the system includes an applicator and a gelled-matrix composition. In accordance with various aspects of this embodiment, the applicator includes a swab connected to a handle or stick. In accordance with various other aspects of the invention, the composition includes one or more active ingredients such as moisturizers, decongestants, and homeopathic agents. In accordance with yet additional aspects of this embodiment, the system includes a container for enclosing the applicator and the composition.

The present invention provides a convenient method and system for applying a composition to a nasal membrane. These and other advantages of the various compositions, methods and systems according to various aspects of the present invention will be apparent to those skilled in the art upon reading and understanding the detailed description below.

DETAILED DESCRIPTION

The following descriptions are of exemplary embodiments of the invention only, and are not intended to limit the scope, applicability or configuration of the invention in any way. Rather, the following description is intended to provide a convenient illustration for implementing various embodiments of the invention. As will become apparent, various changes may be made in the arrangement of elements and content of the compositions described herein without departing from the spirit and scope of the invention. For example, though not specifically described, variations in the shape and orientation of the container in the applicator system should be understood to fall within the scope of the present invention. Further, variations in the contents of the composition should also be understood to fall within the scope of the present invention as defined in the claims.

FIGS. 1 and 2 (see Original Patent) illustrate an exemplary system 10 in accordance with one embodiment of the present invention. System 10 includes an applicator, e.g., a swab 12, a composition 13, and a container 14. As explained in more detail below, system 10 is generally configured to allow quick access to a sealed composition and to facilitate application of composition 13 to a nasal membrane. Generally, systems in accordance with the present invention include an applicator and a composition, which may be sealed to shield the applicator and/or composition from an environment prior to application of the composition.

Applicator 12 is generally configured to assist in removal of composition 13 from container 14 and to aid application of composition 13 to a portion of a nasal membrane. In the illustrated embodiment, applicator or swab 12 includes a straight stick or handle portion 16 and a portion 18 at one end of stick 16. Portion 18 may comprise any suitable material in any suitable shape. For example, portion 18 may include absorbent material such as cotton in a generally bud-type shape, a bud-type shape formed from a sponge or similar material, or other configurations of similar materials.

Container 14 provides a sealed environment for applicator 12 and composition 13. Container 14 is desirably easy to sever such that a user can easily access applicator 12 and composition 13.

Exemplary container 14 is a hollow cylinder which varies in diameter along its length and is preferably comprised of a plastic. Container 14 includes a portion having a small diameter cylinder 20 which can be used as a handle, a portion 22 having a larger cross-section (e.g., diameter) which is used to retain portion 18 of swab 12, and a transition portion 24 between cylinder 20 and portion 22. Container 14 may also include an end 26 that is configured to engage and secure swab 12 in place within container 14. Portion 18 of swab 12 resides in larger portion 22 and contacts a composition in accordance with the present invention which is later described.

As previously stated, it will be understood by those skilled in the art that container 14 may comprise a variety of configurations and shapes. Container 14 may also be comprised of various materials that are capable of being easily and/or manually severed upon application of force. Exemplary materials suitable for container 14 include soft metals, foils, and a variety of plastic materials. It will also be understood by those skilled in the art that portion 22 of sleeve member 14 may be filled with a composition in accordance with the present invention to ensure that an adequate amount of composition is retained on applicator 18 prior to application.

Various exemplary compositions suitable for system 10 will now be described. Although specific compositions are provided below, the invention as set forth herein is not so limited.

In accordance with one embodiment of the invention, composition 13 has a viscosity greater than about 1,500 centipoise. In accordance with various aspects of this embodiment, the viscosity of composition 13 is between about 1,500 to about 40,000 centipoise, preferably about 2,500 to about 10,000 centipoise, and more preferably about 4,000 to about 6,000 centipoise. As described in more detail below, compositions in accordance with this and other embodiments may include one or more materials that alter a the viscosity of the material, one or more active ingredients, and other, additional components.

In accordance with one aspect of this embodiment, the composition has a viscosity in the range of about 1500-2500 centipoise. An exemplary composition in accordance with this aspect has a viscosity in the range of about 1700 to about 2300 centipoise. Another composition in accordance with this aspect has a viscosity in the range of about 1800 to about 2200 centipoise, and yet another composition has a viscosity in the range of about 1900 to about 2100 centipoise. In accordance with still further aspects of this embodiment, the composition has a viscosity in the range of about 1750 to about 2450 centipoise, and in accordance with yet a further aspect, the composition has a viscosity in the range of about 1500 to about 2100 centipoise, and in accordance with yet a further aspect, the composition has a viscosity of about 1800 to about 2500 centipoise.

One exemplary composition in accordance with this aspect of the invention includes an active ingredient. Exemplary active ingredients include homeopathic materials, naturopathic materials, zinc, decongestants, moisturizers, and the like. The composition may also include one or more thickening agents. Suitable thickening agents (e.g., a substance which increases the viscosity of the composition, causes the composition to gel or coagulate, or the like), include materials such as food-grade or pharmaceutical grade thickeners, including, for example, glycerin, carrageenan, sugar, guar gum, methylcellulose, hydroxyethyl cellulose, aloe vera, and the like. The composition may also include other gels, gelling agents, antiseptics, preservatives, permeation enhancers, sequestering agents, buffers, emulsifiers, and any other suitable substance.

Compositions in accordance with another aspect of this embodiment of the invention have a viscosity in the range of about 2500 to about 6000 centipoise. An exemplary composition in accordance with this aspect of this exemplary embodiment has a viscosity in the range of about 5000 to about 6000 centipoise. Another composition in accordance with this aspect has a viscosity in the range of about 4000 to about 6000 centipoise, and yet an additional composition has a viscosity in the range of about 4000 to about 5000 centipoise. In accordance with still further aspects of this embodiment, the composition has a viscosity in the range of about 4500 to about 6000 centipoise, and in accordance with yet a further aspect, the composition has a viscosity in the range of about 2500 to about 4000 centipoise, and in accordance with yet a further aspect, the composition has a viscosity of about 3000 to about 5500 centipoise.

One exemplary composition in accordance with this aspect of the invention includes an active ingredient, such as those described herein The composition may also include one or more thickening agents, as described above. The composition may further include other gels, gelling agents, antiseptics, preservatives, permeation enhancers, sequestering agents, buffers, emulsifiers, and any other suitable substance, as described in more detail below.

Compositions in accordance with yet a further aspect of this embodiment of the invention have a viscosity in the range of about 5000 to about 40,000 centipoise. An exemplary composition in accordance with this aspect of this exemplary embodiment has a viscosity in the range of about 6000 to about 40,000 centipoise. Another composition in accordance with this aspect has a viscosity in the range of about 5000 to about 8000 centipoise, and yet additional compositions has a viscosity in the range of about 5500 to about 10,000 centipoise. In accordance with still further aspects of this embodiment, the composition has a viscosity in the range of about 6000 to about 8000 centipoise, and in accordance with yet a further aspect, the composition has a viscosity in the range of about 6000 to about 10,000 centipoise, and in accordance with yet a further aspect, the composition has a viscosity of about 6000 to about 20,000 centipoise.

Similar to the specific exemplary compositions provided above, one exemplary composition in accordance with this aspect of the invention includes an active ingredient, such as those described herein The composition may also include one or more thickening agents, as described above, other gels, gelling agents, antiseptics, preservatives, permeation enhancers, sequestering agents, buffers, emulsifiers, and any other suitable substance, as described in more detail below.

Viscosity measurements recited herein were obtained using the Brookfield Syncho-Lectric Viscometer for the measurement of the apparent viscosity of Newtonian and Non-Newtonian materials at low shear rates at given rotation speeds according to ASTM D1824087. See also ASTM D1084-88. As described further herein below, viscosity measurements may be made prior to or after administration of the composition, such as after application from a nasal applicator system as described in accordance with the present invention. In accordance with various embodiments of the invention, the composition may thicken where the composition is admixed with other components.

In accordance with one embodiment of the invention, composition 13 is a gelled-matrix composition. In accordance with various aspects of this embodiment of the invention, the gelled-matrix includes at least one fluid component and one thickener component. Exemplary fluid components include any suitable fluid or liquid, such as, for example, water, oil, alcohol, etc. Likewise, the thickener component may include any acceptable thickener (e.g., a substance which increases the viscosity of the composition, causes the composition to gel or coagulate, or the like), such as food-grade or pharmaceutical grade thickeners, including, for example, glycerin, carrageenan, sugar, guar gum, methylcellulose, hydroxyethyl cellulose, aloe vera, and the like. In various other embodiments, the gel matrix may also include other gels, gelling agents, antiseptics, preservatives, permeation enhancers, sequestering agents, buffers, emulsifiers, and any other suitable substance. Further, as described below, the gel matrix may also include an active substance which is maintained in direct contact with the nasal membrane.

In accordance with various aspects of this embodiment, composition 13 includes from about 75% to about 99.999% or 90 to about 99.1 by weight of at least one carrier, and from about 0.000001% to about 10.0% by weight of an a effective amount of an active substance, and more preferably from about 90% to about 99.999% by weight of at least one carrier, and from about 0.001 to about 5% of an effective amount of an active substance. By way of one particular example, the carrier comprises a mixture of purified water and glycerin, for example, about 90.0% to 99.0% by weight purified (de-ionized) water, and about 0.05 to 5.0% by weight of glycerin.

It should be appreciated that the "gelled matrix compositions" of the present invention may have appreciable viscosity. The previously detailed viscosity limits are not necessarily applicable to or limiting as to the gelled matrix composition or other embodiments of the present invention.

In accordance with yet another embodiment of the invention, composition 13 includes a material configured to remain in contact with a nasal membrane for an extended period of time after the material is applied to the membrane. In accordance with one aspect of this embodiment, composition 13 is also configured to allow diffusion of a substance through a portion of the composition.

In accordance with this embodiment of the invention, after application of composition 13 to the nasal membrane, an interface layer is thought to form between the gelled composition and the nasal membrane. As the active substance is delivered to the nasal membrane, the concentration of active substance at the interface layer becomes depleted. Due to the unique properties of the gel, additional amounts of the active substance are permitted to travel down the resulting concentration gradient, from higher concentration to lower concentration, to replenish the concentration of active substance at the interface layer, thereby further driving additional amounts of active substance into contact with the nasal membrane.

When the composition 13 is so configured, it is believed that the active substance is permitted to diffuse through the composition to the nasal epithelial membrane or mucous of the epithelial membrane. This facilitates the availability of a regular supply of active substance, because diffusion within the composition continues to supply the active substance without requiring that the portion of the composition adjacent to the nasal epithelial membrane (or mucous on the membrane) dissolve or dissipate and expose a fresh portion of the composition containing the active substance.

In accordance with the various embodiments of the present invention, such as those described above, composition 13 may include an active substance or ingredient. As used herein, an active substance includes any of one or more substances that produces or promotes a beneficial therapeutic, physiological, homeopathic and/or pharmalogical effect on the body. Such beneficial effects may be brought upon any animal or human patient, and various systems associated therewith, including the immune system, respiratory system, circulatory system, nervous system, digestive system, urinary system, reproductive system, endocrine system, muscular system, skeletal system, and the like, as well as any organs, tissues, membranes, cells, and subcellular components associated therewith.

As will be appreciated by those skilled in the art, beneficial effects include assisting the more efficient functioning of the various systems described above, such as, for example, helping the body fight sickness and disease, helping the body to heal, etc. Exemplary active substances include any element, composition or material producing a beneficial effect, including vitamins, minerals, nucleic acids, amino acids, peptides, polypeptides, proteins, genes, mutagens, antiviral agents, antibacterial agents, anti-inflammatory agents, decongestants, histamines, anti-histamines, anti-allergens, allergy-relief substances, homeopathic substances, naturopathic substances, pharmaceutical substances, and the like.

In accordance with the various embodiments of the invention, composition 13 includes zinc. Zinc may act as a decongestant and/or provide other therapeutic and/or beneficial therapy. It is believed that zinc enhances discharge of mucous and inhibits the generation of new mucous. When a composition comprising zinc is applied to the nasal cavity, zinc ions diffuse from the composition into the mucous or mucous membrane in the nasal cavity. It is believed that the zinc concentration in the mucous or mucous membrane creates a barrier which inhibits viral infection of the nasal epithelial membrane. In accordance with at least one embodiment, as described above, as ionic zinc is absorbed from the gel into the mucous membrane and other nasal epithelial cells, the composition permits new zinc to diffuse into the nasal membrane. In this case, the composition has micelle cell-like properties which facilitate the diffusion of zinc, and other active substances, through the gel matrix. The homeopathic concentration of zinc ions in the zinc gel of the invention is about 4 millimolar (mM) to about 60 millimolar, preferably about 20 mM to about 44 mM or about 15 mM to about 40 mM. Concentrations of zinc in excess of 44 mM are generally not preferred unless an antioxidant or other component is included in the gel composition to protect the nasal epithelial membrane from abnormally high concentrations of zinc. Compositions in accordance with the present invention may also include about 0.01 to about 5 weight percent, 0.01 to about 0.10, or about 0.9 to about 2.0 weight percent zinc gluconate.

In accordance with various aspects of the invention, the composition used in the applicator system of the present invention may be formulated for reducing congestion. In this aspect, the active substance preferably comprises a decongestant--e.g., substances that promote shrinkage of the mucous membrane which makes the breathing process easier, in addition to facilitating drainage of the sinus cavities, substances that promote drying of nasal mucous, discharge of nasal mucous, and the prevention of formation of new nasal mucous. For example, decongestants may include those selected from a group comprising naphazoline hydrochloride, ephedrine, phenylephrine hydrochloride, oxymetazoline hydrochloride (HCL), xylometaxoline hydrochloride and mixtures thereof. Additionally, many aromatic compounds such as those composed primarily of natural oils or extracts therefrom may be decongestants as well such compounds as camphor, eucalyptus oil, menthol, azulen and mixtures thereof. In accordance with exemplary compositions, the decongestant(s) is in a concentration from about 0.000001% to about 0.10% or about 0.01 to about 0.10 by weight.

In accordance with one exemplary embodiment, the decongestant comprises at least oxymetazoline hydrochloride (HCL). Preferably this active substance is present at concentrations from about 0.045% to about 0.055% by weight, and more preferably at about 0.05% by weight.

In accordance with the embodiments of the invention described herein, composition 13 may include glycerin. Glycerin has many properties that facilitate nasal delivery of drugs and other active substances. For example, glycerin supports certain active substances in an ionic state, and permits rapid diffusion of various active substances across the gel matrix. Glycerin also has an ability to permeate nasal mucous and the nasal epithelial membrane, while carrying with it the active substance for appropriate delivery.

Composition 13 may also include thickeners, permeation enhancers, antiseptics, preservatives, buffers, emulsifiers, and any other suitable substance other than the active substance. Composition 13 may also include moisturizers such as aloe vera, glycerin, and the like.

The thickener component or components may be utilized to form colloidal solutions (i.e., suspensions) in order to increase the viscosity of the carrier in the nasal gel composition. Suitable thickeners may include any acceptable thickener, such as food-grade or pharmaceutical-grade thickeners, including, for example, glycerin, carrageenan, sugar, guar gum, methylcellulose, hydroxyethyl cellulose, carbohydrate thickness, aloe barbadensis gel (Aloe Vera), and the like, as well as other gels, gelling agents, antiseptics, preservatives, permeation enhancers, sequestering agents, buffers, emulsifiers, and the like. An exemplary concentration for the thickener is about 0.000001% to about 5.0% by weight, preferably about 0.01 to about 3% by weight, and more preferably about 0.5 to about 25 by weight of the composition.

In accordance with exemplary embodiments of the invention, the composition includes from about 0.05% to about 2.5% of by weight of hydroxy cellulose, and preferably about 1.25% by weight of hydroxyl cellulose. In accordance with further embodiments, the thickener also compromises from about 0.00001% to about 1.0% by weight of aloe barbadensis gel (200:1 concentrate), and preferably about 0.001% by weight. Addition of aloe barbadensis gel may be preferred where practitioners seek to utilize its soothing properties in a composition. Alternatively, however, aloe may be provided in a suitable delivery formulation that does not significantly increase viscosity, such as, for example in suitable granulated and/or powdered forms.

The composition may also include permeation enhancers, which are believed to function by enlarging or loosening tight junctions between cells in the nasal membrane, thereby facilitating passage of the active substance therethrough. Permeation enhancers include liposomes, sequestering agents, ascorbic acid (Vitamin C), glycerol, chitosan, and lysophosphotidylcholin, or any other substance that provides a similar function or result. By way of example, the permeation enhancer may include a sequestering agent, such as EDTA. EDTA is thought to chelate calcium. When applied to the nasal membrane, it is believed to remove calcium from the cell junctions, thereby loosening the junctions to facilitate passage of an active substance therethrough.

Permeation enhancers may be present in any effective amount, with preferable concentrations ranging from about 0.00001% to about 5.0% by weight. In an exemplary composition, the permeation enhancer includes disodium EDTA, at a concentration of about 0.0001% to about 1.0% by weight, and preferably at about 0.10% by weight.

In accordance with another aspect of the invention, a preservative may be added to the composition to facilitate stability of the various ingredients. Any suitable preservative may be used in accordance with the present invention. Exemplary preservatives include a 50% solution of benzalkonium chloride, admixed into the composition at a concentration of about 0% to about 0.1% by weight, about 0.001 to 0.06% by weight, or 0.03% to about 0.06% by weight. Benzalkonium chloride may be preferred due to its recognized properties as an antiseptic. In a further embodiment, the preservative also comprises an alcohol such as benzyl alcohol, at a concentration of about 0 to about 2% by weight, about 0.0001% to about 1.0% by weight, or about 0.1 to about 0.3% by weight. The preservative may also comprise from about 0.001% to about 1.0% by weight or about 0.10% by weight disodium EDTA. It is believed disodium EDTA facilitates stability by combining with metals (chelating) and further by preventing various oxidative processes, as well understood by skilled practitioners in the art.

An emulsion agent, or emulsifier, may also be added to the composition in accordance with the present invention. The emulsifier may be selected from a group containing hydrophobic and hydrophilic substituents, such as glycerolpolyethylene glycol ricinoleate, fatty acid esters of polyethyleneglycol, ethoxylated glycerol, polyethylene glycol, and mixtures thereof. By way of particular example, the composition may emulsifier include an emulsion agent such as hydroxylated lecithin, present at a concentration from about 0 to 2% by weight, about 0.00001% to about 1.0% by weight, or about 0.001% to about 0.002 by weight.

The composition may also include at least one buffer. Any suitable buffer may be used in accordance with the present invention. In an exemplary embodiment, the composition includes from about 0 to about 4 weight percent buffer such as disodium phosphate (heptahydrate), about 0.0001% to about 3.0% by weight disodium phosphate, or about 1 to 2% by weight of disodium phosphate, and from about 0 to about 4%, 0.0001% to about 3.0%, or 1 to 2 percent by weight of monosodium phosphate (monohydrate).
 

Claim 1 of 39 Claims

1. A system for delivering a composition to a nasal membrane, the system comprising: an applicator assembly comprising a handle portion, an applicator portion attached at one end of the handle portion, and a container, wherein the container comprises a first portion for encasing the handle portion and a second portion for encasing the applicator portion; and a gelled-matrix composition comprising ionic zinc enclosed within the container and adjacent the applicator.

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