DESC:
FIELD OF INVENTION
The present invention provides a topical pharmaceutical composition, a method for treating dermatological conditions. Specifically, the invention relates to a novel approach of applying the topical pharmaceutical composition to patients in need thereof.

BACKGROUND
Topical dermatological agents or pharmaceutical active agents have been employed for decades to treat or otherwise alleviate the symptoms of a variety of dermatological conditions not limited to bacterial infection, viral infection, fungal infection, auto-immune response, allergenic response, idiopathic, and the like.

Topical administration is often preferred over oral administration of drugs to treat dermatological problems because substantially less drug enters the bloodstream and systemic side effects are eliminated or significantly reduced.

Various topical drug delivery systems are known in the art that generally include cream, ointment, gel, solution, lotion, spray, or transdermal patches etc.

One problem that arises with the use of many of these topical drug delivery systems is that they may require application over an extended period to be effective in treating a particular disorder, and such extended treatment periods may be inconvenient and disruptive for patients.

Further, patient compliance is also hampered greatly due to the greasy and sticky nature of topical formulations. Moreover, the fluidity of some topical formulations like lotions and ointments often make the application difficult.

In addition to application difficulty, they also do not remain on the application site for longer periods due to easy rub-off by clothes or wash-off by water or by other means and thereby causing the medicament to be only transiently absorbed through patient’s skin. This could result in dose fluctuations that under or over-dose a patient and raise concerns about dose integrity.

Due to low or varied dosing, rub-off or wash-off effect of applied drug, shorter contact time of drug at the affected skin site, the drug products do not show sufficient therapeutic efficacy that would have been otherwise seen in the absence of the said problems.

To overcome such problems and to maintain the drug at the site of application for longer period, dermatologists prefer skin occlusion in the form of dressings over the topically administrated dermatological or pharmaceutical active agents.

The occlusive agents in the form of dressings may not be suitable for many patients as this method is messy, uncomfortable, and inconvenient. Additionally, it could lead to irritation and itching in the infected area, making it intolerable to the patient.

Although a variety of protocols have been developed to increase the efficiency and/or effectiveness of a topical formulation, such protocols have met with limited success.

Hence, in selecting a topical drug delivery system it is essential that the delivery system is resistant to accidental removal and remains on the skin for an extended period with spreadability and patient compliance.

Therefore, there is still a need in the development of new techniques for topically administering pharmaceutical active agents or dermatological agents to patients, Particularly, development of methods that are easy to use, cost effective and efficient in administering the dermatological agent to patients.

OBJECTIVE OF INVENTION
It is an objective of the invention to provide an occlusive film-forming composition to administer topically on skin surface in the form of a spray for effectively treating dermatological conditions.

Another objective of the invention is to provide an occlusive film-forming composition comprising a film-forming agent or film formers, which is sprayed over the skin to form thin transparent occlusive film over the topically administer pharmaceutical composition.

Another objective of the present invention is to facilitate an occlusive therapy in the form of a thin transparent layering system (TTLS) which adheres to the skin surface and forms a transparent film over the topically administered pharmaceutical composition to minimize loss of water from skin surface, thereby increasing skin hydration and contact time of pharmaceutical composition over the skin.

Another objective of the present invention is to provide an occlusive film-forming composition comprising a film forming agent or film formers that can form a stable, non-irritating, non-sticky, with a desired tensile strength.

Another objective of the present invention is to provide a sprayable film-forming composition comprising of at least one film forming agent, one or more solvent, one or more emollient and optionally one or more plasticizers.

Another objective of the present invention is to provide a sprayable film-forming composition in a spray apparatus, wherein the spray apparatus comprises pump or aerosol dispenser, preferably pump dispenser; wherein the spray apparatus is propellant free.

Another objective of the present invention is to provide a sprayable film-forming composition in a spray apparatus, wherein the spray apparatus comprises a container, a dust cap, an arm, an actuator, a stem, a chaplet, a rotating arm, a closure, an insert, a gasket, a spring, a piston, a steel ball, a deep tube.

Yet another objective of the present invention is to improve patient compliance by applying film forming spray on to the already topically administered dosage forms, such as ointment, cream, lotion, gel.

Another objective of the present invention is to form an occlusive and protective thin transparent film/layer over the already topically administered dosage form, wherein the film is non-sticky, non-irritant, and requires less drying time.

Accordingly, it is an object of the invention to provide effective topical treatment with patient compliance for dermatological conditions.

SUMMARY OF INVENTION
The present invention provides an effective topical treatment for dermatological conditions.

In one embodiment, the present invention relates to a method of treating dermatological conditions comprising steps of a) topically applying the pharmaceutical composition to an affected area of a patient and b) thereafter spraying the film-forming composition over the topically administered pharmaceutical composition that forms thin transparent occlusive film layer.

Yet in another embodiment, the film forming spray comprises film forming composition comprising one or more film forming polymer, one or more solvent, one or more emollient and optionally one or more plasticizer.

In another embodiment, the present invention provides methods of using propellant-free film forming sprayable composition comprising at least one film former that can be administered topically directly over the administered pharmaceutical composition.

In another embodiment, the present invention relates to a method of administration of a film forming spray, wherein said film forming spray forms thin transparent occlusive film layer over the topically administered pharmaceutical composition, wherein said film forming spray comprises film forming composition and spray apparatus, wherein said spray apparatus comprises pump or aerosol dispenser. In a specific embodiment, spray apparatus comprises pump dispenser for spraying.

Yet in another embodiment, the film forming spray comprises spray apparatus, wherein said spray apparatus comprises container, dust cap, arm, actuator, stem, chaplet, rotating arm, closure, insert, gasket, spring, piston, steel ball, deep tube.

DETAILED DESCRIPTION OF INVENTION
The present invention relates to a film forming spray composition for topical application to effectively treat several dermatological conditions.

The present invention relates to a film forming composition comprising film forming polymer, solvent system, emollient and optionally plasticizer.

The present invention relates to a film forming spray comprising spray, wherein spray comprises pump or aerosol dispenser for spraying.

The present invention relates to method of treating several dermatological conditions by topically administering pharmaceutical composition to the patient on the affected area and applying the film forming composition over the topically administered pharmaceutical composition, wherein film forming composition forms occlusive film layer over the topically administered pharmaceutical composition,

The present invention relates to a sprayable film forming composition, wherein film forming composition is applied over the topically administered pharmaceutical composition by using spray, wherein spray comprises pump or aerosol dispenser.

The present invention also relates to an improved method of applying a topical administration of pharmaceutical composition to a patient. The term “improved” refers to the delivery of pharmaceutical active agent or dermatological agent through the topically administered pharmaceutical composition which is occluded by occlusive film layer is effective as compared to traditional methods of topical administration of pharmaceutical composition such as rubbing, pouring, spreading by fingertip or any applicator.

The present invention allows patient to wear any type of clothing without any barrier as administered pharmaceutical composition does not adhere to cloths and further,

The present invention also provides no wash-off or rub-off effect due to formed occlusive transparent layer over the topically administered pharmaceutical composition.

Before the present invention is described, it is to be understood that this invention is not limited to embodiments described, as such may vary. It is also to be understood that the terminology used herein is for the purpose of describing embodiments only and is not intended to limit the scope.

Definitions:
The term “Dermatological conditions” as used herein, refers to disease conditions that may affect the skin may originate in another organ or system of the body, but may have manifestations or symptoms that affect the skin.

The term “Dermatological agent” or “pharmaceutical active agent” as used herein, refers to any chemical material or compound for internal or external use for human beings and suitable for topical administration which is intended to be used for or in the diagnosis, treatment, mitigation or prevention of any disease or disorder in human beings.

The term “pharmaceutical composition” as used herein, refers to composition containing pharmaceutically active ingredient or dermatological agent and excipient.

The term “topically administration” as used herein, refers to being applied to a surface such as skin.

The term “film forming spray” as used herein, refers to a spray apparatus containing film forming composition that forms occlusive film layer which is thin and transparent.

The term “film forming composition” as used herein, refers to composition containing film former.

The term “occlusive film layer” as used herein, refers to a thin transparent film formed over the topically administered pharmaceutical composition.

The term “TTLS” as used herein, refers to thin transparent layering system which is meant to adhere the skin and form a transparent film.

The term “film formers” as used herein, refers to compounds, preferably that form a stable film on a surface of skin when applied. In one embodiment, film forming polymer may be construed as film former if it comprises polymeric material or compound that forms stable film on the surface of skin.

The term “emollient” as used herein, refers to a compound or agent that softens, smoothens, and improves oily content of the skin or other mucous membranes. They can be used to correct dryness and scaling of the skin.

The term “plasticizer” as used herein, refers to a compound or agent that imparts flexibility to the film and improve the tensile strength of the film formed.

The term “solvent” as used herein, refers to components that aid in the dissolution of the film formers and/or other excipient present in the film forming composition.

The term “Spray” as used herein, refers to dispense the composition as a mass or jet of droplets from a dispensing system.

The term “about” as used herein, refers to all numerical values relating to amounts, weights, and the like, wherein each particular value is plus or minus 10%.

In one embodiment, pharmaceutical composition comprises dosage form includes but not limited to ointment, cream, lotion, emulsion, gel, foam, microemulsion, nano emulsion, suspension, solution, powder, paste or any marketed product intended to administer topically.

In another embodiment, pharmaceutical composition comprises pharmaceutically active ingredient or dermatological agent includes but not limited to clobetasol, diflorasone diacetate, fluocinonide, halobetasol propionate, amcinonide, desoximetasone, triamcinolone acetonide, betamethasone, fluocinolone acetonide, fluticasone propionate, hydrocortisone butyrate, triamcinolone, loteprednol, momethasone furoate, tofacitinib, apremilast, salicylic acid, metronidazole; and other several an anti-bacterial agent, an anti-viral agent, an anti-fungal agent, an anti-acne agent, anti-inflammatory agent, NSAIDs, anti-proliferative agent, immunomodulatory agent; a vitamin A or its derivative, a vitamin D or its derivative, a vitamin E or its derivative; or mixtures or combinations thereof.

Yet in another embodiment, pharmaceutical composition comprises nutraceuticals or any marketed nutraceutical product intended for topical use.

In another embodiment, the dermatological conditions or diseases include but not limited to Psoriasis, eczema, atopic dermatitis, contact dermatitis, nummular dermatitis, generalized exfoliative dermatitis, stasis dermatitis, perioral dermatitis, ichthyosis, Hailey-Hailey disease, pruritis, localized scratch dermatitis, vitiligo, alopecia, seborrheia, actinic keratosis, pruritis, sun burn, urticaria, localized scratch dermatitis, staphylococcal disorders, ertsipelas, keratoderma, warts, dermatophyte infections, dermatophyte infections.

In one embodiment, film formers includes but not limited to polymer such as octylcyanoacrylate, ethylcyanoacrylate, poly(butylmethacrylate,methylmethacrylate), cellulose or its derivative, cellulose acetate butanoate, poly(methylacrylate), hydroxypropyl methylcellulose, Ethyl cellulose, hydroxypropyl cellulose, polyvinyl pyrrolidine, polyvinyl alcohol (PVA), chitosan, polymethacrylates copolymer, silicones polydimethylsiloxane (PDMS), acrylates copolymer or the like

In another embodiment, film forming composition comprises 0.1 to 10% film forming former, preferably about 5%.

In another embodiment, emollient includes but not limited to glycerin, propylene glycol, isostearic acid derivatives, isopropyl palmitate, lanolin oil, diisopropyl dimerate, diisopropyl adipate, dimethyl isosorbide, maleated soybean oil, octyl palmitate, isopropyl isostearate, cetyl lactate, cetyl ricinoleate, tocopheryl acetate, acetylated lanolin alcohol, cetyl acetate, phenyl trimethicone, glyceryl oleate, tocopheryl linoleate, wheat germ glycerides, arachidyl propionate, myristyl lactate, decyl oleate, propylene glycol ricinoleate, isopropyl lanolate, pentaerythrityl tetrastearate, neopentylglycol dicaprylate/dicaprate, hydrogenated coco-glycerides, isononyl isononanoate, isotridecyl isononanoate, myristyl myristate, triisocetyl citrate, octyl dodecanol, octyl hydroxystearate, almond oil, coconut oil, olive oil, palm oil, peanut oil and the like, fatty acids such as lauric acid, myristic acid, palmitic acid, and stearic acid, monohydric alcohol esters of the fatty acids such as ethyl laurate, isopropyl laurate, ethyl myristate, n-propyl myristate, isopropyl myristate, ethyl palmitate, isopropyl palmitate, methyl palmitate, methyl stearate, ethyl stearate, isopropyl stearate, butyl stearate, isobutyl stearate, amyl stearate, and isoamyl stearate, glycols such as ethylene glycol, diethylene glycol, polyethylene glycol, and propylene glycol, branched aliphatic alcohols such as lauryl alcohol, myristyl alcohol, and stearyl alcohol, and any combinations or mixtures thereof.

In another embodiment, film forming composition comprises from 0 to about 5% emollient, preferably about 4%, more preferably about 2%.

In another embodiment, plasticizer includes but not limited to glycerine, polyethylene glycol,sorbitol, dibutyl phthalate, propylene glycol, triethyl citrate, acetyl triethyl citrate, tributyl citrate, acetyl tributyl citrate, trimethyl citrate, other citrate esters, glycerin, sorbitol, polyalkylene oxides, such as polyethylene glycols, polypropylene glycols, polyethylene-propylene glycols, organic plasticizers with low molecular weights, such as glycerol, glycerol monoacetate, diacetate or polysorbate, cetyl alcohol, or sodium diethylsulfosuccinate.

In another embodiment, film forming composition comprises from 0 to about 10% plasticizer.

In another embodiment, solvent includes but not limited to ethanol, isopropyl alcohol, acetone, n-butanol, methylene chloride, methylene dimethyl ether, water, hydroalcoholic system alone and or in combination of two or more solvents.

In another embodiment, film forming composition comprises from about 20% to 99% solvent, preferably 95%, 96%, 97%.

In another embodiment, film forming composition comprises film formers, plasticizer, humectant, emollient, permeation enhancer.

In another embodiment, film forming spray comprises spray dispenser includes but not limited to aerosol or pump. In a specific embodiment, film forming spray comprises pump dispenser.

In another embodiment, spray apparatus includes but not limited to container, dust cap, arm, actuator, stem, chaplet, rotating arm, closure, insert, gasket, spring, piston, steel ball, deep tube.

In another embodiment, present invention provides dispensing spray apparatus containing propellant-free topical film forming composition, wherein a spray apparatus comprises a container, a pump dispenser, a dip tube, a metering valve, and an actuator, and wherein the pump dispenser is capable of dispensing the composition through a dip tube into a metering valve, and through the actuator fitted with an orifice, such that the film forming composition is consistently released in the form of a substantially uniform spray.

In another embodiment, the container body may be constructed from materials such as metal, glass, ceramics, polyester, polyethylene terephthalate (PET), HDPE or other polymer, or the like. In a specific embodiment, container may be constructed from HDPE, may be as HDPE bottle.

In another embodiment, the present invention provides an example of a dispenser is a unit containing a pump that can be adapted to fit on any type of container, such as by threads that match threading on the container. The pump is capable of dispensing sprayable film forming composition of the present invention through a dip tube extending into a container from an actuator and attached to a valve, which releases the composition from an orifice in the actuator in the form of a spray. The valve may be a metering valve.

In another embodiment, various types of valves that can be used include, but are not limited to, continuous spray valves and metering valves. The actuators allow for easy opening and closing of the valve and are an integral part of a package. This also serves to aid in producing the required type of product discharge.

In another embodiment, various types of actuators include but are not limited to spray actuators, foam actuators, solid-stream actuators, and special actuators. Yet in another embodiment, the actuator may be provided with a protective hood or overcap or dust cap, separate or integral therewith.

In another embodiment, the spray apparatus having pump dispenser operates on mechanical energy provided by depression of actuator. The metering chamber communicates with film forming composition by means of dip tube. By using a metered dose pump it is possible to deliver precise amount of film forming composition on to skin.

In another embodiment, upon actuation, a piston moves descending in the metering chamber, preventing backflow into dip tube, generate pressure which force air before priming or liquid outward through actuator. When the actuation pressure is reduced or taken away, a spring will force the piston to go back to its initial position. This makes a vacuum in the metering chamber which pulls the liquid form the container by lifting the ball from the ball seal over the dip tube at the underside of metering chamber; the ball may be made up of steel.

The following examples are meant to illustrate the present invention and should not be construed as limiting its scope.

EXAMPLES
Example 1: Film forming composition
Table 1: Film forming composition
Ingredients Qt. (%)
Eudragit S100 4.00
Glycerin 1.00
Propylene glycol 1.00%
Isopropyl Alcohol 47.00
Ethanol 47.00

Manufacturing procedure:
1. Preparation of solution:
1.1. In mixing Vessel, charge the Isopropyl Alcohol (47.00%) and Ethanol 95% (47.00%)
1.2. Start Stirring to mix the content.
1.3. Add Eudragit S-100 (4.00%) under stirring until completely dissolves.
1.4 Add Propylene Glycol (1.00%) and Glycerin (1.00%) while stirring.

,CLAIMS:

Claim 1. A film forming spray comprises a film forming composition and spray, wherein said film forming spray is suitable for topical administration.

Claim 2. The film forming composition according to claim 1, wherein the film forming composition comprises at least one film former, at least one solvent, optionally an emollient, and optionally a plasticizer.

Claim 3. The film forming composition according to claim 2, wherein at least one film former is selected from octylcyanoacrylate, ethylcyanoacrylate, poly(butylmethacrylate, methylmethacrylate), cellulose or its derivative, cellulose acetate butanoate, poly(methylacrylate), hydroxypropyl methylcellulose, ethyl cellulose, hydroxypropyl cellulose, polyvinyl pyrrolidine, polyvinyl alcohol (PVA), chitosan, polymethacrylates copolymer, silicones polydimethylsiloxane (PDMS), acrylates copolymer.

Claim 4. The film forming composition according to claim 2, wherein the film former comprises from about 0.1 to about 10%.

Claim 5. The film forming composition according to claim 2, wherein the solvent is selected from ethanol, isopropyl alcohol, acetone, n-butanol, methylene chloride, methylene dimethyl ether, water, hydroalcoholic system alone and or in combination of two or more solvents.

Claim 6. The film forming composition according to claim 2, wherein the solvent comprises from about 20% to about 99%.

Claim 7. The film forming composition according to claim 2, wherein at least one emollient selected from glycerin, propylene glycol, isostearic acid derivatives, isopropyl palmitate, lanolin oil, diisopropyl dimerate, diisopropyl adipate, dimethyl isosorbide, maleated soybean oil, octyl palmitate, isopropyl isostearate, cetyl lactate, cetyl ricinoleate, tocopheryl acetate, acetylated lanolin alcohol, cetyl acetate, phenyl trimethicone, glyceryl oleate, tocopheryl linoleate, wheat germ glycerides, arachidyl propionate, myristyl lactate, decyl oleate, propylene glycol ricinoleate, isopropyl lanolate, pentaerythrityl tetrastearate, neopentylglycol dicaprylate/dicaprate, hydrogenated coco-glycerides, isononyl isononanoate, isotridecyl isononanoate, myristyl myristate, triisocetyl citrate, octyl dodecanol, octyl hydroxystearate, almond oil, coconut oil, olive oil, palm oil, peanut oil and the like, fatty acids such as lauric acid, myristic acid, palmitic acid, and stearic acid, monohydric alcohol esters of the fatty acids such as ethyl laurate, isopropyl laurate, ethyl myristate, n-propyl myristate, isopropyl myristate, ethyl palmitate, isopropyl palmitate, methyl palmitate, methyl stearate, ethyl stearate, isopropyl stearate, butyl stearate, isobutyl stearate, amyl stearate, and isoamyl stearate, glycols such as ethylene glycol, diethylene glycol, polyethylene glycol, and propylene glycol, branched aliphatic alcohols such as lauryl alcohol, myristyl alcohol, and stearyl alcohol.

Claim 8. The film forming composition according to claim 2, wherein the emollient comprises from 0 to about 5%.

Claim 9. The film forming composition according to claim 2, wherein the plasticizer is selected from glycerin, polyethylene glycol, sorbitol, dibutyl phthalate, propylene glycol, triethyl citrate, acetyl triethyl citrate, tributyl citrate, acetyl tributyl citrate, trimethyl citrate, other citrate esters, glycerin, sorbitol, polyalkylene oxides, such as polyethylene glycols, polypropylene glycols, polyethylene-propylene glycols, organic plasticizers with low molecular weights, such as glycerol, glycerol monoacetate, diacetate or polysorbate, cetyl alcohol, or sodium diethylsulfosuccinate.

Claim 10. The film forming composition according to claim 2, wherein the plasticizer comprises from 0 to about 10%.

Claim 11. The film forming composition according to claim 1, wherein the film forming composition is free of propellant.

Claim 12. The film forming spray according to claim 1, wherein the spray comprises a container, a pump dispenser, a dip tube, a metering valve and / or continuous spray valve, and an actuator.

Claim 13. The film forming spray according to claim 12, wherein the container is made from the material comprising metal, glass, ceramics, polyester, polyethylene terephthalate (PET), HDPE.

Claim 14. The film forming spray according to claim 12, wherein the actuator is selected from spray actuators, foam actuators, solid-stream actuators, and special actuators.

Claim 15. The film forming spray according to claim 1, wherein the film forming spray is topically administered for the treatment of dermatological conditions.

Claim 16. The film forming spray according to claim 1, wherein the film forming spray is topically administered on to the pharmaceutical composition.

Claim 17. The film forming spray according to claim 1, wherein administration of the film forming spray comprises a) topically applying the pharmaceutical composition to an affected area of a patient, and b) thereafter spraying the film-forming composition over the topically administered pharmaceutical composition that forms thin transparent occlusive film layer.

Claim 18. The pharmaceutical composition according to claim 16, wherein the pharmaceutical composition comprises ointment, cream, lotion, emulsion, gel, foam, microemulsion, nano emulsion, suspension, solution, powder, paste or any marketed product intended to be administered topically.

Claim 19. The pharmaceutical composition according to claim 16, wherein the pharmaceutical composition comprises dermatological agent.