US20110269704A1 - Method for developing a liquid composition to be applied to the skin as a foam and a composition that can be applied topically - Google Patents

Method for developing a liquid composition to be applied to the skin as a foam and a composition that can be applied topically Download PDF

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Publication number
US20110269704A1
US20110269704A1 US13/143,740 US201013143740A US2011269704A1 US 20110269704 A1 US20110269704 A1 US 20110269704A1 US 201013143740 A US201013143740 A US 201013143740A US 2011269704 A1 US2011269704 A1 US 2011269704A1
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Prior art keywords
foam
composition
main group
foaming agent
active ingredient
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US13/143,740
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English (en)
Inventor
Bernd G. Seigfried
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Mika Pharma Gesell fur Entwicklung und Vermarktung Pharm Prod mbH
Original Assignee
MIKA PHARMA GESELLSCHAFT fur DIE ENTWICKLUNG und VERMARKTUNG PHARMAZEUTISCHER PRODUKTE MBY
Mika Pharma Gesell fur Entwicklung und Vermarktung Pharm Prod mbH
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Application filed by MIKA PHARMA GESELLSCHAFT fur DIE ENTWICKLUNG und VERMARKTUNG PHARMAZEUTISCHER PRODUKTE MBY, Mika Pharma Gesell fur Entwicklung und Vermarktung Pharm Prod mbH filed Critical MIKA PHARMA GESELLSCHAFT fur DIE ENTWICKLUNG und VERMARKTUNG PHARMAZEUTISCHER PRODUKTE MBY
Assigned to MIKA PHARMA GESELLSCHAFT FUR DIE ENTWICKLUNG UND VERMARKTUNG PHARMAZEUTISCHER PRODUKTE MBY reassignment MIKA PHARMA GESELLSCHAFT FUR DIE ENTWICKLUNG UND VERMARKTUNG PHARMAZEUTISCHER PRODUKTE MBY ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: SEIGFRIED, BERND G.
Assigned to MIKA PHARMA GESELLSCHAFT FUR DIE ENTWICKLUNG UND VERMARKTUNG PHARMAZEUTISCHER PRODUKTE MBH reassignment MIKA PHARMA GESELLSCHAFT FUR DIE ENTWICKLUNG UND VERMARKTUNG PHARMAZEUTISCHER PRODUKTE MBH CORRECTIVE ASSIGNMENT ON REEL 026639, FRAME 0830 TO CORRECT THE ASSIGNEE NAME Assignors: SEIGFRIED, BERND G.
Publication of US20110269704A1 publication Critical patent/US20110269704A1/en
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Definitions

  • the present invention is directed in part to a method for making or developing liquid pharmaceutical compositions to be applied as a foam to the skin with the features of the preamble of the patent claim 1 as well as a corresponding topically applicable compositions with the features of the preamble of the patent claim 9 .
  • topically applied pharmaceutical compositions that exist in the liquid state and are present as a foam when applied are familiar.
  • EP 0 510 561 B1 describes one such pharmaceutical composition applied as foam, wherein the basic liquid used in the known pharmaceutical composition is foamed exclusively by mechanical action.
  • the basic liquid composition that is mechanically foamed contains, as ingredients, a surfactant as the foaming agent, a solvent or mixture of solvents, as well as a pharmaceutical active ingredient, wherein this known liquid composition should be foamable simply by mechanical action, without the use of a propellant.
  • a surfactant as the foaming agent
  • solvent or mixture of solvents as well as a pharmaceutical active ingredient
  • this known liquid composition should be foamable simply by mechanical action, without the use of a propellant.
  • an aqueous alkylamidobetaine solution as the surfactant.
  • the composition described in this example is provided with lecithin, which serves solely to form liposomes.
  • DE 197 40 095 A proposes foaming the liquid composition being measured by using a stirrer with a given profile, which is driven at a given speed of rotation. The foam created in this way is visually measured.
  • one underlying problem of the present invention is to provide a method for the development of a liquid pharmaceutical composition to be applied as foam to the skin, by which the development time for such pharmaceutical compositions is substantially simplified and shortened.
  • Another underlying problem of the present invention is to provide a topically applicable composition that can be applied as foam and that contains a systemically or topically acting pharmaceutical active ingredient, whereby this topically applicable composition is developed preferably by the aforementioned development process.
  • the first stated problem is solved by a method according to the characteristics of the patent claim 1 and the further problem, which is mentioned subsequently, is solved by a topically applicable composition with the features of the preamble of the patent claim 9 .
  • the method includes foam volume and the foam stability to be determined by a standardized SITA measurement method, wherein no propellant is used in this measurement method.
  • the at least one foaming agent, the at least one solvent and the at least one pharmaceutical active ingredient are varied in regard to their chemical nature and/or concentration until the foam created by the SITA measurement method under standardized conditions has a foam volume of at least 400 ml, especially a foam volume between 450 and 1400 ml, and preferably a foam volume between 600 and 1200 ml.
  • the foam according to a method of the invention must have such a foam stability that it still has, after a dwell time of up to ten minutes and especially after a dwell time of up to five minutes, at least 50% of the foam volume and especially between 55% and 100% of the foam volume and preferably between 85% and 99% of the foam volume that was originally present immediately after the creation of the foam.
  • the development method according to the invention calls for varying the minimum ingredients (solvent, pharmaceutical active ingredient, and foaming agent) contained in the liquid pharmaceutical composition that is supposed to form the foam when applied in terms of their chemical nature and/or their concentration until they give rise to a foam by the SITA measurement method under standardized conditions whose foam volume possesses the previously quantified volumes and whose foam stability possesses the previously quantified stabilities.
  • the above-described method of the invention has a number of advantages.
  • the method of the invention enables an especially easy and rapid development of such liquid pharmaceutical compositions as can be reproducibly foamed with a number of foam applicators, so that unlike the prior art described at the outset one can develop pharmaceutical foams that are especially reproducible in terms of their foam consistency and their foam composition.
  • the method of the invention one will vary the chemical nature and/or the concentration of the ingredients until a foam results in the SITA measurement method whose foam stability is distinguished in that, within two to four minutes, the foam volume still takes on a value between 50% and 70% of the original foam volume.
  • the chemical nature and/or the concentration of the minimum ingredients of the liquid composition which afterwards forms the foam will be varied so that a foam results whose foam stability is so high that after eight to ten minutes there is still present between 85% and 99% of the foam volume that was originally present immediately after the foaming process.
  • a liquid, foamable composition which has an especially large foam volume is desired, then the nature and/or the concentration of the minimum ingredients of the liquid composition will be varied so that an especially high foam volume results in the SITA measurement method, i.e., a foam volume that varies between 600 ml and 1200 ml or even up to 1400 ml.
  • the method of the invention proposes a standardized method in which, by variation of the chemical nature of the ingredients and/or their concentration, one can develop a foam quantified in the above sense with regard to the foam volume and the foam stability, and which can accordingly be applied to the skin of humans and animals.
  • a first embodiment of the inventive method for development of a liquid pharmaceutical composition to be applied as a foam to the skin proposes that include producing a correlation between the foam as specified by the SITA measurement method and the desired pharmaceutical properties.
  • desired pharmaceutical properties is meant in particular the transport of active ingredient through the layers of the foam into and/or through the skin, i.e., the permeation and/or penetration of the skin and/or the fine distribution of the active ingredient and/or the resulting pharmaceutical effect.
  • a goal of the development in the method of the invention is, that the active ingredient should quickly get onto the skin surface in relatively high concentration
  • one will vary the nature and/or concentration of the ingredients in the liquid composition being foamed by the SITA measurement method so that the resulting foam has a relatively small foam volume, especially a foam volume between 450 ml and 600 ml, and a relatively low foam stability, especially a foam stability after five minutes between 55% and 70% of the foam volume that was originally present immediately after creating the foam.
  • another embodiment calls for selecting a foam applicator for the mechanical foaming of the liquid composition, a foam is created from the liquid composition by the selected foam applicator, and a correlation is produced between the properties, especially the pharmaceutical properties of the foam created via the foam applicator and the foam volume and/or the foam stability as determined via the SITA measurement method.
  • This embodiment of the invented method allows one to develop foams with defined foam volumes and foam stabilities, as measured by the SITA measurement method, especially easily and quickly by varying the nature and/or the concentration of the ingredients of the liquid pharmaceutical composition, which then correlate with the foams that are later applied as foam to the skin by the selected foam applicator.
  • the development method of the invention is used to create a foam from the liquid composition that possesses a foam density between 0.05 g/ml and 0.8 g/ml, preferably between 0.15 g/ml and 0.4 g/ml by the SITA measurement method, it has been found that such liquid compositions provide excellent foams that can be applied with a number of differently designed, mechanical-type foam applicators.
  • the solvent for the production of the liquid composition in the method of the invention may be chosen from the group consisting of: water, at least one alcohol, especially at least one monovalent to trivalent alcohol, at least one polyalcohol and mixtures of the aforementioned solvents.
  • the solvent one will make sure that these solvents are skin-tolerated and especially do not result in any skin irritation, so that they are appropriately pharmaceutically applicable.
  • Preferred solvents are 2-propanol, propylene glycol, glycerin as well as polyols, while the term water comprises all aqueous systems, especially also aqueous pharmaceutical buffer systems.
  • the pharmaceutical active ingredient itself is used as the foaming agent, so that this embodiment of the invented method is based on the fact that it contains, besides the solvent, only the pharmaceutical active ingredient whose concentration and whose chemical nature are varied so that the foam volumes and foam stabilities indicated in the method of the invention and measured according to the SITA method are guaranteed.
  • the foaming agent for the production of the liquid composition is chosen from the group comprising surfactants, especially anionic, cationic, nonionic and ampholytic surfactants, silicones, fats, fatty acids, fatty acid derivates, phospholipids, sugar derivates, lipids, especially sphingolipids and glycolipids, and mixtures and derivates of the aforementioned substances.
  • surfactants especially anionic, cationic, nonionic and ampholytic surfactants, silicones, fats, fatty acids, fatty acid derivates, phospholipids, sugar derivates, lipids, especially sphingolipids and glycolipids, and mixtures and derivates of the aforementioned substances.
  • foaming agents may be capable of provide the aforementioned foam volumes and foam stabilities as soon as the liquid composition is foamed in purely mechanical fashion, without the use of a propellant.
  • Preferred surfactants include the fatty alkyl ether sulfates, the alkyl phosphates, the alkyl ether phosphates, the alkyl benzene sulfonates, the petroleum sulfonates, the olefin sulfonates and/or the esters of sulfosuccinic acid.
  • silicones include modified siloxanes, polydialkyl siloxanes and preferably linear or cyclical polydimethyl siloxanes.
  • Fats and modified fats such as fatty acids, fatty acid derivates, fatty acid esters, as well as synthetic, plant and animal phospholipids, especially phosphatidyl choline and/or hydrogenated phospholipids and preferably hydrogenated phosphatidyl choline, are among the preferred foaming agents, in addition to the sphingolipids, glycolipids and sugar derivates, preferably sugar or sorbitol esters.
  • the sulfates of fatty acids, sulfonates of fatty acids, salts of sulfates of fatty acids, salts of sulfonates of fatty acids, soaps and mixtures and derivates of the aforementioned substances are especially suitable as foaming agents for use in the method of the invention.
  • preferred surfactant foaming agents are chosen from the group consisting of: alkylcarboxylates, alkylsulfates, alkylsulfonates, alkylethercarboxylates, sulfates of fatty acids, phosphates of fatty acids, sulfonates of fatty acids, salts of sulfates of fatty acids, salts of sulfonates of fatty acids, fatty acid amides, polyalkylenes, fluorosurfactants, soap, metal soaps, especially alkaline soaps, such as sodium, potassium and ammonium salts of aliphatic carboxylic acids, organic amino-soaps, especially organic amine soaps of aliphatic carboxylic acids, quaternary ammonium compounds, especially benzalkonium chloride, octadecylammonium chloride, sulfonium salts, amidoamines, fatty acid esters, preferably monoglycerin, diglycerin
  • cationic surfactants that are likewise especially suitable as the foaming agent in the method of the invention for the production of the liquid composition, one will select substances which contain quaternary ammonium compounds, sulfonium salts, amidoamides and their mixtures as well as their derivates.
  • Preferred ampholytic surfactants for the production of the liquid composition will be chosen from the group comprising betaine and betaine derivates.
  • active ingredients used in the method of the invention these will preferably be active ingredients such as are described in further detail in connection with the topically applicable composition according to the invention.
  • the present invention furthermore concerns a topically applicable composition with the features of the preamble of patent claim 9 .
  • the topically applicable composition of the invention which is developed preferably but not exclusively according to the above described method of the invention, has, a pharmaceutical active ingredient, a solvent as well as a foaming agent.
  • the topically applicable composition of the invention proposes a phospholipid foaming agent as the foaming agent.
  • the at least one phospholipid foaming agent, the at least one solvent and the at least one active ingredient in the composition of the invention are attuned to each other in their chemical nature and/or their concentration so that the composition can be mechanically foamed exclusively without the use of an additional propellant.
  • the foam so created by the mechanical foaming during the application has a foam volume of at least 400 ml, preferably between 450 and 1400 ml and especially a foam volume between 600 and 1200 ml.
  • the composition according to the invention has such a foam stability that the foam still has, after a dwell time of up to ten minutes and especially after a dwell time of up to five minutes, at least 50% of the foam volume and especially between 55% and 100% of the foam volume and preferably between 85% and 99% of the foam volume that was originally present immediately after the creation of the foam, wherein both the aforementioned foam volume and the aforementioned foam stability can be determined by the standardized SITA foam measurement method.
  • topically applicable composition of the invention is characterized not only by the nature of its ingredients and/or their concentration, but also by the foam created from it, wherein the foam is specified and quantified in terms of the foam volume and the foam stability by the standardized SITA measurement method.
  • composition of the invention has a number of advantages.
  • skin as already defined above covers the mucous membranes of mouth, nose, vagina and foreskin, the skin areas of the ear and especially the inner ear, the skin areas of the anus and the rectum, the nails and the eyes, especially the conjunctiva, the cornea and the lacrimal sac, the foam created from the composition of the invention has, first of all, an excellent adhesion to these application sites, so that it cannot easily be wiped off unintentionally.
  • the foam produced in exclusive mechanical fashion from the liquid composition of the invention has a naturally homogeneous composition, and the pharmaceutical active ingredient is present in this foam in an especially uniform ultrafine distribution, so that once the foam breaks down after being applied this ultrafine distribution is retained in the liquid layer formed on the skin surface, with the result that the pharmaceutical active ingredient is transported with a high rate of penetration and/or permeation into and/or through the skin.
  • the active ingredient so applied has a high pharmaceutical efficacy, so that if desired the concentration of active ingredient in the composition of the invention can be reduced as compared to traditional compositions or, alternatively, the time intervals between consecutive applications can be lengthened appropriately, especially since the active ingredient forms a depot in the skin.
  • this phospholipid foaming agent Due to the fact that a phospholipid foaming agent is present as the foaming agent in the composition of the invention, this phospholipid foaming agent has the effect of producing a faster penetration or permeation into or through the skin, which proves to be an additional advantage of the composition of the invention.
  • the foam created from the composition of the invention by the SITA measurement method has a foam density between 0.05 g/ml and 0.8 g/ml, preferably between 0.15 g/ml and 0.4 g/ml, such embodiments of the compositions according to the invention have the aforementioned advantageous properties to an enhanced degree.
  • the composition according to the invention includes, as a solvent, especially water, at least one alcohol, especially at least one polyvalent to trivalent alcohol, and/or at least one polyalcohol, and such solvents are chosen in particular for such phospholipid foaming agents as contain a phospholipid and/or a phospholipid mixture isolated from plant components, especially soy beans.
  • the term phospholipid mixture or phospholipids in the above description covers all phospholipids of plant origin, animal origin, or synthetic origin.
  • this includes the ester phospholipids, especially phosphatidyl choline, lyso-phosphatidyl choline, phosphatidyl ethanolamine, lyso-phosphatidyl ethanolamine, phosphatidyl serine, lyso-phosphatidyl serine, phosphatidyl inositol, lyso-phosphatidyl inositol, phosphatidyl glycerin, diphosphatidyl glycerin and the phosphatidic acids, the ether phospholipids, especially choline plasmalogen and ethanol aminoplasmalogen, as well as the sphingosine phospholipids, especially ceramide phosphoryl choline and phytoglycolipid and derivates of the ester phospholipids, the ether phospholipids, especially cho
  • the at least one active ingredient contained in the composition of the invention is one that is suitable for use on humans or animals and especially for topical and systemic application, especially on the skin, wherein an especially preferred active ingredient is chosen from the group comprising local anesthetics, anti-allergic agents, dermatics, active ingredients against flu infections and colds, active ingredients for the treatment of neuropathies, active ingredients for the treatment of disturbed circulation, chemotherapy drugs, quinine, antimycotics, antibiotics, thalidomide, serotonin, eicosanoids, analgesics, anticonvulsants, nonsteroidal antirrheumatics, leukotrienes, leukotriene inhibitors, androgens, antiandrogens, corticoids, opiate receptor antagonists, blood clotting inhibitory substances, thrombocyte aggregation inhibitors, histamine antagonists, regulatory and enzymatically acting peptides and proteins, nucleic acids (single and double-strand), nucleic acids (single and
  • inventive compositions include an active ingredient or a special active ingredient mixture, which is chosen from the following listed special active ingredients, presented under their particular main groups.
  • appetite curbing or antiobesity agents norephedrine, phenylpropanole amine, D-norpseudoephedrin, orlistate and sibutramine
  • ACE-inhibitors benazepril, cilazapril, quinapril, ramipril, spirapril and trandolapril
  • acidosis therapeutic or antihypoxemic agents calcium-sodium-hydrogen-citrate
  • astringents aluminium chloride, aluminum diacetate, aluminum formate, bismuth chloride oxide, bismuth gallate, polycresulene, tannin and zinc oxide
  • acne agents azelainic acid and benzoy
  • composition according to the invention proposes that this embodiment of the invented composition has, as active ingredient, an analgesic, especially an analgesic that is chosen from the above indicated special analgesics, and the concentration of this analgesic in the liquid composition that is mechanically foamed is varied in particular between 0.1 wt. % and 20 wt. %, preferably in a concentration between 2 wt. % and 10 wt. %.
  • composition of the invention includes, as pharmaceutical active ingredient, at least one antimycotic, especially an antimycotic that is chosen from the above indicated special antimycotics.
  • this antimycotic is chosen from the group comprising chlotrimazol, biphonazol, econazol, phenticonazol, isoconazol, oxyconazol, sertaconazol, thioconazol, terbinafin, myconazol, ketoconazol, itraconazol, fluconazol, voriconazol, as well as derivates of the aforementioned substances.
  • concentration of an antimycotic active ingredient varies between 0.01 wt.
  • a foam produced in exclusively mechanical fashion from such a liquid composition during its application can then be used in particular with a very high pharmaceutical efficacy for nail and foot fungal infections and for saccharomycete infections, the high pharmaceutical efficacy being manifested in that these fungal infections are curtailed already after a few applications and also healed in a short time after the application is repeated.
  • composition according to the invention includes as an active ingredient, at least one corticoid active ingredient, especially a corticoid active ingredient that is chosen from the above indicated special corticoid active ingredients, wherein the corticoid active ingredient is chosen preferably from the group consisting of glucocorticoids, mineral corticoids and derivates of these.
  • the concentration of this corticoid active ingredient varies between 0.001 wt. % and 3 wt. %, preferably between 0.1 wt. % and 0.8 wt. %.
  • Preferred glucocorticoids are chosen from the group consisting of clobetasol-17-propionate, diflucortolone-21-valerate, amcinonide, betamethasone-17,21-dipropionate, betamethasone-17-valerate, desocimethasone, diflucortolone-21-valerate, fluocinolone acetonide, fluocinonide, fluocortolone, fluprednidene-21-acetate, fluthicasone-17-propionate, halcinonide, hydrocortisone-21-acetate-17-propionate, hydrocortisone-17-butyrate-21-propionate, hydrocortisone-17-butyrate, methylpredisolonaceponate, momethasone, momethasone furoate, prednicarbate, triamcinolonacetonide, clobethasone butyrate, clocortolone-21-pivalate, fluocort
  • compositions of the invention contain, as active ingredient, at least one topical anesthetic, especially a topical anesthetic that is chosen from the above indicated special topical anesthetics, and the concentration of this topical anesthetic, depending on the particular active ingredient, varies in particular between 3 wt. % and 15 wt. %, especially between 6 wt. % and 12 wt. %, in terms of the concentration of active ingredient in the liquid composition.
  • Topical anesthetics are chosen from the group consisting of benzocaine, procaine, tetracaine, lidocaine, etidocaine, prilocaine, mepivacaine, bupivacaine, S-ropivacaine, articaine and their derivates.
  • compositions according to the invention calls for the composition to contain at least one immunomodulator in a concentration between 0.03 wt. % and 0.1 wt. %, and the above indicated special immunomodulators are especially preferred.
  • composition of the invention comprises, as an active ingredient or mixture of active ingredients, a nonopioid analgesic/antiphlogistic agent, especially a non-opioid analgesic/antiphlogistic that is chosen from the above indicated special non-opioid analgesics/antiphlogictics.
  • salicylates preferably acetylsalicylic acid and/or diflunisal
  • acetic acid derivates such as indomethacin, acemethacin, diclofenac and/or lonazolac
  • propionic acid derivates such as ibuprofen, flurbiprofen, ketoprofen, dexketoprofen, dexibuprofen, tarenflurbil, nimesulide, naproxen and/or thiaprofen acid
  • oxicams such as pyroxicam, tenoxicam, meloxicam and/or lornoxicam
  • anthranylic acid derivates such as mefenaminic acid and/or flufenaminic acid
  • aniline derivates such as paracetamol
  • 1-phenyl-2,3-dimethyl-3-pyrazolin-5-on derivates such as phenazone, propyphenazone and/or metamizol, their
  • the concentration of the analgesic/antiphlogistic active ingredient in the liquid composition will vary between 0.5 wt. % and 8 wt. %, especially between 1 wt. % and 5 wt. %.
  • composition of the invention may include, as active ingredient, a mixture of active ingredients, as long as this mixture of ingredients is mutually compatible.
  • Such embodiments of the composition of the invention will be used for treating generally milder skin ailments, such as milder forms of eczema, acne, lichen, insect bites, mycoses and/or treatments of surface wounds with the foam created from the composition of the invention, in which case the active ingredient or mixture of active ingredients is chosen from the group containing terbinafin, clobethasone butyrate, erythromycin, benzocaine, dexamethasone, calcipotriol, tretinoin, minoxidil, bifonazole, dexpanthenol, salicylic acid, prednicarbate, momethasone furoate.
  • composition of the invention includes, as the phospholipid foaming agent, a phosphatidyl choline isolated from soy beans, and in particular the concentration of this phosphatidyl choline in the phospholipid foaming agent is more than 50 wt. %, preferably between 50 wt. % and 95 wt. %, in relation to the dry substance of the phospholipid foaming agent.
  • this phospholipid foaming agent contains at most 15 wt. % of lyso-phosphatidyl choline, at most 10 wt. % of phosphatidic acid and at most 10 wt. % of phosphatidyl ethanolamine, one can create a foam with this special foaming agent that can be diversely adapted to the particular requirements of the application site by varying its concentration.
  • the concentration of the phospholipid foaming agent contained in the liquid composition should be chosen so that the foams mentioned at the outset for the method of the invention and for the composition of the invention and specified by the foam volume and by the foam stability can be created.
  • the liquid composition which is purely mechanically foamed has the phospholipid foaming agent in a concentration between 2 wt. % and 25 wt. %, especially in a concentration between 4 wt. % and 15 wt. %.
  • composition of the invention contains, besides water, preferably an alcohol and especially propylene glycol, whose concentration, depending on the desired and above-specified foam, varies between 2 wt. % and 25 wt. %, especially between 5 wt. % and 15 wt. %.
  • the liquid composition of the invention has a pH value that is skin-tolerated and, depending on the particular site of application, lies between 4.8 and 8.8.
  • At least one buffer especially sodium dihydrogen phosphate dihydrate and/or disodium hydrogen phosphate dodecahydrate.
  • composition of the invention as described in detail above can principally be foamed with any suitable foam applicator, e.g., the applicators made by Rexam/Airspray (www.rexamairspray.com) and made and marketed under the name M3 mini foamer (“M3 MiniMobileumer”) or those of made by Calmar/MeadWestvaco (Keltec).
  • M3 mini foamer M3 MiniCoumer
  • Calmar/MeadWestvaco Calmar/MeadWestvaco
  • the present invention contemplates a foam applicator that includes a composition of the invention as described in detail above.
  • the present invention relates to methods for treatment of the following illnesses.
  • a method in a first embodiment, includes the treatment of atopic eczema or neurodermitis, wherein the treatment method of the invention involves the applying of a foam containing an immunomodulator, as is produced in particular from the previously described composition of the invention, to the skin of a warm-blooded mammal in need thereof.
  • an immunomodulator as is produced in particular from the previously described composition of the invention.
  • tacrolimus is chosen as the immunomodulator.
  • its concentration will vary preferably between 0.03 wt. % and 0.1 wt. %.
  • a method for the treatment of inflammatory or pruritic skin ailments, psoriasis, dermatitis, neurodermitis or psoriasis in a patient in need thereof, comprising the application of a foam containing a glucocorticoid, as is produced in particular from described compositions, to the skin of a warm-blooded mammal.
  • the glucocorticoid in this treatment method is chosen from the group consisting of betamethasone, dexamethasone, predincarbate, mometasone furoate and clobetasone butyrate.
  • its concentration varies between 0.01 wt. % and 0.4 wt. %.
  • a method for the treatment of of pain, inflammation, rheumatic ailments or acute trauma in a patient in need thereof and comprises the application of a foam containing an analgesic, as is produced in particular from the previously described composition of the invention, to the skin of a warm-blooded mammal.
  • the analgesic in this treatment method is chosen from the group consisting of diclofenac, ketoprofen and ibuprofen.
  • concentration varies between 0.5 wt. % and 10 wt. %.
  • a method for the treatment of of mycotic infections comprises the application of a foam containing an antimycotic, as is produced in particular from the previously described composition of the invention, to the skin or nails respectively hooves of a warm-blooded mammal in need thereof.
  • the antimycotic is chosen from the group comprising bifonazole and terbinafin.
  • its concentration varies between 0.1 wt. % and 20 wt. %, preferably between 2 wt. % and 10 wt. %.
  • a method for the treatment of infections with Gram positive microbes, anaerobic microbes and mycoplasms, especially for treatment of acne, in a patient in need thereof, and comprises the application of a foam containing an antibiotic, as is produced in particular from the previously described composition of the invention, to the skin of a warm-blooded mammal.
  • the antibiotic chosen is erythromycin, especially in a concentration between 2 wt. % and 4 wt. %.
  • a method for the treatment of itching of the skin comprises the application of a foam containing a topical anesthetic, as is produced in particular from the previously described composition of the invention, to the skin of a warm-blooded mammal.
  • the topical anesthetic chosen is benzocaine and/or lidocaine, especially in a concentration between 1 wt. % and 20 wt. %, preferably 2 wt. % and 10 wt. %.
  • a method for the treatment of psoriasis comprises the application of a foam containing calcipotriol, as is produced in particular from the previously described composition of the invention, to the skin of a warm-blooded mammal in need thereof.
  • the calcipotriol in this treatment method is provided in a concentration between 0.005 wt. % and 0.05 wt. %.
  • a method for the treatment of acne comprises the application of a foam containing tretinoin, as is produced in particular from the previously described composition of the invention, to the skin of a warm-blooded mammal in need thereof.
  • the tretinoin is provided in a concentration between 0.05 wt. % and 0.1 wt. %.
  • a method for treatment of hair loss comprises the application of a foam containing minoxidil, as is produced in particular from the previously described composition of the invention, to the skin of a warm-blooded mammal in need thereof.
  • the minoxidil is provided in a concentration between 3 wt. % and 6 wt. %.
  • a method for the antiseptic treatment of superficial wounds comprises the application of a foam that includes an antimycotic to the wound of a warm-blooded mammal in the need thereof, whereby the foam is preferably produced from the previously described composition of the invention.
  • the dexpanthenol is provided in a concentration between 0.03 wt. % and 1 wt. %.
  • a method for the treatment of herpes and the side effects accompanying herpes in a patient need thereof and comprises the application of a foam containing aciclovir, as is produced in particular from the previously described composition of the invention, to the skin of a warm-blooded mammal.
  • the aciclovir is provided in a concentration between 3 wt. % and 7 wt. %.
  • a method for the treatment of mild to medium severe psoriasis of the scalp in a patient in need thereof and comprises the application of a foam containing salicylic acid, as is produced in particular from the previously described composition of the invention, to the scalp of a warm-blooded mammal.
  • the salicylic acid is provided in a concentration between 8 wt. % and 12 wt. %.
  • the term skin used throughout the text covers not only the particular ailing regions of the skin, but also all surfaces of the human or animal body accessible to the application of the foam produced from the composition of the invention, and thus in particular, besides the skin or scalp itself, also nails, hair, teeth, hooves or the mucosa in mouth, nose, vagina or foreskin, the regions of the ear and especially the inner ear, the region of the anus and the colon, the region of the eyes, especially the region under the eyelid, such as conjunctiva, cornea and lacrial sac, while the term mammal comprises animals and humans.
  • the present invention concerns a topically applicable liquid composition
  • a topically applicable liquid composition comprising at least one phosphlipidic foaming agent, at least one pharmaceutical active ingredient and at least one solvent.
  • the inventive composition is foamable exclusively by a mechanically foaming without using an propellant to such an extent, that by mechanically foaming of 250 ml of the liquid composition a foam is created having a foam volume of at least 400 ml and a foam stability, that the foam still has after a dwell time of nearly five minutes and preferably of a dwell time up to five minutes, measured at 25 ° C., at least 50% of the foam volume that was originally present immediately after the creation of the foam.
  • Both the afore mentioned foam volume and the afore mentioned foam stability are measured by a standardized SITA foam measurement method, described hereafter.
  • liquid composition specified by the foam volume and foam stability, is exclusively mechanically foamed prior to use without using a propellant, as repeated described before, so that the foam, created in that way is used for topical application.
  • This embodiment of the inventive composition has identical or analogue all the benefits, as described before. This is also the same for the afore described embodiments.
  • the afore described inventive composition has a foam volume, which varies between 450 ml and 1400 ml, especially between 600 ml and 1200 ml.
  • this embodiment of the inventive composition has a high pharmaceutical efficacy.
  • This advantage is also present, when the foam volume is within ten minutes after creating the foam at least 50%, preferably between 85% and 100%, of the foam volume that was originally present immediately after the creation of the foam.
  • the foam created from the inventive liquid composition a density between 0.05 g/ml and 0.8 g/ml, preferably between 0.15 g/ml and 0.4 g/ml.
  • this solvent is preferably an anorganic and/or an organic solvent, whereby the anorganic solvent is preferably water and the organic solvent is an alcohol or a mixture of alcohols and more preferably a polyalcohol and/or is the solvents described before in claim 5 .
  • the present invention preferably concerns a method for making and/or development of a foamable liquid composition, for topical use, whereby the inventive method comprises the following steps:
  • a “SITA foam tester R-2000” manufactured by SITA Messtechnik GmbH, Dresden was used, as is described in detail in EP 1 092 970.
  • This measurement device was provided with a rotor as shown in FIGS. 2 and 3 of DE 197 40 095 and also described there.
  • This rotor consists of a stirring shaft and a circular disk oriented perpendicular to this, with a diameter of 70 mm, above and below the circular disk there being provided four symmetrical stirring blades, oriented at right angles to each other.
  • Each stirring blade has a rectangular base surface of 23 mm ⁇ 12 mm.
  • each stirring blade has the shape of a triangle, with a height of 5 mm, so that each stirring surface accordingly forms a roof with a ridge angle of 90 degrees.
  • the stirring blades each consist of a Conidur fine perforated plate (manufactured by HeinLehmann, Krefeld) and have a plate thickness of 0.5 mm, a perforation of 0.5 and a spacing of 3.2.
  • the sample volume was 250 ml, being automatically withdrawn by the measuring device from the reservoir tank, filled with at least 300 ml of sample.
  • the sample was placed carefully into the reservoir tank, avoiding any foam formation if possible. After a waiting time of ten minutes, so that any air bubbles formed during the filling could migrate to the surface and thus not falsify the volume, 250 ml of the sample being investigated was drawn into the measuring space and measured.
  • the sample being measured in the measuring space was subjected to five rotor cycles of 20 seconds each to create the foam. Between rotor cycles there was a pause of around 15 seconds.
  • the foam volume was measured immediately after the five rotor cycles were completed.
  • the foam stability was automatically detected by the instrument over a period of 35 minutes in total for which the foam volume was measured every 50 seconds by means of the needle detectors.
  • the volume values so obtained were recorded directly by dedicated software and hardware of the instrument.
  • the control system of the SITA foam tester is such that, after the measurement space is filled with 250 ml of sample, the needle detectors travel only as far as the surface of the sample and, accordingly, place the zero point for the foam volume on the surface of the measurement sample and not on the floor of the measurement space.
  • diclofenac is indicated as the active ingredient contain this active ingredient in the form of the sodium salt of diclofenac, meaning as diclofenac-sodium.
  • ketoprofen one containing lidocaine hydrochloride, one containing prednicarbate, one containing diclofenac and one containing clotrimazol were prepared, having the following ingredients:
  • composition Ingredient in wt. % 1 Lidocaine hydrochloride 10.00 2 Propylene glycol 10.00 3 2-Propanol 11.00 4 Phospholipid foaming agent A 10.00 5 Sodium dihydrogen phosphate dihydrate 0.12 6 Disodium hydrogen phosphate dodecahydrate, cryst. 0.66 7 Sodium hydroxide 20% w/w 4.00 8 Peppermint oil 0.15 9 Ultrapure water 54.07 TOTAL 100.00
  • Composition Ingredient in wt. % 1 Prednicarbate 0.10 2 Propylene glycol 15.00 3 2-Propanol 9.35 4 Phospholipid foaming agent B 5.00 5 Sodium dihydrogen phosphate dihydrate 0.50 6 Disodium hydrogen phosphate dodecahydrate, cryst. 1.14 7 Sodium hydroxide 10% w/w 1.00 8 Tegosoft GC 8.60 9 Ultrapure water 59.31 TOTAL 100.00
  • the ailing area of the right foot was treated with a composition 5, identical in ingredients, while this composition 5 was foamed by means of a “M3 mini foamer” from Rexam/Airspray immediately prior to application.
  • the fungal infections were eliminated after a total treatment time of eight days, in six subjects the healing time was eleven days, and in four subjects the healing time was 14 days. It is to be noted that the latter four subjects were the most heavily affected by the fungal infection. No subject could find a difference between the foam created by the SITA measurement method and the foam produced by the “M3 mini foamer”.
  • compositions 6 to 8 were prepared and investigated in regard to the concentrations of active ingredient diclofenac.
  • compositions 9 to 11 were prepared and investigated in regard to the concentration of phospholipid foaming agent.
  • compositions 12 to 14 were prepared and investigated in regard to the concentration of isopropanol.
  • Composition Ingredient in wt. % 1 Diclofenac 4.000 2 Propylene glycol 15.000 3 2-Propanol 5.000 4 Ascorbylpalmitate 0.020 5 Phospholipid foaming agent A 13.330 6 Sodium dihydrogen phosphate dihydrate 0.120 7 Disodium hydrogen phosphate dodecahydrate, cryst. 0.660 8 EDTA 0.040 9 Ultrapure water 61.630 10 Peppermint oil, rectified 0.200 TOTAL 100.00
  • the foam behavior of this composition 12 is shown in FIG. 12 .
  • Composition Ingredient in wt. % 1 Diclofenac 4.000 2 Propylene glycol 15.000 3 2-Propanol 10.000 4 Ascorbylpalmitate 0.020 5 Phospholipid foaming agent A 13.330 6 Sodium dihydrogen phosphate dihydrate 0.120 7 Disodium hydrogen phosphate dodecahydrate, cryst. 0.660 8 EDTA 0.040 9 Ultrapure water 56.630 10 Peppermint oil, rectified 0.200 TOTAL 100.00
  • Composition Ingredient in wt. % 1 Diclofenac 4.000 2 Propylene glycol 15.000 3 2-Propanol 20.000 4 Ascorbylpalmitate 0.020 5 Phospholipid foaming agent A 13.330 6 Sodium dihydrogen phosphate dihydrate 0.120 7 Disodium hydrogen phosphate dodecahydrate, cryst. 0.660 8 EDTA 0.040 9 Ultrapure water 46.630 10 Peppermint oil, rectified 0.200 TOTAL 100.00
  • the foam volume increases as a function of the concentration of isopropanol with rising concentration of isopropanol from 5 wt. % to 10 wt. % and then decreases again in the range of 10 wt. % to 20 wt. %, so that no stable foam is formed at a concentration of 20 wt. % of isopropanol.
  • the slight foam volume shown initially in FIG. 14 should be disregarded.
  • compositions 15 to 17 were prepared, differing in terms of the concentration of propylene glycol.
  • compositions 15 to 17 Based on the comparison of the compositions 15 to 17 and the corresponding FIGS. 15 to 17 , one can say that the concentration of propylene glycol has no or only a very slight influence on the foam volume and the foam stability.
  • the treatment was done per application with a defined amount of 0.4 mg foam per half of the face.
  • the foam was applied directly to the area being treated and massaged in by circular motions with 2 fingers.
  • the total therapy time amounted to 60 days.
  • the first success could already be determined for both foams after 30 days application: the lesions on the left side of the face were reduced by around 19% and those of the right half by around 21%.
  • the artificial UV erythemas were created at 16 test fields (each one 2 ⁇ 2 cm) on the back, 4 test fields to each the left and right of the spinal column, as well as 4 test fields each in the upper and lower region of the back.
  • the 8 upper test fields were exposed to a UV dose of 1.5 ⁇ MED and the lower test fields with 2.5 ⁇ MED.
  • ECG rings with an inner diameter of 16 mm were glued to the centers of the UV-exposed test fields.
  • the untreated fields were likewise marked with ECG rings.
  • the distance between the test fields was around 3 cm.
  • composition 19 c) (ketoprofen-free composition) is shown in FIG. 19 .
  • the foams containing active ingredient showed distinct differences at 1.5 MED and 2.5 MED in the final measurement after 8 hours.
  • a value of 1 was found for the foam containing diclofenac (slight suppression of the erythema, easily identifiable), a value of 2 for the foam containing ketoprofen (distinct suppression of the erythema but still visible) and a value of ⁇ 1 for the ketoprofen-free foam (more pronounced erythema).
  • the foam made from the composition containing ketoprofen shows a clear therapeutic superiority over the foam containing diclofenac, the ketoprofen-free foam, and the untreated test fields.
  • the phospholipid foaming agent A used above in examples 1 and 2, as well as 4 to 17, has the following composition, with the following values referring to the dry substance.
  • the phospholipid foaming agent B used above in examples 3 and 18 has the following composition, with the following values referring to the dry substance.
  • the above indicated peroxide number indicates the milliequivalents of oxygen which are contained in 1000 g of a sample (dry substance). This value, after reacting the sample with potassium iodide in a mixture of chloroform and acetic acid, is determined by titrating the iodine produced in this way with sodium thiosulfate and a potentiometric determination.
  • the acid number indicates how many mg of potassium hydroxide are needed to neutralize the free, nonesterified fatty acids that are contained in 1 g of phospholipid foaming agent (dry substance). This value is determined by titration of a corresponding dissolved sample with potassium hydroxide solution, using phenolphthalein as indicator.

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CA2752849C (en) 2014-07-08
PT2387391T (pt) 2017-04-20
US9693956B2 (en) 2017-07-04
MX2011008660A (es) 2011-09-22
HRP20170376T1 (hr) 2017-05-05
BRPI1006790A2 (pt) 2017-05-02
US20110059117A1 (en) 2011-03-10
WO2011009436A3 (de) 2011-09-15
BRPI1006790B1 (pt) 2020-10-20
JP2013500239A (ja) 2013-01-07
US20180104185A1 (en) 2018-04-19
WO2011009436A9 (de) 2011-03-31
SI2387391T1 (sl) 2017-04-26
ES2622097T3 (es) 2017-07-05
WO2011009436A2 (de) 2011-01-27
DE102010027315A1 (de) 2011-01-27
EP2387391B1 (de) 2017-01-11
RU2011134420A (ru) 2013-02-27
EP2387391A2 (de) 2011-11-23
BRPI1006790B8 (pt) 2021-05-25
RU2532027C2 (ru) 2014-10-27
US20160022579A1 (en) 2016-01-28
US9005626B2 (en) 2015-04-14

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