Local composition containing ambroxol

FIELD: medicine.

SUBSTANCE: present invention refers to application of antiinflammatory and local anaesthetic pharmaceutical compositions containing ambroxol or one of its pharmacologically acceptable salts for local application for skin diseases chosen from the group including anaesthesia, burning, itching, inflammation, mosquito stings and skin redness of allergic, immunologic or idiopathic origin, applied directly on the skin.

EFFECT: invention provides antiinflammatory and local anaesthetic action in skin application, increases duration of application and do not show collateral actions.

6 cl, 15 ex

 

The present invention relates to possess anti-inflammatory and mestnoanesteziruushim properties, pharmaceutical compositions containing Ambroxol or one of its pharmacologically acceptable salts, preferably Ambroxol in the form of its hydrochloride, and intended for local use by direct application or applying to the skin and/or mucous membrane.

For the application of medicinal substances on the skin and mucous membranes in pharmacy there are various main dosage forms. Review the information about them can be found in ordinary textbooks of pharmaceutical technology, for example in the book U.Schöffing, "Arzneiformenlehre", publishing house Deutscher Apotheker Verlag Stuttgart, 4th ed., 2003, or in the book Gurny/Junginger, "Bioadhesion - Possibilities and Future Trends", published by Wissenschaftliche Verlagsgesellschaft Stuttgart, 1990. In WO 00/38653 described improved dosage form intended for transdermal administration of corticosteroids, and along with many other antioxidants also mentioned Ambroxol as excipients, suitable for protection against oxidative decomposition. Known further containing Ambroxol lozenges (lozenges), designed to eliminate pain in the throat and pharynx (EP 1200070, WO 03/072094). However, with therapeutic effect of a composition containing Ambroxol or its salt as the act is its substance and intended for local use by direct application to the skin, accordingly, the mucous membrane and to treat them in the level technique is not described. When using dosage forms for topical application which contain has anesthetic or anti-inflammatory compounds, frequently observed side effects.

Based on the foregoing, the present invention was based on the task to propose compositions (pharmaceutical form) for local use, which together with high anti-inflammatory and anaesthetic efficacy have not had any side effects or at least would have only minor side effects.

Description of the invention

With the invention it has been unexpectedly found that pharmaceutical compositions for topical application containing Ambroxol or one of its pharmacologically acceptable salts and intended for direct application or applying to the skin and/or mucous membranes, anti-inflammatory and mestnoanesteziruushim properties. Exceptional Toxicological profile of Ambroxol also allows the use of such containing compositions on large areas of skin and/or mucous membranes, as well as to increase the duration of their application.

The object of the present invention are suitable for the and it has anti-inflammatory and mestnoanesteziruushim properties of pharmaceutical compositions for local application, containing Ambroxol or one of its pharmacologically acceptable salts and intended for direct application or applying to the skin and/or mucous membrane, preferably on the skin or mucous membrane of the mouth, most preferably on the skin.

Preferred pharmaceutical compositions for topical application containing Ambroxol in the form of its hydrochloride.

Preferred further pharmaceutical compositions for topical application in the form of a dosage form selected from the group including gels, hydrophilic paste, mash and solutions, preferred among which are gels and hydrophilic paste.

Especially preferred pharmaceutical compositions for topical application in the form of a dosage form selected from the group including gels, hydrophilic paste, mash and solutions containing Ambroxol from 0.1 to 20 wt.%, preferably from 0.5 to 5 wt.%.

Especially preferred pharmaceutical compositions for topical application in the form of a dosage form selected from the group including candles, hydrophobic pastes, ointments, creams, lotions and pencils, preferred among which candles, hydrophobic paste and pencils.

In one of the preferred embodiments of the invention provides pharmaceutical compositions for local application is in the form of mucoadhesive patches, buccal strips or mucoadhesive tablets, preferred among which mucoadhesive the buccal patches or strips.

In another preferred embodiment, the invention provides pharmaceutical compositions for topical application in the form mucoadhesive patches containing Ambroxol from 1 to 50 wt.%, preferably from 5 to 40 wt.%, most preferably from 10 to 30 wt.%, in terms of the total weight of the hydrophilic layer of the carrier.

In addition, the above-described preferred composition for local application, providing the possibility of extending the time spent Ambroxol or one of its pharmaceutically acceptable salts on the skin and/or mucosa compared to non-ionic hydrophilic cream 0.1%content Ambroxol according to the German Pharmacopoeia 2003 year of publication.

The next object of the present invention is the use of Ambroxol or one of its pharmacologically acceptable salts for the preparation of pharmaceutical compositions for local application intended for pain relief or to eliminate burning or itching of the skin and/or mucous membranes, preferably for pain and eliminate the burning of mucous membranes, or itching and burning of the skin, it is most preferable for pain and eliminate igen what I mucous membrane.

The object of the present invention is also the use of Ambroxol or one of its pharmacologically acceptable salts for the preparation of pharmaceutical compositions for local application, intended for the treatment of inflammation.

Another object of the present invention is the use of Ambroxol or one of its pharmacologically acceptable salts for the preparation of pharmaceutical compositions for local application, intended for the treatment of pathological conditions selected from the group comprising a painful inflammation in the mouth or vaginal area, mosquito bites, skin allergic, immunological or idiopathic origin and accompanied by itching or burning hemorrhoids, preferably from the group comprising a painful inflammation in the mouth or vaginal area and accompanied by itching or burning hemorrhoids.

As examples of acids suitable for the formation of salts of Ambroxol, can be called hydrochloric acid, Hydrobromic acid, sulfuric acid, phosphoric acid, nitric acid, oxalic acid, malonic acid, fumaric acid, maleic acid, tartaric acid, citric acid, ascorbic acid and methansulfonate acid, preferred among which hydrochloric acid.

Gels, hydrophilic paste is oltuski and solutions

Proposed in the invention gels, hydrophilic paste, mash and solutions contain water in varying amounts and one or more auxiliary substances from the group comprising natural, semisynthetic and synthetic polymers, inorganic gelling compounds, flavors, fragrances, sweeteners, dyes, preservatives, lower alcohols, polyols, pH regulators, activators absorption and girotropnye soljubilizatory.

It is suitable for use polymers include pharmaceutically acceptable compound selected from the group comprising gum Arabic, cellulose, cellulose derivatives, preferably nonionic and mucoadhesive derivatives of cellulose, most preferably methylcellulose (MC), carboxymethylcellulose (CMC) and its salts, hydroxypropylcellulose (GOC), hydroxyethyl cellulose (SCE), hypromellose (HPMC) and metilcellulose (YEC), copolymers vinylalcohol ethers with maleic anhydride and their salts, gelatin, pectin, polyethylene glycol (PEG), polyvinyl alcohol (PVA), polyvinylpyrrolidone (PVP), tragakant, carrageenan, xanthan gum, chitosan chloride chitosan, agarose, agar, alginates, poloxamer, starch, derivatives of starch, guar gum, galactomannan, polyacrylates, cross-linked polyacrylates, polyhydroxyethyl, polyhydroxy the l - and polyhydroxyethylmethacrylate.

It is suitable for use inorganic gel-forming compounds include colloidal silica and bentonite.

It is suitable for use lower alcohols according to the present invention include ethanol, 1-propanol and 2-propanol.

It is suitable for the application of the polyols include compounds selected from the group including ethylene glycol, propylene glycol, glycerin and polyalcohols, xylytol, preferably glycerol, sorbitol and ▫ maltitol.

It is suitable for use pH regulators and activators absorption include the same compounds as mentioned below in the section "Hydrophilic ointments, pastes, creams and lotions" auxiliary substances.

Girotropnye soljubilizatory, fragrances, dyes, sweeteners and preservatives can be used in pharmaceutically acceptable amounts.

For the preparation of the above-described hydrophilic paste or mash you can add insoluble inorganic fine grinding, for example zinc oxide, titanium dioxide.

Proposed in the invention mucoadhesive patches consist of at least one hydrophilic layer and not necessarily more hydrophobic the back or top layer, which in some cases may be connected with mucoadhesive layer separate connection layer.

The hydrophilic layer contains the SBA is oxol or one of its pharmaceutically acceptable salts, for example contains Ambroxol at a concentration factor of 1 to 50 wt.%, preferably from 5 to 40 wt.%, most preferably from 10 to 30 wt.%, in terms of the total weight of the dried hydrophilic layer.

Hydrophilic mucoadhesive layer is formed of one or more natural, semisynthetic or synthetic hydrocolloid polymers and optionally one or more plasticizers. In addition, hydrophilic mucoadhesive layer may also contain pharmaceutically acceptable auxiliary substances, for example affecting the viscosity and/or flexibility auxiliary agents, crystallization inhibitors, flavors, fragrances, sweeteners, dyes, preservatives, lower alcohols, activators absorption, pH regulators and/or girotropnye soljubilizatory.

The rear or outer layer formed of natural, semisynthetic or synthetic film-forming compound which is insoluble or poorly soluble in water and has a lower mucoadhesive properties compared with hydrocolloid polymer contained in the hydrophilic layer, and which is preferably selected from the group of polyacrylates and cellulose derivatives. In a preferred embodiment, the back or top layer contains one or more plasticizers and optional the strong flavors, fragrances, sweeteners and dyes. To get back or top layer of film-forming component can be used in the form of an aqueous dispersion containing additional additives to ensure its stabilization and/or contributing to plenkoobrazovatel, such as surfactants, preservatives or antispyware.

The back or top layer may contain separately obtained and suitable for pharmaceutical use plastics (polymers)such as polyethylene, polyethylene terephthalate, polypropylene, and/or polyvinyl chloride.

Mucoadhesive patch may also include a connecting layer for bonding the functional layers. Such a connecting layer formed by the polymer, with the appropriate level of adhesion, and optionally contains a plasticizer, dye and other influencing adhesiveness and/or flexibility excipients.

It is suitable for use hydrocolloid polymers include compounds selected from the group comprising mucoadhesive derivatives of cellulose, such as methylcellulose (MC), carboxymethylcellulose (CMC), hydroxypropylcellulose (GOC), hydroxyethyl cellulose (SCE), hypromellose (HPMC) and metilcellulose (YEC), gelatin, soluble Brahma the s and their pharmacologically acceptable derivatives, pectin, tragakant, alginic acid and its pharmaceutically acceptable salt, guar gum, gum karaya, polyethylene oxide, polyvinyl alcohol (PVA), polyvinylpyrrolidone (PVP), polyvinyl acetate, copolymers vinylalcohol ether with maleic anhydride and their pharmacologically acceptable salts, polyacrylates, cross-linked polyacrylates, polyhydroxyethylmethacrylate, polyhydroxyethylmethacrylate, polyhydroxyethylmethacrylate and mixtures of these compounds with polyisobutylene.

As a film-forming compounds can be used regenerated cellulose (cellophane), hydrophobic derivatives of cellulose, such as hydroxypropylcellulose (GOC), ethylcellulose (EC) or cellulose acetate, polyacrylates, polymethacrylates, polyhydroxyethylmethacrylate, polyhydroxyethylmethacrylate or polyhydroxyethylmethacrylate.

As plasticizers can be used phthalates, such as dibutyl phthalate, sebacate, such as dibutylsebacate, adipate, such as dibutyltin, polyols, such as alkalophile, glycerin or polyethylene glycol, polyalcohols, xylytol, for example sorbitol or ▫ maltitol, triacetin or triethylcitrate.

As the polymer binder, you can use agar, polyvinylpyrrolidone, polyvinyl alcohol, polyacrylate, polymethacrylate, polyhydroxyethylmethacrylate, polyhydroxyethyl ethacrylate or polyhydroxyethylmethacrylate, as well as derivatives of cellulose, such as methylcellulose (MC), carboxymethylcellulose (CMC) or hypromellose (HPMC).

For use as pH regulators and activators absorption suitable compounds are described below in the section "Hydrophilic ointments, pastes, creams and lotions".

Used according to the invention girotropnye soljubilizatory, flavourings, colourings, sweeteners and preservatives are pharmaceutically acceptable excipients.

Mucoadhesive tablets

Proposed in the invention mucoadhesive tablets contain Ambroxol or one of its pharmaceutically acceptable salts in a concentration that corresponds to the content of Ambroxol from 0.1 to 30 wt.%, preferably from 1 to 20 wt.%. In addition mucoadhesive tablets contain at least one mucoadhesive polymer and optional additional excipients, such as binders, fillers, regulators fluidity and lubricants. In some cases mucoadhesive tablets may also contain pH regulators and/or activators absorbed. In addition, the composition mucoadhesive tablets can also include fragrances, flavors, sweeteners and/or dyes.

It is suitable for use mucoadhesive polymer is according to the invention are cellulose or its derivatives, preferably nonionic derivative of cellulose, such as methylcellulose (MC), carboxymethylcellulose (CMC), hydroxypropylcellulose (GOC), hydroxyethylcellulose (SCE), hypromellose (HPMC) or metilcellulose (YEC), copolymers vinylalcohol ether with maleic anhydride or their salts, gelatin, pectin, polyethylene glycol (PEG), polyvinyl alcohol (PVA), polyvinylpyrrolidone (PVP), polyvinyl acetate, tragakant, carrageenan, xanthan gum, chitosan, chitosan chloride, agarose, agar, alginic acid or its salts, poloxamer, starch, derivatives of starch, guar gum, galactomannan, polyacrylate, polymethacrylate, polyhydroxyethylmethacrylate, polyhydroxyethylmethacrylate or polyhydroxyethylmethacrylate.

As binders and fillers used pharmaceutically acceptable excipients, such as starch or derivatives of starch, cellulose or its derivatives, dextrin, tragakant, gelatin, polyvinylpyrrolidone, polyvinyl alcohol, sugars such as sucrose or lactose, polyalcohols, xylytol or calcium phosphate.

The fluidity regulators and lubricants, it is preferable to choose among the pharmaceutically acceptable compounds from the group comprising talc, colloidal silicon dioxide, stearic acid and its salts, fats, such as glyceryltrinitrate, oski, the polyethylene glycol and fumaric acid.

Used according to the invention flavors, colors and sweeteners are pharmaceutically acceptable excipients.

For use as pH regulators and activators absorption suitable compounds are described below in the section "Hydrophilic ointments, pastes, creams and lotions".

Hydrophobic ointments, pastes, candles

Proposed in the invention ointments, pastes, candles consist of a lipophilic base, in which is dissolved or dispersed Ambroxol or in which are dissolved or dispersed one of its pharmaceutically acceptable salts. Such dosage forms to improve their adhesion to the mucosa and/or to prevent recrystallization may additionally contain pharmaceutically acceptable hydrocolloids. Equally such dosage forms may contain pharmaceutically acceptable fragrances, sweeteners, colouring agents, activators absorption, as well as preservatives and/or antioxidants.

Lipophilic base is chosen from the group comprising synthetic and natural hydrocarbons, for example paraffins, polyethylene and vaseline gel, vegetable and animal oils and fats, solid fats, synthetic glycerides, waxes and liquid polyalkyloxy.

Formats whitesky acceptable hydrocolloids are selected from the group including cellulose and its derivative, preferably nonionic and mucoadhesive derivatives, such as methylcellulose (MC), carboxymethylcellulose (CMC), hydroxypropylcellulose (GOC), hydroxyethyl cellulose (SCE), hypromellose (HPMC) and metilcellulose (YEC), copolymers vinylalcohol ethers with maleic anhydride and their salts, gelatin, pectin, polyethylene oxide, polyvinyl alcohol (PVA), polyvinylpyrrolidone (PVP), tragakant, carrageenan, xanthan gum, chitosan, chitosan chloride, agarose, agar, alginic acid and its salts, poloxamer, starch, derivatives of starch, guar gum, gum karaya, galactomannan, polyacrylate, polymethacrylate, polyhydroxyethylmethacrylate, polyhydroxyethylmethacrylate and polyhydroxyethylmethacrylate.

For use as preservatives, antioxidants and activators absorbed fit any described below in the section "Hydrophilic ointments, pastes, creams and lotions".

Hydrophilic ointments, pastes, creams and lotions

Proposed in the invention, hydrophilic ointments, pastes, creams and lotions consist of a lipophilic base, and surface-active substances such as emulsifiers for the formation of emulsions of the type oil-in-water" and/or "water in oil". Such dosage forms can also choose to add water in various quantities. In the depending on the water quantity and type of emulsifier system can be an emulsion of the type oil-in-water" or "water in oil". According to the invention such dosage forms contain Ambroxol or its salts in a concentration of from 0.1 to 50%, preferably from 1 to 40%, most preferably from 1.5 to 5% in the case of water-containing systems and from 5 to 30% in the case of anhydrous systems. Along with Ambroxol and its pharmaceutically acceptable salts in the composition of these dosage forms can also include preservatives, antioxidants, activators absorption, polyols, contributing to the spreading means, thickeners, dyes, flavors and fragrances and pH regulators.

For use as lipophilic bases suitable the following pharmaceutically acceptable excipients or mixtures thereof:

- hydrocarbons, such as white petrolatum, yellow petrolatum, liquid or plastic paraffin, ceresin, microcrystalline wax, paraffin oil, polyethylene, squalene or perhydrosqualene,

- glycerides, such as partial glycerides, polyglyceryl, mono-, di - or triglycerides,

fatty acids, such as stearic acid, palmitic acid or oleic acid,

fatty oils of vegetable origin, such as oil from the seeds of the cucumber herbs, oil from the seeds of the Thistle, peanut oil, coconut oil, or oil from corn germ, (semi)synthetic fatty oils, such as triglycerides medium is nd the length of the chain,

fatty and solid glycerides of vegetable origin, for example utverjdenie peanut oil, castor oil or cocoa butter,

fats of animal origin such as lard, or semi-synthetic fats, such as cured fat or fat oil from the fruit of the tree,

natural and synthetic waxes, such as yellow beeswax, bleached beeswax, microcrystalline wax, beeswax, cetylpalmitate or its derivatives, preferably acetylated wax, polyethylene wax, tetravinyl wax or THG-wax,

- resin, such as rosin, or

- silicones, such as silicone oil, Dimethicone, simethicone or cyclomethicone.

For use as surface-active substances suitable for the following pharmaceutically acceptable excipients:

- anionic emulsifiers, such as stearates, alkali metal, preferably potassium stearate, or metallic stearates, preferably aluminum monostearate, amine Soaps, preferably triethanolamine or triethanolamines, as well as alkyl sulphates, preferably sodium dodecylsulfate,

- cationic emulsifiers such as Quaternary ammonium compounds, preferably benzylaniline or cetylpyridinium,

- amphoteric emulsifiers, such as natural or synthetic is their phospholipids, first of all, lecithin, phosphatidylcholine, phosphatidylethanolamine, phosphatidylglycerol, phosphatidylinositol, phosphatidylserine or sphingomyelin, or betaine,

- nonionic emulsifiers, such as higher fatty alcohols, preferably cetyl alcohol, stearyl alcohol or cetylstearyl alcohol partial esters of polyhydric alcohols, preferably esters of fatty acids and ethylene or propylene, most preferably monostearate or distearate of ethylene glycol or propylene glycol monostearate, fatty acid esters and glycerol, preferably monopalmitate glycerin, dipalmitate glycerin, tripalmitin of glycerol, monostearate of glycerol, monoisostearate glycerin, distearate glycerin, diisostearate glycerin, tristearate glycerin, trihydroxystearin glycerin, monooleate glycerin or dioleate glycerol esters of fatty acids and sorbitan, preferably corbicular, orbitalia, armitstead, servicemanual, servicesecurity or sarbatorile, ethers and esters of polyethylene glycol, mainly ethers of fatty alcohols and polyethylene glycol, preferably lauric ester of polyethylene glycol, cetyl ether glycol stearyl ether, polyethylene glycol, cetylstearyl ether of polyethylene glycol or ministratively ether polietilene is Kolya, esters of fatty acids and of polyethylene glycol, preferably monolaurate of polyethylene glycol, polyethylene glycol monostearate, distearate of polyethylene glycol, steelsheet of polyethylene glycol or ricinoleate of polyethylene glycol, fatty acid esters, sorbitan and polyethylene glycol, preferably Polysorbate, esters of fatty acids, glycerol and polyethylene glycol, preferably glycerol monostearate and polyethylene glycol, DISTEARYL glycerol and polyethylene glycol, hydroxystearic glycerol and polyethylene glycol, tripalmitin glycerol and polyethylene glycol, trilinolein glycerol and polyethylene glycol, Triolet glycerol and polyethylene glycol, ricinoleic glycerol and polyethylene glycol or cocoat glycerol and polyethylene glycol, stearic alcohol, preferably cholesterol or alcohol, wool wax, and block copolymers of polyethylene oxide/polypropyleneoxide, preferably poloxamer, wool wax or wool alcohols of the wax, and a mixture of two or more of these emulsifiers.

For use as preservatives according to the invention is suitable for the following connections:

the alcohols and phenols, such as ethanol, isopropanol, benzyl alcohol, chlorobutanol, phenethyl alcohol, Phenoxyethanol, phenol, chlorocresol, thymol or triclosan,

- carboxylic acids and their salts, such as benzoic acid, benzo is tons of sodium, sorbic acid, potassium sorbate, RNV-ether (4-hydroxybenzoate), preferably methyl-4-hydroxybenzoate, ethyl-4-hydroxybenzoate, propyl-4-hydroxybenzoate or butyl-4-hydroxybenzoate, as well as their connections with sodium,

- nitrogenous compounds, such as benzylaniline, chlorhexidine, pyrithione zinc or CIS-1-(3-chlorallyl)-3,5,7-triaza-1-azoniabicyclo, or

- propylene carbonate, and mixtures of two or more of these preservatives.

For use as antioxidants according to the invention suitable natural antioxidants, such as ascorbic acid, salicylic acid or α-tocopherol, synthetic antioxidants, such as esters of ascorbic acid or Gallic acid, primarily palmitoylcarnitine acid or propylgallate, synthetic antioxidants, such as butylhydroxyanisole that is equivalent or sulphites, primarily sodium bisulfite, complexing agents, such as medicinova acid or sodium salt etc, as well as a mixture of two or more of these antioxidants.

For use as polyols according to the invention is suitable glycerin, polyalcohols, xylytol, such as sorbitol, mannitol, ▫ maltitol or smalltit, ethylene glycol, propylene glycol, hexyleneglycol or glycols.

For use as a contributing Rast is aniu means according to the invention suitable myristoleate, isopropylmyristate, isopropyl, isopropylene, diisopropylamide and debutylation.

For use as pH regulators according to the invention is suitable acid, such as acetic acid, tartaric acid, citric acid, lactic acid, hydrochloric acid, sulfuric acid or phosphoric acid, bases such as ammonia, sodium hydroxide, potassium hydroxide, lithium hydroxide, aluminum hydroxide or trometamol, as well as salts such as sodium bicarbonate, monohydratefast sodium, sodium dihydrophosphate, monohydratefast potassium dihydrophosphate potassium, sodium chloride, sodium citrate, sodium oxalate, sodium lactate, calcium lactate, magnesium sulfate, monohydrocalcite ammonium or demoniality.

For use as activators absorption according to the invention is suitable urea, dimethyl sulfoxide, sodium salt of hyaluronic acid, alkanols, such as lauric alcohol or alerby alcohol, alcamovia acids, such as oleic acid, 1-dodecylsulfate-2-he, ethylene glycol, propylene glycol or menthol and other activators absorption of groups of substances, including 1-acyclicity, 1-allpolicies, 1-allshare, 2-n-arylcyclohexylamine, 2-n-acyl-1,3-dioxolane (SEPA), 1,2,3-triacylglyceride, 1-alkanols, 1-alcamovia acid, 1-allylacetate, 1-alkylamines followed, 1-alkyl-n-alquilo oxyethylene, 1-alkalinity, n-alkyl-β-D-thioglucoside, 1-acylglycerides, 1-alkylpiperidines, 1-alkylpolyoxyethylene, 1-alkyl-2-pyrrolidone, allylacetate, alkalophile, alkylarylsulfonate, alkylphosphonate, alkyl sulphates, vallaccia, diacyl-N,N-diethylaminoacetate, diacyl-N,N-dimethylaminopropionic and fenilalkilaminov.

As thickeners can be used natural, semisynthetic and synthetic polymers, and inorganic gelling compounds listed above in the description of gels and hydrophilic paste.

Used according to the invention fragrances, dyes and fragrances are pharmaceutically acceptable excipients.

Pencils

Proposed in the invention pencils contain from 0.1 to 50 wt.%, preferably from 1 to 45 wt.%, most preferably from 2 to 40 wt.% Ambroxol or its pharmaceutically acceptable salts. Along with this, the offered invention pencils contain from 4 to 8 wt.% sodium Soaps, primarily sodium Soaps of palmitic acid, stearic acid, stearamide and Staromonetnyi, as well as ethanol, isopropanol and/or water in variable mass quantities. In another embodiment, the active substance can also be implemented in the basis of one or more glycols with different length of the second chain to obtain the corresponding pencil.

In addition, we offer in the invention pencils may contain emulsifiers, preservatives, antioxidants, contributing to the spreading means, polyols, activators absorption and fragrances. Such excipients can be selected from the respective groups of compounds described above in the section "Hydrophilic ointments, pastes, creams and lotions".

Proposed in the invention dosage forms are prepared in known literature methods.

The following are some specific examples proposed in the invention dosage forms (compositions). These examples are only illustrative and do not limit the scope of the invention.

Examples

Example 1: Solution 1%content of Ambroxol hydrochloride

Amount [g/100g]
Hydrochloride Ambroxol1,0
Glycerol 85%20,0
Ethanol 96%5,0
Menthol0,01
Mint flavor0,02
Indigocarmine is 85% (dye) 0,000015
Purified water73,97

Example 2: the Gel with a 3%content of Ambroxol hydrochloride

Amount [g/100g]
Hydrochloride Ambroxol3,0
Polyvinylpyrrolidone, type 9030,0
Purified water67

Example 3: the Gel with 0.5%content hydrochloride Ambroxol

Amount [g/100g]
Hydrochloride Ambroxol0,5
The polyethylene glycol 40049,75
Polyethylene glycol 100049,75

Example 4: the Gel with 2%content of Ambroxol hydrochloride

Amount [g/100g]
Hydrochloride Ambroxol2,0
Tartaric acid0,1
Benzylaniline0,01
Hydroxyethylcellulose5,0
Sodium salt of saccharin0,03
Glycerol 85%10
Fragrant substance (flavor with a refreshing cooling effect, the firm Düllberg, Hamburg)0,24
Blue patented V (dye, manufactured by Givaudan Deutschland GmbH, Dortmund)0,003
Polysorbate 801,5
Purified waterto 100.0

No swelling ingredients dissolved in water. To the resulting solution was added gelling components and allow to swell. The mixture is gently stirred to obtain a homogeneous solution or formation of a homogeneous gel.

Example 5: Mucoadhesive patch with a three-layer structure

Number in%, calculated on the dry weight of the layer
The layer of hydrocolloid polymerHydrochloride Ambroxol20
The hypromellose72
Propylene glycol8
The back layerEthylcellulose (type 14)90
Propylene glycol10
The connecting layerPolyvinylpyrrolidone, type 90100

Example 6: Mucoadhesive patch with a two-layer structure

Number in%, calculated on the dry weight of the layer
The layer of hydrocolloid polymerHydrochloride Ambroxol20
The hypromellose72
Propylene glycol8
Back with the Oh Ethylcellulose (type 14)49,1
Sodium lauryl sulfate2,4
Cetyl alcohol3,0
Dibutyl45,5

The ingredients are dissolved in a suitable solvent, for example isopropanol and/or water, and the bulk solution is applied on a suitable non adhesive backing layer of the desired thickness with the formation of the film, which is allowed to dry. Hydrocolloid layer and the back layer can also be manufactured separately from each other and then glued one upon the other with a solution of a binder or both layers can directly apply one to another in bulk. In the manufacture of dosage forms of the above examples of hydrocolloid layer was applied with a filling such a rate that after drying, it is the specific gravity (weight, referred to the unit area) was about 0.02 g/cm2. Unit weight of the back layer was approximately 0.015 g/cm2in example 5, and 0.06 g/cm2example 6. The specific gravity of the connecting layer was 0.02 g/cm2. The thickness of the layers, in principle, it is possible to vary and optimize the way the dosage of active ingredient per unit area and it is the logical properties of the film, for example, stickiness or flexibility.

Example 7: Mucoadhesive tablets from 1.76%content hydrochloride Ambroxol

Amount [%]
Hydrochloride Ambroxol1,76
Hydroxypropylcellulose (L-MPC LH 21 company ShinEtsu)73,31
Polyacrylate (carbopol 940)24,44
Magnesium stearate0,49

The ingredients are mixed among themselves and from the mixture obtained in tablet press machine pressed tablets of desired shape, preferably with a flat or slightly convex sides with a height of the convex part from about 0.5 to 2 mm.

Example 8: Candles containing Ambroxol hydrochloride 500 mg

Amount [g/candle]
Hydrochloride Ambroxol0,5
The cured fat3,0

Cured fat is melted in a water bath. In the molten basis suspended hydrochloride ambrox the La, the resulting mixture is poured into the appropriate shape and leave to cool until hardened candles.

Example 9: Mucoadhesive hydrophobic ointment with 30%content of Ambroxol hydrochloride

Amount [%]
Hydrochloride Ambroxol30
Paraffin33,25
Polyethylene2,5
Gelatin16,7
Pectin16,7
Sodium salt of carboxymethylcellulose16,7

Example 10: Mucoadhesive hydrophobic ointment with 30%content of Ambroxol hydrochloride

Tragakant powder
Amount [%]
Hydrochloride Ambroxol30,0
The copolymer vinylmation ether with maleic anhydride10,0
Carboxymethylcellulose10,0
10,0
Paraffin38,0
Polyethylene2,0

Hydrocolloids are mixed among themselves and add in the gel of polyethylene and paraffin components. In this basis, then suspended hydrochloride Ambroxol.

Example 11: Hydrophilic ointment with 10%content of Ambroxol hydrochloride

Amount [g]
Hydrochloride Ambroxol10,0
White petrolatum31,5
Liquid paraffin31,5
Cetosteatil alcohol24,3
Cetostearyl sodium2,7

White vaseline, liquid paraffin, cetosteatil alcohol and cetostearyl sodium melted in a water bath. The resulting melt is suspended hydrochloride Ambroxol and the resulting mixture is stirred until it gelled.

Example 12: Hydrophilic cream with an emulsion of oil-in-water" and from 2.1%to the content of Ambroxol hydrochloride

Amount [g]
The hydrophilic phaseHydrochloride Ambroxol2,1
Purified water67,9
Lipophilic phaseWhite petrolatum10,5
Liquid paraffin10,5
Cetosteatil alcohol8,1
Cetostearyl sodium0,9

White vaseline, liquid paraffin, cetosteatil alcohol and cetostearyl sodium melted in a water bath. To this mixture add Ambroxol hydrochloride, dissolved in heated water, and the resulting mixture is stirred until it gelled.

Example 13: Hydrophilic cream with an emulsion of oil-in-water" and from 1.2%content hydrochloride Ambroxol

Amount [g]
Guide Oficina phase Hydrochloride Ambroxol1,2
Purified water39,5
Propylene glycol9,9
Glycerol monostearate and polyethylene glycol 1006,9
Lipophilic phaseWhite petrolatum25,2
Triglycerides medium chain length7,4
Cetyl alcohol5,95
Glycerol monostearate3,95

White petrolatum, triglycerides of medium chain length, cetyl alcohol and glycerol monostearate melted in a water bath. In purified water mixed propylene glycol and glycerol monostearate and polyethylene glycol 100 and the mixture is heated to approximately the temperature of the oil phase. In the aqueous mixture is dissolved hydrochloride Ambroxol. Then, the hydrophilic phase is added to the lipophilic phase. The resulting mixture is stirred until it gelled.

Example 14: the Pencil on the basis of sodium stearate from 2.95%content hydrochloride Ambroxol

Amount [g]
Hydrochloride Ambroxol3,0
Ethanol 96%86,0
Stearic acid6,0
Glycerin6,0
Sodium hydroxide0,84

Stearic acid, glycerin and the sodium hydroxide is dissolved in ethanol (96%). To the resulting solution was added the hydrochloride Ambroxol and the solution is poured on the appropriate forms.

Example 15: Pencil polyethyleneglycol with a 30%content of Ambroxol hydrochloride

Amount [g]
Hydrochloride Ambroxol15,0
Polyethylene glycol 100030,0
Polyethylene glycol 6005,0

Polyethylene glycol 1000 and polyethylene glycol 600 melted in a water bath, the resulting melt is suspended hydrochloride Ambroxol and the solution poured into with the relevant forms.

1. The application has anti-inflammatory and mestnoanesteziruushim properties, pharmaceutical compositions containing Ambroxol or one of its pharmacologically acceptable salts, for local use in skin disorders, selected from the group comprising pain, burning, itching, inflammation, mosquito bites and redness allergic, immunological or idiopathic origin, direct application to the skin.

2. The use according to claim 1, which contains Ambroxol in the form of its hydrochloride.

3. The use according to claim 1 or 2 in the form of a drug selected from the group including gels, hydrophilic paste, mash and solutions.

4. The use according to claim 3, characterized in that the content of Ambroxol is from 0.1 to 20%.

5. The use according to claim 1 or 2 in the form of a drug selected from the group including candles, hydrophobic pastes, ointments, creams, lotions and pencils.

6. Use according to one of claims 1 to 5, providing the possibility of extending the time spent Ambroxol or one of its pharmaceutically acceptable salts on the skin compared to non-ionic hydrophilic cream 0.1%content Ambroxol according to the Pharmacopoeia of the 2003 edition.



 

Same patents:

FIELD: medicine.

SUBSTANCE: treatment of the patients with the facial nerve syndrome involves facial nerve block. A needle is pricked in the vertex of right angle with its one side being a straight line in parallel to the mastoid axis on its anterior surface. The other side is a line drawn along the lower edge of external acoustic meatus. The needle is pushed on towards the stylomastoid foramen that corresponds to a right angle bisector. The depth of needle penetration makes 8-16 mm.

EFFECT: method allows for considerably reduced risk of potential damages of significant adjacent anatomic formations, providing thereby adequate anaesthesia of facial nerve.

1 dwg

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely, to anesthesiologia and can be used as anesthesiological help in operations on upper extremity and clavicle. For this, needle is punctured at level C6 between the front and medium inter scalariform muscles. Needle is, first, directed caudally to insert local anesthetic into area of trunks of brachial plexus. Then, needle is pulled out at bit to insert anesthetic subcutaneously into area of surface cervical plexus. Now, needle is directed caudally toll upper edge of first rib to insert local anesthetic after paresthesia.

EFFECT: adequate anaesthesia of brachial plexus and upper cervical plexus by single occupuncture.

3 ex

FIELD: medicine.

SUBSTANCE: invention concerns medicine, particularly anesthesiology, and can be applied as anesthesiological medium in surgical correction of scoliotic spine deformations. It involves intravenous and endotracheal narcosis based on propofol, fentanyl and sevoflurane. Additionally epidural blockade by ropivacaine is performed in sequence at respective operated chest and waist level before each stage of surgical intervention and after operation.

EFFECT: adequate anesthesia both during surgical intervention and in post-operation period despite reduced dosage of narcotic analgetics due to optimal combination of various anesthesia types and sequential epidural anesthesia before each operation stage.

1 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to surgery and anaesthesiology, and can be used for pain management in early postoperative period following minimally invasive surgeries. Therefor, a principal stage of the limited-incision operation with use of an apparatus "Miniassistant" or a laparoscopic operation is followed by sticking a needle in a point along the abdominal midline 1-2 cm above a navel and 1 cm to the right perpendicularly to skin. The needle is penetrated therein to pierce aponeurosis of wide abdominal muscles to downfall sensation and inserted into round ligament of liver with adjusting the needle position visually. Then along the needle lumen, a conductor and a catheter are delivered through. Within the first postoperative days, exactly immediately after operations, then in 12 and 24 hours, Naropin dosed 2.5 mg/ml in 0.9% normal saline is introduced into the catheter.

EFFECT: method allows providing the most safe and effective anaesthesia with decreasing in doses of anaesthetising preparations and eliminating narcotic analgesics.

2 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine and can be used as local anaesthesia in various interventions. It is ensured by injecting a local anaesthetic solution with a vasoconstrictor under specified delivery pressure, specifically 0.7 to 1.6 atm.

EFFECT: method improves effectiveness local anaesthesia ensured by higher pressure of anaesthetic delivery with a vasoconstrictor, and thereby, such optimal anaesthetic vascular embarrassment maintained by the vasoconstrictor found in the composition that inhibits anaesthetic resorption in the systemic circulation.

2 ex

FIELD: medicine.

SUBSTANCE: way concerns medicine, namely to traumatology and orthopedy, and can be used for elimination of a painful syndrome at patients at traumas and diseases in the field of a humeral joint. For this purpose a line of the projection of an upper edge of arista of scapula is chosen as a reference point. On this line a point located on border of its internal and average third is determined. Needle puncture is performed in the received point. The needle is pulled to the area of scapula cutting from the puncture point, thus carry out it concerning back surface of the scapula.

EFFECT: maintenance of adequate and safe anaesthesia of a suprascapular nerve at the expense of its carrying out is more distal than a cutting of a scapula away from large nervous and vascular formations.

3 ex, 1 dwg

FIELD: medicine.

SUBSTANCE: invention concerns medicine, namely, to traumatology and orthopedy and can be used at treatment of patients with a facioscapulohumeral periarthrosis. For this purpose 2 ml of a 2% solution of lidocaine is injected intradermally. Introduction is carried out in a paravertebral manner along cervical and thoracal regions of a backbone, over a scapula and round a joint.

EFFECT: increase of facioscapulohumeral periarthrosis treatment efficiency, excluding possible complications, at the expense of use of local anaesthetic in doses, much less than recommended.

1 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to neurology, and can be used in treatment of peroneal syndrome. For this purpose in syringe preliminarily filled with 0.25-0.5 ml of dexamethasone and 8-10 ml of 1% lidocaine solution 2-4 ml of auto-blood are taken in. Intake of blood is performed from spongy tissue of fibula head. Mixture is introduced intraosteously into place of blood intake.

EFFECT: stimulation of reparative regeneration of bone tissue and osteogenesis, revascularisation of muscles, ligaments, nerve trunks, vessels, reduction of irritation of maximal number of intraosteous receptors, radial infiltration of affected surrounding tissues, which allows to eliminate secondary triggering zones.

1 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to neurology, and can be used in treatment of clinical presentations of multiple sclerosis. For this purpose autoblood 2-4 ml is sampled into the syringe prefilled with dexamethasone 0.25-0.5 ml and 1% lidocaine solution 8-10 ml. Autoblood is sampled from sponge tissue of scapular spine or spinous process of 4th thoracic vertebra. The mixture is injected intraosseously in autoblood sampling point or sponge tissue of the other bone.

EFFECT: therapy provides higher effectiveness with respect to clinical presentations of multiple sclerosis due to bone tissue metabolism activated and immunopoesis stimulation.

1 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to neurology, and can be used for regional upper-limp pain syndrome management ensured by autoblood 2-4 ml sampled in a syringe prefilled with dexamethasone 0.25-0.5 ml and 1% lidocaine solution 8-10 ml. Autoblood is sampled from spongy tissues of mesoscapula. The mixture is injected intraosseously in autoblood sampling point.

EFFECT: method provides improved therapeutic blocking effect ensured by complex influence on reparative regeneration of bone tissue and osteogenesis, revasculisation of muscles, ligaments, nerve trunk, vessels, reduced irritation of maximum intraosseous receptors.

1 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to pulmonology and phthisiology, and can be applied in case of necessity of carrying out diagnostic bronchoalveolar lavage in patients. For this purpose first, instillation of 5-7 ml of 10% fluimucil solution is performed during 4-6 minutes. 10 minutes after that fibrobronchscopy with diagnostic bronchoalveolar lavage by means of physiological solution is carried out.

EFFECT: method allows to increase efficiency of diagnostic procedure due to preliminary dilution of bronchial secretion, which ensures its free removal.

2 ex

FIELD: medicine.

SUBSTANCE: group of inventions relates to pharmaceutical compositions meant for treating diseases for which there is excess mucus in the respiratory channel, such as cytofibrosis and chronic obstructive pulmonary disease. Proposed is a composition which promotes excretion of mucus, containing one or several glycosaminoglycans and amino acid, which is a dry mixture lung inhalation. Proposed is use of a pharmaceutical composition, which promotes excretion of mucus, in therapy. A method of treating lung disease is proposed. A method of producing a composition, involving spray drying of one or more glycosaminoglycans, is proposed. A method of producing a composition, involving jet grinding of one or more glycosaminoglycans, is proposed.

EFFECT: possibility of effective dosing mucoactive agents in form of dry powders.

32 cl, 3 tbl, 4 dwg

FIELD: chemistry.

SUBSTANCE: invention concerns new compounds of the formula I: , where: a is 0 or whole number of 1 to 3; each R1 is selected independently out of the halogens; b is 0 or whole number of 1 to 3; each R2 is selected independently out of the halogens; W is linked in 3 or 4 position against the nitrogen atom in piperidine ring and is O; c is 0 or whole number of 1 to 4; each R3 is selected independently out of (1-4C)alkyls; or two groups of R3 are linked together forming (1-3C)alkylene or oxyrane-2,3-diyl; R4 is a bivalent group of the formula: -(R4a)d-(A1)e-(R4b)t-Q-(R4c)g-(A2)h-(R4d)i-, where each of d, e, f, g, h and i is selected independently out of 0 or 1; each of R4a, R4b, R4c and R4d is selected independently out of (1-10C)alkylene, where each alkylene group is unsubstituted or substituted by 1-5 substitutes selected independently out of (1-4C)alkyl, fluorine and hydroxy-; each of A1 and A2 is selected independently out of (3-7C)cycloalkylene, (6-10C)arylene, -O-(6-10C)arylene, (6-10C)arylene-O-, (2-9C)heteroarylene and (3-6C)heterocyclene where each cycloalkylene is unsubstituted or substituted by 1-4 substitutes selected independently out of (1-4C)alkyl, and each arylene, heteroarylene or heterocyclene group is unsubstituted or substituted by 1-4 substitutes selected independently out of halogens, (1-4C)alkyl, (1-4C)alkoxy-, -S(O)2-(1-4C)alkyl, hydroxy-, nitro- and trifluormethoxy; Q is selected out of -O-, -S(O)2-, -N(Qa)C(O)-, -C(O)N(Qb)-; -N(QC)S(O)2-, -S(O)2N(Qd)-, -N(Qe)C(O)N(Qf)- and -N(Qk) links; each of Qa, Qb, Qc, Qd, Qe, Qf and Qk is selected independently out of hydrogen, (1-6C)alkyl and A3, where alkyl group is unsubstituted or substituted by 1-3 substitutes selected independently out of fluorine, hydroxy- and (1-4C)alkoxy-; or together with nitrogen atom and R4b or R4c group to which they are linked they form 4-6-membered azacycloalkylene group; A3 is selected independently out of (3-6C)cycloalkyl, (6-10C)aryl, (2-9C)heteroalkyl and (3-6C)heterocyclyl, where each cycloalkyl is unsubstituted or substituted by 1-4 substitutes selected independently out of (1-4C)alkyl, and each aryl, heteroaryl or heterocyclyl group is unsubstituted or substituted by 1-4 substitutes selected independently out of halogen, (1-4C)alkyl and (1-4C)alkoxy-, if the number of adjacent atoms in the shortest chain between two nitrogen atoms, to which R4 is linked, lies within 4 to 16; R5 is hydrogen or (1-4C)alkyl; R6 is -NR6aCR6b(O), and R7 is hydrogen; either R6 and R7 together form -NR7aC(O)-CR7b=CR7c-; each of R6a and R6b is hydrogen or (1-4C)alkyl independently; and each of R7a, R7b and R7c is hydrogen or (1-4C)alkyl independently; or the pharmaceutically acceptable salts, solvates or stereoisomers of the claimed compounds. The invention also concerns compounds of the formula I, 1-[2-(2-chlor-4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinoline-5-yl)ethylamino]methyl}-5-methoxuphenylcarbamoyl)ethyl] piperidine-4-yl ether of biphenyl-2-ylcarbamine acid or its pharmaceutically acceptable salt or solvate, pharmaceutical composition, method of pulmonary disease treatment, method of bronchial lumen dilation for a patient, method of treatment of chronic obstructive pulmonary disease or asthma, method of obtaining the compound of the formula I, medicine based on it, and application of compounds described in any of the paragraphs 1, 13, 14, 24, 25, 26, 27 or 28.

EFFECT: obtaining of new biologically active compounds with high activity rate of both antagonist of muscarine receptors and β2 agonist of adrenergic receptors.

42 cl, 186 ex

FIELD: medicine.

SUBSTANCE: method involves introducing ozonized physiologic saline once a day during 30 min in addition to traditionally applied drugs. The ozonized solution has ozone in concentration of 100-150 mcg/l in the amount of 100-150 ml when treating children younger than 3 years. Children being elder then 3 years, ozone concentration is 200-250 mcg/l, its amount is 200-250 ml. The total therapy course is 5 days long. The traditionally applied drugs are not to be used within 30 min before and after ozonized physiologic saline application.

EFFECT: accelerated treatment course; no antibiotics being used; reduced risk of adverse side effects.

1 tbl

FIELD: pharmaceutical industry, in particular mucolytic pharmaceutical agent.

SUBSTANCE: claimed composition contains therapeutically effective amount of bromohexin as active ingredient and sugar, starch and stearinic acid salt as target additives. Pharmaceutical composition is provided in form of tablets.

EFFECT: composition with improved physical and pharmaceutical properties, such as dissolving and active ingredient releasing.

8 cl, 2 tbl, 4 ex

The invention relates to therapeutic tools, specifically setidentityproviderid N-substituted nitrogenous heterocyclic compounds and methods of producing such compounds, intermediate products used in obtaining, compositions containing such compounds and the use of such heterocycles

The invention relates to the field of medicine and for the application of polymer alkylarylsulfonates for effective inhibition of oxidant in chemical or biological system, as well as medications, including those polymeric compounds

FIELD: medicine.

SUBSTANCE: there are described oral dosage forms of risedronate containing safe and effective amount of a pharmaceutical composition containing risedronate, a chelating agent and an agent for effective delayed release of risedronate and the chelating agent in small intestine. The pharmaceutical composition is directly released in a small intestine of a mammal with ensuring pharmaceutically effective absorption of bisphosphonate together with or without food or drinks. Present invention essentially reduces interaction between risedronate and food or drinks which leads to that the active component of bisphosphonate becomes inaccessible to absorption. Thus, the final oral dosage form can be taken with and without food. Further, present invention covers delivery of risedronate and the chelating agent in a small intestine, essentially reducing irritation of upper gastrointestinal tract associated with bisphosphonate therapy. These advantages simplify previous, complicated regimens and can lead to more complete observance of the bisphosphonate therapy regimen.

EFFECT: present invention essentially reduces interaction between risedronate and food or drinks which leads to that the active component of bisphosphonate becomes inaccessible to absorption.

23 cl, 12 ex

FIELD: medicine.

SUBSTANCE: there are described oral dosage forms of risedronate containing safe and effective amount of a pharmaceutical composition containing risedronate, a chelating agent and an agent for effective delayed release of risedronate and the chelating agent in small intestine. The pharmaceutical composition is directly released in a small intestine of a mammal with ensuring pharmaceutically effective absorption of bisphosphonate together with or without food or drinks. Present invention essentially reduces interaction between risedronate and food or drinks which leads to that the active component of bisphosphonate becomes inaccessible to absorption. Thus, the final oral dosage form can be taken with and without food. Further, present invention covers delivery of risedronate and the chelating agent in a small intestine, essentially reducing irritation of upper gastrointestinal tract associated with bisphosphonate therapy. These advantages simplify previous, complicated regimens and can lead to more complete observance of the bisphosphonate therapy regimen.

EFFECT: present invention essentially reduces interaction between risedronate and food or drinks which leads to that the active component of bisphosphonate becomes inaccessible to absorption.

23 cl, 12 ex

FIELD: medicine.

SUBSTANCE: invention refers to chemical-pharmaceutical industry and concerns preparation of a solid dosage form for treating respiratory allergosis and arresting nasopharynx edema. There is offered a tableted medical product containing mixed active substance and excipient. As an active substance, it contains a corticosteroid preparation, and according to the invention, additionally contains an active substance presented with adrenaline or noradrenaline. The inside of a tablet contains the corticosteroid preparation, while the exterior contains adrenaline. As a corticosteroid preparation it contains dexamethasone, prednisolone or celestone. Also there is offered a tableted medical product that contains mixed active substance and excipient. As an active substance, it contains a corticosteroid preparation, and additionally contains active substances presented with adrenaline or noradrenaline, and also aminophylline and mesatone. The tablet is multilayered, its inside contains mesatone, the layer containing aminophylline adjoins the inside, then the layer containing the corticosteroid preparation is executed, and the exterior contains adrenaline or noradrenaline.

EFFECT: there is offered a tableted medical product.

4 cl, 3 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to pharmaceutical industry and concerns galenicals that ensure to improve intestinal absorption of the oral agents; to the method of making thereof, and also to application if lipid excipients combined with one or more surface-active substances for inhibition of an efflux pump.

EFFECT: invention allows improving intestinal absorption of the oral agents.

34 cl, 2 ex, 4 tbl, 5 dwg

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