Adhesive dosage forms

FIELD: medicine.

SUBSTANCE: invention refers to medicine. What is disclosed is a dosage form containing a base and a self-adhesive layer which contains a medicinal agent and covers at least one of the base sides; wherein the base consists of a polyester film of the thickness of 0.5 to 6.0 mcm, and a polyester non-woven material directly coupled with the film. The base is coated with the self-adhesive layer either directly or through an intermediate layer from the non-woven material.

EFFECT: adhesive preparation have sufficient elasticity for the purpose of tracking of the skin shape, as well as shows low ability to irritate the skin and high stability.

7 cl, 5 tbl, 7 ex

 

The technical field to which the invention relates

The present invention relates to adhesive dosage forms, comprising a substrate and a self-sealing adhesive layer which contains a drug and deposited at least on one side of the substrate.

Background of the invention

Adhesive dosage forms, which are superimposed on the surface of the skin, intended for the introduction of drugs into the body through the skin. When developing adhesive dosage forms necessary to achieve ease of use, flexibility to movements of the skin surface (flexibility), lack of skin irritation and the like, because the surface on which are superimposed the dosage form, is the surface of the skin.

In addition, the adhesive dosage forms required properties, such as resistance self-adhesive layer in General, and the drug over an extended period of time (stability during storage), and sufficient adhesion of self-adhesive layer with the substrate (chaining effect).

In Japan patent No. 2688778 disclosed an adhesive patch that is designed for the treatment of diseases, which consists of a substrate formed by applying a non-woven material on the basis, consisting of a film that has no holes; and a layer, with the holding of a drug, which is self-adhesive at ordinary temperatures and deposited on a substrate from the side of the nonwoven material. In the mentioned patent States that the substrate was prepared as follows: non-woven material applied to the film between the film and nonwoven material is placed sheet/film of hot melt adhesive and the obtained layered structure linked by heating; or non-woven material put on film, and between them is placed a binder adhesive. In addition, stated that this a sticky adhesive layer containing a drug and having self-adhesive properties at ordinary temperatures, demonstrates improved adhesion to the substrate due to the presence of non-woven material.

In Japan patent No. 3081858 disclosed an adhesive patch, which consists of a substrate obtained by the imposition of a polyester film having a thickness of 0.5-6 μm on a polyester non-woven material, having a density of from 5 to 20 g/m2; as well as self-adhesive layer applied to the substrate from the side of the nonwoven material. Argues that the imposition of a polyester film on non-woven polyester material is applied, for example, on film, any desired adhesive in a quantity calculated on dry substance. In addition, stated that described adhesive patch is improved for stephanieledigo layer to the substrate, as the adhesive tape disclosed in the above-mentioned Japan patent No. 2688778, and that the adhesive patch has a moderate samoderzhavie properties, due to the structure of the substrate, and from this point of view, it is very easy to use.

However, because these adhesive patches between the film and nonwoven material placed another material such as an adhesive sheet, hot-melt adhesives and the like (hereinafter referred to in this document collectively known as "binder"), the flexibility or pliability of these patches to movements of the skin may be degraded due to the stiffness of the binder. This trend is found mainly in adhesive plasters, substrates which are applied thin film. Furthermore, these adhesive patches while wearing the skin bring about skin discomfort (feeling of stiffness) due to the increased thickness of the substrate, which occurs due to the fact that the binder has a certain thickness. In addition, because of the increased thickness of the side edges of the substrate raises the possibility that contacts the side edges with the skin can sometimes irritate the skin when wearing the patch.

In addition, there is a probability that some medicines will react with the binder, being the I to the destruction of the latter and, thus, the impaired binding of the film with non-woven material with their separation from each other. There is also a concern that the destruction may be some drugs themselves. Thus, to apply such adhesive patches as commercial dosage forms will require additional studies of the structure of the substrate, the selection of drugs or similar actions.

In addition, in the case when the production of adhesive plaster adhesive solution containing an organic solvent, is applied directly to the nonwoven material, there is a possibility that the solvent contained in the adhesive the adhesive solution, which penetrated through the non-woven material, can destroy the binder, thereby breaking the adhesion between the film and nonwoven material and causing their separation from each other. To avoid this problem, for example, an adhesive solution containing an organic solvent, is applied on the separately manufactured gasket and dried, obtaining the self-adhesive layer, and then the resulting layer is transferred onto the substrate. However, this method is undesirable since the implementation of the above stages is difficult and the gasket, the presence of which in the product is not necessary, it is necessary to produce separately. After vetelino, the above-described adhesive patches have a low degree of freedom in the choice of the stages and from this point of view, there are opportunities for improvement.

In Japan patent No. 2939123 related to self-adhesive sheets, indicated that the nonwoven material obtained from a thermoplastic resin, can be applied to one side of the substrate opposite that containing the drug adhesive layer. However, this patent does not describe how to apply non-woven material on a substrate.

As mentioned above, the adhesive dosage forms, comprising a substrate in which the film and the nonwoven material bonded to each other directly, not disclosed in the technique known level.

The invention

In effect the above objective of the present invention is to develop adhesive dosage forms, which has sufficient flexibility to conform to the shape of the skin, and also has a low irritant effect on the skin and high resistance.

Accordingly, the invention relates to the next.

(1) Adhesive dosage form, including:

substrate; and

self-adhesive layer, which contains the drug and deposited at least on one side of the substrate,

where the substrate comprises a polyester film having a thickness of 0.5 to 6.0 μm, and Polief REGO nonwoven material, directly associated with the specified film.

(2) Adhesive dosage form under item(1), where the self-adhesive layer directly or through an intermediate layer deposited on a substrate from the side of the nonwoven material.

(3) Adhesive dosage form under item(1) or (2)where the polyester fiber in the specified non-woven material is directly associated with a part of the polyester film is attached to the specified non-woven material.

(4) Adhesive dosage form according to any one of paragraphs.(1)-(3)where the specified non-woven material has a density of 5-40 g/m2.

(5) Adhesive dosage form according to any one of paragraphs.(1)to(4), where the drug has in its molecule at least one primary, secondary or tertiary amino group.

(6) Adhesive dosage form according to any one of paragraphs.(1)-(5)where the specified film and the nonwoven material are connected to each other by the method of fusion.

(7) Adhesive dosage form according to any one of paragraphs.(1)to(6), where the self-adhesive layer deposited on a substrate from a side of the given film.

In adhesive dosage form of the present invention, the substrate comprises a polyester film having a thickness of from 0.5 to 6.0 μm, and a polyester non-woven material, which is directly attached to the polyester film without the use of binders. In adhesive dosage form according to the present invention incorporated in the substrate film itself is fine, and the stiffness of the binder under no circumstances does not affect the adhesive properties of the dosage form. Therefore, the adhesive dosage form of the present invention has satisfactory flexibility and ease of movement of the surface of the skin.

In addition, the film thickness itself is insignificant, the adhesive dosage form of the present invention does not require mandatory application of the binder, and the thickness of the layer of binder does not contribute to the thickness of the substrate. This allows you to make small the thickness of the adhesive dosage forms, and the specified adhesive dosage form is less unpleasant sensations (sensations of stiffness) of the skin. In addition, the adhesive dosage form of the present invention has an advantage from the point of view of the minor irritations of the skin caused by contact of the skin with the edge of the substrate while wearing the dosage form on the skin due to the small thickness of the edge of the substrate.

If self-adhesive layer deposited on a substrate from the side of the nonwoven material, self adhesive envelops polyester fiber non-woven fabric substrate. Therefore, self-adhesive shows excellent adhesion to the substrate.

In addition, in case when Malaysia adhesive layer deposited on a substrate from the side of the nonwoven material, direct binding of non-woven material with a film without a binder provided in the present invention, avoids the destruction of the binder due to the reaction of the medicinal product with the binder. Consequently, it is possible to avoid separation of the film from the non-woven material. Similarly, it is possible to avoid destruction of the medicinal product due to the reaction of the drug with the binder. Thus, in high-performance adhesive dosage forms of the present invention, in which the self-adhesive layer deposited on a substrate by non-woven fabric and non-woven material attached to the film without binders, almost can apply to a wide range of medicines.

In addition, if the self-adhesive layer deposited on a substrate by a non-woven material, adhesive dosage form of the present invention that do not contain binders, it is possible to avoid the destruction of the binder under the influence of organic solvent present in the adhesive solution layer and penetrating through the non-woven material, and, consequently, it is possible to avoid the necessity of separating these layers, even when there is a stage at which the adhesive solution layer containing the organic solution is tel, apply directly to the non-woven material. Therefore, if the self-adhesive layer is applied to the substrate from the side of the nonwoven material, adhesive dosage forms of the present invention are preferred because of the high degree of freedom in selection stages.

In addition to the above, if the self-adhesive layer deposited on a substrate from the side of the nonwoven material, adhesive dosage form of the present invention has excellent stability as possible to avoid the destruction of the binding agents in the reaction medicine/binder, the destruction of the medicinal product in the reaction with the binder and separation of non-woven material from the film due to the destruction of the binder.

Detailed description of the invention

Adhesive dosage form of the present invention includes a substrate and a self-sealing adhesive layer which contains a drug and deposited at least on one side of the substrate. The substrate includes a polyester film having a thickness of from 0.5 to 6.0 μm, and a polyester non-woven material directly related to the film. In the present description, the terms "polyester film", "polyester non-woven material" and "polyester fiber" means that corresponds to the public, film, non-woven material and fiber, each of which contains a polyester as its main component.

In the present invention the thickness of the polyester film should be from 0.5 to 6.0 μm. From the point of view of reducing skin irritation edges of the substrate, is preferred as the smaller the thickness of the substrate. From the point of view of practical applications, it is preferable to use ultra-thin film having a thickness of about 1-5 μm, in particular about 1.5 to 4.5 μm. If the film thickness is less than 0.5 μm, it is not applicable due to the complexity of the receiving substrate of the present invention when applying this film to the nonwoven material, which will be described below. If the film thickness exceeds 6 μm, the adhesive dosage form becomes rigid due to the film itself and gives discomfort (feeling of stiffness) when worn on the skin's surface.

Polyester non-woven material used in the present invention, consists of irregularly spaced polyester fibers. This material is preferred because it has a higher degree of surface roughness compared to woven or knitted polyester material, in which polyester fibers are geometrically correct, and, consequently, the formation of self-adhesive sticky with the HH on the substrate from the side of the nonwoven material leads to a satisfactory grip.

The density of the polyester non-woven fabric in the present invention are not specifically limited. However, from the viewpoint of reducing discomfort that may appear when worn on the skin surface, in the present invention preferably use a polyester nonwoven material having less density than the material of General use. Thus, the preferred density is from 5 to 40 g/m2more preferred from 5 to 25 g/m2even more preferred from 5 to 20 g/m2and most preferred from 8 to 20 g/m2.

If the density of the nonwoven fabric is less than 5 g/m2then there are cases when the self-adhesive layer applied to the substrate from the side of the nonwoven material, does not demonstrate sufficient adhesion to the substrate. If the density of non-woven material is more than 40 g/m2there are some cases when the adhesive dosage form when worn on the skin brings discomfort because of this non-woven material.

Incidentally, in case of non-woven material is connected with the film using a binder material, as in the traditional products, non-woven material having a lower density and a reduced thickness, can be used for, for example, improve flexibility and pliability adhesive medicinal F. RMI to deformation of the skin. However, you may receive the following problem. In this case, damage to the film binder penetrates through the non-woven material and reaches the side of non-woven material, which is the opposite of the film. If the substrate, in which there are layers of nonwoven material and a film is folded in a roll, the binder can contaminate the film side of the substrate.

This problem is eliminated direct bond film and nonwoven material without the use of binders, as in the present invention. Accordingly, the present invention is particularly preferred if the non-woven material has a low specific gravity. The terms "without the use of binders", "without the need for binders, binding substance is absent or does not contain binders", or similar expressions in the present description means the cases, which include the case when the adhesive dosage form mainly contains no binders, i.e. the case when the binder is present in small quantities, provided that it does not reduce the effect of the present invention.

The polyesters which are used to obtain the polyester film and polyester non-woven material is not specifically limited. Their examples include poly(ethyleneterephthalate), poly(butylene eftalit), poly(etiennette) and poly(butylnaphthalene). From the point of view of security (nontoxicity) for a living organism, convenience, practical and General use, etc. it is preferable to use a polyester composed mainly of poly(ethyleneterephthalate).

For example, it is possible to use a homopolymer of ethyleneterephthalate, a copolymer containing as a main structural unit ethyleneterephthalate links and optionally containing other ester units, a mixture of homopolymer of ethyleneterephthalate and polymer containing ester linkages, or the like.

For the formation of other ester units upon receipt of such copolymers or mixtures can be used, for example, the following dicarboxylic acids and diols. Suitable for application of the dicarboxylic acid include aromatic dicarboxylic acids such as isophthalic acid, diphenylcarbonate acid, dicarboxylic acid, which is derived from diphenyl simple ether, diphenylcarbonate acid and natalijagolosova acid, and aliphatic dicarboxylic acids such as adipic acid and sabotinova acid. Suitable for use diols include alkalophile, such as triethyleneglycol, tetraethyleneglycol and hexamethyleneimine, aromatic diols, such as gitahi is he, resorcinol and bisphenol A, aliphatic diols such as bis(hydroxyethoxyphenyl)sulfon and bis(hydroxyethoxyphenyl)propane and diethylene glycol.

The substance, which made the film, and a substance made of non-woven material, can be the same or different, provided that both substances are polyesters. From the viewpoint of improving compatibility between the film and nonwoven material and facilitate due to this direct link between them, it is preferable that both substances were identical. The term "identical" in this case implies that it is enough to apply the same monomers. Such polyesters, even when differences in the degree of polymerization, are "the same."

In the present invention requires that the non-woven material and the film were directly related to each other. The term "directly connected" in the present description means that the film and the nonwoven material are connected to each other, at least part of the surface they are in contact with each other, without the use of the component, located between them, for example, a binder. Methods of directly bonding a nonwoven material, the film is not specifically limited. For example, the binding is carried out by fusion of the film to the nonwoven material, at least part of the surface the displacement of the contact between them by heating, the action of the solvent, etc. From the point of view of getting rid of the danger associated with the use of an organic solvent, and facilities is preferred binding by fusing when heated.

Whether non-woven material and the film directly with each other or not can be judged based on the following criterion. Namely, if at least part of the surface of contact between the film and the nonwoven material in the substrate is investigated using instrumental analysis or similar method, and it is not detected components that differ from the film and nonwoven material, you can come to the conclusion that the non-woven fabric and film are directly connected with each other.

Incidentally, it is expected that the direct relationship polyester film with a polyester non-woven material provides an effect of improving the transparency of the substrate. It is assumed that partial melting polyester fiber non-woven material leads to a decrease of the surface area of the fibers of the nonwoven material, which causes a decrease in light scattering. In this case, as a result of improved transparency of the substrate can also expect the effect of facilitating the detection of foreign inclusions in adhesive formulations during their production.

In the present invention is a polyester fiber netcong the material can be directly connected preferably with a part of the polyester film, which are attached to non-woven material. Specifically, if the communicating part of the non-woven material, i.e., associated with a film of polyester fiber, relate to the film surface, in this case the area touch the communicating part may be the part of the area of non-woven material, which relates to the film surface, in case of non-woven material touches the surface of the film.

In case of polyester fiber non-woven material directly associated with a part of the polyester film to which is attached a non-woven material, some polyester fiber non-woven fabric is not associated with the film and, therefore, can move somewhat freely. These substrates are more flexible than the substrate, in which the non-woven material associated with the film through the binder. It is believed that poor flexibility of the substrate, in which the nonwoven material is bonded (glued) with a film layer of binder, is a consequence of the properties of the binders that during the gluing binding substance capable of flowing and, therefore, during the bonding of nonwoven material to the film covers almost the entire surface of contact between the nonwoven material and the binder. This substrate, in which the nonwoven material is bonded (glued) with a film layer of binder is about substance, is in a state in which a polyester fiber non-woven binding material associated with a polyester film through a binder, mainly in all areas of non-woven material. It is assumed that the substrate has a smaller share of polyester fiber non-woven material, which can freely move relative to the film and, therefore, this substrate has poor flexibility.

From this perspective, the share of polyester fiber non-woven material related to the film, i.e. the [100×(the area of the parts performing the binding fibers of non-woven polyester material with a film that relate to the film surface in the case, if the connecting part relate to the film surface)/(area of non-woven material applied to the surface of the film, in case of non-woven material placed on the surface of the film)] is preferably from 10 to 80%, more preferably from 20 to 70%. If the specified value is set to less than 10%, there is a fear that the strength of binding between the film and the nonwoven material may be insufficient. If this ratio exceeds 80%, there is a possibility that the substrate can give a feeling of resistance when worn on the skin.

The area of the parts engaged linking polyester fiber non-woven fabric with plank the th, which relate to the film surface, is a value, which is measured as follows. If it is difficult to observe fiber non-woven fabric, fused with the film, in the study from non-woven material using optical or electron microscope, implement the following methodology. Non-woven material associated with the film, with tear force using a commercially available adhesive tape or remove the plucking and explore film using an optical or electron microscope to locate remaining on the film traces binding. The foot print of binding calculated using image analysis by binarization. Alternatively, if the fiber is associated with a film of non-woven material are observed in the study from non-woven material using optical or electron microscope, the area occupied by the parts associated fiber nonwoven, which is directly estimated using image analysis by binarization.

In one of the embodiments of the present invention self-adhesive layer directly or through an intermediate layer deposited on a substrate from the side of the nonwoven material. In this embodiment, adhesive an adhesive that demonstrates satisfactory scale the s with the substrate, as briefly indicated herein above. This alternative implementation has certain advantages, for example, that the adhesive dosage form has excellent stability as largely can be prevented the destruction of the binder in the reaction medicine/binder, the destruction of the medicinal product as a result of interaction with the binder, as well as the stratification of nonwoven material and a film due to the destruction of the binder.

The term "marked" in the present description means that the self-adhesive layer deposited on the non-woven material without placing adhesive between the adhesive layer and non-woven material of any component. The term "applied through the intermediate layer" means that the self-adhesive layer applied to the nonwoven material through any component located between the self-adhesive layer and non-woven material, for example, through any layer, such as an underlying layer. Preferably, the underlying layer is a layer which improves the adhesion of the adhesive between the adhesive layer and non-woven material.

Examples of layers that improve the adhesion of the adhesive between the adhesive layer and non-woven material includes a layer containing acrylonitril, modified ethylenimines, and the layer containing polyethylenimine. Such layers are preferred because they result in obtaining satisfactory adhesion. It is assumed that this is due to the following reasons. The active amino groups in the layer containing an acrylic polymer modified with ethylenimine, or polyethylenimine form chemical bonds, such as ionic bonds or amide bond with the functional groups of the self-adhesive layer, such as a carboxyl group. Resulting in an improved adhesion of the adhesive between the adhesive layer and non-woven material.

Such acrylic polymer-modified ethylenimines, is an acrylic polymer modified with addition of structural units formed by the reaction of ethylenimine with the molecules of the acrylic polymer, which is accompanied by ring opening. This polymer can be obtained by reaction of ethylenimine carried out simultaneously with obtaining the acrylic polymer, or by prior receipt of acrylic polymer and its modification by interaction with ethylenimine. Polyethylenimine is a polymer having the repeating unit represented by the formula-CH2CH2-NH-.

Incidentally, in the case where the film and the nonwoven material are connected to each other with what omashu binder, the proportion of fibers of non-woven material, which can freely move relative to the film, as mentioned above, tends to be quite small. The result is a situation in which, if the self-adhesive layer as in this embodiment, deposited on a substrate from the side of the nonwoven material, there are difficulties with obtaining adhesion between the nonwoven material and self-adhesive layer in a short period of time, or obtained adhesive dosage form has poor adhesion. On the other hand, in the case of reducing the number of binders to increase the proportion of fibers of non-woven material capable of free movement, in anticipation of a normal clutch, it becomes difficult to obtain satisfactory strength of bonding between the nonwoven material and a film.

In contrast to the situation described, particularly with the embodiment of the invention, in which a polyester fiber non-woven material directly associated with a part of the polyester film to which is attached a non-woven material, the substrate has a fiber non-woven fabric, freely moving relative to the film. Accordingly, if the production of adhesive dosage forms self-adhesive layer is applied on the substrate side of the nonwoven mother is La, sufficient adhesion of self-adhesive layer to the substrate can be achieved in a short period of time. Consequently, it is possible the efficient production of adhesive dosage forms.

The application method self-adhesive layer on the substrate from the side of the nonwoven material are not specifically limited. For example, you can use the method in which the solution is self-adhesive sticky substance applied directly to the substrate from the side of non-woven material and then dried to obtain self-adhesive layer (direct formation), or a method in which a solution of an adhesive substance applied to separately manufactured gasket and dried to obtain self-adhesive layer, and then transfer the layer onto the substrate from the side of the nonwoven material.

On an adhesive should be used for the formation of a self-adhesive layer, not imposed specific restrictions. Examples of such substances include acrylic adhesives containing acrylic polymer; adhesives based on rubber, such as block copolymers of styrene/isoprene/styrene block copolymers, styrene/butadiene/styrene, polyisoprene, polyisobutylene, and polybutadiene; adhesives based on silicone, such as silicone rubbers, polymers based dimethylsiloxane and polymers OS is ove diphenylsiloxane; adhesives based on vinyl ethers, such as poly(vinylethylene ether), poly(vinylethylene ether) and poly(minimizebutton ether); adhesives based on vinyl esters, such as copolymers of vinyl acetate/ethylene; and adhesives based on polymers of esters obtained from derivatives of carboxylic acids, for example, dimethyl terephthalate, dimethylsulfate or dimethylphthalate and polyhydric alcohols, e.g. ethylene glycol. You can apply the same adhesive, or a combination of two or more adhesives.

Among these adhesives are preferred acrylic adhesive. The reason for this is that acrylic adhesives are easily cross-linking and form a self-adhesive layer, which can hold a significant amount of liquid ingredient and, therefore, to create a feeling of softness when worn on the skin. Examples of such acrylic adhesives include adhesives based on esters of acrylic acid, containing as a main component a polymer obtained by polymerization of one or more monomers, which is C2-18alkylamino esters of (meth)acrylic acid. From the viewpoint of satisfactory adhesion to human skin, the preferred adhesive ve is esta based on esters of acrylic acid, obtained using acrylic acid as a copolymer ingredient. From the point of view of ease of re-overlays/deletions, preferred adhesives obtained by copolymerization of 2-ethylhexyl acrylate as Olkiluoto ether (meth)acrylic acid, acrylic acid and N-vinyl-2-pyrrolidone in a weight ratio of (40-99,9):(0,1-10):(0-50).

On the other hand, from the viewpoint of the stability of the medicinal product, the preferred adhesives based on rubber. Examples of such adhesives based on rubber include adhesive containing as a main component, at least one component selected from polyisobutylene, polyisoprene and copolymers of styrene/diene/styrene. Preferred is an adhesive containing a mixture of high molecular weight polyisobutylene having srednevozrastnoe molecular weight of from 500,000 to 5500000, and low molecular weight polyisobutylene having srednevozrastnoe molecular weight of from 10,000 to 200,000 mass ratio of from 95:5 to 5:95, since this adhesive is a high stability of drugs and there is the possibility of combining the necessary forces of adhesion and cohesion. If necessary, you can add a substance enhancing the adhesiveness.

The thickness of the adhesive the adhesive layer does not impose the I specific restrictions. However, as a rule, it is from 10 to 200 μm, preferably from 15 to 150 microns.

If necessary, the composition of the self-adhesive layer may be included organic liquid ingredient compatible with the adhesive, in an amount of from about 0.1 to 60% by weight, preferably from about 30 to 50% by weight, in order to give a self-adhesive layer, a feeling of softness and to reduce the irritating properties when worn on the skin surface. If necessary, during the formation of the self-adhesive layer can be carried out processing of causing cross-linking of polymer molecules.

Examples of organic liquid ingredients include glycols such as ethylene glycol, diethylene glycol, propylene glycol, triethylene glycol, polyethylene glycol and polypropyleneglycol; fats and oils such as olive oil, castor oil, squalene, and lanolin; hydrocarbons such as liquid paraffin; various surfactants; atoxicity alcohol; monoether of glycerol, such as monoglyceride, oleic acid monoglyceride Caprylic acid and a monoglyceride of lauric acid; diesters of glycerol, truefire glycerol and mixtures thereof; alkalemia esters of fatty acids, such as tillaart, isopropylmyristate, strideselect, octylpyrimidine, isopropyl, etiloleat and d is isopropylacetate; fatty acids such as oleic acid and Caprylic acid; and other compounds, including N-organic and 1,3-butanediol.

Examples of processing, leading to cross-linking, include physical cross-linking under the action of radiation, wherein the radiation is ultraviolet radiation or electron beams; and chemical cross-linking using various crosslinking agents such as isocyanate compounds, for example, trifunctional isocyanates, organic peroxides, ORGANOMETALLIC salts, metal alcoholate, chelate metal compounds and polyfunctional compounds (external polyfunctional crosslinking agent and a polyfunctional monomer for internal cross-linkage, such as diacrylate and dimethacrylate).

The drug contained in the adhesive the adhesive layer is not imposed specific restrictions. However, the preferred drugs are those that are able to penetrate the skin. You can apply the drug systemic or local action. Specifically, applicable drugs include corticosteroids, analgesic and anti-inflammatory agents, hypnotics sedatives, tranquilizers, protivogipertonicheskoe funds protivogipertonicheskoe diuretics, antibioti and, anesthetic tools, antimicrobial agents, antifungal agents, vitamin preparations for the expansion of coronary vessels, antihistamines, medicines for cough, sex hormones, antidepressants, medicines for expansion of blood vessels of the brain, anti-emetics, anti-cancer drugs and biomedical tools. If necessary, the adhesive composition of the dosage form may include a combination of two or more of these medicines.

The invention is particularly effective if the molecule medicinal product contains at least one primary, secondary or tertiary amino group. The reasons for this are as follows. As a connecting means between the polyester film and polyester non-woven material often used polyester resin with a low degree of polymerization due to the adhesion between the film and nonwoven material. There are cases when such binder has a low acidity, as at the ends of its molecules contain a substantial amount of carboxyl groups. For this reason, the drug-containing amine fragment, tend to migrate to the acid binder due to the basicity of the amino group. In the binder may break down under the action of lcars the public funds and may be stratification of the film and nonwoven material. In addition, there is the possibility of simultaneous collapse of medicines. Therefore, the present invention is particularly effective if the self-adhesive layers used medicines containing at least one primary, secondary or tertiary amino group, since the substrate and the drug acquire high stability due to the fact that the film and the nonwoven material are connected to each other directly without the binder.

A suitable content of the drug can be determined in accordance with a specific form of medication and purpose of the introduction. However, as a rule, the drug contained in the adhesive of adhesive layer in an amount of about 0.5 to 40% by weight, preferably about 1 to 30% by weight. If the content of the drug is less than 0.5 mass%, there is a probability that it will be impossible to expect the release of the drug in a number needed to treat. If the content of the medicinal product exceeds 40% by mass, there is the likelihood that treatment will reach its limit and a large number of medicines will be economically inefficient.

In addition, the present invention provides the possibility of applying sa is oleaselect adhesive layer on a substrate, not only by non-woven material, but with the film. These implementation options have the following advantage. If this adhesive dosage forms placed and Packed in the packing material, non-woven fabric adhesive dosage forms it comes in contact with the inner surface of the packaging material. Therefore, decreases the actual contact area with the adhesive dosage form and, accordingly, the frictional force between them. In the adhesive dosage form can be easily removed from the packaging material.

Examples

The present invention will be disclosed in more detail by reference to the following specific examples. The following examples are given only as examples and should not be inferred that the invention is limited. Later in this document, the term "parts" means "mass parts", unless otherwise indicated.

Example 1

In the atmosphere of inert gas at 60°C were subjected to the polymerization reaction dissolved in ethyl acetate 95 parts of 2-ethylhexyl acrylate, 5 parts of acrylic acid and 0.2 part of benzoyl peroxide, to obtain a solution of acrylic adhesive A. was Mixed with 5.5 parts acrylic adhesive A in the calculation of the solid material, 40 parts of isopropylmyristate and 5 parts of isosorbide dinitrate and stirred in a vessel until the eye the mixture is smooth. Added ethylacetoacetate diisopropylate aluminum in the amount of 0,165 part and regulate the viscosity of the resulting mixture by the addition of ethyl acetate. The described method has been self-adhesive adhesive solution.

This adhesive solution was applied from the side of the nonwoven material on a substrate obtained by thermal fusion of non-woven material made from poly(ethyleneterephthalate) (density of 12 g/m2) on a film of poly(ethyleneterephthalate) (thickness 2 μm)in an amount such that the thickness after drying was 80 μm. Coated substrate was dried at 100°C for 3 minutes in a drying oven with circulation of hot air and then subjected to 24-hour heat treatment. A layer of poly(ethyleneterephthalate) (75 μm), treated silicone composition to enhance exfoliation and pasted the treated side self-adhesive layer to obtain an adhesive dosage forms of the present invention.

Thus, using the above described method adhesive adhesive layer according to the present invention can be directly formed on the substrate.

Comparative example 1

On a multilayer film obtained by bonding non-woven fabric of poly(ethyleneterephthalate) (density of 12 g/m2) film made of poly(e is interelate) (thickness 2 μm), using adhesive polyester type (1-2 g/m2), from the side of the nonwoven material was applied adhesive solution obtained by the method similar to example 1, in an amount such that the thickness after drying was 80 μm. However there was the destruction of the substrate on the surface of the binding of poly(ethyleneterephthalate) non-woven fabric and poly(ethyleneterephthalate) film due to partial separation of the film before coated with a multilayer film was placed in a drying oven with circulation of hot air.

Example 2

Adhesive obtained analogously to example 1, was applied to a strip of poly(ethyleneterephthalate) (75 μm), treated silicone composition to improve exfoliation, in such a quantity to obtain a thickness after drying of 80 μm. This gasket with coating was dried at 100°C for 3 minutes in a drying oven with circulation of hot air, and then subjected to 24-hour heat treatment. Thus, the received self-adhesive layer. A substrate similar to the substrate of example 1, pressed side non-woven fabric adhesive to the adhesive layer using a rubber roller, receiving adhesive dosage form of the present invention.

Comparative example 2

Received adhesive dosage form in the same way, is that in example 2, except that he applied the same substrate, which was used in comparative example 1.

Comparative example 3

Received adhesive dosage form in the same way as in example 2, except that the applied substrate used in example 1, and the thickness of the poly(ethyleneterephthalate) film of the substrate was 25 μm.

Example 3

Received the solution acrylic adhesive A in ethyl acetate, containing no drugs, in accordance with the following recipe. This adhesive solution was applied to a strip of poly(ethyleneterephthalate) (75 μm), treated silicone composition to improve exfoliation, in an amount such that the thickness after drying was 75 μm. This gasket with coating was dried at 100°C for 3 minutes in a drying oven with circulation of hot air, and then subjected to heat treatment for 24 hours. Thus, the received self-adhesive layer. To obtain adhesive dosage forms obtained self-adhesive layer is pressed with a rubber roller to the same substrate as in example 1, from the side of the nonwoven material. In addition, the obtained adhesive dosage forms removed the gasket and the surface self-adhesive layer with the unit for coating with shtam the om inflicted nicotine, for absorption of the latter in an amount such that the self-adhesive layer contained 10 parts of nicotine to 60 parts acrylic adhesives A. Thus obtained adhesive dosage form of the present invention. By the way, nicotine is the substance in the molecule of which contains two tertiary amino groups.

Recipe

Adhesive ingredient:
acrylic adhesive A60 parts
Liquid ingredient:
isopropyl30 parts
Crosslinking agent:
ethylacetoacetate diisopropylate aluminum0.18 parts

Comparative example 4

Adhesive dosage form was obtained in the same manner as in example 3, except that he applied the same substrate as in comparative example 1.

Example 4

Received the solution of sticky substance in toluene, containing the drug, according to the following recipe. This solution was applied to a strip of poly(ethyleneterephthalate) (75 μm), obrabotan the Yu silicone composition to improve exfoliation, in an amount such that the thickness after drying was 80 μm. This gasket with coating was dried at 100°C for 3 minutes in a drying oven with circulation of hot air. Thus, the received self-adhesive layer. To obtain adhesive dosage forms of the present invention obtained self-adhesive layer is pressed with a rubber roller to the same substrate as in example 1 from the film.

Recipe

Adhesive ingredient:
polyisobutylene (srednevozrastnoe molecular weight of about 4000000)18 pieces
polyisobutylene (srednevozrastnoe molecular weight of approximately 55,000)18 pieces
Means for increasing adhesiveness:
saturated alicyclic hydrocarbon resin24 pieces
Liquid ingredient:
isopropylmyristate25 parts
Drug:
emedastine (with a couple of the e tertiary amino group) 15 pieces

Comparative example 5

Adhesive dosage form was obtained in the same manner as in example 4, except that he applied the same substrate as in comparative example 1.

Example 5

Received the solution adhesives in hexane, containing the drug, according to the following recipe. The resulting solution was applied to a strip of poly(ethyleneterephthalate) (75 μm) - treated fluorine-containing composition to improve exfoliation, in an amount such that the thickness after drying was 60 μm. This gasket with coating was dried at 80°C for 5 minutes in a drying oven with circulation of hot air. In this way received a self-adhesive layer. To obtain adhesive dosage forms of the present invention obtained self-adhesive layer is pressed with a rubber roller to the same substrate as in example 4, from the side of the nonwoven material.

Recipe

Adhesive ingredient:
silicone adhesive (condensate polydimethylsiloxane and silicone rubber66 parts
Liquid ingred the UNT:
isopropylmyristate2 pieces
Liquid ingredient:
oleic acid2 pieces
Drug:
the salbutamol (having one secondary amino group)30 parts

Comparative example 6

Adhesive dosage form was obtained in the same manner as in example 5, except that he applied the same substrate as in comparative example 1.

Example 6

Received the solution of sticky substance in toluene, containing the drug, according to the following recipe. The resulting solution was applied to a strip of poly(ethyleneterephthalate) (75 μm), treated silicone composition to improve exfoliation, in an amount such that the thickness after drying was 80 μm. This gasket with coating was dried at 100°C for 3 minutes in a drying oven with circulation of hot air. In this way received a self-adhesive layer. To obtain adhesive dosage forms of the present invention obtained self-adhesive layer is pressed with a rubber roller to the same substrate, as the example 1, from the side of the nonwoven material.

Recipe

Adhesive ingredient:
polyisobutylene (srednevozrastnoe molecular weight of about 4000000)18 pieces
polyisobutylene (srednevozrastnoe molecular weight of approximately 55,000)18 pieces
Means for increasing adhesiveness:
saturated alicyclic hydrocarbon resin24 pieces
Liquid ingredient:
isopropylmyristate30 parts
Drug:
propranolol (having one secondary amino group)10 pieces

Comparative example 7

Adhesive dosage form was obtained in the same manner as in example 6, except that he applied the same substrate as in comparative example 1.

Example 7

Adhesive dosage form of the present invention was obtained in the same manner as in example 3, except h is about used the same substrate, as in example 1, and the thickness of the poly(ethyleneterephthalate) film was 4.5 μm.

Example testing of dosage forms

1. Test wearing

Samples of size 5 cm × 5 cm was cut from adhesive dosage forms, obtained in example 2, comparative example 2 and comparative example 3. These samples were placed in the center of the upper part of the thorax and upper part of the chest near the armpit each of the six volunteers. Volunteers wore the samples on the skin for 24 hours and evaluated the samples from the point of view of the experiencing of sensations according to the following criteria.

A feeling of stiffness

1: satisfactory wearing almost without feeling the stiffness

2: a slight feeling of stiffness

3: significant feeling of rigidity.

The feeling of tension

1: satisfactory wearing almost without feeling tension

2: a slight feeling of tension

3: significant tension.

Table 1
The results of the test on wearing
A feeling of stiffnessThe feeling of tension
Example 2The center of the upper chest 11
The area of the upper part of the breast near the armpit11
Comparative example 2The center of the upper chest12
The area of the upper part of the breast near the armpit11
Comparative example 3The center of the upper chest33
The area of the upper part of the breast near the armpit33

Adhesive dosage form of example 2 and comparative example 2 gave almost no sensation of stiffness, because they used a substrate consisting of a thin film and non-woven material of low density. Adhesive dosage form of example 2 gave almost no sense of tension during wear on the moving parts of the body. Adhesive dosage form of comparative example 3 was made as a noticeable feeling of stiffness, and a noticeable sense of tension, and was unsuitable for use.

2. Test transmission

the adhesive dosage forms of examples 3-7 and comparative examples 4-7 were removed the protective strip and examined with a spectrophotometer at an optical density at a wavelength of 610 nm, moreover, the side on which were self-adhesive layer, was turned towards the radiation detector of the spectrophotometer.

Table 2
Test results transmission
Transmission (610 nm)
Example 356%
Example 455%
Example 555%
Example 657%
Example 759%
Comparative example 445%
Comparative example 544%
Comparative example 647%
Comparative example 745%

Investigated the transmission of adhesive dosage forms of examples 3-7 and comparative examples 4-7 at a wavelength of 610 nm. Adhesive dosage forms, which used a substrate obtained by thermal fusion, had a higher transmittance and higher is prozracnosti.

3. Test the strength of the fixing film in the substrate.

The test was performed with respect to the products of examples 3-7 and comparative examples 4-7, and these adhesive dosage forms were placed in a multilayer packaging material aluminum/polyacrylonitrile and kept at 50°C for 2 months. After that, each of the products was cut into squares with sides of 16 mm and after removal of the protective strip was pasted onto a plate made of bakelite. Held your finger on the film side adhesive dosage forms, while strongly pressing your finger on the tape. Researched adhesive dosage form for the Department of the films in this movement of the finger.

Table 3
The results of the test for durability of the fixing film substrate
The strength of the fixing film (2-month storage at 50°C)
Example 3the Department did not happen
Example 4the Department did not happen
Example 5the Department did not happen
Example 6the Department did not happen
Example 7the Department did not happen
Comparative example 4the separation took place
Comparative example 5the separation took place
Comparative example 6the separation took place
Comparative example 7the separation took place

After 2-month storage at 50°C the strength of the fastening film substrates preparations of examples 3-7 and comparative examples 4-7 was next. In the examples, which used a substrate obtained by thermal fusion, adhesive dosage forms did not allow separation of the film. On the contrary, in the comparative examples, which used a substrate obtained by using the binder, adhesive dosage forms allowed the Department of film.

4. The test on the stability of drugs during storage

Adhesive dosage forms of example 6, example 7 and comparative example 7 were placed in a multilayer packaging material aluminum/polyacrylonitrile and kept at 50°C for 1 month. Comparing the content of the drug in the preparations after storage with the original content to define the share of the surviving medicines in percent. In each case, the content of drug was determined using the dilution/extraction adhesive dosage forms with an organic solvent and determine the percentage of drugs by HPLC method.

Table 4
The test results on the stability of drugs during storage
Saving medicines (1-month storage at 50°C)
Example 6of 98.2±0,2%
Example 7of 99.3±0,6%
Comparative example 773,1±0,7%

Adhesive dosage form of comparative example 7, which used a substrate containing a binder, showed reduced stability of the medicinal product during storage. On the other hand, the adhesive dosage form of example 7 showed a very satisfactory stability of the medicinal product, as it used a substrate obtained by thermal fusion of poly(ethyleneterephthalate) film on the nonwoven poly(ethyleneterephthalate).

5. what he eats for clutch

Substrate adhesive dosage forms of example 6, example 7 and comparative example 7 were taped pressure 2-kg rubber roller, laminating it on the substrate once forward and backward. Adhesive dosage forms were left at room temperature for a certain period of time, and then one of them was cut down by two sample having a size of 3×5 cm, being careful not to apply pressure to them. After removal of the protective strip end portion of each of the adhesive dosage forms straight back to a width of about 5 mm, forming part, for which you can hold with your hand. Open the self-adhesive surface of adhesive layer lightly glued to each other and the sample was left to stand for 10 minutes. In the obtained sample was separated one piece of the substrate from the other, holding the bent ends. Evaluated the adhesion to the substrate, based on the following criteria.

1: self-adhesive adhesive layers could not be separated from each other

2: part of the self-adhesive layer remained on the substrate

3: most of the self-adhesive layer remained on the substrate

4: self-adhesive adhesive layers partially remained on the protective pads

5: self-adhesive adhesive layers largely remained on protective pads.

Table 5
The results of the Gosta grip
The grip test
after 1 hafter 3 hafter 6 hafter 12 h
example 62111
example 72111
comparative example 75421

Adhesive dosage forms of example 6 and example 7 were acquired satisfactory adhesion in a short time. In contrast, the adhesive dosage form of comparative example 7 was required 12 hours to reach the clutch.

Although the present invention has been described in detail and with reference to specific variations in its implementation, the specialist in the art it will be obvious that you can make many changes and modifications to the described embodiments without going outside the scope of the invention.

This application is based the analysis on the patent application of Japan No. 2006-315751, filed November 22, 2006, the contents of which are entirely incorporated into the present application by reference.

In addition, all sources cited in this application, included in its entirety.

1. Adhesive dosage form for introducing medicines into the body through the skin, consisting of
substrate; and
self-adhesive sticky layer that contains a drug that can penetrate the skin, and applied at least on one side of the substrate,
where the substrate consists of a polyester film having a thickness of from 0.5 to 6.0 μm, and a polyester nonwoven material directly associated with the specified film.

2. Adhesive dosage form according to claim 1, where the self-adhesive layer directly or through an intermediate layer deposited on a substrate from the side of the nonwoven material.

3. Adhesive dosage form according to claim 1 where the polyester fiber of the specified non-woven material is directly associated with a part of the polyester film is attached to the specified non-woven material.

4. Adhesive dosage form according to claim 1, where the specified non-woven material has a density of from 5 to 40 g/m2.

5. Adhesive dosage form according to claim 1, where in the molecule drugs include at least one primary, secondary or tertiary amino group.

6. Adhesive lekarstvennayaforma according to claim 1, where this film and the nonwoven material are fused with each other.

7. Adhesive dosage form according to claim 1, where the self-adhesive layer deposited on a substrate from a side of the given film.



 

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19 cl, 7 tbl, 1 dwg, 63 ex

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5 cl, 3 tbl, 3 dwg, 3 ex

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26 cl, 8 dwg, 8 ex

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17 cl, 7 ex

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10 cl, 12 ex

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12 cl, 1 tbl, 1 dwg, 1 ex

FIELD: medicine, pharmaceutics.

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8 cl, 18 ex

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EFFECT: provided dressing cleanliness.

14 cl, 4 tbl, 3 ex, 7 dwg

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