KR101883410B1 - Transdermal drug delivery system and preparation method thereof - Google Patents

Abstract

The present invention relates to percutaneous absorption preparations and methods for their preparation. In the percutaneous absorption preparation of the present invention, a drug-containing layer containing a drug is present, and a drug-protecting layer made of a non-permeable material is disposed on the drug-containing layer. The drug- And a release-controlling adhesive layer provided on the release-controlling adhesive layer.
The transdermal absorption preparation of the present invention is prepared by including a drug-containing layer as a drug reservoir capable of preventing the loss of drug during processing or storage of the product, and a release-controlling adhesive layer capable of controlling the release of the drug and having the function of a release- Loss prevention and skin permeation control of the drug.

Description

[0001] The present invention relates to a transdermal drug delivery system and preparation method thereof,

The present invention relates to a percutaneous absorption preparation for delivering a drug through the skin and a method for producing the same.

Smoking is a major risk factor for coronary heart disease and lung disease, accounting for approximately 30% of all deaths from cancer. As these health hazards have been focused on the harmfulness of smoking, interest in smoking has increased in each field of society. However, contrary to this interest, the success rate of smoking cessation remains low. Therefore, attempts to increase smoking cessation success rate through the use of smoking cessation aids are continuing. The key to success in smoking cessation is the effective elimination of withdrawal symptoms caused by nicotine addiction. These cigarette supplements will help you quit smoking by feeding as much nicotine as you need to reduce nicotine withdrawal symptoms.

In the case of oral administration of nicotine directly through the mouth in the form of such a smoking cessation aid, it is consumed in the form of a candy, etc. In case of attempting to quit smoking, it should be frequently administered as a temporary administration method, Because of the need for direct contact with the inner wall of the esophagus, the toxic nature of nicotine causes unpleasant side effects such as unpleasant taste, heartburn, discomfort, and hiccups.

Alternatively, the nicotine-containing solution is injected into a single-use or multi-dose plastic container, and the nicotine solution contained in the container is inserted into the nasal cavity for direct administration through the nasal mucosa. However, this method is not preferable from the viewpoint of hygiene because the container is in direct contact with the nasal mucosa. In addition, handling and management is tricky. In addition, frequent administration is necessary because temporary effects can be expected as in the above-mentioned method. Particularly, this method involves a process of inserting the container into the nasal cavity, and therefore, there is a problem that it is difficult to apply it to others.

Unlike the above-mentioned two administration methods, the transdermal absorption type nicotine transdermal preparation can solve the drawbacks of the above-mentioned two kinds of smoking cessation aids, and it is in the spotlight to develop an effective transdermal absorption preparation in the industry related to the smoking cessation aid It is a fact that it is spurting.

There are two types of nicotine transdermal absorption formulations: a single-layer matrix type that includes a transdermal formulation in the form of a reservoir and a volatile liquid drug.

Among these, the percutaneous absorption formulations in the form of reservoirs are difficult to control the reservoir layer containing a high concentration of drug, and also require a discharge control membrane to be applied, so that the process is difficult and the manufacturing cost is also increased.

On the other hand, a monolayer matrix-type percutaneous absorption preparation has a disadvantage in that it is difficult to prevent the loss of the drug during the process or during storage.

SUMMARY OF THE INVENTION In order to solve the problems of the prior art as described above, the present invention provides a matrix type transdermal preparation that compensates for disadvantages of the matrix type and accommodates advantages of the storage type.

In order to solve the above problems, according to one aspect of the present invention, there is provided a percutaneously absorbable preparation for administering a drug, which comprises a drug-containing layer containing a drug and is located on the drug-containing layer, And a drug-protecting layer formed thereon. And a release-controlling adhesive layer positioned below the drug-containing layer and having a function of controlling the release of the drug when the drug is permeated.

Another aspect of the present invention is to provide a percutaneously absorbable preparation for administration of a medicament, which comprises a medicament-containing layer containing a medicament and a medicament-protecting layer which is located on the medicament-containing layer and which is made of a non- do. And a primer layer positioned between the drug-containing layer and the drug-protecting layer and for bonding the drug-containing layer and the drug-protecting layer. And a release-controlling adhesive layer positioned below the drug-containing layer, the release-controlling adhesive layer being capable of controlling release of the drug when the drug is permeated.

The percutaneous absorption preparation is a percutaneous absorption preparation characterized by comprising a release layer on the lower part of the release-controlling adhesive layer.

Wherein the drug in the drug-containing layer is a volatile liquid drug, and is preferably a nicotine.

Wherein the drug-containing layer comprises a mixture of the drug and the pressure-sensitive adhesive.

Wherein the pressure-sensitive adhesive is an acrylic pressure-sensitive adhesive containing a tackifier resin or a rubber-based pressure-sensitive adhesive comprising a rubber material mixed with a tackifier resin or a mineral oil.

Wherein the mixture further comprises a skin penetration enhancer.

Wherein the release-controlled adhesive layer comprises a pressure-sensitive adhesive, and the release-controlled adhesive layer further comprises a skin penetration enhancer.

Wherein the primer layer is a pressure-sensitive adhesive.

In another aspect of the present invention, there is provided a method for preparing a drug-containing layer, comprising the steps of: preparing a drug-containing layer solution by mixing nicotine, a pressure-sensitive adhesive, and a tackifier resin; And a step of laminating a release-controlling adhesive layer on the other surface of the drug-containing layer.

According to another aspect of the present invention, there is provided a method for producing a drug-containing layer, comprising the steps of: laminating one side of a primer layer with a drug protecting layer; mixing a nicotine, a pressure-sensitive adhesive, and a tackifier resin to prepare a drug- Containing layer on the other side of the drug-containing layer, and a step of laminating a release-controlling adhesive layer on the other side of the drug-containing layer.

The percutaneous absorption preparation of the present invention can contain a drug-containing layer to effectively prevent the loss of drug during the manufacturing process or storage, and can control the release of the drug, including a release-controlling adhesive layer having the function of a release-controlling membrane. Accordingly, the transdermal absorption preparation of the present invention can prevent drug loss and control the degree of skin permeation of the drug.

Fig. 1 shows the results of the preparation of percutaneous absorption preparation according to Example 1 of the present invention.
Fig. 2 shows the results of the preparation of percutaneous absorption preparation according to Example 23 of the present invention.

The inventors of the present invention have made intensive studies to overcome the problems of the prior art, and as a result, they have found that a drug-containing layer having a drug storage function is adopted, and a release-controlling adhesive layer having a function of controlling release and providing a proper adhesive force is included The present invention has been completed.

Accordingly, the transdermal absorption preparation of the present invention is characterized by comprising a drug-containing layer and a release-controlling adhesive layer.

More specifically, the percutaneous absorption preparation of the present invention comprises a drug-protecting layer made of an impermeable material for the drug on the drug-containing layer containing the drug.

In addition, a release-controlling adhesive layer having a release-controlling function at the time of permeation of the drug is located under the drug-containing layer.

In the present invention, the drug to be delivered by percutaneous absorption is preferably a volatile liquid drug, and nicotine is preferably used, but not limited thereto.

The drug-containing layer of the present invention is formed by mixing a percutaneous absorption drug and a pressure-sensitive adhesive.

The percutaneous absorption drug may be contained in an amount of 5 to 40 parts by weight based on 100 parts by weight of the drug-containing layer.

The pressure-sensitive adhesive is mixed with the percutaneous absorption medicament to suppress the loss of the medicament. Any pressure-sensitive pressure-sensitive adhesive can be used without limitation as the pressure-sensitive adhesive. Preferably, an aminoalkyl methacrylate copolymer or an adhesive resin or a mineral oil containing a tackifier resin as an acrylic pressure-sensitive adhesive is mixed with a rubber material and a rubber pressure-sensitive adhesive having appropriate adhesive strength is used. Examples of the rubber material include a styrene-ethylene-isoprene-styrene copolymer, a styrene-butadiene-styrene copolymer, a styrene-butadiene copolymer, One or two or more selected from the group consisting of styrene-isoprene copolymer, styrene-isoprene-styrene copolymer, silicone rubber, and polyisobutylene can be used One, other biocompatible rubber is not limited and can be used. Further, the tackifying resin may be rosin glycerin ester Hydrogenated rosin glycerin ester resin, rosin pentaerythritol ester resin, hydrogenated rosin pentaerythritol ester resin, alpha methyl styrene resin, alicyclic saturated hydrocarbon resin having 5 to 9 carbon atoms, aliphatic hydrocarbon resin having 5 to 9 carbon atoms, aromatic hydrocarbon A resin, a hydrogenated dicyclopentadiene resin, a terpene resin, a coumarone indene resin, and a terpene phenol resin may be used, but not limited thereto.

The drug-containing layer may further include a skin penetration enhancer for enhancing transdermal permeation of the drug. Examples of such skin permeation accelerators include fatty acid ethers having 2 to 18 carbon atoms, nonionic surfactants, isopropyl myristate, transcutol, triacetin, pyrrolidone derivatives, fatty acids having 2 to 18 carbon atoms, fatty acid alcohols having 2 to 18 carbon atoms , Fatty acid esters having 2 to 18 carbon atoms, and plasticizers. Of these, isopropyl myristate and triacetin can be preferably used.

In the case of the drug-containing layer containing the skin permeation enhancer, the weight of the pressure-sensitive adhesive is adjusted to be 30 to 90 parts by weight, more preferably 40 to 80 parts by weight, based on 100 parts by weight of the drug-containing layer. 0 to 30 parts by weight, and more preferably 3 to 15 parts by weight. The pressure sensitive adhesive may contain 5 to 40 parts by weight, more preferably 15 to 25 parts by weight, of the rubber material with respect to 100 parts by weight of the pressure-sensitive adhesive, and the pressure-sensitive adhesive may contain 10 to 60 parts by weight, Preferably 10 to 30 parts by weight.

In the present invention, a polyester film, a polypropylene film, a polyethylene film, a polyester film, a polyacrylonitrile film and a polyester film on which a metal is deposited may be used alone or a plurality of films selected from two or more thereof may be used A multilayered film may be used, or a nonwoven fabric-laminated polyester film may be used.

In the release-controlling pressure-sensitive adhesive layer of the present invention, the pressure-sensitive adhesive to be used may be any pressure-sensitive pressure-sensitive adhesive which can be used without limitation, but is preferably a polyacrylate type having a carboxyl group, a polyacrylate type having a carboxyl group and a hydroxyl group, A polyacrylate-vinyl acetate-based pressure sensitive adhesive having a carboxyl group, a polyacrylate-vinyl acetate pressure sensitive adhesive having a hydroxyl group, a polyacrylate-vinyl acetate pressure sensitive adhesive having no functional group, and a rubber hybrid acrylate- Rate-based adhesive may be used. Further, a rubber-based pressure-sensitive adhesive composed of polyisobutylene, a tackifier resin, a mineral oil, or the like can be used.

The release-controlling pressure-sensitive adhesive layer may be a skin permeation promoting agent if necessary, and the skin permeation promoting agent may contain 0 to 30 parts by weight based on 100 parts by weight of the release-controlling pressure-sensitive adhesive layer, Is 3 to 15 parts by weight.

The acrylic pressure sensitive adhesive may be used without limitation in the pressure sensitive adhesive used as the primer layer in the present invention, but a polyacrylate pressure sensitive adhesive having a carboxyl group may be preferably used.

The release layer used in the present invention is separated and removed immediately before use to allow the release-controlled adhesive layer to adhere to the skin. The release layer can be used together with a silicone resin or a fluorine resin coated on the polymer film as selected from the group consisting of polyester, polyvinyl chloride, polyvinylidene chloride, polyethylene terephthalate and copolymers thereof .

Hereinafter, the present invention will be described in detail with reference to the preferred embodiments, which will be readily apparent to those skilled in the art to which the present invention pertains. The present invention may, however, be embodied in many different forms and should not be construed as limited to the embodiments set forth herein.

Example  One:

26 g of nicotine, 54 g of Eudragit E100 as an aminoalkyl methacrylate copolymer as a pressure-sensitive adhesive and 20 g of hydrogenated rosin glycerin ester were completely dissolved in 60 g of methylene chloride (MC) to prepare a drug-containing coating solution .

Then, a PET film coated with a silicone resin is prepared.

Thereafter, the prepared coating solution containing the drug was coated on the PET film (release layer) coated with the silicone resin using a lab coater (Mathis, Switzerland) and dried at 50 DEG C for about 1 minute to obtain a coating solution containing about 66 Mu] m thick.

Thereafter, the polyester film (drug-protecting layer) was lapped.

Then, Duro-Tak 87-4098 (Henkel), which is a polyacrylate-vinyl acetate-based pressure-sensitive adhesive without a functional group, was applied and dried to form a pressure-sensitive adhesive layer having a thickness of about 100 탆.

Thereafter, after removing the release layer, the release-controlling adhesive layer was laminated on the drug-containing layer.

And cut to a required size to prepare a patch-type transdermal preparation.

Example  2:

As the pressure-sensitive adhesive to be used in the release-controlled pressure-sensitive adhesive layer in Example 1, the same method as in Example 1 was used except that Duro-Tak 87-2287 (Henkel), which is a polyacrylate-vinyl acetate- To prepare a percutaneous absorption preparation.

Example  3:

In the same manner as in Example 1, except that Duro-Tak 87-503A (Henkel), which is a rubber hybrid polyacrylate adhesive, was used as a pressure-sensitive adhesive for use in the release-controlled pressure-sensitive adhesive layer in Example 1, transdermal absorption The formulation was prepared.

Example  4:

A percutaneous absorption preparation was prepared in the same manner as in Example 1, except that Duro-Tak 87-9301 (Henkel), which is a polyacrylate-based adhesive having no functional group, was used as a pressure-sensitive adhesive for use in the release- .

Example  5:

A percutaneous absorption preparation was prepared in the same manner as in Example 1, except that Duro-Tak 87-900A (Henkel), which is a polyacrylate-based adhesive having no functional group, was used as a pressure-sensitive adhesive for use in the release- .

Example  6:

In the same manner as in Example 1 except that Duro-Tak 87-2074 (Henkel), which is a polyacrylate type having a carboxyl group and a hydroxyl group, was used as the pressure-sensitive adhesive to be used in the release-controlled pressure-sensitive adhesive layer in Example 1, transdermal absorption The formulation was prepared.

Example  7:

18 g of nicotine, 62 g of Eudragit E100 as an aminoalkyl methacrylate copolymer as a pressure-sensitive adhesive and 20 g of hydrogenated rosin glycerin ester were completely dissolved in 60 g of methylene chloride (MC) to prepare a drug-containing coating solution .

Then, a PET film coated with a silicone resin is prepared.

Thereafter, the drug-containing coating solution thus prepared was applied onto the PET film (release layer) coated with the silicone resin using a wrap coater and dried at 50 DEG C for about 1 minute and 30 seconds to form a drug-containing layer having a thickness of about 95 mu m Respectively.

Thereafter, a polyester film (drug-protecting layer) was laminated.

Then, Duro-Tak 87-4098 (Henkel), which is a polyacrylate-vinyl acetate-based pressure-sensitive adhesive without a functional group, was applied and dried to form a pressure-sensitive adhesive layer having a thickness of about 100 탆.

Thereafter, after removing the release layer, the release-controlling adhesive layer was laminated on the drug-containing layer.

Then, the preparation was cut to a necessary size to prepare a patch-type transdermal preparation.

Example  8:

20 g of nicotine, 60 g of Eudragit E100 as an aminoalkyl methacrylate copolymer as a pressure-sensitive adhesive and 20 g of hydrogenated rosin glycerin ester were completely dissolved in 60 g of methylene chloride (MC) to prepare a drug-containing coating solution . A percutaneous absorption preparation was prepared in the same manner as in Example 7 except that the prepared solution was dried to a thickness of 86 탆.

Example  9:

22 g of nicotine, 58 g of Eudragit E100 as an aminoalkyl methacrylate copolymer as a pressure-sensitive adhesive and 20 g of hydrogenated rosin glycerin ester were completely dissolved in 60 g of methylene chloride (MC) to prepare a drug-containing coating solution . A percutaneous absorption preparation was prepared in the same manner as in Example 7, except that the prepared solution was dried to a thickness of 78 mu m.

Example  10:

24 g of nicotine, 56 g of Eudragit E100 as an aminoalkyl methacrylate copolymer as a pressure-sensitive adhesive, and 20 g of hydrogenated rosin glycerin ester were completely dissolved in methylene chloride (MC) to prepare a drug-containing coating solution . A percutaneous absorption preparation was prepared in the same manner as in Example 7 except that the prepared solution was dried to a thickness of 71 탆.

Example  11:

In the same manner as in Example 7, except that Duro-Tak 87-504A (Henkel, USA), which is a rubber hybrid polyacrylate type pressure-sensitive adhesive, was used as the pressure-sensitive adhesive to be used for the emission- To prepare a percutaneous absorption preparation.

Example  12:

As a pressure-sensitive adhesive to be used for the emission-controlling pressure-sensitive adhesive layer in Example 8, a rubber hybrid polyacrylate-based pressure-sensitive adhesive Duro-Tak 87-504A (Henkel, USA) was used and the pressure- A percutaneous absorption preparation was prepared in the same manner as in Example 8, except that it was applied.

Example  13:

As a pressure-sensitive adhesive to be used in the release-controlled pressure-sensitive adhesive layer in Example 9, a rubber hybrid polyacrylate-based pressure-sensitive adhesive Duro-Tak 87-504A (Henkel, USA) was used and the pressure- The percutaneous absorption preparation was prepared in the same manner as in Example 9, except that it was applied.

Example  14:

As the pressure-sensitive adhesive to be used for the emission-controlling pressure-sensitive adhesive layer in Example 10, a rubber hybrid polyacrylate-based pressure-sensitive adhesive Duro-Tak 87-504A (Henkel, USA) was used and the pressure- A percutaneous absorption preparation was prepared in the same manner as in Example 10, except that it was applied.

Example  15:

As the pressure-sensitive adhesive to be used for the release-controlled pressure-sensitive adhesive layer in Example 4, a polyacrylate-based pressure-sensitive adhesive, Duro-Tak 87-9301 (Henkel, USA) was used and applied so that the dry thickness of the pressure- A percutaneous absorption preparation was prepared in the same manner as in Example 4.

Example  16:

As the pressure-sensitive adhesive to be used in the release-controlled pressure-sensitive adhesive layer in Example 4, Duro-Tak 87-9301 (Henkel, USA), which is a polyacrylate adhesive without a functional group, was used and applied so that the dry thickness of the pressure- A percutaneous absorption preparation was prepared in the same manner as in Example 4.

Example  17:

As the pressure-sensitive adhesive to be used for the release-controlled pressure-sensitive adhesive layer in Example 4, a polyacrylate-based pressure-sensitive adhesive Duro-Tak 87-9301 (Henkel, USA) was used and the pressure-sensitive adhesive layer was applied so that the dry thickness of the pressure- A percutaneous absorption preparation was prepared in the same manner as in Example 4.

Example  18:

24 g of nicotine, 56 g of Eudragit E100 as an aminoalkyl methacrylate copolymer as a pressure-sensitive adhesive and 20 g of hydrogenated rosin glycerin ester were completely dissolved in 60 g of methylene chloride (MC) to prepare a drug-containing coating solution .

Then, a PET film coated with a silicone resin is prepared.

Thereafter, the drug-containing coating solution thus prepared was applied to a PET film (release layer) coated with the silicone resin using a lab coater (Mathis, Switzerland) and dried at 50 DEG C for about 1 minute, Thick drug-containing layer was formed.

Thereafter, the polyester film (drug-protecting layer) was lapped.

As a pressure-sensitive adhesive, Doru-Tak 87-4098 (Henkel, USA), which is a polyacrylate-vinyl acetate pressure-sensitive adhesive having no functional group, was applied and dried to prepare a drug-containing layer. The release layer is removed from the thus-prepared drug-containing layer. And Doru-Tak 87-4098 (Henkel, USA), which is a polyacrylate-vinyl acetate-based pressure-sensitive adhesive having no functional group, is used as a pressure-sensitive adhesive to be used for the release- Thus, the release-controlling adhesive layer was laminated with the above drug-containing layer and cut to a necessary size to prepare a percutaneous absorption preparation.

Example  19:

A percutaneous absorption preparation was prepared in the same manner as in Example 18, except that the thickness of the release-modifying pressure-sensitive adhesive layer laminated in Example 18 was 60 占 퐉.

Example  20:

26 g of nicotine, 49 g of Eudragit E100 as an aminoalkyl methacrylate copolymer as a pressure-sensitive adhesive, 20 g of hydrogenated rosin glycerin ester and 5 g of isopropyl myristate were completely dissolved in 60 g of methylene chloride (MC) Containing coating solution was prepared in the same manner as in Example 1. The results are shown in Table 1. < tb >< TABLE >

Example  21:

26 g of nicotine, 49 g of Eudragit E100 as an aminoalkyl methacrylate copolymer as a pressure-sensitive adhesive, 20 g of hydrogenated rosin glycerin ester and 5 g of triacetin were completely dissolved in 60 g of methylene chloride (MC) Transdermal preparation was prepared in the same manner as in Example 1, except that the solution was prepared.

Example  22:

26 g of nicotine, 54 g of Eudragit E100 as an aminoalkyl methacrylate copolymer as a pressure-sensitive adhesive and 20 g of hydrogenated rosin glycerin ester were completely dissolved in 60 g of methylene chloride (MC) to prepare a drug-containing coating solution

Then, a PET film coated with a silicone resin is prepared.

Thereafter, the prepared coating solution containing the drug was coated on the PET film (release layer) coated with the silicone resin using a lab coater (Mathis, Switzerland) and dried at 50 DEG C for about 1 minute to obtain a coating solution containing about 66 Mu] m thick.

Thereafter, the polyester film (drug-protecting layer) was lapped.

Then, 20 g of high molecular weight polyisobutylene, 50 g of low molecular weight polyisobutylene, 10 g of isopropyl myristate, 19.7 g of hydrogenated rosin glycerin ester and 0.3 g of butylated hydroxytoluene were added to 257.14 g of heptane And dried at 100 DEG C for 7 minutes to form a release-controlled pressure-sensitive adhesive layer having a thickness of about 80 mu m.

The release-controlled pressure-sensitive adhesive layer prepared by the above method was lapped with the drug-containing layer from which the release layer had been removed, and then cut to a required size to prepare a transdermal preparation.

Example  23:

The primer layer was coated on the release layer using a lab coater (Lab coater, Mathis, Switzerland) so as to have a thickness of 20 탆 after drying using Duro-Tak 87-2852 (Henkel, USA), which is a polyacrylate having a carboxyl group , And dried at 100 DEG C for about 3 minutes. Thereafter, the film was laminated with a drug protective layer (polyester film) on which aluminum was deposited, which functioned to prevent transmission of light and oxygen.

In the drug-containing layer, 30 g of nicotine, 33 g of styrene copolymer, 33 g of alicyclic hydrocarbon resin, 3.12 g of mineral oil and 0.88 g of butylated hydroxytoluene are weighed and completely dissolved in 138.2 g of methylene chloride (MC). The prepared solution was applied on a PET film (release layer) coated with a silicone resin using a lab coater (Mathis, Switzerland) so as to have a thickness of about 63 μm after drying, dried at 50 ° C. for about 1 minute, And a primer layer laminated on an ester film (drug protective layer) to prepare a drug-containing layer. In this case, one surface of the primer layer to be laminated is laminated to the opposite surface of the drug-protected layer, and the drug-containing layer to be produced has its opposite surface to the one surface of the primer layer laminated with the release layer. After removing the release layer from the drug-containing layer thus prepared, a polyacrylate-based adhesive layer (Duro-Tak 87-2852, manufactured by Henkel, USA) having carboxyl groups used for a release- ) Was combined with the drug-containing layer and cut to the required size to prepare a transdermal preparation.

Comparative Example  One:

A storage-type nicotium with a release-controlling membrane commercially available from abroad was used as a comparative example (content-114 mg).

Experimental Example  1: Skin penetration test

Examples 1,2,3,4,5,6,7,8,9,10,11,12,13,14,15,16,17,18,19,20,21,21,23 and Comparative Example 1, and the content of nicotine introduced into the receptor solution was determined by HPLC (High Performance Liquid Chromatography), and the cumulative skin permeation amount was measured for 24 hours. The results are shown in Table 1.

High performance liquid chromatography (HPLC) operating conditions

Mobile phase: acetonitrile: water: triethylamine: 300: 700: 1

Flow rate: 1.0 ml / min

Wavelength: 260 nm

Injection amount: 50 μl

Column: L1 (C18), 4.6 mm x 12. cm column

Temperature: 30 ℃

Skin penetration test method

Transmission device: Frantz Diffusion cell

Sample area: 0.636 cm ²

Receptor solution: Phosphate buffer (PBS, pH = 7.4)

Stirring speed: 600 rpm

Skin: Human skin (male, age 48, Hans Bio)

As shown in Table 1, the percutaneous absorption preparation of Example 1 of the present invention showed a permeation equal to or higher than that of the nikodum of Comparative Example 1, which is an off-the-shelf product. In addition, in Example 20 of the present invention using a skin penetration enhancer, the permeation amount was remarkably superior to that of Comparative Example 1.

While the present invention has been particularly shown and described with reference to exemplary embodiments thereof, it is to be understood that the invention is not limited to the disclosed exemplary embodiments, but, on the contrary, is intended to cover various modifications and equivalent arrangements included within the spirit and scope of the appended claims. It is natural.

1. Drug protection layer
2. Drug-containing layer
3. Release control adhesive layer
4. Release layer
5. Primer layer (primary adhesive layer)

Claims (13)

A transdermal absorption formulation for administration of nicotine,
a) a drug-containing layer consisting of a mixture of nicotine, hydrogenated rosin glycerin ester, aminoalkyl methacrylate copolymer and methylene chloride;
b) a drug protective layer located on top of the drug-containing layer and made of a non-permeable material for the nicotine; And
c) a release-controlling adhesive layer positioned below the drug-containing layer and having a release-controlling function upon permeation of the nicotine; / RTI >
The mixture contains 20 to 26 g of nicotine and 49 to 60 g of aminoalkyl methacrylate copolymer with respect to 20 g of hydrogenated rosin glycerin ester,
Wherein the release-controlling pressure-sensitive adhesive layer comprises at least one of a polyacrylate-vinyl acetate-based pressure-sensitive adhesive free from a functional group and a rubber hybrid polyacrylate pressure-sensitive adhesive.
The method according to claim 1,
The percutaneous absorption preparation comprises
A primer layer positioned intermediate between the drug-containing layer and the drug-protecting layer and for binding thereto;
≪ / RTI >
The method according to claim 1,
And a release layer on the lower part of the release-controlled pressure-sensitive adhesive layer.
delete delete delete delete The method of claim 1, wherein
Wherein the mixture further comprises a skin penetration enhancer.
delete The method according to claim 1,
Wherein the release-controlled pressure-sensitive adhesive layer further comprises a skin penetration enhancer.
3. The method of claim 2,
Wherein the primer layer is a pressure sensitive adhesive.
Preparing a drug-containing layer solution by mixing 20 to 26 g of nicotine and 49 to 60 g of aminoalkyl methacrylate copolymer with 20 g of hydrogenated rosin glycerin ester in methylene chloride;
Applying the solution to form a drug-containing layer;
Laminating a drug protecting layer on one side of the drug containing layer; and
Containing layer on the other side of the drug-containing layer,
Wherein the release-controlling pressure-sensitive adhesive layer comprises at least one of a polyacrylate-vinyl acetate-based pressure-sensitive adhesive free from a functional group and a rubber hybrid polyacrylate pressure-sensitive adhesive.
Laminating one side of the primer layer with the drug protective layer;
Preparing a drug-containing layer solution by mixing 20 to 26 g of nicotine and 49 to 60 g of aminoalkyl methacrylate copolymer with 20 g of hydrogenated rosin glycerin ester in methylene chloride;
Applying the solution to the other surface of the primer layer to form one side of the drug-containing layer;
A step of laminating a release-controlling adhesive layer on the other side of the drug-containing layer; Lt; / RTI >
Wherein the release-controlling pressure-sensitive adhesive layer comprises at least one of a polyacrylate-vinyl acetate-based pressure-sensitive adhesive free from a functional group and a rubber hybrid polyacrylate pressure-sensitive adhesive.

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