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JP2638635B2 - Percutaneous absorption preparation - Google Patents

Percutaneous absorption preparation


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JP2638635B2 JP1023074A JP2307489A JP2638635B2 JP 2638635 B2 JP2638635 B2 JP 2638635B2 JP 1023074 A JP1023074 A JP 1023074A JP 2307489 A JP2307489 A JP 2307489A JP 2638635 B2 JP2638635 B2 JP 2638635B2
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adhesive layer
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JPH02202813A (en
弘子 塚原
正人 東
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【発明の詳細な説明】 (産業上の利用分野) 本発明は薬物を含有する経皮投与形製剤に関する。 BACKGROUND OF THE INVENTION (FIELD OF THE INVENTION) The present invention relates to a transdermal dosage form preparations containing a drug. 本発明は,特に,該薬物の形皮吸収性を高めた経皮吸収製剤に関する。 The present invention particularly relates to a transdermal absorption preparation having enhanced shape skin absorbability of the drug.

(従来の技術) 全身もしくは局部での薬効を得るために,経皮投与経製剤を用い,薬物(生理活性物質)を皮膚を介して吸収させることが行われている。 To obtain a (prior art) efficacy of systemic or local, with transdermal administration via formulation, and drug (physiologically active substance) taking place be absorbed through the skin. この経皮投与法は,従来の経口投与法に比べて利点が多い。 The transdermal administration are often advantages over conventional oral administration. 例えば,薬物を経口投与すると,腸で吸収された薬物は肝臓へ循環して代謝を受けるため,その薬効を発揮する前にかなりの量が分解されてしまう。 For example, when the drug is administered orally, drug is absorbed in the intestine for receiving a circulating metabolites to the liver, a significant amount before exert their efficacy from being degraded. これに対して,経皮投与法では,吸収された薬物は体内の初回循環時に肝臓を通過しない。 In contrast, in the transdermal administration method, drug absorbed does not pass through the liver at the time of the first circulation in the body. そのため,肝臓での代謝により薬効が大幅に減じるということがあに。 Therefore, the fact that efficacy is greatly reduced by metabolism in the liver brother. 非ステロイド系抗炎症剤を経口投与すると胃腸障害を生じやすいが,経皮投与法ではこのような胃腸障害が生じにくい。 The non-steroidal anti-inflammatory drugs prone to gastrointestinal disorders when administered orally, but such gastrointestinal disorders are less likely to occur in the transdermal administration. 薬物の吸収性をコントロールすれば,薬物が短時間に大量に吸収されるために起こる副作用を軽減することが可能となる。 If control the absorption of the drug, it is possible to reduce the side effects occur because the drug is absorbed in large quantities in a short period of time. 長時間にわたり一定の薬物血中濃度を維持できれば薬物の投与回数を減らすこともできる。 It is also possible to reduce the frequency of administration of the drug if maintain a constant drug blood concentration over a long period of time.

しかし,経皮吸収製剤を用いて薬物を投与しても,該薬物が皮膚を投下しにくく生体利用率(バイオアベイラビリティ)が低くなる場合が多い。 However, the administration of drug with a transdermal absorption preparation, the drug is hardly bioavailability dropped the skin (bioavailability) is often lower. 特に,皮膚表面には角質層が存在し,この角質層は体内へ異物が侵入するのを防ぐバリアー機能を有するため,薬理効果を発揮しうるに充分な量の薬物が皮膚を通して吸収されない場合が多い。 In particular, the skin surface is present stratum corneum, the stratum corneum because of its barrier function to prevent the invasion of foreign substances into the body, if a sufficient amount of drug can exert a pharmacological effect is not absorbed through the skin many.

角質層のバリアー機能を弱めて充分な量の薬物を吸収させるべく吸収促進剤を含有させた製剤が製造されている。 Formulations which contains an absorption enhancer in order to absorb a sufficient amount of drug weaken the barrier function of the stratum corneum is manufactured. 例えば,特開昭57−9714号公報,特公昭58−43368 For example, JP 57-9714, JP-Sho 58-43368
号公報,特開昭58−52216号公報,特開昭58−79918号公報,特開昭60−13720号公報および特開昭60−11431号公報には,吸収促進剤を粘着剤層に含有させた貼付剤などが開示されている。 JP, Sho 58-52216, JP-Sho 58-79918 and JP Sho 60-13720 and JP 60-11431, the content of the absorption enhancer in the adhesive layer such adhesive patch was is disclosed.

上記吸収促進剤のうち,例えば,サリチル酸,尿素, Among the absorption enhancers, such as salicylic acid, urea,
ジメチルスルホキシドは角質を溶解することが知られているが,これらを添加しても薬物の経皮吸収性は必ずしも良好でない。 Dimethyl sulfoxide is known to dissolve the horny but percutaneous absorption of the drug be added which are not necessarily good. プロピレングリコール,グリセリン,ピロリドンカルボン酸ソーダなどは角質層に水分を保持させ得るが,薬物吸収促進効果がほとんど認められない。 Propylene glycol, glycerin, etc. pyrrolidone carboxylic acid soda capable of retaining the moisture in the stratum corneum, drug absorption promoting effect is not substantially observed.
ジメチルスルホキシドなどは,皮膚を刺激して紅斑やかぶれを生じやすい。 It is such as dimethylsulfoxide, susceptible to erythema and rash and skin irritation. アジピン酸ジイソプロピルなどのジカルボン酸エステルや脂肪酸エステルを粘着剤層に含有させてテープ製剤とすると,粘着剤と薬物との相溶性が低下するため,薬物が粘着剤から析出しやすく,粘着性が低下することもある。 When tape preparation of dicarboxylic acid esters and fatty acid esters such as diisopropyl adipate is contained in the adhesive layer, the compatibility between the adhesive and the drug is decreased, the drug tends to precipitate from the adhesive, decrease tack sometimes it is. チオグリコール酸カルシウムなどのイオウ含有化合物は悪臭の原因ともなる。 Sulfur-containing compounds such as thioglycolic acid calcium also causes odor. 上記化合物の他,ミリスチン酸エステル,アジピン酸エステル, Besides the above compounds, myristic acid esters, adipic acid esters,
ラウリル硫酸エステル,ポリオキシエチレンアルキルエーテルなども開示されているが,これらの吸収促進剤を用いても皮膚を通しての薬物の吸収量は必ずしも充分であるとはいえない。 Lauryl sulfate, have been also disclosed such as polyoxyethylene alkyl ethers, absorption of the drug through the skin even with these absorption promoters can not be said to be always sufficient. このように,薬物を効果的に吸収させうる経皮吸収製剤はいまだ得られていないのが現状である。 Thus, a percutaneous absorption preparation which can drug effectively to absorb is at present not yet been obtained.

(発明が解決しようとする問題点) 本発明は上記従来の欠点を解決するものであり,その目的とするところは,含有する薬物を効果的に皮膚を通じて吸収させうる製剤を提供することにある。 (To be Solved by the Invention Problems) The present invention has been made to solve the above-mentioned conventional drawbacks, and has as its object to provide a formulation that can effectively be absorbed through the skin the drug containing . 本発明の他の目的は,含有される薬物の経皮吸収性を高め,かつ皮膚に対する刺激性がなく生体に対して安全な吸収促進剤を含有する経皮吸収製剤を提供することにある。 Another object of the present invention is to provide a percutaneous absorption preparation which enhances percutaneous absorbability of the drug to be contained, and contain a safe absorption enhancing agent to a biological, non-irritating to the skin. 本発明のさらに他の目的は,基剤の性質を変化させることがなく,しかも,薬物が析出することがなく,かつ含有される薬物の変性が生じることのない吸収促進剤を含有する経皮吸収製剤を提供することにある。 Still another object of the present invention, without altering the nature of the base include, yet, without drug is precipitated, and transdermal containing that no absorption enhancer degeneration occurs in drug contained It is to provide an absorbent formulations.

(問題点を解決するための手段) 本発明の経皮吸収製剤は,支持体の片面に薬物および該薬物の吸収促進剤を含有する粘着剤層が設けられた経皮吸収製剤であって、該薬物が硝酸イソソルビドであり,該粘着剤層の粘着基剤がアクリル酸2エチルヘキシルおよびビニルピロリドンからなる共重合体であり,該吸収促進剤が没食子酸アルキルエステルであり,該没食子酸アルキルエステルのアルキル基の炭素数が1〜18であり,そのことにより上記目的が達成される。 Percutaneous absorption preparation of the present invention (means for solving the problem) is a percutaneous absorption preparation which adhesive layer is provided which contains an absorption enhancer of drugs and drug on one side of a support, drug is isosorbide dinitrate, a copolymer adhesive base of the pressure-sensitive adhesive layer is composed of an acrylic acid 2-ethylhexyl and vinylpyrrolidone, the absorption-promoting agent is gallic acid alkyl esters, of the gallic acid alkyl ester the number of carbon atoms in the alkyl group is 1 to 18, the objects can be achieved.

本発明に用いられる吸収促進剤は,下記式で示される没食子酸アルキルエステル(3,4,5−トリヒドロキシ安息香酸アルキルエステル)である: Absorption accelerator used in the present invention is a gallic acid alkyl ester represented by the following formula (3,4,5-hydroxybenzoic acid alkyl ester): ここでRは炭素数1〜18のアルキル基である。 Wherein R is an alkyl group having 1 to 18 carbon atoms. 上記没食子アルキルエステルのアルキル基としては,メチル基,エチル基,n−プロピル基,iso−プロピル基,n−ブチル基,iso−ブチル基,sec−ブチル基,tert−ブチル基,n Examples of the alkyl group gallic alkyl esters, methyl group, ethyl group, n- propyl group, iso- propyl, n- butyl, iso- butyl group, sec- butyl group, tert- butyl radical, n
−アミノ基,iso−アミル基,sec−アミル基,tert−アミル基,ネオペンチル基,ヘキシル基,ヘプチル基,オクチル基,2エチルヘキシル基,ノニル基,デシル基,ラウリル基,セチル基,ステアリル基,アリル基などが挙げられる。 - amino group, iso- amyl, sec- amyl group, tert- amyl group, a neopentyl group, a hexyl group, heptyl group, octyl group, 2-ethylhexyl group, nonyl group, decyl group, lauryl group, cetyl group, stearyl group, such as allyl group and the like. このような没食子酸アルキルエステルは製剤中に0.5〜30重量%の割合で含有される。 Such gallic acid alkyl ester is contained in a proportion of 0.5 to 30 wt% in the formulation. この割合は,薬物含有層(粘着剤層)に対する含有量を示す。 This ratio indicates the content to the drug-containing layer (adhesive layer). 後述の薬物含有量についても同様である。 The same applies to the drug content will be described later. 吸収促進剤の量が過少であると薬物の吸収促進効果が得られない。 The amount of absorption enhancer can not be obtained absorption promoting effect of the drug to be too small. 過剰であっても薬物の吸収性はそれ以上向上しないばかりか,粘着物性が低下し,粘着剤との相溶性が悪化する。 Absorption of the drug even in excess not only not improved any more, the adhesive property is lowered, compatibility with the adhesive is deteriorated.

使用される薬物(生理活性物質)は,硝酸イソソルビドに限定される。 Drugs used (physiologically active substance) is limited to isosorbide dinitrate.

硝酸イソソルビドの配合量は,製剤の使用目的により異なるが,通常,薬物含有層(粘着剤層)中に0.1〜30 The amount of isosorbide dinitrate may vary depending on the intended use of the formulation, usually in the drug-containing layer (adhesive layer) from 0.1 to 30
重量%の割合で含有される。 It is contained in a proportion of weight%.

本発明の経皮吸収製剤としては,テープ製剤,パッチ剤などがある。 The percutaneously absorbable preparation of the present invention, there is such a tape preparation, patch.

本発明の経皮吸収製剤は,支持体の片面に薬物と吸収促進剤とを含有する粘着剤層が形成されている。 Percutaneous absorption preparation of the present invention, the pressure-sensitive adhesive layer containing a drug on one side of the support and the absorption enhancer is formed. 本発明の経皮吸収製剤の基剤(粘着剤)は該製剤を常温で皮膚方面に長時間固定しうる粘着力が必要であり,アクリル酸2エチルヘキシルおよびビニルピロリドンからなる共重合体が用いられる。 Bases of the percutaneously absorbable preparation of the present invention (adhesive) is required adhesive strength capable of prolonged secured to the skin surface of the formulation at room temperature, the copolymer is used consisting of acrylic acid 2-ethylhexyl and vinylpyrrolidone .

上記粘着剤中には必要に応じて各種配合剤,例えばロジン系樹脂,ポリテルペン樹脂,クマロン−インデン樹脂,石油系樹脂,テルペンフェノール樹脂などの粘着性付与剤;液状ポリブテン,鉱油,ラノリン,液状ポリイソプレン,液状ポリアクリレートなどの可塑剤;充填剤;老化防止剤;が添加される。 The pressure-sensitive adhesive various additives in accordance with need, for example, rosin resins, polyterpene resins, coumarone - indene resins, petroleum resins, tackifiers such as terpene phenol resins; liquid polybutene, mineral oil, lanolin, liquid poly isoprene, plasticizers such as liquid polyacrylate; fillers; antioxidants; are added.

本発明の経皮吸収製剤に用いられる支持体としては, As the support for use in the percutaneous absorption preparation of the present invention,
貼付剤に通常利用される支持体が用いられる。 Support typically used in patch is used. このような支持体の素材としては,酢酸セルロース,エチルセルロース,ポリエチレンテレフタレート,可塑化酢酸ビニル−塩化ビニル共重合体,ナイロン,エチレン−酢酸ビニル共重合体,可塑化ポリ塩化ビニル,ポリウレタン, Such material of the support, cellulose acetate, ethyl cellulose, polyethylene terephthalate, plasticized vinyl acetate - vinyl chloride copolymer, nylon, ethylene - vinyl acetate copolymer, plasticized polyvinyl chloride, polyurethane,
ポリエチレン,ポリ塩化ビニリデン,アルミニウムなどがある。 Polyethylene, polyvinylidene chloride, and the like of aluminum. これらは,例えば,単層のシート(フィルム) These include, for example, a single-layer sheet (film)
や二枚以上の積層(ラミネート)体として用いられる。 And used as a two or more layered (laminated) form.
アルミニウム以外の素材は織布や不織布として利用してもよい。 Other than aluminum material may be used as a woven fabric or a non-woven fabric.

上記支持体表面に薬物と吸収促進剤とを含有する薬物含有(粘着剤)層が形成されてテープ製剤やパッチ剤が得られる。 Drug-containing (PSA) layer containing a drug and absorption promoter in the support surface is formed tape preparation and patches is obtained. 粘着剤層を形成するには,溶剤塗工法,ホットメルト塗工法,電子線硬化エマルジョン塗工法など種々の塗工法が用いられうる。 To form the adhesive layer, a solvent coating method, hot melt coating method, various coating methods such as electron beam curing emulsion coating method may be employed. なかでも溶剤塗工法が好適に用いられる。 Of these solvents coating method is preferably used. 溶塗工法で粘着剤層を形成するには,例えば,粘着剤を適当な溶媒で稀釈し,これに薬物,吸収促進剤,さらに必要に応じて配合剤を加えて均一に混合し,得られた溶液を支持体表面に塗布・乾燥する。 In order to form the adhesive layer 溶塗 method, for example, to dilute the adhesive with a suitable solvent, to which a drug, an absorption enhancer uniformly mixed by adding the compounding agents if necessary, to obtain the solution coated and dried on a support surface. 溶液を直接支持体表面に塗布せずにシリコーン樹脂などをコーティングした剥離紙上に塗布し,乾燥後に支持体と密着させてもよい。 The solution was applied to a release paper coated with a silicone resin without applied directly support surface may be brought into close contact with the support after drying. このような剥離紙は,使用時まで貼付剤の粘着剤層表面を保護するために用いられる。 Such release paper is used to protect the adhesive layer surface of the adhesive patch until use. 溶剤塗工法以外の塗工法においても粘着剤層形成後,粘着剤層表面保護のために剥離紙を配することが推奨される。 After the pressure-sensitive adhesive layer formed in a coating method other than the solvent coating method, it is recommended to arrange the release paper to the adhesive layer surface protection. 粘着剤層の厚みも使用目的により異なるが,通常,30〜200 Varies depending also intended use thickness of the adhesive layer, usually 30 to 200
μmである。 It is μm. 30μmを下まわると必要量の薬物を含有することができず,粘着性も不充分である。 It can not contain the required amount of the drug when falls below 30 [mu] m, is also insufficient tack. 200μmを上まわると支持体付近の粘着剤層に含有される薬物が充分に拡散せず,薬物及び放出性が低下する。 200μm without drug sufficiently diffused contained in the pressure-sensitive adhesive layer in the vicinity of the support exceed the drug and release is reduced.

(作用) 本発明の経皮吸収製剤を皮膚に密着させると含有される薬物が容易に皮膚を通して吸収される。 (Function) The percutaneously absorbable preparation of the present invention is drug contained and brought into close contact with the skin is readily absorbed through the skin. その詳細な機構は不明であるが,吸収促進剤が皮膚に作用し,その蛋白質を変性させ,含水率を上昇させて軟化させるためと考えられる。 Its detailed mechanism is unknown, absorption enhancer acts on the skin, to denature the protein, believed to soften at elevated moisture content. そのため,通常,薬物を投下しにくい皮膚表面の角質層も軟化して含有される薬物が容易に皮膚を通して吸収されると考えられる。 Therefore, usually, the stratum corneum of the drug dropped hard skin surface is also considered drug contained softened is easily absorbed through the skin.

必要な薬効を得るのに充分な量の薬物が容易に吸収されるため,従来のように大量の薬物を製剤中に含有させる必要がない。 Since a sufficient amount of the drug is easily absorbed to obtain the required efficacy, it is not necessary to be contained in a conventional formulation in a large amount of the drug as. つまり,薬物のバイオアペイラビリティが高い。 In other words, the high drug of bio Ape desirability. このような経皮吸収促進効果は吸収促進剤を用いたときよりもはるかに高い。 Such percutaneous absorption promoting effect is much higher than with an absorption promoting agent. さらに,本発明に用いる吸収促進剤は皮膚に対する刺激性がなく安全性が高い。 Moreover, absorption enhancers for use in the present invention is highly safe, non-irritating to the skin.
吸収促進剤自体が副作用を生じることもない。 Absorption-promoting agent itself does not cause side effects. 含有される薬物を変性させることもない。 No denaturing the drug contained. 基剤との相溶性にも優れる。 Also excellent in compatibility with the base. 薬物と基剤との相溶性に変化を与えないため,調製後の製剤から薬物が析出することもない。 Since the compatibility between the drug and the base does not give change, drug from the formulation after preparation nor deposited. 吸収促進剤自体が粘着剤の粘着機能を低下させるなど粘着剤の物性に悪影響をおよぼすこともない。 Absorption enhancers itself nor adversely affect the physical properties of the adhesive such as to lower the adhesive function of the adhesive.

(実施例) 以下に本発明を実施例について説明する。 (Example) On the invention the following examples will be described.

実施例1 (A)貼付剤(テープ製剤)の調製:アクリル酸2エチルヘキシル85重量部およびビニルピロリドン15重量部からなる共重合体を20重量%の割合で含有する酢酸エチル溶液を調製した。 Example 1 (A) Preparation of the patch (tape preparation) was prepared: ethyl acetate solution containing a proportion of a copolymer comprising 2-ethylhexyl 85 parts by weight of vinyl pyrrolidone 15 parts by weight of acrylic acid 20% by weight. この溶液100重量部に対して,薬物として硝酸イソソルビド(ISDN)3重量部,経皮吸収促進剤として没食子酸n−プロピル1重量部を添加し,ディゾルバーで充分に撹拌して均一な溶液を得た。 Obtained for this solution 100 parts by weight, isosorbide dinitrate (ISDN) 3 parts by weight as a drug, and 1 part by weight of gallic acid n- propyl as percutaneous absorption promoter, sufficiently stirred to a uniform solution in a dissolver It was. これを片面が離型処理された厚さ45μmのポリエチレンテレフタレート(PET)フィルム上に乾燥後の厚さが40μmとなるように塗布し,65℃のギアオーブンで20分間乾燥した。 This one side was coated to a dry thickness of the release treated thickness 45μm polyethylene terephthalate (PET) on the film is 40 [mu] m, and dried for 20 minutes at 65 ° C. gear oven. 得られた粘着剤層表面に支持体として厚さ10μmの The resultant pressure-sensitive adhesive layer surface of the thick 10μm as a support
PETフィルムをラミネートした。 It was laminated PET film. この貼付剤の粘着剤層中の薬物濃度は12.5重量%,そして吸収促進剤の濃度は Drug concentration 12.5% ​​by weight of the adhesive layer of the patch, and the concentration of absorption enhancer
4.2重量%である。 4.2 percent by weight.

(B)貼付剤の性能評価:(A)項で得られた貼付剤を (B) patch Evaluation of: a patch obtained in item (A)
10cm 2の大きさに裁断し,これを日本白色家兎の脱毛した背部の皮膚表面に貼付した。 Was cut into a size of 10cm 2, it was attached it to the depilated skin surface of the back of a Japanese white rabbit. 0.5時間後,1時間後,2時間後,4時間後,6時間後,10時間後および24時間後に家兎の耳介静脈から採血し,遠心分離を行って血漿を得た。 After 0.5 hours, 1 hour, 2 hours, 4 hours, 6 hours, blood was collected from the auricular vein of the rabbit after 10 hours and 24 hours to obtain plasma by centrifugation.
これをヘキサンで抽出し,Ni 63 ECDガスクロマトグラフィーにかけ薬物濃度を測定した。 This was extracted with hexane, it was measured drug concentration over the Ni 63 ECD gas chromatography. その結果を表1に示す。 The results are shown in Table 1.
24時間後に貼付剤を剥離したが,皮膚表面に発赤,かぶれなどの障害は認められなかった。 Peeling the patch after 24 hours, redness on the skin surface, disorders such as rash was observed.

比較例1 (A)貼付剤(テープ製剤)の調製:吸収促進剤を加えなかったこと以外は実施例1(A)項と同様である。 Preparation of Comparative Example 1 (A) patch (tape preparation): except that no addition of absorption enhancers is the same as in Example 1 (A) section.

(B)貼付剤の性能評価:本比較例(A)項で得られた貼付剤を用い,実施例1(B)項と同様に行った。 (B) patch Evaluation of: using a patch obtained in this Comparative Example (A) section, was carried out in the same manner as in Example 1 (B) section. その結果を表1に示す。 The results are shown in Table 1. 24時間後に貼付剤を剥離したが,皮膚表面に発赤,かぶれなどの障害は認められなかった。 Peeling the patch after 24 hours, redness on the skin surface, disorders such as rash was observed.

比較例2 (A)貼付剤(テープ製剤)の調製:吸収促進剤としてサリチル酸1重量部を用いたこと以外は実施例1と同様である。 Preparation of Comparative Example 2 (A) patch (tape preparation): except for using salicylic acid 1 part by weight of absorption enhancer is the same as the first embodiment.

(B)貼付剤(テープ製剤)の性能評価:本比較例(A)項で得られた貼付剤を用い,実施例1(B)項と同様に行った。 Evaluation of (B) the patch (tape preparation): using the patch obtained in this Comparative Example (A) section, was carried out in the same manner as in Example 1 (B) section. その結果を表1に示す。 The results are shown in Table 1. 24時間後に貼付剤を剥離したところ,皮膚表面にわずかな発赤が認められた。 Was peeling off the patch after 24 hours, a slight redness was observed on the surface of the skin.

(発明の効果) 本発明によれば,このように,没食子酸アルキルエステルを吸収促進剤として製剤中に含有させることにより,薬物の経皮吸収性を極めて優れた製剤が得られる。 According to the present invention (Effect of the Invention), thus, by incorporating in the formulation a gallic acid alkyl ester as an absorption promoting agent, excellent formulations percutaneous absorption of the drug is obtained.
薬物の吸収性が優れているため,必要な薬理効果を得るために従来のような大量の薬物を製剤中に含有させる必要がない。 The absorption of the drug is excellent, it is not necessary to be contained in the formulation in the conventional large amounts of drugs such as to obtain a pharmacological effect required. 用いられる吸収促進剤は皮膚に対する刺激性がないため,長時間貼付してもかぶれが生じない。 Because there is no irritating absorption enhancer to the skin to be used, it does not occur rash be affixed long. 吸収促進剤自体が吸収されて副作用を示すこともない。 Absorption enhancers itself is absorbed nor to exhibit side effects. 薬物を変質させることもない。 There is no possible to alter the drug. さらに,吸収促進剤が原因となって薬物が析出したり,粘着性が低下することもない。 Additionally, or drug precipitates causing absorption enhancer, it is not reduced stickiness. このような製剤では,硝酸イソソルビドを経皮吸収させることができ,該製剤を用いたときの治療効果も高い。 In such formulations, it is possible to transdermally absorb the isosorbide dinitrate, therapeutic effect is high when using the formulation.

Claims (3)

    (57)【特許請求の範囲】 (57) [the claims]
  1. 【請求項1】支持体の片面に薬物および該薬物の吸収促進剤を含有する粘着剤層が設けられた経皮吸収製剤であって, 該薬物が硝酸イソソルビドであり, 該粘着剤層の粘着基剤がアクリル酸2エチルヘキシルおよびビニルピロリドンからなる共重合体であり, 該吸収促進剤が没食子酸アルキルエステルであり, 該没食子酸アルキルエステルのアルキル基の炭素数が1 1. A transdermal preparation of pressure-sensitive adhesive layer is provided which contains an absorption enhancer of drugs and drug on one side of a support, the drug is isosorbide dinitrate, the adhesive of the adhesive layer a copolymer based agent consisting of acrylic acid 2-ethylhexyl and vinylpyrrolidone, the absorption-promoting agent is gallic acid alkyl ester, the carbon number of the alkyl group of the alkyl gallate is 1
    〜18である, 経皮吸収製剤。 It is to 18, percutaneous absorption preparation.
  2. 【請求項2】前記吸収促進剤を0.5〜30重量%の割合で含有する特許請求の範囲第1項に記載の経皮吸収製剤。 2. A percutaneous absorption preparation according to paragraph 1 the claims containing the absorption enhancer in a proportion of 0.5 to 30 wt%.
  3. 【請求項3】テープ製剤である特許請求の範囲第1項に記載の経皮吸収製剤。 3. A percutaneous absorption preparation according to paragraph 1 claims a tape preparation.
JP1023074A 1989-01-31 1989-01-31 Percutaneous absorption preparation Expired - Fee Related JP2638635B2 (en)

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AU2514292A (en) * 1991-08-27 1993-03-16 Cygnus Therapeutic Systems Transdermal formulations for administering prazosin
FR2719770B1 (en) * 1994-05-11 1997-02-21
AU4031897A (en) * 1996-08-29 1998-03-19 Sekisui Kagaku Kogyo Kabushiki Kaisha Stanozolol-containing percutaneously absorbable preparation
US5962522A (en) * 1997-09-05 1999-10-05 Avmax, Inc. Propyl gallate to increase bioavailability of orally administered pharmaceutical compounds
US6193996B1 (en) * 1998-04-02 2001-02-27 3M Innovative Properties Company Device for the transdermal delivery of diclofenac
JP4880813B2 (en) * 2000-10-26 2012-02-22 第一三共ヘルスケア株式会社 Topical anti-inflammatory analgesic composition
NO20014746D0 (en) * 2001-09-28 2001-09-28 Clas M Kjoelberg Analgesic agent
CA2561082C (en) * 2003-03-27 2014-07-15 Santosolve As Anti-inflammatory treatment based on strontium compounds
ES2336214T3 (en) 2003-10-27 2010-04-09 Universitat Basel System transdermal drug delivery.
CA2580329C (en) 2004-09-13 2015-01-06 Chrono Therapeutics, Inc. Biosynchronous transdermal drug delivery
US8252321B2 (en) 2004-09-13 2012-08-28 Chrono Therapeutics, Inc. Biosynchronous transdermal drug delivery for longevity, anti-aging, fatigue management, obesity, weight loss, weight management, delivery of nutraceuticals, and the treatment of hyperglycemia, alzheimer's disease, sleep disorders, parkinson's disease, aids, epilepsy, attention deficit disorder, nicotine addiction, cancer, headache and pain control, asthma, angina, hypertension, depression, cold, flu and the like
US8372040B2 (en) 2005-05-24 2013-02-12 Chrono Therapeutics, Inc. Portable drug delivery device including a detachable and replaceable administration or dosing element
US10105487B2 (en) 2013-01-24 2018-10-23 Chrono Therapeutics Inc. Optimized bio-synchronous bioactive agent delivery system

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