JPS5984815A - Pharmaceutical for prolonged release of chemical - Google Patents
Pharmaceutical for prolonged release of chemicalInfo
- Publication number
- JPS5984815A JPS5984815A JP57195647A JP19564782A JPS5984815A JP S5984815 A JPS5984815 A JP S5984815A JP 57195647 A JP57195647 A JP 57195647A JP 19564782 A JP19564782 A JP 19564782A JP S5984815 A JPS5984815 A JP S5984815A
- Authority
- JP
- Japan
- Prior art keywords
- chemical
- drug
- storage layer
- impermeable
- layer
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- Medicinal Preparation (AREA)
- Materials For Medical Uses (AREA)
Abstract
Description
【発明の詳細な説明】
本発明は、薬理活性を有する薬剤を長期にわたって、制
御された速度で放出する薬剤徐放性製剤に関する。DETAILED DESCRIPTION OF THE INVENTION The present invention relates to sustained release drug formulations that release pharmacologically active drugs at a controlled rate over an extended period of time.
薬剤を投与して所期の治療効果を達成するには、疾患部
又は循環系に長期間にわたって薬剤を有効濃度以上に維
持することが望ましく、このため、従来より薬剤を制御
された速度で放出する徐放性薬剤が種々提案されている
。代表的には、特公昭５４−４６５６６号公報に記載さ
れているように、外側表面をなす裏打ち部材と、皮膚又
は粘膜との接着面をなす感圧性接着剤層と、これら裏打
ち部材及び接着剤層との間の薬剤を含有する薬剤貯蔵層
とからなる積層体である。貯蔵層は、薬剤を透過させて
、その放出速度を制御する樹脂層と、このような樹脂層
中に例えば、単に分散され、或いはマイクロカプセルと
して分散された薬剤とからなり、薬剤は貯蔵層から接着
剤層を拡散して、制御された速度で表面から徐放され、
接着面における皮膚若しくは粘膜から体内に吸収される
。場合によっては、貯蔵層と接着剤層との間に、薬剤の
拡散速度が貯蔵層よりも小さい制御層を介在させること
がある。To achieve the desired therapeutic effect by administering a drug, it is desirable to maintain the drug at an effective concentration or higher in the diseased area or the circulatory system for a long period of time, and for this reason it is conventional to release the drug at a controlled rate. Various sustained release drugs have been proposed. Typically, as described in Japanese Patent Publication No. 54-46566, a backing member forming the outer surface, a pressure-sensitive adhesive layer forming the adhesive surface to the skin or mucous membrane, and these backing members and adhesive It is a laminate consisting of a drug storage layer containing a drug between the layers. The storage layer consists of a resin layer that is permeable to the drug and controls its release rate, and a drug that is dispersed, for example, simply or as microcapsules, in such a resin layer, and the drug is released from the storage layer. diffuses through the adhesive layer and is released slowly from the surface at a controlled rate.
It is absorbed into the body through the skin or mucous membrane at the adhesive surface. In some cases, a control layer in which the diffusion rate of the drug is lower than that of the storage layer may be interposed between the storage layer and the adhesive layer.
しかし、このような徐放性製剤においても、尚、長゛期
間にわたって薬剤が実質的に一定の速度で放出する徐放
性が十分満足すべきものではなく、更に、薬剤の種類に
応じてその放出速度を種々変化させて制御することが困
難であって、放出速度が限定されることが多い。更に、
上記のような徐放性製剤によれば、長期間にわたって皮
膚等に適用すると、貼着面が発メモ等によりかぶれを生
しることがある。However, even in such sustained-release preparations, the sustained-release property of releasing the drug at a substantially constant rate over a long period of time is not fully satisfactory, and furthermore, the release rate varies depending on the type of drug. The rate of release is often limited because it is difficult to vary and control the rate. Furthermore,
When such sustained-release preparations are applied to the skin for a long period of time, the surface to which they are applied may develop a rash due to memos, etc.
本発明は」−記した間１題をＩＷ決するためになされた
ものであって、長期間にわノこって薬剤を実質的に一定
の速度で放出して、適用面から体内に吸収される薬剤の
血中ａ度を実質的に−・定に保つ徐放性にずくれ、更に
、薬剤の放出速度を広い範囲で制御することができると
共に、皮屑等への貼着面が通気性を有するため、かふれ
の生しない徐放性製剤を提供することを目的と３−る。The present invention has been devised to solve the problem mentioned above, and is to release a drug at a substantially constant rate over a long period of time so that it is absorbed into the body from the surface to which it is applied. It has a sustained release property that keeps the blood concentration of the drug at a substantially constant level, and also allows the release rate of the drug to be controlled over a wide range, and the surface to which it is attached to skin debris is breathable. Therefore, the purpose of the present invention is to provide a sustained release preparation that does not cause rash.
本発明の徐放性製剤は、（δ）裏打ち７ｉ１（祠と、（
ｂ）薬剤を含有し、上記裏打５９１書７ｊの上に積）饗
された薬剤貯蔵層と、（Ｃ１この薬剤貯蔵層の上に積層
された゛薬剤不透過Ｘ性圏と、Ｔｄ）薬剤透過性の・前
壁を有し、その開口ｆ＋１Ｍが上記薬剤不透過層を貫通
して上記薬剤貯蔵層内に開口する中空繊維とからなるこ
とを特徴とするものである。The sustained release preparation of the present invention has (δ) lining 7i1 (shrine) and (
b) A drug storage layer containing a drug and layered on top of the above-mentioned lining 591-7j; The device is characterized in that it has a front wall, and an opening f+1M thereof is made of a hollow fiber that penetrates the drug impermeable layer and opens into the drug storage layer.
以下に実施例を示す図面に基づいて本発明を説明する。The present invention will be described below based on drawings showing examples.
軒打ち部＋４１は非ｒｉＪ撓性又は可撓性いＪ゛れてあ
ってもよいが、徐放性製剤の多くカ皮喝”や粘膜上に接
着されて適用されるので、打ましくは可撓性の薬剤不透
過性のシー！−＋」料てあ・って、好ましい具（２（８
例として、ｌ！’（Ｉｌ：ｉｕ ｉシルロース、ニーブ
ールセルし＋ −ス、セＩ゛１ハン、ボリエ・チし・ン
テレフタレー１−３可塑化湧Ｙ酸ヒュルー塩１ヒビニル
共市合体 ポリアミド、ポリエチレン、ポリ塩化ビｊ−
リー）′−ン等の樹脂シート若しくはフィルノ１、アル
ミニウム箔等の金属箔、及びこれらの２以上の積層体を
挙げることができる。The eave part 41 may be non-flexible or flexible, but since many sustained release preparations are applied by adhering to the skin or mucous membranes, it is preferable to A flexible, drug-impermeable sheet!
As an example, l! '(Il: iu i silulose, niebour cell + -se, sei 1 han, borie chisi, ntelephthalate 1-3 plasticizing spring Y acid fur salt 1 hibinyl combination polyamide, polyethylene, polyvinyl chloride
Examples include resin sheets such as LEAN) or FILNO 1, metal foils such as aluminum foil, and laminates of two or more of these.
本発明の徐放性製剤において４Ｊ、この裏゛打り部相］
の一表「１１１上に薬剤１１’ｉ’ｉｒ１瓦Ｊｅｔ ２
か、１７１層されている。In the sustained release preparation of the present invention, 4J, this backing part]
A table of ``111 on drug 11'i'ir1 tile Jet 2
There are 171 layers.
この貯蔵層は、薬剤透過性樹脂又ｔｉｔ薬剤溶解性溶剤
と、これに含有される薬剤とからなる。薬剤透過性樹脂
中に薬剤が含゛有される態様は特に制限されない、例え
ば、樹脂と薬剤とを溶融混合し、シー ｌ−状に成形さ
れたものでも、Ｊ、く、また、薬剤を粉末又は液状で樹
脂層中に均一に分散させたものでもよい。更に、薬剤は
マイク１：ｉカプセルとして樹脂層中に分散されていて
もよい。薬剤溶解性溶剤中に薬剤が含有される場合は、
通常、薬剤は溶剤に溶解された溶液として薬剤貯蔵層を
形成する。This storage layer consists of a drug-permeable resin or a tit drug-soluble solvent and a drug contained therein. The manner in which the drug is contained in the drug-permeable resin is not particularly limited. Alternatively, it may be in liquid form and uniformly dispersed in the resin layer. Additionally, the drug may be dispersed in the resin layer as Microphone 1:i capsules. If the drug is contained in a drug-soluble solvent,
Typically, the drug is dissolved in a solvent to form the drug reservoir.
本発明におい−Ｃ用いる薬剤は、皮ｊ首や粘ｊ模から体
内に吸収されて、所期の薬理効果を発現する薬剤であれ
ば、特に制限されるものでばないが、例えば、二１・１
コグリセリン、硝酸イソソルビ１等の抗狭心症剤、アト
ロビン、スコポラミン等の抗ｋｊ１里剤、ペニシリン、
デトラジ・イクリン、クロｌ」テトラサイクリン、オキ
シテトラザイクリン、スルボンアマイド等の抗生物質、
パルビクール、フェノハルビタール、ペントハルヒター
ル、α−ジブ１：１モイソバレリル尿素：ｌディン等の
鎮痛ｆ１旧ＩＩ（剤、インドメザシン、メフェナム酸、
ジクロツェナツク、アルクロフエナ゛ンク、フコニニル
）゛タソ゛ン等の消炎鎮痛剤、りｌ：ｌ ｌ：Ｉプロマ
シン、チオリダジン、ディアセバム、レセルピン、へロ
ペリドール等の精神安定剤、３−（２−アミノブチル）
インドールアセテート等の精神活力剤、ブレドニゾＩコ
ン・ハイドロコルチゾン、フルオシノロンアセトニ１゛
、トリアムシノロノア−１トトニ）、メチルテストステ
１：１ン、メゲスヲーＬ：ｌ−ルアセテ〜１・、フルレ
オご１−ジムステＬＪン、エステじノン、ニス１シジオ
ール、エチニルエストラジオール、Ｊ７α−ヒ１１，１
キシプロゲステＩ′Ｊンアセテー１、Ｌ９−ノルプロヶ
ステロン、ノドしＪキシプ１１−１ゲステ１：Ｊンアセ
テートー等のステＩコ−（）ホルモン、アセチルヅ″リ
チル酸、す′リチルアマイ゛ト、ザリヂル散り・１リウ
ム等の解ｐＪＨ剤等を含む。尚、これらの薬剤が皮屑゛
又は粘１１ｆｆｉがら吸収され難いときは、薬学的Ｑこ
許容される溶液とされてよく、また、必要に応じて薬学
的に許容される誘導体とされてもよい。The drug used in the present invention is not particularly limited as long as it is absorbed into the body through the skin or mucous membrane and exerts the desired pharmacological effect.・1
Anti-anginal agents such as coglycerin and isosorbic acid nitrate, anti-KJ1 agents such as atrophin and scopolamine, penicillin,
Antibiotics such as detradi-iclin, chlorotetracycline, oxytetracycline, sulvonamide, etc.
Analgesic f1 old II (agents such as parvicur, phenoharbital, pentohalchtal, α-dibu 1:1 moisovaleryl urea:l din, indomezacin, mefenamic acid,
Anti-inflammatory analgesics such as diclozenac, alclofenac, fuconinil), tranquilizers such as Ipromacin, thioridazine, diasebam, reserpine, heroperidol, 3-(2-aminobutyl)
Mental energizers such as indole acetate, hydrocortisone, fluocinolone acetate, triamcinolone, methyltestosterone 1:1, megesuwo L:l-acetate, Flureo Go 1-Jimste LJ, Esteninone, Nis 1 Sidiol, Ethinyl Estradiol, J7α-Hi 11,1
Xyprogesteone acetate 1, L9-norprogesterone, Nodoshi Jxyp11-1 gesteone 1: Stereoco-() hormones such as acetate, acetyl lythyl acid, lythyl amide, xyridyl scattering. Contains anti-PJH agents such as 1lium.If these drugs are difficult to absorb through skin or mucus, they may be made into a pharmaceutically acceptable solution, and if necessary, pharmaceutically acceptable solutions may be used. may be a legally acceptable derivative.
薬剤貯蔵層を構成するための樹脂は、薬剤透過性を有す
れば、特に制限されないが、例えば、ポリシメチルシ１
フキリーンのようなシリ、：１−ン樹刀ｎ、ボｊｌヒト
ロキシルエナル（ツタ）アクリレート、ポリメチルアク
リレート、ポリブチルアクリレート等の３よ・うなポリ
（ツタ）アクリル酸エステル、ポリアクリル酸、その
塩、ポリビニルアルコール、ポリ酢酸ビニル、ポリエチ
レンワックス、ポリエチレンオキサイド、ポリビニルピ
ロリドン、ヒドロキシエチルセルロース、カルボキシメ
チルセルロース、可塑化ポリ塩化ビニル、可塑化ポリア
ミド、ポリウレタン、ポリイソブチレン、スチレン−ブ
タジェンゴム、エチレン−酸化炭素共重合体、コラーゲ
ン、ゼラチン、アカシアゴム、トラガカントゴム等の合
成又は天然の樹脂やゴムが好ましく用いられる。The resin for forming the drug storage layer is not particularly limited as long as it has drug permeability;
Poly(vine) acrylic esters, polyacrylic acid, etc. Salt, polyvinyl alcohol, polyvinyl acetate, polyethylene wax, polyethylene oxide, polyvinylpyrrolidone, hydroxyethyl cellulose, carboxymethyl cellulose, plasticized polyvinyl chloride, plasticized polyamide, polyurethane, polyisobutylene, styrene-butadiene rubber, ethylene-carbon oxide copolymer Synthetic or natural resins and rubbers such as , collagen, gelatin, gum acacia, and gum tragacanth are preferably used.
また、薬剤貯蔵層を形成するための溶剤としては、薬剤
の種類及び制御すべき薬剤の放出速度を考慮して適宜に
選ばれるが、例えば、鉱油、シリコーン油のほか、ジエ
チレングリコール、プロピレングリコール、ポリエチレ
ングリコール等のグリコール類、オリーブ油、スクアレ
ン、ラノリン等の油脂類等が好ましく用いられる。尚、
必要に応じて、上記樹脂にこれらの溶剤を混合し、薬剤
を含有させて薬剤貯蔵層としてもよい。In addition, the solvent for forming the drug storage layer is appropriately selected in consideration of the type of drug and the release rate of the drug to be controlled, but examples include mineral oil, silicone oil, diethylene glycol, propylene glycol, polyethylene glycol, etc. Glycols such as glycol, oils and fats such as olive oil, squalene, and lanolin are preferably used. still,
If necessary, these solvents may be mixed with the resin to contain a drug to form a drug storage layer.
本発明の徐放性製剤においては、この薬剤貯蔵層の上に
薬剤不透過層３が設けられている。この薬剤不透過層は
前記した裏打ち部材を構成する”樹脂のほか、例えば、
ポリプロピレン、エチレン−酢酸ビニル共重合体、ポリ
塩化ビニル、塩化ビニル−エチレン共重合体、ポリスル
ホン、ポリフェニレンオキサイド、ポリカーボネート、
芳香族ポリアミド、ポリアセタール、ポリフルオロエチ
レン等からなるシート又はフィルムが好ましいが、必要
ならば、エポキシ樹脂、メラミン樹脂等も用いられる。In the sustained release preparation of the present invention, a drug impermeable layer 3 is provided on this drug storage layer. This drug-impermeable layer includes, in addition to the above-mentioned "resin" that constitutes the backing member, for example,
Polypropylene, ethylene-vinyl acetate copolymer, polyvinyl chloride, vinyl chloride-ethylene copolymer, polysulfone, polyphenylene oxide, polycarbonate,
Sheets or films made of aromatic polyamide, polyacetal, polyfluoroethylene, etc. are preferred, but if necessary, epoxy resins, melamine resins, etc. may also be used.
本発明の徐放性製剤においては、薬剤透過性の管壁を有
する中空繊維４が薬剤不透過層を貫通し、その開口端５
を薬剤貯蔵層中に開口すると共に、中空繊維の大部分を
占める本体部６が、不透過層に関して薬剤貯蔵層と反対
側から外部に露出される。中空繊維は既に種々の重合体
からなるものが知られており、容易に入手できる。本発
明においては、好ましくは、中空繊維は予め織布又は編
布化され、薬剤不透過層と一体的に構造化されて、薬剤
貯蔵層上に積層される。このように中空繊維の開口端が
薬剤不透過層を貫通する構造物は、例えば、中空繊維織
布を所定形状に裁断した後、開目端を有するその周縁部
を薬剤不透過性樹脂の溶液又は溶融液の液面より高く保
ちつつ、織布をこれらに浸漬した後、上記溶液又は熔融
液を加熱して溶剤を蒸発させ、若しくは冷却して凝固さ
せればよい。但し、これらの方法に限定されるものでは
なく、例えば、注型によることもできる。In the sustained release preparation of the present invention, hollow fibers 4 having drug-permeable tube walls penetrate the drug-impermeable layer, and the open ends 5
is opened into the drug storage layer, and the main body portion 6, which occupies most of the hollow fibers, is exposed to the outside from the side opposite to the drug storage layer with respect to the impermeable layer. Hollow fibers made of various polymers are already known and easily available. In the present invention, the hollow fibers are preferably woven or knitted in advance, structured integrally with the drug-impermeable layer, and then laminated onto the drug storage layer. A structure in which the open ends of the hollow fibers penetrate the drug-impermeable layer can be obtained by, for example, cutting a hollow fiber woven fabric into a predetermined shape, and then cutting the periphery with the open ends into a drug-impermeable resin solution. Alternatively, the woven fabric may be immersed in the molten liquid while keeping the temperature higher than the liquid level, and then the solution or molten liquid may be heated to evaporate the solvent, or may be cooled and solidified. However, it is not limited to these methods; for example, casting may also be used.
本発明において、中空繊維は、管壁自体が薬剤を拡散透
過させてもよく、或いは薬剤不透過性の管壁が薬剤を透
過さゼる微孔を有してもよい。中空繊維の素材、壁厚、
径等は用いられる薬剤の種類、所要の拡散速度等によっ
て適宜に選ばれるが、例えば、管径は通常５０〜１００
０μｍであり、管壁が微孔を有する場合は、その孔径は
１０ ｔｔ ｍ以下が適当である。In the present invention, the hollow fiber may have a tube wall itself that allows the drug to diffuse through it, or a drug-impermeable tube wall that has micropores that allow the drug to pass through. Hollow fiber material, wall thickness,
The diameter etc. are appropriately selected depending on the type of drug used, the required diffusion rate, etc., but for example, the tube diameter is usually 50 to 100 mm.
0 μm, and if the tube wall has micropores, the appropriate pore diameter is 10 tt m or less.
また、必要に応して、」二記した中空繊維管内に薬剤貯
蔵層の形成に用いられる溶剤を充填させて、中空繊維内
を薬剤が拡散する速度を調整することもできる。Furthermore, if necessary, the speed at which the drug diffuses within the hollow fibers can be adjusted by filling the hollow fiber tubes described in section 2 with a solvent used to form the drug storage layer.
以上のように、本発明の徐放性製剤によれば、薬剤透過
性樹脂層に含有された薬剤は、貯蔵層を拡散して、この
貯蔵層内に開口している開口端から中空繊維内を薬剤不
透過層を越えて外部に拡散し、中空繊維の管壁から直接
に皮膚若しくは粘膜に接する表面に拡散するので、実質
的に一定の制御された速度で放出される。特に、本発明
の徐放性製剤によれば、中空繊維の材質、管壁の厚みや
その微孔孔径を調整することにより、種々の薬剤につい
てその放出速度を所要の一定値に調整して、体内に吸収
された薬剤の血中濃度をほぼ−・定に保つことができる
と共に、更に、中空繊維からなる織布のような通気性の
ある構造物が皮膚、粘膜等に接するので、従来の徐放性
製剤と異なり、接触面が通気性を有するために、接触面
における斤等による皮膚のかぶれが起こらない。As described above, according to the sustained release preparation of the present invention, the drug contained in the drug-permeable resin layer diffuses through the storage layer and enters the hollow fibers from the open end opening into the storage layer. diffuses outward across the drug-impermeable layer and from the tube wall of the hollow fiber directly to the surface in contact with the skin or mucous membrane, thereby being released at a substantially constant and controlled rate. In particular, according to the sustained-release preparation of the present invention, the release rate of various drugs can be adjusted to a required constant value by adjusting the material of the hollow fiber, the thickness of the tube wall, and the diameter of the micropores. It is possible to maintain the blood concentration of drugs absorbed into the body at a nearly constant level, and in addition, because the breathable structure such as woven fabric made of hollow fibers comes into contact with the skin, mucous membranes, etc., conventional Unlike sustained-release preparations, the contact surface is breathable, so skin irritation due to the contact surface does not occur.
以下に実施例を挙げて本発明を説明するが、本発明はこ
れら実施例により何ら限定されるものではない。The present invention will be explained below with reference to Examples, but the present invention is not limited to these Examples in any way.
実施例１
ポリアミド系中空繊維（内径３００μ、管壁厚み１００
μｍ、管壁微孔孔径平均３０人）を厚み０．２鶴、見掛
は空隙率４０％の織布となし、これを直径ＩＱｃ＋ｎの
円形に裁断した。この織布において、その周縁の中空繊
維の開口端が、ポリ塩化ビニルのテトラヒドロフラン溶
液の液面より上に位置するように保持しつつ、溶剤を蒸
発させて、ポリｆｆｉ化ビニルをフィルム化し、このよ
うにして、厚み０．２ ｉｎのフィルムの一方の面上に
開口端を有する中空繊維と樹脂フィルムとからなる構造
物を形成した。Example 1 Polyamide hollow fiber (inner diameter 300μ, tube wall thickness 100μ)
A woven fabric having a thickness of 0.2 mm and an apparent porosity of 40% was cut into a circular shape with a diameter of IQc+n. In this woven fabric, the open ends of the hollow fibers at the periphery are held above the level of the solution of polyvinyl chloride in tetrahydrofuran, and the solvent is evaporated to form the polyvinyl into a film. In this way, a structure consisting of a resin film and a hollow fiber having an open end on one side of a 0.2 inch thick film was formed.
次に、これをポリエチレングリコール（分子量４００）
のエタノール溶液に浸漬した後、乾燥させて、中空繊維
内にポリエチレングリコールを含浸させた。Next, add this to polyethylene glycol (molecular weight 400)
The hollow fibers were immersed in an ethanol solution and dried to impregnate polyethylene glycol into the hollow fibers.
別に、３０％硝酸イソソルビドー乳糖混合物１０重量部
、ポリエチレングリコール（分子量４００）１重量部及
びヒドロキシエチルアクリレート−エチルアクリレート
（重量比３／１）共重合体８９重量部をメタノール−ア
セトン混合溶剤に熔解して、均一な溶液とし、これをア
ルミニウム箔上に塗布し、５０℃の温度で溶剤を蒸発乾
燥させて、厚み０．２ ｍｍの薬剤貯蔵層を形成した。Separately, 10 parts by weight of 30% isosorbide nitrate lactose mixture, 1 part by weight of polyethylene glycol (molecular weight 400), and 89 parts by weight of hydroxyethyl acrylate-ethyl acrylate (weight ratio 3/1) copolymer were dissolved in a methanol-acetone mixed solvent. This was applied to an aluminum foil to form a homogeneous solution, and the solvent was evaporated and dried at a temperature of 50° C. to form a drug storage layer with a thickness of 0.2 mm.
この薬剤貯蔵層の上に上記の中空繊維とポリ塩化ビニル
フィルムとからなる構造物を、中空繊維開口端が薬剤貯
蔵層内に゛埋没されるように積層接着して、本発明の徐
放性製剤を得た。A structure made of the hollow fibers and polyvinyl chloride film described above is laminated and bonded on top of the drug storage layer so that the open ends of the hollow fibers are buried in the drug storage layer. A formulation was obtained.
この製剤を体！ ３．７ ｋｇのウサギの脱毛した背部
に貼付して、硝酸イソソルビドの血中濃度を測定した。Take this formulation to your body! The blood concentration of isosorbide nitrate was measured by applying it to the depilated back of a 3.7 kg rabbit.
結果を表に示す。尚、血中濃度の測定方法は次の通りで
ある。製剤を上記のように貼付した後、所定時間ごとに
３ｍｌずつ採血し、血漿を分離した後、４ｍｌのへキサ
ンで抽出した。次に、これを不活性ガス中で蒸発乾固し
、１００μρの酢酸エチルに溶解し、ＥＣＤ−ガスクロ
マトグラフィーにて測定した。The results are shown in the table. The method for measuring blood concentration is as follows. After applying the preparation as described above, 3 ml of blood was collected at predetermined intervals, plasma was separated, and extracted with 4 ml of hexane. Next, this was evaporated to dryness in an inert gas, dissolved in 100 μρ of ethyl acetate, and measured by ECD-gas chromatography.
また、この製剤は長期にわたる使用によっても、接触面
に発汗によるかぶれ等は認められなかった。Furthermore, even after long-term use of this preparation, no rash caused by sweat was observed on the contact surface.
実施例２
ポリスルボン中空繊維（内径３００μ、□管壁厚み１０
０μ、管壁微孔孔径平均１００人）を厚み０、３ ｘｍ
、見掛は空隙率４０％の織布となし、これを直径１０印
の円形に裁断した。この織布周縁の中空繊維の開口端が
ポリエチレン溶融浴上に位置するように保持して浴に浸
漬し、次いで、ポリエチレンを冷却凝固させて、厚みＱ
、 ２ｍｍのポリエチレンフィルムめ一方の面上に中空
繊維が開口端を有する構造物を形成した。Example 2 Polysulfone hollow fiber (inner diameter 300μ, □tube wall thickness 10
0 μ, tube wall micropore diameter (average 100), thickness 0.3 x m
A woven fabric with an apparent porosity of 40% was cut into a circle with a diameter of 10. The open ends of the hollow fibers at the periphery of this woven fabric are held so as to be positioned above the polyethylene molten bath and immersed in the bath, and then the polyethylene is cooled and solidified to a thickness of Q.
The hollow fibers formed a structure with open ends on one side of a 2 mm polyethylene film.
次に、これをポリエチレングリコールの１０％エタノー
ル溶液に浸漬した後、乾燥させて、中空繊維内にポリエ
チレングリコールを含浸させた。Next, this was immersed in a 10% ethanol solution of polyethylene glycol and then dried to impregnate polyethylene glycol into the hollow fibers.
別に、インドメタシン２重量部をアクリル酸−２−エチ
ルヘキシル／アクリル酸（重量比９６／４）共重合体１
００重量部と共に酢酸エチルに一溶解させた溶液をアル
ミニウム箔上に塗布し、溶剤を蒸発乾燥させて、薬剤貯
蔵層を形成し、この上に上記した中空繊維構造物をその
開口端が貯蔵層内に埋没されるように積層して、本発明
の徐放性製剤を得た。Separately, 2 parts by weight of indomethacin was added to 1 part of 2-ethylhexyl acrylate/acrylic acid (96/4 weight ratio) copolymer.
A solution prepared by dissolving 00 parts by weight in ethyl acetate is applied onto an aluminum foil, the solvent is evaporated and dried to form a drug storage layer, and the above-described hollow fiber structure is placed on top of the drug storage layer so that the open end thereof forms a storage layer. The sustained-release preparation of the present invention was obtained by stacking the tablets so that they were buried in each other.
図面は本発明の徐放性製剤の要部断面図を示す。
１・・・裏打ち部材、２・・・薬剤貯蔵層、３・・・薬
剤不透過層、４・・・中空繊維、５・・・中空繊維開口
端。
特許出願人 栢水化学工業株式会社
代表者藤 沼 基 利The drawing shows a sectional view of essential parts of the sustained release preparation of the present invention. DESCRIPTION OF SYMBOLS 1... Lining member, 2... Drug storage layer, 3... Drug impermeable layer, 4... Hollow fiber, 5... Hollow fiber open end. Patent applicant: Mototoshi Fujinuma, representative of Kayakami Chemical Industry Co., Ltd.
Claims (1)
裏打ち部材の上に積層された薬剤貯蔵層と、（Ｃ１この
薬剤貯蔵層の上に積層された薬剤不透過性層と、＋ｄ）
薬剤透過性の管壁を有し、その開口端が上記薬剤不透過
層を貫通して上記薬剤貯蔵層内に開口する中空繊維とか
らなることを特徴とする薬剤徐放性製剤。(11(a) a lining member; (b) a drug storage layer containing a drug and laminated on the lining member; (C1) a drug-impermeable layer laminated on the drug storage layer; +d)
1. A drug sustained release preparation comprising a hollow fiber having a drug-permeable tube wall, the open end of which penetrates the drug-impermeable layer and opens into the drug storage layer.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP57195647A JPS5984815A (en) | 1982-11-08 | 1982-11-08 | Pharmaceutical for prolonged release of chemical |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP57195647A JPS5984815A (en) | 1982-11-08 | 1982-11-08 | Pharmaceutical for prolonged release of chemical |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS5984815A true JPS5984815A (en) | 1984-05-16 |
| JPH046169B2 JPH046169B2 (en) | 1992-02-05 |
Family
ID=16344647
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP57195647A Granted JPS5984815A (en) | 1982-11-08 | 1982-11-08 | Pharmaceutical for prolonged release of chemical |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS5984815A (en) |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS62281815A (en) * | 1986-05-27 | 1987-12-07 | Teisan Seiyaku Kk | Application agent and production thereof |
| JPS62281814A (en) * | 1986-05-27 | 1987-12-07 | Teisan Seiyaku Kk | Slow-releasing plaster |
| JPS62281816A (en) * | 1986-05-27 | 1987-12-07 | Teisan Seiyaku Kk | Sustained release pharmaceutical |
| US4801458A (en) * | 1985-06-24 | 1989-01-31 | Teijin Limited | Sustained release pharmaceutical plaster |
| US4990340A (en) * | 1986-01-22 | 1991-02-05 | Teijin Limited | Sustained release pharmaceutical preparation |
| WO2014111812A1 (en) * | 2013-01-17 | 2014-07-24 | Tamicare Ltd. | All direction stretchable dressing article associated with curable materials |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5731611A (en) * | 1980-07-31 | 1982-02-20 | Nitto Electric Ind Co Ltd | Tape or pieace pharmaceutical preparation |
-
1982
- 1982-11-08 JP JP57195647A patent/JPS5984815A/en active Granted
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5731611A (en) * | 1980-07-31 | 1982-02-20 | Nitto Electric Ind Co Ltd | Tape or pieace pharmaceutical preparation |
Cited By (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4801458A (en) * | 1985-06-24 | 1989-01-31 | Teijin Limited | Sustained release pharmaceutical plaster |
| US4990340A (en) * | 1986-01-22 | 1991-02-05 | Teijin Limited | Sustained release pharmaceutical preparation |
| JPS62281815A (en) * | 1986-05-27 | 1987-12-07 | Teisan Seiyaku Kk | Application agent and production thereof |
| JPS62281814A (en) * | 1986-05-27 | 1987-12-07 | Teisan Seiyaku Kk | Slow-releasing plaster |
| JPS62281816A (en) * | 1986-05-27 | 1987-12-07 | Teisan Seiyaku Kk | Sustained release pharmaceutical |
| JPH0427212B2 (en) * | 1986-05-27 | 1992-05-11 | Teisan Seiyaku Kk | |
| JPH0427210B2 (en) * | 1986-05-27 | 1992-05-11 | Teisan Seiyaku Kk | |
| JPH0427211B2 (en) * | 1986-05-27 | 1992-05-11 | Teisan Seiyaku Kk | |
| WO2014111812A1 (en) * | 2013-01-17 | 2014-07-24 | Tamicare Ltd. | All direction stretchable dressing article associated with curable materials |
| US9480829B2 (en) | 2013-01-17 | 2016-11-01 | Tamicare Ltd. | All direction stretchable dressing article associated with curable materials |
Also Published As
| Publication number | Publication date |
|---|---|
| JPH046169B2 (en) | 1992-02-05 |
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