JPS60169417A - Pharmaceutical preparation of tape containing colchicine - Google Patents

Pharmaceutical preparation of tape containing colchicine

Info

Publication number
JPS60169417A
JPS60169417A JP2656084A JP2656084A JPS60169417A JP S60169417 A JPS60169417 A JP S60169417A JP 2656084 A JP2656084 A JP 2656084A JP 2656084 A JP2656084 A JP 2656084A JP S60169417 A JPS60169417 A JP S60169417A
Authority
JP
Japan
Prior art keywords
colchicine
polymer substance
high polymer
meth
acrylic acid
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.)
Pending
Application number
JP2656084A
Other languages
Japanese (ja)
Inventor
Masahiro Takigawa
滝川 雅浩
Toshiyuki Yamamoto
敏幸 山本
Ichiro Kobayashi
一郎 小林
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Nitto Denko Corp
Original Assignee
Nitto Electric Industrial Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Nitto Electric Industrial Co Ltd filed Critical Nitto Electric Industrial Co Ltd
Priority to JP2656084A priority Critical patent/JPS60169417A/en
Publication of JPS60169417A publication Critical patent/JPS60169417A/en
Pending legal-status Critical Current

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  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

PURPOSE:To obtain the titled pharmaceutical preparation useful for skin diseases such as Behcet's disease, necrotic blood inflammation, etc., capable of being administered endermically without causing side effect, by forming a high polymer substance layer consisting of a high polymer substance pressure-sensitive at normal temperature and colchicine on a substrate. CONSTITUTION:An effective amount of colchicine is added to a high polymer substance pressure-sensitive at normal temperature, preferably (meth)acrylate high polymer substance [e.g., (meth)acrylic acid butyl ester, (meth)acrylic acid pentyl ester, etc.] in such a way that colchicine is dispersed uniformly or in high content at the surface layer part, and a high polymer substance layer is formed on a flexible substrate (e.g., cloth, plastic film, etc.), to give the titled pharmaceutical preparation. Colchicine administration is quantitatively carried out with a sufficient ODT effect, a partial concentration can be effectively raised, and diseases can be effectively remedied while lowering side effects. Colchicine is preferably adjusted to 1-500mug strength/cm<2>.

Description

【発明の詳細な説明】 本発明は皮膚疾患に対して直接的に外皮へ貼付適用して
コルヒチンを経皮吸収せしめて治療するだめのテープ製
剤に関するものであシ、詳しくはベーチェット症候群、
壊死性血管炎、尋常性乾膚。
DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a tape preparation that can be applied directly to the outer skin to treat skin diseases by allowing colchicine to be absorbed transdermally, and more specifically, to treat skin diseases such as Behcet's syndrome,
Necrotizing vasculitis, dry skin vulgaris.

無菌性膿逅疾患、皮膚癌などの症例に対して有効なコル
ヒチンを副作用の発現を抑制しながら疾患部位に投与す
るための新規なテープ製剤に関するものである。
The present invention relates to a novel tape preparation for administering colchicine, which is effective against cases of sterile pus-filled diseases and skin cancer, to diseased areas while suppressing the occurrence of side effects.

一般に局所疾患部の治療には薬物を経口、注射、軟膏な
どの剤瀧で投与する方法が用いられているが、外皮疾患
の治療に対して経口や注射による薬物投与を行なうと効
果は現われる反面、副作用の発現が無視し難い問題とし
て生じていた0特に皮膚疾患のうち、ベーチェット症候
群、壊死性血管炎、尋常性乾肩、無菌性腺、ん性疾患な
どの治療においてステロイド系又は非ステロイド系薬物
などを適用しているが、副作用の面で使用し難い場合も
あシ、また有効でない症例も多々あった。更にこれらの
難治性皮膚疾患に対して著効を示すといわれるコルヒチ
ンの投与が一部で検討されておシ、1〜21/日の内服
投与によって薬理効果としての白血球代謝阻害作用、白
血球代謝阻害作用、ライリゾーム安定化作用、細胞***
抑制作用が発現し顛著な治療効果が得られるが、その反
面下痢などの胃腸障害が頻出し1時には無***症、***
欠乏症などの生殖器障害や白血球減少などの副作用も見
られ、投与に大きく細限が加わる場合もあったO また、特開1l156−49316号公報にコルヒチン
を併用薬として含有させた液剤、軟膏剤の開示があるが
、これらの剤屋では一定量の薬物を塗布し難く、また衣
服などの接触による薬物の損失も無視し難く、上記問題
点は未だ解決されていないのが現状である。
In general, administering drugs orally, by injection, or in the form of ointment, etc., is used to treat localized disease areas. , the occurrence of side effects has been a problem that cannot be ignored. Especially in the treatment of skin diseases, such as Behcet's syndrome, necrotising vasculitis, dry shoulder, sterile gonads, and cancerous diseases, steroidal or non-steroidal drugs are used. However, there were cases where it was difficult to use due to side effects, and there were many cases where it was not effective. Furthermore, the administration of colchicine, which is said to be highly effective against these intractable skin diseases, has been studied in some areas. However, on the other hand, gastrointestinal disorders such as diarrhea frequently occur, and reproductive organs disorders such as anovulation and sperm deficiency, as well as decreased white blood cells, occur. In addition, Japanese Patent Application Laid-Open No. 11156-49316 discloses liquid preparations and ointments containing colchicine as a concomitant drug, but these drug manufacturers However, it is difficult to apply a certain amount of drug, and the loss of drug due to contact with clothing is also difficult to ignore, and the above problems have not yet been solved.

本発明者らは、上記の薬物投与法及び副作用の問題点を
解消するために鋭意研究を重ねた結果、常温で粘着性を
有する高分子物質と薬理学的に有効な量のコルヒチンか
らなる高分子物質層を担持体上に設けた新規なテープ製
剤を皮膚疾患部に直接的に貼付することによシ、疾患部
に対するコルヒチン投与を定量的に行なえ、且つ局所濃
度を有効に高めることが出来、副作用の低減化を計シな
がら疾患治癒を有効に行なえることを見い出し、本発明
に至ったものである。
The present inventors have conducted intensive research to resolve the above-mentioned drug administration method and side effects problems, and as a result, we have discovered that a drug consisting of a polymer substance that is sticky at room temperature and a pharmacologically effective amount of colchicine. By directly applying a new tape formulation with a molecular substance layer on a carrier to diseased areas of the skin, colchicine can be quantitatively administered to diseased areas and the local concentration can be effectively increased. They discovered that it is possible to effectively cure diseases while reducing side effects, leading to the present invention.

即ち、本発明は柔軟性を有する担持体上に設けられた常
温で粘着性を示す高分子物質層に、薬理学的有効量のコ
ルヒチンを均一に含有或いは表層部に高濃度で含有させ
たことを特徴とするコルヒチン含有テープ製剤を提供す
るものである0本発明に用いられる柔軟性を有する担持
体としては、皮膚の屈曲面に使用した際にも充分な追従
性を有する材質であれに制限はなく、また穿孔処理又は
エンボス処理などの処理加工を施こして柔軟性を付与し
てもよい。これらの担持体としては、例えば各種プラス
チックフィルム又は発泡シート、不織布、織布、紙類、
金属箔、或い紘これらとプラスチックフィルムとの積層
フィルムなどが挙げられるが、貼付使用時の適用皮膚面
の角質層の保水量を高めて経皮吸収性を向上させるため
に上記担持体は実質的に透湿性を有しないものを選択す
るか、或いは組み合わせることによって所謂充分なOD
T効果が得られるようにしてもよい。
That is, the present invention provides a polymer material layer that is adhesive at room temperature and is provided on a flexible carrier, and contains a pharmacologically effective amount of colchicine uniformly or at a high concentration in the surface layer. The flexible carrier used in the present invention is limited to materials that have sufficient conformability even when used on the curved surface of the skin. Alternatively, a treatment such as perforation or embossing may be applied to impart flexibility. These carriers include, for example, various plastic films or foam sheets, nonwoven fabrics, woven fabrics, papers,
Examples include metal foils and laminated films of these and plastic films, but in order to increase the water retention capacity of the stratum corneum on the skin surface to which it is applied during application and improve transdermal absorption, the above-mentioned carriers are substantially So-called sufficient OD can be achieved by selecting or combining materials that do not have moisture permeability.
It may also be possible to obtain the T effect.

本発明に用いられる常温で粘着性を有する高分子物質は
本発明のコルヒチン含有テープ製剤を治療のために皮膚
面へ直接的に貼付適用した際に充分な皮膚接着性とOD
T効果を与え、薬物の放出を満足する速度で可能とする
基剤を提供することを目的としている。これらの為分子
物質として、例えばシリコーンゴム、ポリイソプレンゴ
ム、スチレン−ブタジェンゴム、スチレン−イソプレン
−スチレンブロック共重合体ゴム、アクリルゴム、天然
ゴムの如きゴム系高分子物質、ポリビニルアルキルエー
テル、ポリビニルアルコール、ポリ酢酸ヒニルノ如キビ
ニル系高分子物質、カルボキシメチルセルロースの如き
セルロース系高分子物質、(メタ)アクリル酸アルキル
エステルを主成分とした(メタ)アクリレート系高分子
物質などが挙げられる。上記高分子物質の9ち、コルヒ
チンの分解に対する安定性、放出性、皮膚接着性を考慮
すると、(メタ)アクリレート系高分子物質が好ましく
、例えは(メタ)アクリル酸ブチルエステル1 (メタ
)アクリル酸ペンチルエステル、(メタ)アクリル酸ヘ
キシルエステル、(メタ)アクリル酸イクチルエステル
、(メタ)アクリル酸ノニルエステル タ)アクリル酸テトラデシルエステルの如きフルキル基
の炭素数が4〜14個である(メタ)アクリル酸フルキ
ルエステ)v50〜99重量%と、凝集性及び皮膚線4
w性の向上を目的とする該エステルと共重合可能な単量
体、例えば(メタ)アクリル酸、イタコン酸、マレイン
Wa、無水マレイン酸。
The polymer substance used in the present invention, which is sticky at room temperature, has sufficient skin adhesion and OD when the colchicine-containing tape formulation of the present invention is applied directly to the skin surface for treatment.
The aim is to provide a base that provides a T effect and allows release of the drug at a satisfactory rate. For these purposes, molecular substances include, for example, rubber-based polymer substances such as silicone rubber, polyisoprene rubber, styrene-butadiene rubber, styrene-isoprene-styrene block copolymer rubber, acrylic rubber, natural rubber, polyvinyl alkyl ether, polyvinyl alcohol, Examples include polyvinyl acetate-based polymers, cellulose-based polymers such as carboxymethyl cellulose, and (meth)acrylate-based polymers containing an alkyl (meth)acrylic acid ester as a main component. Considering the stability against decomposition, release properties, and skin adhesion of colchicine among the above-mentioned polymeric substances, (meth)acrylate-based polymeric substances are preferable, such as (meth)acrylic acid butyl ester 1 (meth)acrylic acid The number of carbon atoms in the furkyl group is 4 to 14, such as acid pentyl ester, (meth)acrylic acid hexyl ester, (meth)acrylic acid ictyl ester, (meth)acrylic acid nonyl ester, and (meth)acrylic acid tetradecyl ester. ) Furkylester acrylate) v50-99% by weight, cohesiveness and skin line 4
Monomers copolymerizable with the ester for the purpose of improving w properties, such as (meth)acrylic acid, itaconic acid, maleic Wa, and maleic anhydride.

クロトン酸、(メタ)アクリル酸2−ヒドロキシエチル
エステル、(メタ)アクリルW12ーヒドロキシブqピ
ルエステル、7クリロニトリルの如キ官能性本量体、酢
酸ビニル、プロピオン酸ビニpの如きビニル系単量体、
(メタ)アクリル酸メチル、(メタ)7クリル酸エチル
、スチレンなどの単量体のうち少なくとも一種の単量体
が1・〜5。
Functional monomers such as crotonic acid, (meth)acrylic acid 2-hydroxyethyl ester, (meth)acrylic W12-hydroxybutyl ester, 7-crylonitrile, vinyl monomers such as vinyl acetate, vinyl propionate, etc. ,
At least one monomer selected from among monomers such as methyl (meth)acrylate, ethyl (meth)7acrylate, and styrene is 1. to 5.

重量%とからなる共重合物を使用することが出来る0 本発明のテープ製剤に使用するコルヒチンは前述した如
く白血球遊走能抑制作用や細胞***抑制作用などの薬理
効果を有するために、ベーチェット病、壊死性血管炎,
無菌性膿苑疾患、尋常性乾廟などの白血球遊走因子が存
在する皮膚疾患に対して極めて有効な薬物であシ、上述
した高分子物質層に均一に含有せしめるか、或いは表層
部に高濃度で含有せしめて、テープ製剤の単位!i[ 
(t4)中l〜s o o pgの範囲の力価にimm
するのが望ましい。
A copolymer consisting of necrotizing vasculitis,
It is an extremely effective drug for skin diseases where leukocyte chemotactic factors are present, such as sterile phlegm disease and xerosis vulgaris. It is contained in a unit of tape formulation! i[
(t4) imm to a titer in the range of medium to so pg.
It is desirable to do so.

またコルヒチンを適用皮膚面上に効率よく放出させたシ
、適用皮膚面を経皮吸収に対して活性化(所謂ルーズ化
)させるための経皮吸収補助物質として、例えはプロピ
レングリコール、ジエチレングリコール、ポリエチレン
グリコールの如きグリコール類、エチルアルコール、サ
リチル酸、R素、7ラントイン、ジメチルスルホキシド
、ジメチルアセトアミド、ジメチルホルムアミド、ジイ
ソプロピルアジペート、ジエチルセパケート、エチルラ
ウレート、ラノリン、鉱油の如き物質を必要に応じて一
種類以上添加することが出来る。添加量は皮膚接着力及
び凝集力とのハラシスを考慮して、高分子物質100重
量部に対して30重量部以下が望ましい。
In addition, in order to efficiently release colchicine onto the skin surface to which it is applied, propylene glycol, diethylene glycol, polyethylene glycol, etc. Glycols such as glycol, ethyl alcohol, salicylic acid, R, 7-lantoin, dimethyl sulfoxide, dimethyl acetamide, dimethyl formamide, diisopropyl adipate, diethyl sepacate, ethyl laurate, lanolin, mineral oil, etc., if necessary. or more can be added. The amount added is desirably 30 parts by weight or less based on 100 parts by weight of the polymeric substance, taking into account the effects of skin adhesion and cohesive strength.

本発明のテープ製剤中に含有されるコルヒチンの経日保
存時の分解を抑制するために、ブチルヒドロキシアニソ
ール、ブチルヒドロキシトルエン、トコフェロール、ビ
タ【ンCなどの抗酸化剤や、ポリリン酸、エチレンジア
ミン四酢酸又はその塩などのキレート化剤を高分子物質
100重量部に対して5重量部以下の量で添加してもよ
い。
In order to suppress the decomposition of colchicine contained in the tape formulation of the present invention during storage over time, antioxidants such as butylated hydroxyanisole, butylated hydroxytoluene, tocopherol, and vitamin C, as well as polyphosphoric acid and ethylenediamine tetra A chelating agent such as acetic acid or a salt thereof may be added in an amount of 5 parts by weight or less based on 100 parts by weight of the polymeric substance.

本発明のコルヒチン含有テープ製剤L1例えは常温で粘
着性を有する高分子物質の溶液にコルヒチン単体を添加
混合するか、或いはコルヒチンをアルコールやクロロホ
ルムの如き可溶性溶剤にあらかじめ溶解させ、必要に応
じて高分子物質との親和性又鉱溶解性を高める目的で各
種界面活性剤を添加したのち、常温で粘着性を有する高
分子物質の溶液と充分に混合し、柔軟性を有する担持体
上にコルヒチン含有高分子物質層を形成させるか、あら
かじめ担持体上に形成させた高分子物質層の −表面上
に、上記の如く作成4したコルヒチン溶液を塗布して高
分子物質層の表層部にコルヒチンを溶解し高濃度で含有
させることによって製造することが出来る。
For example, the colchicine-containing tape preparation L1 of the present invention can be prepared by adding and mixing colchicine alone to a solution of a polymeric substance that is sticky at room temperature, or by dissolving colchicine in advance in a soluble solvent such as alcohol or chloroform, and adding a high After adding various surfactants for the purpose of increasing the affinity with molecular substances and mineral solubility, the colchicine-containing mixture is thoroughly mixed with a solution of a polymer substance that is sticky at room temperature, and is deposited on a flexible support. Either form a polymeric material layer or apply the colchicine solution prepared in step 4 above on the surface of the polymeric material layer previously formed on the carrier to dissolve colchicine in the surface layer of the polymeric material layer. It can be manufactured by containing it at a high concentration.

以上に示したように本発明のコルヒチン含有テープ製剤
は、皮膚疾患部に直接的に貼付適用することによって高
分子物質層中を拡散移動したコルヒチンが皮膚面に供給
され、充分なODT効果によって皮内吸収し、白血球遊
走因子などに基づく皮膚疾患に著効を発揮するものであ
る。特に高分子物質層の表層部にコルヒチンを偏在させ
た場合は持続的な放出よりも大量投与による治療に適し
てお#)、よシ確実な供給による治療効果が期待出来る
ものでおる。
As shown above, when the colchicine-containing tape preparation of the present invention is applied directly to a skin disease area, colchicine that has diffused and moved through the polymeric material layer is supplied to the skin surface, resulting in a sufficient ODT effect on the skin. It is absorbed internally and is highly effective against skin diseases caused by leukocyte migration factors. In particular, when colchicine is unevenly distributed in the surface layer of the polymer material layer, it is more suitable for treatment by large-dose administration than by continuous release, and a therapeutic effect can be expected through reliable supply.

以下に本発明の実施例を示し、さらに具体的に説明する
が、本発明はこれらに何ら限定されるものではなく、技
術的思想を逸脱しない範囲において種々の応用が可能で
ある。なお、実施例中で部とあるのは重量部を意味する
Examples of the present invention will be shown below and explained in more detail, but the present invention is not limited to these in any way, and various applications are possible without departing from the technical idea. In addition, parts in the examples mean parts by weight.

実施例1 不活性カス雰囲気下において撹拌器、還流冷却器、温度
計を伽えた四つ目フラスコにアクリル酸イソオクチルエ
ステル95部、アクリル酸5部、酢酸エチル200部、
7ゾイソブテロニトリル0.2部を仕込み、内温温度を
62〜65℃で撹拌しながら重合を島始させ、該温度範
囲に制御しながら6時間重合したのち、内温を75〜8
0℃に昇温して3時間熟成し、常温で粘着性を有する高
分子物質の溶液を得た。
Example 1 Under an inert gas atmosphere, 95 parts of acrylic acid isooctyl ester, 5 parts of acrylic acid, 200 parts of ethyl acetate,
7. Add 0.2 part of zoisobuteronitrile, start polymerization while stirring at an internal temperature of 62 to 65°C, and polymerize for 6 hours while controlling the temperature within the range, then raise the internal temperature to 75 to 8°C.
The temperature was raised to 0° C. and aged for 3 hours to obtain a solution of a polymeric substance that was sticky at room temperature.

上記にて得られた高分子物質溶液の固形分100部に、
コルヒチン0.5部を添加して充分に混合、均一溶解し
iヒのち、コロナ放電処理を施した25μ票厚のポリエ
チレンフィルム上に乾燥後の厚みが40μ飢となるよう
に塗布、乾燥し、コルヒチンの含有量が20μm17c
dのテープ製剤を得た。
To 100 parts of the solid content of the polymer substance solution obtained above,
After adding 0.5 parts of colchicine and thoroughly mixing and dissolving it uniformly, it was coated on a 25 μm thick polyethylene film that had been subjected to corona discharge treatment so that the thickness after drying was 40 μm, and dried. Colchicine content is 20μm17c
A tape formulation of d was obtained.

実施例2 不活性ガス雰囲気下において撹拌器、還流冷却器、温度
針、滴下ロートを備えた四つ目フラスコにアクリル酸2
−エチルヘキシルエステル70部。
Example 2 Acrylic acid 2 was added to a fourth flask equipped with a stirrer, reflux condenser, temperature needle, and dropping funnel under an inert gas atmosphere.
- 70 parts of ethylhexyl ester.

メタクリル酸2−エトキシエチルエステル20部。20 parts of methacrylic acid 2-ethoxyethyl ester.

酢酸ビニル10部、7ゾイソブチロニトリル0.2部を
仕込み、内温温度を62〜65℃に制御しながら反応希
釈溶剤の酢酸エチルを滴下して反応を8時間行なったの
ち、更に内温を75〜80℃に昇温して3時間熟成し、
常温で粘着性を有する高分子物質の溶液を得た。
10 parts of vinyl acetate and 0.2 parts of 7zoisobutyronitrile were charged, and while controlling the internal temperature at 62 to 65°C, ethyl acetate as a reaction dilution solvent was added dropwise to carry out the reaction for 8 hours. The temperature was raised to 75-80℃ and aged for 3 hours,
A solution of a polymeric substance that is sticky at room temperature was obtained.

上記にて得られた高分子物質溶液をシリコーン処理を施
した剥離紙の処理面上に乾燥後の厚みが40μ悔となる
ように塗布、乾燥したのち、ポリウレタンフィルムの片
面に転着し、担持体上に設けられた高分子物質層の表・
面上にコルヒチンの1%エタノール溶液を塗布し、充分
に含浸させたのち乾燥を行ない、コルヒチンの含有:!
120μm1/14のテープ製剤を得た。
The polymer substance solution obtained above was applied onto the treated side of silicone-treated release paper so that the thickness after drying was 40μ, and after drying, it was transferred to one side of a polyurethane film and supported. The surface of the polymer material layer provided on the body.
A 1% ethanol solution of colchicine is applied on the surface, thoroughly impregnated, and then dried.Contains colchicine:!
A tape formulation of 120 μm 1/14 was obtained.

試験例1 ヒト培養細胞HeLa−8s株を滅菌プラスチックシャ
ーレ内でイーグルMEM培養液に10%FetA1ca
lf serumを加えた培地で培養した。
Test Example 1 Cultured human cells HeLa-8s strain were added to Eagle MEM culture solution with 10% FetA1ca in a sterile plastic Petri dish.
The cells were cultured in a medium supplemented with lf serum.

培養2日後に各実施飢にて得られたコルヒチン含有テー
プ製剤に無菌化処理を施した試料片1d、2cj、4c
jを培地51に対してそれぞれ粘着面が培地に接するよ
うに加え、6時間経過後の有糸***中期にある細胞数を
カウントし、細胞の生育度、細胞***の活動度を示す有
糸***指数を調べた。
Sample pieces 1d, 2cj, 4c obtained by sterilizing colchicine-containing tape preparations obtained in each experiment after 2 days of culture
Add J to the medium 51 so that the sticky side is in contact with the medium, and count the number of cells in the metaphase of mitosis after 6 hours.Mitosis indicates the degree of cell growth and cell division activity. I looked into the index.

また対照品として試料片を加えなかったものを用い、結
果を第1表に示した。
In addition, a control product to which no sample piece was added was used, and the results are shown in Table 1.

第1表 第1表から明らかな如く、各*九個のテープ製剤から放
出されるコルヒチンが培養細胞に作用し、***時のミク
ロフィラメントの合成を阻書したために、試料片を加え
ない場合と比べて有糸***中期の細胞数が増加、集積し
ておシ、フルとチンが有効にテープ製剤中から放出され
ていることがわかった。
As is clear from Table 1, the colchicine released from each of the *9 tape preparations acted on the cultured cells and inhibited the synthesis of microfilaments during division. In comparison, it was found that the number of cells in metaphase of mitosis increased, and that the cells accumulated and were effectively released from the tape preparation.

試験例2 8週齢のHartley系モルモット(体重300〜3
50g)の背部を刺毛し、実施例1によって得られたコ
ルヒチン含有テープ製剤を40μIActi・回。
Test Example 2 8-week-old Hartley guinea pigs (body weight 300-3
50 g) was pricked with hair on the back, and the colchicine-containing tape preparation obtained in Example 1 was applied 40 μl Acti·times.

80μI/kcI/・回、160μllk&・回の投与
量となるように裁断、貼付し、また対照として40μ#
/kl?・回を経口投与した。1群を10匹とし、毎日
1回投薬して症状観察1体重測定を行ない副作用として
の下痢の発現度を調べ、症状の結果を第2表及び第1図
に示した。なお投与量はヒトの場合の1〜2■/人・d
a7からラットに換算した。
It was cut and pasted to give a dosage of 80μI/kcI/・times, 160μllk&・times, and 40μ# as a control.
/kl?・Administered orally. A group of 10 animals was administered once a day, symptoms were observed, and body weight was measured to determine the incidence of diarrhea as a side effect. The results of the symptoms are shown in Table 2 and Figure 1. The dosage for humans is 1 to 2 cm/person/d.
Converted to rat from a7.

第2表 第2表から明らかな如く、本発明のコルヒチン含有テー
プ製剤は:JA/ヒチン投与時の主な副作用の1つであ
る下痢症状紘全く発現せず、また体重の減少もほとんど
見られず、従来の経口薬と比べて副作用の面で著しく改
善されていることがわかった。
Table 2 As is clear from Table 2, the colchicine-containing tape preparation of the present invention: did not exhibit any diarrheal symptoms, which is one of the main side effects when administering JA/hicine, and almost no weight loss was observed. It was found that side effects were significantly improved compared to conventional oral drugs.

【図面の簡単な説明】[Brief explanation of the drawing]

第1図は実施例1によって得られたコルヒチン含有テー
プ製剤を1日に1回モルモット背部に連続貼付した際の
絹目的体重変化、及び経口薬における絹目的体重変化を
示す。 曲線1〜実施例1のテープ製剤;投与量4oplAv回
曲線2〜 N ; /l gQμめへ1回曲線3〜 〃
; tt 160119/kl/”回曲線4〜経口薬 
; 〃 4oμIAI!・回特許出願人 E東電気工業株式会社 代表者土方三部
FIG. 1 shows the change in silk target body weight when the colchicine-containing tape preparation obtained in Example 1 was continuously applied to the back of a guinea pig once a day, and the change in silk target body weight after oral administration. Curve 1 - Tape formulation of Example 1; Dose 4 oplAv times Curve 2 - N; /l gQμ once curve 3 - 〃
; tt 160119/kl/” curve 4 ~ Oral drug
;〃4oμIAI!・Applicant for patent E Tokyo Electric Industry Co., Ltd. Representative Hijikata Sanbe

Claims (1)

【特許請求の範囲】[Claims] 1)柔軟性を有する担持体上に設けられた常温で粘着性
を示す高分子物質に、薬理学的有効量のコルヒチンを均
一に含有或いは表層部に高濃度で含有させたことを特徴
とするコルヒチン含有テープ製剤。
1) It is characterized by containing a pharmacologically effective amount of colchicine uniformly or at a high concentration in the surface layer of a polymeric substance that is sticky at room temperature and provided on a flexible carrier. Colchicine-containing tape preparation.
JP2656084A 1984-02-14 1984-02-14 Pharmaceutical preparation of tape containing colchicine Pending JPS60169417A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2656084A JPS60169417A (en) 1984-02-14 1984-02-14 Pharmaceutical preparation of tape containing colchicine

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP2656084A JPS60169417A (en) 1984-02-14 1984-02-14 Pharmaceutical preparation of tape containing colchicine

Publications (1)

Publication Number Publication Date
JPS60169417A true JPS60169417A (en) 1985-09-02

Family

ID=12196914

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2656084A Pending JPS60169417A (en) 1984-02-14 1984-02-14 Pharmaceutical preparation of tape containing colchicine

Country Status (1)

Country Link
JP (1) JPS60169417A (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0565530A1 (en) * 1989-07-18 1993-10-20 GERTNER, Sheldon Method for treating arthritically inflamed body joints, particularly joints having gouty arthritis

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0565530A1 (en) * 1989-07-18 1993-10-20 GERTNER, Sheldon Method for treating arthritically inflamed body joints, particularly joints having gouty arthritis
EP0565530A4 (en) * 1989-07-18 1994-04-06 Sheldon Gertner

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