JPS58134020A - Pharmaceutical preparation - Google Patents
Pharmaceutical preparationInfo
- Publication number
- JPS58134020A JPS58134020A JP1707982A JP1707982A JPS58134020A JP S58134020 A JPS58134020 A JP S58134020A JP 1707982 A JP1707982 A JP 1707982A JP 1707982 A JP1707982 A JP 1707982A JP S58134020 A JPS58134020 A JP S58134020A
- Authority
- JP
- Japan
- Prior art keywords
- drug
- copolymer
- base layer
- pharmaceutical preparation
- base
- 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
Links
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- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【発明の詳細な説明】
本発明は狭心症の発作の抑制又は予防に有効な硝酸イン
ンルビトール（工５ＤＮ）を基剤中に含む経皮吸収投与
型の医薬製剤に関するものである。DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a percutaneous absorption type pharmaceutical preparation containing inrbitol nitrate (5DN) in a base, which is effective for suppressing or preventing attacks of angina pectoris.
狭心症用の薬物（冠状血管拡張剤）としては通常ニトロ
グリセリンが知られてなり、該薬物は密閉保存が可能な
軟膏タイプで使用されてい、５゜近時、ニトログリセリ
ンを感圧接着剤に配合して担持体上に形成したチーブ製
剤が提某さｎているが、揮発性が高くて保存できないと
いう間頌と、過度の唖皮吸収性を有するために急激な血
圧低下などの副作用の問題があり、実用化されＣいない
のが現状である〇
一万、工８ＤＮは狭心症の発作を抑制又は予防する薬物
として知られており、一般には錠剤の形で使用されてい
る。Nitroglycerin is commonly known as a drug for angina pectoris (coronary vasodilator), and this drug is used in the form of an ointment that can be stored in a sealed container. Some people have proposed a chive formulation prepared on a carrier by blending it into a carrier, but the problem is that it is highly volatile and cannot be stored, and that it has excessive cystic absorption, resulting in side effects such as a sudden drop in blood pressure. Currently, it has not been put into practical use due to the problems of 010,000 and 8DN, which is known as a drug that suppresses or prevents attacks of angina pectoris, and is generally used in the form of tablets.
工ＳＤＭは抑制又は予防という点から、体内に定量で、
しかも長時間徐々に提供されることが望ま【７いもので
ある。From the point of view of suppression or prevention, engineering SDM is administered in a quantitative amount to the body.
Moreover, it is desirable that the drug be provided gradually over a long period of time.
かかる目的を達成する丸めに、錠剤の溶解能を種々制御
する試みがなされているが、胃又は場内のＰＨ１内容物
の有無などの状態にＬつＣ１薬物の吸収能が鴨なる丸め
に、一般には定着で陽時間徐々に供給されないものであ
るう
従って本発明の目的は、ＩＥＩＤＮを走書で、長時間徐
々に供給する唖皮吸収役４タイプの医薬製剤を提供する
ことにある。Various attempts have been made to control the dissolution ability of tablets to achieve this purpose, but in general, the absorption ability of L-C1 drugs depends on the presence or absence of PH1 contents in the stomach or in the body. Therefore, it is an object of the present invention to provide a four-type medicinal preparation that can be absorbed gradually over a long period of time by scanning the IEIDN.
かかる目的は、アクリル酸エステルを主成分とする５温
で感圧接着性を有する共重合１勿とｒ８ＤＮとを必貢成
分とする基剤を柔軟な担持体上に均一に形成した医薬製
剤とすることＫよって適成さｎる０
本発明の医＃＆製剤は、前述の錠剤にＬる投与における
遣々の欠点を解決する疋けではなく、一般に薬物を含む
溶液をスプレー塗布したり、軟膏を用いたりしたときに
多く見られる不正確な投与量の問題や衣服などに擦り取
らｎるといつ九様々な問題をも充分に解決するものであ
る。This purpose is to create a pharmaceutical preparation in which a base containing acrylic acid ester as a main component and having pressure-sensitive adhesive properties at 5 temperatures and r8DN as essential components is uniformly formed on a flexible carrier. The pharmaceutical preparations of the present invention can be prepared by spraying or spraying a solution containing the drug, rather than by using the above-mentioned tablet administration methods. It satisfactorily solves the problems of inaccurate dosages often encountered when using ointments and when rubbing off on clothing.
本発明者達は、ｌ８ＤＮが皮膚から確実に、しかも一定
量が長時間徐々に供給される経皮吸収製剤について、様
々な角度から鋭意検討した。The present inventors have intensively studied from various angles a transdermal absorption preparation that can reliably and gradually supply a constant amount of l8DN from the skin over a long period of time.
七の結束、製剤が皮膚に所定期間確実に密着しているこ
と、基剤を構成すする共重合物と薬物との関に適度な相
溶性を有する１こと、薬物が基剤中で□
大部分が結晶化しないこと、及び基剤から皮膚に対１：
、
して適度な放出性を有するととなどが最低条件であるこ
とを見い出した。7) The preparation must remain in close contact with the skin for a predetermined period of time, the copolymer constituting the base must have adequate compatibility with the drug, and the drug must be □ large in the base. Parts do not crystallize, and from the base to the skin:
It has been found that the minimum condition is that the material has appropriate release properties.
そしてこれらの条件を充分且つ確実に満足しうる、工８
ＤＮと組み合せｔｉｆ能なものは、アクリル酸エステル
とアクリル酸又はメタクリル酸との共重合物であること
を知見し九。And there are 8 works that can fully and reliably satisfy these conditions.
It has been found that what is capable of tif in combination with DN is a copolymer of acrylic ester and acrylic acid or methacrylic acid.
鍍共重合物は、Ｃ数が４〜１０個のアクリル酸エステル
が８５〜９５重量％と、アクリル酸又はメタクリル酸が
１〜１５重量−とから構成されるものである。The plated copolymer is composed of 85 to 95% by weight of acrylic ester having 4 to 10 carbon atoms and 1 to 15% by weight of acrylic acid or methacrylic acid.
アクリル酸エステルのエステル部の０１１！１０個颯上
、又はアクリル酸又はメタクリル酸の量が１重量−以下
の共重合物では、基剤の保型性が低下すると共に皮膚へ
残留物ができ、しかも剥離時物理的な刺激を皮膚に与え
るので好ましくないものであり、Ｃ数が４個以下、又は
アクリル酸、又はメタクリル酸の量が１５重量−以上の
共重合物では、共重合物中での薬物の移動能が低Ｆする
免めに放出性がｇ＜なり、しかも皮膚への密着性が低下
するので好〕シ＜ないものであり、さらに基１１゜
剤を製造する際め薬物の共重合物への溶解分散性が不充
分となり、大部分の薬物が治療に寄辱しないことがある
ので好ましくないものである。Copolymers with more than 011!10 ester moieties of acrylic acid ester, or with less than 1 weight of acrylic acid or methacrylic acid, will reduce the shape retention of the base and leave a residue on the skin. Moreover, it is undesirable because it causes physical irritation to the skin when peeled off, and in copolymers with 4 or less carbon atoms or 15 weight or more of acrylic acid or methacrylic acid, This is undesirable because the drug's mobility is low, the release property is low, and the adhesion to the skin is reduced. This is undesirable because the solubility and dispersibility in the copolymer becomes insufficient and most of the drugs may not contribute to treatment.
本発明者の実験によれば、前述の密着性、相溶性、溶解
性及び放出性の各要件を、１８ＤＮとの組み合せの系に
おいて、最も確実に且つ比駿的簡単な製造操作で満足し
うる共重合物は、エステル部のＣ数が６〜８個のアクリ
ル酸エステルとアクリル酸との共重合物で前者：ｔｉ１
者＝９３〜９６：４〜７重量−の比の共重合物であるこ
とが川明し丸。According to the experiments of the present inventor, the above-mentioned requirements of adhesion, compatibility, solubility, and release properties can be most reliably satisfied in a combination system with 18DN and with a relatively simple manufacturing operation. The copolymer is a copolymer of an acrylic ester having 6 to 8 carbon atoms in the ester moiety and acrylic acid, and the former is ti1.
Kawakashimaru is a copolymer with a ratio of 93 to 96:4 to 7 by weight.
＃共重合物は、皮膚への密着性及び薬物シζ対する溶解
性が良好であり、しかも皮膚を刺激することが少なく、
薬°吻を安定的に保持する。#The copolymer has good adhesion to the skin and good solubility for drugs, and is less irritating to the skin.
Hold the proboscis stably.
アクリル酸又はメタクリル酸モノマーは、七の添加部数
に１って共重合物の１１１１！蟻性を変化させることが
できるので、基剤からの薬物の放出速度又は緻を制御で
き、ま九モノン−の１項を通訳することに工って共重合
物の親水相を高めることができる。The amount of acrylic acid or methacrylic acid monomer added is 1 to 7, which is 1111 parts of the copolymer! Since the properties can be changed, the release rate or density of the drug from the base can be controlled, and the hydrophilic phase of the copolymer can be increased by interpreting the first term of the monomer monomer. .
さらにＭＪ記の共１合物にはアクリル酸エステルと他の
共重合可能な酢酸ビニルの如きビニルエステルモノマー
との共重合物をも含むことが出来る。Furthermore, the copolymer described in MJ may also include a copolymer of an acrylic ester and other copolymerizable vinyl ester monomers such as vinyl acetate.
咳モノマーはＯ〜４０Ｊｌｌｌチ、好ましくは１０〜３
゜重量−のｔＳで配付するのがよい０該モノマーを含む
共重合物は薬物の溶解性が高いものである。The cough monomer is 0 to 40 Jlll, preferably 10 to 3
The copolymer containing the monomer preferably has a distribution of tS in °wt., which has a high drug solubility.
アクリル系共重合物を構成するのに使用さｎる前記モノ
マーとして、Ｊ＝Ｊ、Ｆのものを例示することができる
。Examples of the monomers used to form the acrylic copolymer include those where J=J and F.
アクリル酸エステルとしては、ｎ−ブチルアクリレート
、インアミルアクリレート、ヘキシルアクリレート、２
−エチルブチルアクリレート、インオクチルアクリレー
ト、２−エチルへキシルアクリレート、ノニルアクリレ
ート、イソノニルアクリレート、デシルアクリレートな
どを挙げることができる。Examples of acrylic esters include n-butyl acrylate, inamyl acrylate, hexyl acrylate, 2
Examples include -ethylbutyl acrylate, inoctyl acrylate, 2-ethylhexyl acrylate, nonyl acrylate, isononyl acrylate, and decyl acrylate.
前記共重合物と薬物とからなる基剤中の薬物量は、１〜
２５重量％、好ましくは２〜１５重ｆｋｑＩｂとなる工
うＫＩｌｌ整される０
このように調整された基剤は、柔軟な担持体上に、通常
５〜３００／１２１の４みで形成さｎる。The amount of drug in the base consisting of the copolymer and drug is 1 to 1.
25% by weight, preferably 2 to 15 times FkqIb. The thus prepared base is formed on a flexible carrier, usually with 5 to 300/121. Ru.
基剤は、担持体上に全面或いは部分的例えば筋状、格子
状、波形状などに＠成することができる。The base material can be formed entirely or partially on the carrier, for example, in the form of stripes, grids, waves, or the like.
一つの好ましい製剤の変形は、一つの担詩体上に２つ以
上のアクリル酸エステルのＷＩ類又はアクリル酸又はメ
タクリル酸の配合部数の異なる共重合物を用い九基剤を
、担持体の一方熾から１に＃に所定幅づつ形成したり、
所定幅で交互に形成し九り、或いは海鳥状に形成したり
することである。One preferred variation of the formulation is to use two or more WIs of acrylic acid esters or copolymers of different proportions of acrylic acid or methacrylic acid on one carrier, and place nine bases on one of the carriers. Forming a predetermined width from #1 to #,
They are formed alternately with a predetermined width, or shaped like a seabird.
かかる変形された基剤パターンは、基剤を構成する共重
合物のわずかなガラス転移温度（Ｔｇ）の違いによる薬
物の放出速度又は量の１いに１って、単一のＴＩＪから
なる共重合物を用いた基剤に比して、全体として放出時
間を長くすることができるという利点がある。かかるパ
ターンの効果は、基剤の厚み及び／又は薬物含有量を変
化させることにＬつでも得らｔＬ７ｙ）
他の一つの好ましい変形は、担持体上Ｋｌ［数の基剤層
を砿ね合せることである。このとき基剤層中の薬物量は
内部に行くに従偽多くしておき、外［（７）基剤１へ順
次薬物が供給さ・ｎる１うに工夫しておく。かかる積層
タイプは、−剤を皮膚に密着させた直後に１大量の薬物
が経皮吸収するのを防止する効咲があるが、この逆の積
層タイプは短時間で薬物を経皮吸収させる速効性用の製
剤として使用できることが理解されるであろう。Such a modified base pattern may result in a copolymer consisting of a single TIJ, in which the rate or amount of drug release is due in part to slight differences in glass transition temperature (Tg) of the copolymers constituting the base. Compared to bases using polymers, this has the advantage that the overall release time can be extended. The effect of such a pattern can also be obtained by varying the base thickness and/or drug content. Another preferred variation is to combine several base layers on the support. That's true. At this time, the amount of drug in the base layer is increased toward the inside, and measures are taken to ensure that the drug is sequentially supplied to the base 1 (7) outside. This laminated type has the effect of preventing a large amount of drug from being absorbed through the skin immediately after the agent is brought into close contact with the skin, but the opposite laminated type has an immediate effect that allows the drug to be absorbed through the skin in a short period of time. It will be appreciated that it can be used as a sexual formulation.
基剤を保持する担持体は、皮膚に適用させたときに著し
い違和感を感じさせず、ＩＥＩＤＮの飛散を防止しうる
もので柔軟性を有するものであｎ＃ｉ特に制限されず、
例えばポリオレフイ゛ン、ポリエステル、ポリウレタン
、ポリビニルアルコール、塩化ビニリデン、ポリアミド
などのフィルム又はシート（或いはこれらに金ｌｌ４ｓ
着し九もの）、ゴム及び／又は合成５ＦｉＩ製独立気泡
シート又はフィルム、箔などを挙げることができる。The carrier that holds the base is not particularly limited, as long as it does not cause a noticeable discomfort when applied to the skin, can prevent IEIDN from scattering, and is flexible.
For example, films or sheets made of polyolefin, polyester, polyurethane, polyvinyl alcohol, vinylidene chloride, polyamide, etc. (or gold coated with these)
Examples include closed-cell sheets or films made of rubber and/or synthetic 5FiI, foils, etc.
しかして、単位面積当りの１８ＤＮ含有量を基剤層の厚
みで制御しようとする場合、含有量が少ないときは然程
問題はないが、含有量が多いときは基剤層の厚みが薄い
と、ＸＢＤＮが基剤層の表面で結晶化して基剤層の接着
力を著しく低下させるも′１・１：
のである。これを解決する九めに基剤１を厚くすると皮
膚からの剥離時刺激を与えたり、糊残りを起生じたりす
るという問題がある。Therefore, when trying to control the 18DN content per unit area by the thickness of the base layer, there is no problem when the content is small, but when the content is high, the thickness of the base layer is thin. , XBDN crystallizes on the surface of the base layer and significantly reduces the adhesive strength of the base layer. The ninth problem to solve this problem is that if the base material 1 is made thicker, it may irritate the skin when removed from the skin or cause adhesive residue.
かかる問題は、前記担持体として、基剤ノーとの接着界
面部分にｌ５ＤＮが移行しつる高分子物質ｆ−を全面又
は部分的に被覆して２くことに１って解決される。蚊物
質としてはエチレン−酢酸ビニル共重合物、ポリ酢酸ビ
ニルなどを挙げることができ、こｎらの物質は共重合物
に過飽和に配合さｎたｌ８ＤＮを一時的に吸収して結晶
化を防止すると共に１基剤層中の工ＳＤＮが減少すると
基剤層中へ移行するものである。This problem can be solved by completely or partially covering the support with a polymeric material f-, in which l5DN migrates to the adhesive interface with the base material. Mosquito substances include ethylene-vinyl acetate copolymer, polyvinyl acetate, etc., and these substances temporarily absorb nl8DN that is supersaturated in the copolymer to prevent crystallization. At the same time, when the SDN in one base layer decreases, it migrates into the base layer.
また担持体は、少なくとも５％伸びる材質のものを選択
するのが、製剤が剥れ走り、違和感を少なくするうえか
ら好ましいものである。In addition, it is preferable to select a carrier that is made of a material that stretches by at least 5% in order to prevent the formulation from peeling off and causing discomfort.
前記基剤には、基剤の採型性を保つ丸めに、或いは皮膚
からの薬物の吸収能を高める九めなどの目的をエリ確実
に達成するｔめに、充填剤又は吸収促進剤表どを配合す
ることができる。ま九基剤には一般的な接着性付与檎り
旨、軟化剤の如き配合剤を又はカユミ止め剤の如き他の
薬物を少量添加してもよい。The base may be filled with fillers or absorption enhancers to ensure that the purpose of the base is rounded to maintain moldability or to increase absorption of the drug through the skin. can be blended. A small amount of a common compounding agent such as an adhesive agent, a softener, or other drug such as an anti-itch agent may be added to the base.
充填剤としては、微粉末シリカ、チタン白、炭酸カルシ
ュラムなどを挙げることができ、吸収促０
通則とじ１、グロピレングリコール、ジェｆ Ｌ／ ７
クリコールの知きア化コール項、サリチル酸、尿素、ア
ラントイン、ジメチルスルオキシド、ジメチルア七ドア
ミド、ジメチルホルムアミド、ジイソプロピルアジベー
ト、ジエチルセパケート、エチルラフレート、ニコチン
酸メチル、ラノリンなどを挙げることができる。Examples of fillers include finely powdered silica, titanium white, calcium carbonate, etc., absorption promotion 0, general binding 1, glopylene glycol, JEF L/7
Examples include the acetic acid derivatives of glycol, salicylic acid, urea, allantoin, dimethyl sulfoxide, dimethyl amide, dimethyl formamide, diisopropyl adibate, diethyl sepacate, ethyl laflate, methyl nicotinate, and lanolin.
前者は基剤に対しＣ２ｏｔｔ＊以下の量で、後者は３０
重量Ｓ以丁の量で添加することができる。The former has an amount of C2ott* or less relative to the base, and the latter has an amount of 30
It can be added in an amount equal to or less than weight S.
本発明の医薬製剤の４Ｉ黴は、以ドの実施例にＬす、具
体的に実証さｎるが、定量で、長時間皮膚ＫＩ８ＤＮが
供給さ０％吸収さｎる事実が顕著である０
以下本発明の実施例を示す。文中部とあるのは重量部を
示す。The 4I mold of the pharmaceutical formulation of the present invention is specifically demonstrated in the following examples, but it is remarkable that 0% of the 4I mold is absorbed by the skin over a long period of time in a quantitative manner. Examples of the present invention will be shown below. The words "part of the text" indicate parts by weight.
実施例１
４つロフラスコにアクリル酸イソアミル９５部とメタク
リル酸５部と酢酸エチル二へブタン（３：１）２５部を
仕込み、重合開始剤としてのアゾビスイソブチロニトリ
ルを０゜２５部添加し、不活性ガス中で重合反応を開始
し、酢酸エチルを滴ドしつつ反応’Ｎ度５８〜６２℃で
７時間重合を行い、固形分濃度３４．８重量優、粘度（
ａｔ３０℃）３３０ポイズの共重合物の溶液を得る。Example 1 95 parts of isoamyl acrylate, 5 parts of methacrylic acid, and 25 parts of ethyl dihebutane acetate (3:1) were placed in a four-bottle flask, and 0.25 parts of azobisisobutyronitrile was added as a polymerization initiator. Then, the polymerization reaction was started in an inert gas, and while ethyl acetate was added dropwise, the polymerization was carried out at a reaction temperature of 58 to 62°C for 7 hours, and the solid content concentration was 34.8% by weight, and the viscosity was (
A copolymer solution of 330 poise (at 30° C.) is obtained.
該共重合物溶液の固形分９５部に対し、ｌ５ＤＮを５部
添加して攪拌し、とｎｔｍ型ライう−上に乾燥後の厚み
が５０声馬となる１うに＃！１布乾燥して造撲化し、厚
さ９声ｍのポリエステルフィルムに転着して医薬製剤を
得る。To 95 parts of the solid content of the copolymer solution, 5 parts of 15DN was added and stirred to form a sea urchin #1 with a thickness of 50 mm after drying. 1. Dry the cloth to form a mold and transfer it to a polyester film with a thickness of 9 m to obtain a pharmaceutical preparation.
実施例２
実施例１の共重合物溶液の固形分９０部に対し、ｌ５Ｄ
Ｎを１０部添加して攪拌し、こｎを厚さ５゜ｐｍのエチ
レン−酢酸ビニル共重合物フィルム（ｌｌｖＡ％酢酸ビ
ニ酢酸ビニル含有量２２冫量Ｌｓｍのポリエステルフィ
ルムとのラミネートフィルムのＫＶＡｒＩｉに、乾燥後
の厚みが５０声ｍとなる１つ番て塗布乾燥１１
して医薬製剤を得る。Example 2 For 90 parts of solid content of the copolymer solution of Example 1, 15D
10 parts of N was added and stirred, and this was mixed into a KVArIi film of ethylene-vinyl acetate copolymer film having a thickness of 5 pm (LLVA% vinyl acetate) and a polyester film having a vinyl acetate content of 22% Lsm. A pharmaceutical preparation is obtained by applying and drying the first coat to a thickness of 50 m after drying.
□［３鵠
アクリル酸２−エチルヘキシル９４部とアクリル酸６部
とを用い、以ド実施例１と同様の操作にＬり共重合物溶
液（固形分層ＴＩＬ３０重量−１粘度２８０ポイズ）を
得ろう
義兵を合物溶液の固形分９２部に対し、ｌ５ＤＮを８部
添加し、厚さ２０声ｍの鷹化ビニルー虐化ビニリデン共
１合吻フィルムに、乾燥後の厚みが５０）ＩＩｎとなる
Ｌうに塗布乾燥して医４ｇ！４剤を得る０実施例４
実施例３の共重合−物溶液の固形分８７部に対し、１８
ＤＮを１３部添加し、厚さ４０ｐｒｎのＥ７Ａフィルム
（酢酸ビニル含有量４０重量％）と６メｍのポリエステ
ルフィルムとのラミネートフィルムの１１ＶＡ面に、乾
燥後の厚みが５０／馬となるように塗布乾燥して医薬製
剤を得る。□[3] Using 94 parts of 2-ethylhexyl acrylate and 6 parts of acrylic acid, a L-copolymer solution (solid layer TIL 30 weight - 1 viscosity 280 poise) was obtained in the same manner as in Example 1. 8 parts of 15DN was added to 92 parts of the solid content of the compound solution, and a 20 m thick film of hawkified vinyl and denatured vinylidene was made into a film having a thickness of 50 mm after drying. L Apply to sea urchin and dry it, 4g! 0 Example 4 to obtain 4 agents For 87 parts of solid content of the copolymer solution of Example 3, 18
13 parts of DN was added to the 11VA side of a laminate film of a 40prn thick E7A film (vinyl acetate content 40% by weight) and a 6mm polyester film so that the thickness after drying was 50/horse. A pharmaceutical preparation is obtained by coating and drying.
実施例５
実施例２において、担持体として厚さ９メｍのポリエス
テルフィルムを用い＋１１かは、実施例２と１
同じである。 ：・ＩＩ”””１ｌｌｆ。Example 5 In Example 2, a polyester film with a thickness of 9 mm was used as the carrier, and the difference was +11 as in Example 2 and 1. :・II”””1llf.
第１〜２表は実″施例１〜５の試験結束を示すものであ
る。Tables 1-2 show the test bundles of Examples 1-5.
第 ２ 衆
□□□」
第１表中のサンプルは、医薬製剤作成後４日のものを使
用した。The samples in Table 1 were used 4 days after the preparation of the pharmaceutical preparation.
第１表中の試験方法
４物残存率：上腕内１１１ＩＫサンプル（５ｃｍ＋Ｘ５
ｃ謙）を２４時間貼り付は後剥離して、そのま１３０１
１１１の＃貸エチルで溶解（４００２６時間振 ）シ、
さらシζｍ酸エチルで５０１１１にメスアップし、ガス
クロマトグラフィーで定量する。原体を１００−とじて
計算する。Test method 4 in Table 1 Survival rate: 111IK sample in upper arm (5cm+X5
After pasting C Ken) for 24 hours, peel it off and leave it as it is 1301.
Dissolve in #111 ethyl (shake for 40026 hours),
The solution was further diluted to 50111 with ethyl citrate and quantified by gas chromatography. Calculate by subtracting the original substance by 100.
３
第 １ 表
第２表中の試噴方法
ヒトの胸部にサンプル（１０Ｃ園ＸＩＱｃ■）を貼り付
け、所定時間後に３■ｌづつ採血を行い、血ｔを分離し
、これを２■ｌのｎ−へキサンで抽出しＣ遠心分離し、
不活性ガス下で０．１＋Ｚｔζ濃１ｍ−ｆる。さらに１
騰ｌのアセトニトリルで抽出して、アセトニトリルで抽
出して、アセトニトリル層を不活性ガス下で乾固し、と
ｎを１００戸ｌのベンゼンに溶解し、ガスクロマトグラ
フィーで測定し九。3. Test injection method in Table 2. Paste the sample (10Cen Extracted with n-hexane and centrifuged at C.
0.1+Ztζ concentration 1 m-f under inert gas. 1 more
Extract with 1 liter of acetonitrile, dry the acetonitrile layer under an inert gas, dissolve n in 100 liters of benzene, and measure by gas chromatography.
上記実施例からも明らかな如く、本発明の医薬製剤は、
皮膚への密着性に優ｎ、Ｌかも放出性が１５
良好である慣実が顕著である。As is clear from the above examples, the pharmaceutical formulation of the present invention is
It is a common practice that the adhesion to the skin is excellent and the release property is good.
特許出願人 日東電気工業株式会社 代表者出方三部patent applicant Nitto Electric Industry Co., Ltd. Three representatives
Claims (1)
ル８５〜９９Ｉｉｌ１％とアクリル酸又はメタクリル酸
１〜１５重量％とからなる共重合物と硝酸イソンルビト
ールとを含む基剤層と、該層を保持する担持体とからな
る医薬製剤。 ２）担持体の基剤１接着ｒｆＩ硝酸インンルピトールが
移行しつる高分子白質、１ｆ ｆ：１覆して々るもので
ある特許請求の範囲第１項記載の医薬製剤。[Scope of Claims] 1) A group containing a copolymer of 85-99Iil1% of an acrylic ester having 4-10 carbon atoms in the ester moiety and 1-15% by weight of acrylic acid or methacrylic acid and isonelubitol nitrate. A pharmaceutical preparation comprising a drug layer and a carrier that holds the layer. 2) The pharmaceutical preparation according to claim 1, wherein the base 1 of the carrier is a polymeric white matter to which the adhesion rfI inlupitor nitrate is transferred, 1f f:1.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP1707982A JPS58134020A (en) | 1982-02-04 | 1982-02-04 | Pharmaceutical preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP1707982A JPS58134020A (en) | 1982-02-04 | 1982-02-04 | Pharmaceutical preparation |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP60254363A Division JPH0742228B2 (en) | 1985-11-13 | 1985-11-13 | Pharmaceutical formulation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPS58134020A true JPS58134020A (en) | 1983-08-10 |
Family
ID=11933964
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP1707982A Pending JPS58134020A (en) | 1982-02-04 | 1982-02-04 | Pharmaceutical preparation |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS58134020A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS61100520A (en) * | 1984-10-22 | 1986-05-19 | Sekisui Chem Co Ltd | Tape drug of percutaneous administration type |
| JPS61112015A (en) * | 1985-11-13 | 1986-05-30 | Nitto Electric Ind Co Ltd | Pharmaceutical preparation |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3742951A (en) * | 1971-08-09 | 1973-07-03 | Alza Corp | Bandage for controlled release of vasodilators |
| JPS577411A (en) * | 1980-06-14 | 1982-01-14 | Nitto Electric Ind Co Ltd | Plaster |
-
1982
- 1982-02-04 JP JP1707982A patent/JPS58134020A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3742951A (en) * | 1971-08-09 | 1973-07-03 | Alza Corp | Bandage for controlled release of vasodilators |
| US3742951B1 (en) * | 1971-08-09 | 1982-11-23 | ||
| JPS577411A (en) * | 1980-06-14 | 1982-01-14 | Nitto Electric Ind Co Ltd | Plaster |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS61100520A (en) * | 1984-10-22 | 1986-05-19 | Sekisui Chem Co Ltd | Tape drug of percutaneous administration type |
| JPH0137375B2 (en) * | 1984-10-22 | 1989-08-07 | Sekisui Chemical Co Ltd | |
| JPS61112015A (en) * | 1985-11-13 | 1986-05-30 | Nitto Electric Ind Co Ltd | Pharmaceutical preparation |
| JPH0742228B2 (en) * | 1985-11-13 | 1995-05-10 | 日東電工株式会社 | Pharmaceutical formulation |
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