JPS59227820A - Production of pharmaceutical preparation - Google Patents
Production of pharmaceutical preparationInfo
- Publication number
- JPS59227820A JPS59227820A JP10374883A JP10374883A JPS59227820A JP S59227820 A JPS59227820 A JP S59227820A JP 10374883 A JP10374883 A JP 10374883A JP 10374883 A JP10374883 A JP 10374883A JP S59227820 A JPS59227820 A JP S59227820A
- Authority
- JP
- Japan
- Prior art keywords
- drug
- adhesive layer
- sensitive adhesive
- carrier
- absorption
- 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
Landscapes
- Medicinal Preparation (AREA)
Abstract
Description
【発明の詳細な説明】
本発明は適用皮膚面に対する放出性のすぐれた医薬製剤
の製法に関するものである。DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a method for producing a pharmaceutical formulation with excellent release properties to the skin surface to which it is applied.
経皮吸収性薬物を経皮吸収させる医薬製剤として、担持
体上に経皮吸収性薬物と感圧性接着剤との混合物からな
る薬物投与層を形成してなるものが知られている。BACKGROUND ART As a pharmaceutical preparation for transdermally absorbing a transdermally absorbable drug, one is known in which a drug administration layer made of a mixture of a transdermally absorbable drug and a pressure-sensitive adhesive is formed on a carrier.
一般に、感圧性接着剤層は、有機溶剤などの溶媒などで
希釈して担持体上に塗布後加熱乾燥するか、或いは加熱
溶融して担持体に塗布して形成されるので、七〇造層工
程中に受熱を免れることができないものである。Generally, a pressure-sensitive adhesive layer is formed by diluting it with a solvent such as an organic solvent and applying it onto a carrier and then heating and drying it, or by heating and melting it and applying it to a carrier. Heat cannot be avoided during the process.
そのためにかかる感圧性接着剤と薬物とを混合して薬物
投与層を形成する場合には１例えば熱による損失を見込
んで多い目に配合しなければならないという不都合があ
る。For this reason, when such a pressure-sensitive adhesive and a drug are mixed to form a drug administration layer, there is a disadvantage that, for example, a large amount must be mixed to take into account loss due to heat.
かかる不都合を解決する方法として、感圧性接着剤１−
に油成分を含有させておき、この層面に油成分に溶解し
た薬物を塗布することにより）薬物を油成分相互の親和
性を利用して接着剤層に吸収させる方法も提案されてい
るが、塗布された油成分にて接着剤層が著しく可塑化さ
れ、適用皮膚面から剥離したときに皮膚面に多肴の残留
物が付着するという欠点を有する。As a method to solve this problem, pressure sensitive adhesive 1-
A method has also been proposed in which the drug is absorbed into the adhesive layer by making use of the mutual affinity of the oil components (by adding an oil component to the adhesive layer and applying the drug dissolved in the oil component to the surface of this layer). The adhesive layer is significantly plasticized by the applied oil component, and has the disadvantage that when it is peeled off from the applied skin surface, residues of various ingredients adhere to the skin surface.
本発明はかかる従来技術の欠点を解決した新規な医薬製
剤の製法を提供するもので、その要旨とするところは、
溶解セグメントが０．５〜２０重敞％である架橋系感圧
性接着剤層を担持体上に形成する工程と、該層面に常温
で液状である経皮吸収性薬物を塗布するか或いは常温で
固形状である経皮吸収性薬物の溶解及び又は分散液を塗
布して前記溶解セグメントに薬物を吸収させる工程とか
らなることにある。The present invention provides a novel method for producing pharmaceutical preparations that solves the drawbacks of the prior art, and its gist is as follows:
A step of forming a cross-linked pressure-sensitive adhesive layer having a soluble segment content of 0.5 to 20% by weight on a carrier, and applying a transdermal drug that is liquid at room temperature to the surface of the layer, or applying a transdermal drug that is liquid at room temperature. The method comprises the step of applying a solution of a solid transdermal drug to be dissolved and/or dispersing it to absorb the drug into the dissolved segment.
本発明の製法によれば、溶解セグメント率が０．５〜２
０重駄％と適度に調整された架橋系感圧性接着剤層面に
、経皮吸収性薬物を塗布して、薬物を接着剤層中の溶解
セグメント部分に吸収させるので、接着剤層は可塑化さ
れることがなく、良好な凝集性を維持し、しかも薬物は
拡散移動し易い溶解セグメント部分に吸収されているの
で確実に適用皮膚面に放出される医薬製剤が得られるも
のである。According to the manufacturing method of the present invention, the dissolved segment ratio is 0.5 to 2.
A transdermal absorbable drug is applied to the surface of the cross-linked pressure-sensitive adhesive layer, which has been appropriately adjusted to 0% weight, and the drug is absorbed into the dissolved segments in the adhesive layer, so that the adhesive layer becomes plasticized. A pharmaceutical preparation can be obtained that maintains good cohesive properties and is reliably released onto the skin surface to which it is applied, since the drug is absorbed into the dissolving segment portion where it is easily diffused.
本発明における特許請求の範囲及び詳細な説明の欄で用
いてなる溶解セグメント率なる用語は、架橋系感圧性接
着剤のサンプルをトルエン（１１０℃）に３０分間浸漬
して後サンプルを取り出し、下式にて算出すること及び
その値を指称する。The term dissolved segment ratio used in the claims and detailed description of the present invention refers to a sample of a cross-linked pressure-sensitive adhesive that is immersed in toluene (110°C) for 30 minutes, then taken out and placed under the Indicates that it is calculated using a formula and its value.
本発明の実施に当って用いられる架橋系感圧性接着剤は
、主剤として合成樹脂及び又はゴムを用いてなるもので
、溶解セグメント率が０．５〜２０重眼％の範囲となる
ように架橋（又は加硫）されてなるものである。溶解セ
グメント率が０．５軍歌％以ドでは接着剤層の檗物吸収
蝋が小さく、塗布した郷゛勿が接着剤層面で結晶化した
りするために好ましくなく、２０重駄％以上では４物又
は薬物溶解及び又は分散液の吸収によって接着剤層が６
エ塑化され、適用皮膚面から剥離したときに糊残１）が
生じるので好ましくないものである。The cross-linked pressure-sensitive adhesive used in the practice of the present invention uses synthetic resin and/or rubber as the main ingredient, and is cross-linked so that the dissolved segment ratio is in the range of 0.5 to 20%. (or vulcanized). If the dissolved segment rate is less than 0.5%, the adhesive layer will have a small amount of wax absorbed by the adhesive layer, and the applied particles may crystallize on the surface of the adhesive layer, which is undesirable. Or, the adhesive layer becomes 6 due to drug dissolution and/or absorption of the dispersion liquid.
This is undesirable because it is eplasticized and leaves adhesive residue 1) when peeled off from the skin surface to which it is applied.
架橋系感圧性接着剤層は、ゴム及び又は合成樹脂を主剤
とする常温で感圧接着性を有する物質に加硫剤（主剤が
ゴムの場＠）或いはポリイソシアネート化合物、有機過
酸化物、多官能性化合物などの架橋成分を配合し、これ
を担持体りに所望の厚みで塗布した後加熱反応させるか
、或いは前記感圧接着性を有する物質を担持体上に塗設
後紫外線、電子線、放射線などの活性線を照射して架橋
することによって形成さ几る。しかして例えば金属架橋
、プラズマ処理架橋などの手段を用いて架橋してもよい
ものである。The cross-linked pressure-sensitive adhesive layer is made by adding a vulcanizing agent (if the main material is rubber), a polyisocyanate compound, an organic peroxide, or A crosslinking component such as a functional compound is blended, and this is applied to a carrier at a desired thickness, followed by a heating reaction. Alternatively, the material having pressure-sensitive adhesive properties is coated on a carrier and then exposed to ultraviolet rays or electron beams. It is formed by crosslinking by irradiation with actinic rays such as radiation. For example, crosslinking may be carried out using means such as metal crosslinking or plasma treatment crosslinking.
ゴム及び又は合成樹脂を主剤とする常温で感圧接着性を
有する物質としては、天然ゴム又はシリコ尺ｌゴム、ス
チレン−イソプレン−スチレンブロック共！合体ゴム、
イソプレンゴムの如き合成ゴムを主剤とし、これに粘着
性付与樹脂、軟化剤、充填剤を配合してなるゴム系と、
（メタ）アクリル酸エステルの重合物又は該エステルと
官能性モノマーとの共重合物からなるポリ（メタ）アク
リル系或いはポリビニルアルキルエーテル系などに代表
される含酸樹脂系が挙げられる。Examples of substances that are based on rubber and/or synthetic resin and have pressure-sensitive adhesive properties at room temperature include natural rubber, silico rubber, and styrene-isoprene-styrene blocks! combined rubber,
A rubber system whose main ingredient is synthetic rubber such as isoprene rubber and which is compounded with a tackifying resin, a softener, and a filler;
Examples include acid-containing resin systems typified by poly(meth)acrylic systems and polyvinyl alkyl ether systems made of polymers of (meth)acrylic acid esters or copolymers of the esters and functional monomers.
前記ゴム系物質（シリｊつゴム系ヲ除く）には硫黄、硫
黄含有化合物、キノンジオキシムなどに代表される加硫
剤（ゴム成分１００軍歌部に対して０．０１〜２重喰部
軍歌び／又はチアゾール系、チオユリア系、チウラム系
、ジチオカルバメート系などに代表される加硫促進剤（
ゴム成分１００重量部に対して０．０１〜３重噴部）な
どの加硫成分が配合され、またシリニ巨しゴム系には有
機過酸化物（ゴム成分１００重量部に対して０．０１〜
２重量部）が配合さオする。The rubber-based substances (excluding silicone rubber-based substances) include sulfur, sulfur-containing compounds, vulcanizing agents such as quinone dioxime, etc. and/or vulcanization accelerators such as thiazole-based, thiourea-based, thiuram-based, dithiocarbamate-based, etc.
Vulcanizing components such as 0.01 to 3 injection parts per 100 parts by weight of the rubber component are blended, and organic peroxides (0.01 to 3 parts by weight per 100 parts by weight of the rubber component) are added to the Sirini rubber system. ~
2 parts by weight).
合成樹脂物質には、ポリイソシアネート化合物。Synthetic resin materials include polyisocyanate compounds.
有機過酸化物、多官能性化金物などの架橋成分が主成分
１００重晴部上対して０．０１〜１重晴部部上さ扛る。A crosslinking component such as an organic peroxide or a polyfunctional metal compound is added in an amount of 0.01 to 1 part by weight per 100 parts by weight of the main component.
このように加硫又は架橋成分が配合された物質ヲ、ポリ
エステルフィルム、ポリオレフィン系フィルム、ポリビ
ニルアルコールフィルム、ボリアグリレートフィルム２
ポリアミドフイルム、セロファンフィルム、ポリ塩化ビ
ニルフィルムなどのフィルム（金属蒸着フィルムを含む
）或いは金属箔、布、不織布、紙など、並びにこれらの
積層フィルムなどからなる担持体上に、５〜２００μｍ
（固形分）の厚みで塗布し、加熱操作を加えて加硫又は
架橋反応を起生させることにより５担持体上に目的とす
る溶解セグメント率を有し且つ実質的に加硫又は架橋成
分が残存しない架橋系感圧性接着剤層が得られる。Materials containing vulcanized or crosslinked components as described above, polyester films, polyolefin films, polyvinyl alcohol films, polyacrylate films 2
5 to 200 μm on a carrier made of films such as polyamide film, cellophane film, polyvinyl chloride film (including metallized films), metal foil, cloth, nonwoven fabric, paper, etc., and laminated films of these.
(solid content) and heat it to cause a vulcanization or crosslinking reaction.5. A crosslinked pressure-sensitive adhesive layer that does not remain is obtained.
しかして、前記常温で感圧接着性を有する物質に、前述
の如き加硫又は架橋成分を配合せず、上記物質を担持体
上＋Ｖ塗設後紫外線、電子線、放射線などの活性線を所
定は照射して０．５〜２０重隈％の溶解セグメント率を
有する架橋系感圧性接着剤層を形成してもよいものであ
る。Therefore, without blending the vulcanizing or crosslinking component as described above with the substance that has pressure-sensitive adhesive properties at room temperature, the substance is coated with +V on a carrier and then active rays such as ultraviolet rays, electron beams, and radiation are applied. may be irradiated to form a crosslinked pressure-sensitive adhesive layer having a dissolved segment ratio of 0.5 to 20 weight percent.
このように担持体上に形成した、溶解セグメント率が（
）、５〜２０重叶％となるように設計した架橋系感圧性
接着剤層面に、コルチコステロイド劃。In this way, the ratio of dissolved segments formed on the support is (
), a corticosteroid was applied to the surface of the cross-linked pressure-sensitive adhesive layer, which was designed to have a concentration of 5 to 20%.
消炎鎮痛剤、抗高血剤、降圧利尿剤などに代表される経
皮吸収性薬物を単独又は、該薬物の溶解及び又は分散し
た混合液にして塗布して溶解セグメント部分に薬物を吸
収させつつ或いは吸収後、この面にポリエステルフィル
ム、ポリオレフィンフィルムなどのプラスチックフィル
ムに代表さオする薬物非移行性剥離フィルムを貼０８せ
ることによ＋ｌ、塗布塗布金物着剤層の溶解セグメント
部分に吸着させた。良好な放出性を有する医薬製剤が得
られるものである。Transdermal absorbable drugs such as anti-inflammatory analgesics, antihypertensive drugs, antihypertensive diuretics, etc. are applied alone or as a mixture of dissolved and/or dispersed drugs, and the drug is absorbed into the dissolved segment while the drug is absorbed. Alternatively, after absorption, a non-drug migration release film, typically a plastic film such as a polyester film or a polyolefin film, is attached to this surface, and the drug is adsorbed to the soluble segment portion of the coated metal adhesive layer. . A pharmaceutical formulation with good release properties can be obtained.
前記経皮吸収性薬物が常温で液状である場合は、単独で
前記接着剤層面に塗布さ肚る。し、かして。When the transdermal drug is liquid at room temperature, it is applied alone to the surface of the adhesive layer. Yes, please.
塗布する薬物の濃度調整や展延性向上などを目的として
、該薬物を溶解及び又は分散しつる低沸点（１２０℃以
下）の溶媒と混合してもよい。For the purpose of adjusting the concentration of the drug to be applied, improving spreadability, etc., the drug may be mixed with a low boiling point (120° C. or less) solvent that can dissolve and/or disperse the drug.
該溶媒としては、メチルアルコール、エチルアルコール
、ｎ−プロピルアルコールの如キアルコール類、クロロ
ホルム、塩化メチレン、アセトン。Examples of the solvent include alcohols such as methyl alcohol, ethyl alcohol, and n-propyl alcohol, chloroform, methylene chloride, and acetone.
トルエン、ジメキサン或いは酢酸エチ７Ｌ／の如キエス
テル類或いは水などがあげられ、こｆ１５らは屯独或い
は混合系で用いられる。しかして１例えばプロピレング
リコール、ジエチレングリコールの如キ多価アルコール
類、その他ジメチルスルホキシドド、ジイソプロピルア
ジベート、ジエチルセｌくケート、エチルラウレート、
ラノリン、ｆｆｌｅ乳化剤、サリチル酸．サリチル酸メ
チル、サリチル酸モノグリコールエーテル、原票、アラ
ントインの如き薬物の経皮吸収能を促進する助剤類を前
記溶媒の代ζ）に用いることもできる，１
これらの溶媒類を用いる場合，その（ａは多くても３０
重は部以ド（接着剤層１ ０ ０重に部に対して）、好
ましくは２〜１ ５ ｆｉ ４１部の１囲とするのが望
ましいものである。Examples include toluene, dimexane, esters such as ethyl acetate 7L/water, and these f15 are used alone or in a mixed system. For example, polyhydric alcohols such as propylene glycol, diethylene glycol, dimethyl sulfoxide, diisopropyl adibate, diethyl selcate, ethyl laurate, etc.
Lanolin, ffle emulsifier, salicylic acid. Auxiliary agents that promote the transdermal absorption ability of drugs, such as methyl salicylate, salicylic acid monoglycol ether, original tablets, and allantoin, can also be used in place of the above solvent (ζ).1 When these solvents are used, the (a) is at most 30
The weight is desirably 1 part (per 100 parts of adhesive layer), preferably 2 to 15 parts to 41 parts.
また薬物が常温で固体である場合は．薬物は前記溶媒に
溶解及び又は分散させた混合液とされ、接着剤層に塗布
される。Also, if the drug is solid at room temperature. The drug is dissolved and/or dispersed in the solvent to form a mixed solution and applied to the adhesive layer.
こ牡らの溶解及び又は分散液における薬物含有量は０．
０５〜１５重量％の範囲にするのが好ましいものである
。The drug content in the dissolution and/or dispersion liquid of this species is 0.
A preferable range is 0.05 to 15% by weight.
これらの薬物並びに薬物溶解及び又は分散液は。These drugs and drug solutions and/or dispersions.
平方センチメートル当り．１〜３００μｍの薬物が吸着
されるように接着剤層に塗布される。per square centimeter. The adhesive layer is applied so that 1-300 μm of drug is adsorbed.
接着剤層への薬物の吸着速度を促進するために低温（８
０℃以下）で加熱してもよい。A low temperature (8
(below 0°C).
本発明の製法によれば．製造工程中に薬物を揮散又は変
質させる高熱を加えないので薬物の損失がなく，シかも
接着剤層が薬物並びに薬物溶解及び又は分散液で可塑化
されることがないので製剤を皮膚から剥離しても残留物
がない医薬製剤が得られるという特徴を有する。According to the manufacturing method of the present invention. Since no high heat is applied during the manufacturing process to volatilize or alter the drug, there is no loss of the drug, and the adhesive layer is not plasticized by the drug and drug solution and/or dispersion, making it easy to peel the preparation from the skin. It is characterized by the fact that it is possible to obtain pharmaceutical preparations with no residue.
以ド本発明の実施例を示す。文中部とあるのは重１部を
意味する。Examples of the present invention will now be described. ``Bunchubu'' means the first part of the text.
実施例１
４つロフラスコに，アクリル酸２ーエチルヘキシル６０
部、酢酸ビニル３５部及びアクリル酸５部を仕込み，不
活性ガス下でさらに酢酸エチルを２５部添加する。これ
に重合開始剤としてのアゾビスイソブチロニトリルを０
．１５部添加し，酢酸エチルを滴ドしつつ反応温度６０
〜６３℃で１１時間屯合を行い、固形分濃度３３．８重
頃％、粘度（ａｔ３０℃）５１Ｏボイズの共重合体溶液
を得る。Example 1 60 2-ethylhexyl acrylate in 4 flasks
1 part, 35 parts of vinyl acetate and 5 parts of acrylic acid, and further added 25 parts of ethyl acetate under an inert gas. Add 0 azobisisobutyronitrile as a polymerization initiator to this.
．． 15 parts were added, and the reaction temperature was increased to 60°C while adding ethyl acetate dropwise.
The copolymerization is carried out at ~63°C for 11 hours to obtain a copolymer solution having a solid content concentration of 33.8% by weight and a viscosity (at 30°C) of 51O voids.
該溶液の固形分１ ０ ０部に対して架橋剤としての過
酸化ベンゾイル（ＢＰＯ）を０． ２部添加して攪拌し
，これを厚さ１２μｍのポリエステルフィルム面に乾燥
後の厚みが５０μ情となるよう処塗布し。Benzoyl peroxide (BPO) as a crosslinking agent was added at 0.00 parts per 100 parts of the solid content of the solution. 2 parts were added and stirred, and this was coated on the surface of a 12 μm thick polyester film so that the thickness after drying was 50 μm.
１５０℃で５分間乾燥し、溶解セグメント率が２重酸％
の架橋系感圧性接着剤層を有する接着フィルムを得る。Dry at 150°C for 5 minutes, and the dissolved segment rate is 2 double acid%.
An adhesive film having a crosslinked pressure-sensitive adhesive layer is obtained.
このフィルムの接着剤層面に、１００プのエチルフルコ
ールに２ ０ ０”ｆのプロピオン酸クロベタゾールを
溶解した混合液を乎方セン千メートル当１〕６μ２とな
るように塗布して４０℃で風乾し、この上に薬物非移行
性ポリエステル製剥離フィルムを貼Ｃ）介せて、医薬製
剤を得た。A mixture of 200"f of clobetasol propionate dissolved in 100% of ethyl fluorol was applied to the adhesive layer surface of this film at a concentration of 6μ2 per 1,000m, and air-dried at 40°C. A non-drug migration polyester release film was pasted thereon to obtain a pharmaceutical preparation.
実施例２ ポリイソプレンゴム３０ｆｆｌＳ、天然ゴム２０部。Example 2 30fflS of polyisoprene rubber, 20 parts of natural rubber.
ラノリン１５部、脂肪族系石油樹脂３５部、微粉末イオ
ウ１．５部及びトルエン１５０からなる配合物を溶解混
合し、これを離型ライナー上に乾燥後の厚みが４０μｍ
となるように塗布して１５０℃で６分間乾燥し、溶解セ
グメント率が１３重１４％の架橋系感圧性接着剤フィル
゛ムを得る。A mixture consisting of 15 parts of lanolin, 35 parts of aliphatic petroleum resin, 1.5 parts of finely powdered sulfur, and 150 parts of toluene was dissolved and mixed, and this was placed on a mold release liner to a thickness of 40 μm after drying.
The adhesive was applied and dried at 150° C. for 6 minutes to obtain a crosslinked pressure-sensitive adhesive film having a dissolved segment ratio of 13% by weight and 14%.
このフィルムを軟質ポリ塩化ビニルフィルム（厚さ６０
μｍ）に転着して接着フィルムを作り。This film is made of soft polyvinyl chloride film (thickness 60
μm) to make an adhesive film.
この接着剤フィルム層面に、１（１ｍＪの酢酸エチ／Ｌ
７と５ ｍｌのジエチルセバケートとの混合溶媒に５０
π２のクロニジンを溶解せしめた混合液を平方七ン千メ
ートル当Ｚ）５０μ２となるように塗布して４０℃で風
乾し、この上に薬物非移行性ポリエステル製剥離フィル
ムを貼ζ】合せて、医薬製剤を得た。1 (1 mJ of ethyl acetate/L) on the surface of this adhesive film layer.
50 in a mixed solvent of 7 and 5 ml of diethyl sebacate.
A mixed solution of clonidine with π2 dissolved therein was applied to the surface at an amount of 50μ2 per 7,000 square meters, air-dried at 40°C, and a release film made of non-drug-migrating polyester was pasted on it. A pharmaceutical formulation was obtained.
実施例３
実施例１の共ＩＦ’−９体溶液の固形分１００部に対し
て、ジメチルスルホキシド７部及びトリメチロールプロ
パントリアグリレート０．４ 部ヲ配含り、、これを離
型ライナー上に乾燥後の厚みが５０μｍとなるように塗
布して１（）０℃で７分間乾燥して接Ｋｔ剤フィルムを
得る。Example 3 Contains 7 parts of dimethyl sulfoxide and 0.4 parts of trimethylolpropane triacylate based on 100 parts of the solid content of the co-IF'-9 body solution of Example 1. This was applied onto a mold release liner. The film was coated to a thickness of 50 μm after drying and dried at 10° C. for 7 minutes to obtain a Kt adhesive film.
一方、ポリエチレンとエチレン−酢酸ビニル共重合体と
の複合フィルムを用意し、この共■合体面に前記接着剤
フィルムを転着し、この表面に８Ｍｒａｄの電子線を照
射して、溶解セグメント率が７重電％の架橋系感圧性接
着剤層を葺する接着フィルムを得る。On the other hand, a composite film of polyethylene and ethylene-vinyl acetate copolymer was prepared, the adhesive film was transferred onto the surface of the composite film, and the surface was irradiated with an electron beam of 8 Mrad to increase the dissolved segment ratio. An adhesive film having a cross-linked pressure-sensitive adhesive layer of 7% heavy duty is obtained.
この接着剤層面に５０ｍＪのクロロホルムに４０■のプ
ロプラノロールを溶解した混合液を’Ｆ方センチメート
ル当り２０μｉどなるように塗布して４０℃で風乾し、
この上に薬物非移行性ポリエステル製剥離フィルムを貼
り合せて、医薬製剤を得る。A mixture of 40 μl of propranolol dissolved in 50 mJ of chloroform was applied to the surface of this adhesive layer at a rate of 20 μl per centimeter in the F direction, and air-dried at 40°C.
A non-drug migration polyester release film is laminated thereon to obtain a pharmaceutical preparation.
実施例４
実施例１と同様の操作にて、アクリル酸イソアシル９０
部、アクリル酸ヒドロキシエチル１０部とを酢酸エチル
中で共重合して共重合体溶液を得る。この溶液の固形分
濃度は４（１，２ｉ１１％、（ａｔ３０℃）即粘度は６
２０ボイズである。該溶液の固形分１００部に対してト
ルエンジイソシアナートとトリメチロールプロパン付加
物を０．１部添加し、厚さ８０μｍのポリエチレンフィ
ルムセニ塗布乾繰後の厚みが５０μｍとｔｘるように塗
布し、５０℃で１２時間乾燥する。得られた接着フィル
ムの糊面にサリチル酸メチル液を２５０μｆ／ｌａにな
るように表面塗布を行ない、そしてこの上に薬物非移行
性ポリエステル製剥離フィルムを貼Ｃ〕合わせて。Example 4 Isoacyl acrylate 90 was prepared in the same manner as in Example 1.
part and 10 parts of hydroxyethyl acrylate in ethyl acetate to obtain a copolymer solution. The solid concentration of this solution is 4 (1,2i11%, (at 30℃) the immediate viscosity is 6
There are 20 voices. 0.1 part of toluene diisocyanate and trimethylolpropane adduct was added to 100 parts of the solid content of the solution, and a polyethylene film with a thickness of 80 μm was coated so that the thickness after drying was 50 μm. , and dry at 50° C. for 12 hours. A methyl salicylate solution was applied to the adhesive surface of the obtained adhesive film at a concentration of 250 μf/la, and a non-drug transferable polyester release film was pasted thereon.
医薬製剤を得る。Obtain a pharmaceutical formulation.
第１表に実施例１〜４の特性評価結果を示す。Table 1 shows the characteristics evaluation results of Examples 1 to 4.
なお第１表中の比較例１ａは実施例１においてＢＰＯを
含む溶液に直接薬物を配合して塗布乾燥（１５５℃で５
分間）したもの、ｌｂはＢＰＯを用いずに薬物を配合し
て塗布乾燥（１００℃で８分間）したもの、比較例２は
実施例２において微粉末イオウを用いない配合物に薬物
を配合して塗布乾燥（１２０℃で８分間）したものであ
る。Comparative Example 1a in Table 1 is the same as Example 1, in which the drug was directly added to the solution containing BPO, applied and dried (at 155°C for 50 minutes).
Comparative Example 2 is the one obtained by blending the drug without using BPO and applying and drying (8 minutes at 100°C). The coating was applied and dried (at 120°C for 8 minutes).
第１表中の試験方法 溶出率二本文中の方法による。Test methods in Table 1 Elution rate 2 According to the method in the text.
経日薬物残存陵：初期及び第１表中の条件下で保存した
サンプルを、３０℃の酢酸エチルで５回（但し比較例は
３回）抽出し、液体グロマトグラフイーで測定する。Drug residual over time: Samples stored initially and under the conditions shown in Table 1 are extracted with ethyl acetate at 30° C. 5 times (3 times in the comparative example), and measured using liquid chromatography.
水中放出性；作製後３０℃で７日間保存したサンプル（
２５ｔｖｌ ）を１００ｔ／（３０℃）に浸漬して振と
うして３時間後の放出眺を液体グロマトグラフィーで測
定し、初期値を１００％として計算した。Release in water; samples stored at 30°C for 7 days after preparation (
25tvl) was immersed in 100t/(30°C) and shaken, and the release profile after 3 hours was measured by liquid chromatography, and calculations were made with the initial value as 100%.
皮膚移行率：作製後３０℃で７日間保存したサンプル（
５Ｘ１０ｍ角）を、ウサギ（体重１．８ｋｆ）の背部を
除毛して貼り付け、２４時間後に剥がしてサンプル中の
残存晴を測定し、初期値を１ｏ。Skin transfer rate: Sample stored at 30°C for 7 days after preparation (
5 x 10 m square) was pasted on the back of a rabbit (weight 1.8 kf) after hair removal, and after 24 hours, it was removed and the residual fineness in the sample was measured, and the initial value was 1 o.
％として計算した。Calculated as %.
特許出願人 日東電気工業株式会社 代表者土方三部patent applicant Nitto Electric Industry Co., Ltd. Representative Sanbe Hijikata
Claims (1)
圧接着剤層を担持体上に形成する工程と、該層面に常温
で液状である経皮吸収性薬物を塗布するか或いは常温で
固形状である経皮吸収性薬物の溶解及び又は分散液を塗
布して前記溶解セグメントに薬物を吸収させる工程とか
らなる医薬製剤の製法。A step of forming a cross-linked pressure-sensitive adhesive layer with a dissolved segment ratio of 0.5 to 20% by weight on a carrier, and applying a transdermal drug that is liquid at room temperature to the surface of the layer, or applying a transdermal drug that is liquid at room temperature. A method for producing a pharmaceutical preparation comprising the step of applying a solution and/or dispersion of a solid transdermal drug to absorb the drug into the dissolved segment.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP10374883A JPS59227820A (en) | 1983-06-09 | 1983-06-09 | Production of pharmaceutical preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP10374883A JPS59227820A (en) | 1983-06-09 | 1983-06-09 | Production of pharmaceutical preparation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPS59227820A true JPS59227820A (en) | 1984-12-21 |
Family
ID=14362197
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP10374883A Pending JPS59227820A (en) | 1983-06-09 | 1983-06-09 | Production of pharmaceutical preparation |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS59227820A (en) |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS577413A (en) * | 1980-06-14 | 1982-01-14 | Nitto Electric Ind Co Ltd | Plaster |
| JPS5846959A (en) * | 1981-09-12 | 1983-03-18 | 日東電工株式会社 | Production of adhesive drug |
-
1983
- 1983-06-09 JP JP10374883A patent/JPS59227820A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS577413A (en) * | 1980-06-14 | 1982-01-14 | Nitto Electric Ind Co Ltd | Plaster |
| JPS5846959A (en) * | 1981-09-12 | 1983-03-18 | 日東電工株式会社 | Production of adhesive drug |
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