JPS58128314A - Preparation for mucous membrane - Google Patents
Preparation for mucous membraneInfo
- Publication number
- JPS58128314A JPS58128314A JP1129982A JP1129982A JPS58128314A JP S58128314 A JPS58128314 A JP S58128314A JP 1129982 A JP1129982 A JP 1129982A JP 1129982 A JP1129982 A JP 1129982A JP S58128314 A JPS58128314 A JP S58128314A
- Authority
- JP
- Japan
- Prior art keywords
- water
- soluble
- macromolecular substance
- plasticizer
- pharmaceutically acceptable
- 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
Links
Abstract
Description
【発明の詳細な説明】
本発明、は湿潤粘膜に適用される製剤に関するものであ
って、更に詳しく湿潤粘膜から投与する薬物を口月史な
どの粘膜面に固定被損する粘膜製剤を提供するものであ
る。DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a preparation that is applied to moist mucous membranes, and more specifically provides a mucosal preparation that fixes and damages a drug to be administered through moist mucous membranes on a mucosal surface such as a mucous membrane. It is.
口放粘膜などの湿潤粘Ｉ漠への薬物の投与は、該粘膜が
疾患部位である場合以外に、該粘膜部位が比較的高い薬
物吸収性を有することから、例えばホルモン剤の如く経
口では吸収されにくい薬物の投与に利用する試みがなさ
れている。When administering drugs to moist mucous membranes such as the oral mucosa, in addition to cases where the mucous membrane is the site of disease, it is difficult to administer drugs orally, such as with hormonal drugs, since the mucosal membrane has relatively high drug absorption. Attempts are being made to use it to administer drugs that are difficult to treat.
しかして、このような粘膜部位、殊に口かツ粘膜から薬
物の投与に際する最大の障害は、唾液などの分泌液或い
は会話等に伴う粘膜部位の伸縮などにより、配置した薬
物が吸収されるまでに洗い流されること、及び薬物量に
比して充分な薬理効果が得られないことである。However, the biggest obstacle when administering drugs from such mucous membrane sites, especially oral mucosa, is that the placed drug is absorbed by secretions such as saliva or by expansion and contraction of the mucosal site due to conversation, etc. The problem is that the drug is washed away by the time the drug is absorbed, and that a sufficient pharmacological effect cannot be obtained compared to the amount of drug.
近時、薬物の滞留性及び薬理効果を高めることを目的と
した製剤或いはその類似物として、ポリアクリル酸ナト
リュウノ・を配合したペーストや水溶性高分子物質から
なるスポンジ或いはタブレット基剤中に薬物を含有せし
めたものが提案されている。Recently, as preparations or analogues thereof aimed at increasing drug retention and pharmacological effects, drugs are being incorporated into pastes containing sodium polyacrylate, sponges or tablet bases made of water-soluble polymeric substances. It has been proposed that it contains
かかるペースト又は層剤は、従来の軟膏タイプなどに比
較すれば、滞留性などはかなり改善されているが、次の
点において充分なものとは言えないのが現状である。Although such pastes or layer agents have considerably improved retention properties when compared to conventional ointment types, they are currently not satisfactory in the following respects.
即ち、ペーストにおいては充分な物理的強度を崩してい
ないために、会話時における粘膜の伸縮又はこすれなど
によって除去され易いという欠点を有するものである。That is, since the paste does not have sufficient physical strength, it has the disadvantage that it is easily removed by the expansion and contraction of mucous membranes or rubbing during conversation.
また製剤化したものは、疾患の種類又は症状によって、
投与する薬物の種類や量を調節することが困難であった
り、剤型としたために薬物の効力が低下したりするとい
う欠点がある。In addition, the formulated products vary depending on the type or symptoms of the disease.
There are disadvantages in that it is difficult to control the type and amount of the drug to be administered, and the efficacy of the drug may be reduced due to the formulation.
また上記の基剤中に薬物を含有させることなく、薬物を
固定被覆するために製剤を用いると、スポンジ基剤は物
理的強度に劣るうえに、多孔質であるために薬物の拡散
流出が起生し易いという問題があり、タブレット基剤は
剛性を有するために適用部位が制限されるという使用上
の問題がある。Furthermore, if a formulation is used to fix and coat the drug without incorporating the drug into the above-mentioned base, the sponge base has poor physical strength and is porous, causing drug diffusion and outflow. There is a problem in that the tablet base is easily sticky, and the rigidity of the tablet base limits the application sites, which is a problem in use.
本発明はかかる従来技術の情況に鑑み鋭意研究の結果発
明された新規な薬物固定用の粘膜製剤を提供するもので
あって、その要旨とするところは、薬学的に許容し得る
水溶性高分子物質の群から選ばれた一塊以上と薬学的に
許容し得る可塑剤とを必須成分とする水に溶解又は水で
ゲル化して粘着性を示す水親和性高分子物質層と、薬学
的に許容し得る水浴性高分子物質の群から選ばれた一種
以−ヒの架橋物と薬学的に許容し得る可塑剤とを必須成
分とする水に非又は遅延溶解性の為分子＠質層とからな
ることである。The present invention provides a novel mucosal preparation for drug immobilization invented as a result of intensive research in view of the situation of the prior art, and its gist is to provide a pharmaceutically acceptable water-soluble polymer. a water-affinity polymeric material layer that exhibits adhesive properties when dissolved in water or gelled with water, and which contains as essential components one or more lumps selected from a group of substances and a pharmaceutically acceptable plasticizer; A layer of molecules with non- or delayed solubility in water, the essential components of which are one or more cross-linked products selected from the group of water bathable polymeric substances that can be used, and a pharmaceutically acceptable plasticizer. It is what happens.
本発明の粘膜製剤によれば、水に溶解又は水でゲル化し
２て粘着性を示す水親和性高分子物質層と、水に非又は
遅延溶解性の高分子物質層とから構成されているので、
粘膜に対する粘着性が良好で、しかも違和感がないとい
う特徴のほかに、系全体の溶解性を比較的簡単に調整す
ることができるという特徴を有するものである。According to the mucosal preparation of the present invention, it is composed of a water-affinity polymer material layer that dissolves in water or gels in water and exhibits tackiness, and a polymer material layer that does not dissolve or is slowly soluble in water. So,
In addition to having good adhesion to mucous membranes and causing no discomfort, it also has the feature that the solubility of the entire system can be adjusted relatively easily.
本発明を実施するに当って使用される薬学的に許容し得
る高分子物質としては、水に溶解又は水でゲル化して粘
着性を有するものであれば殊に制限されないが、例えば
アルギン酸す） ＩＪニウム、トラテカントゴム、アラ
ビアゴム、デキストラン、デキストラン、プルラン、ア
ミロース、ゼラチンの如き天然系、メチルセルロース（
置換度１６〜２）、エチルセルロース（［換Ｉｆ １〜
１．５）、ヒドロキシエチルセルロース、ヒドロキシプ
ロピルセルロース、カルボキシメチルセルロースの如き
半合成系、ポリアクリル酸及びその塩、アクリル酸共重
合体及びその塩、ポリビニルアルコール、無水マレイン
酸共重合物、ポリビニルピロリドンの如き合成系などの
水溶性高分子物質を挙げることができるが、得られる物
質層の層強度などの点から、アルキン酸すトリュウム、
カルボキシメチルセルロース、ポリアクリル酸及びその
塩が好ましいものであり、とりわけアルギン酸ナトリュ
ウム、カルボキシメチルセルロースの一種以上とポリア
クリル酸及びその塩との併用は、よりすぐれた１爾強度
と柔軟性を有する物質層を提供するものであり、ポリア
クリル酸及びその塩は、０．５〜３０重量％（固形分比
）の範囲で含有させるのが好ましいものである。The pharmaceutically acceptable polymeric substance used in carrying out the present invention is not particularly limited as long as it dissolves in water or gels with water and has adhesive properties, but for example, alginic acid, etc.) Natural systems such as IJium, gum tratechanth, gum arabic, dextran, dextran, pullulan, amylose, gelatin, methylcellulose (
degree of substitution 16-2), ethylcellulose ([degree of substitution If 1-2),
1.5), semisynthetic systems such as hydroxyethyl cellulose, hydroxypropyl cellulose, and carboxymethyl cellulose, polyacrylic acid and its salts, acrylic acid copolymers and its salts, polyvinyl alcohol, maleic anhydride copolymers, and polyvinylpyrrolidone. Synthetic water-soluble polymer substances can be mentioned, but from the viewpoint of the layer strength of the obtained material layer, thurium alkynate,
Carboxymethylcellulose, polyacrylic acid and its salts are preferred, and in particular, the combination of sodium alginate and one or more carboxymethylcellulose with polyacrylic acid and its salts provides a material layer with superior strength and flexibility. It is preferable to contain polyacrylic acid and its salt in a range of 0.5 to 30% by weight (solid content ratio).
筐た薬学的に許容しうる可塑剤としては、グリセリン、
プロピレングリコール、ポリエチレングリコール、エチ
ルアルコールなどを挙げることができるが、水浴ａ高分
子物質に対する柔軟性付与能或いは製剤の香味付与など
の点からグリセリン及びプロピレングリコールが殊に好
ましいものである。Pharmaceutically acceptable plasticizers include glycerin,
Examples include propylene glycol, polyethylene glycol, and ethyl alcohol, but glycerin and propylene glycol are particularly preferred from the viewpoint of their ability to impart flexibility to the polymeric substance in the water bath or to impart flavor to the preparation.
これらの水溶性高分子物質と可塑剤とを必須成分として
、水に溶解又は水でケル化して粘着性を示す水親和性高
分子物置Ｊ偏が構成されるものであるが、該物質：可塑
剤の割合は１：０．３〜３、実剛的には１：１〜２５（
重量比）の範囲とするのが好ましいものである。可塑剤
の配合量が上記の範囲外であると、適度な柔軟性及び溶
解性が得られにくいものである。These water-soluble polymer substances and plasticizers are essential components of the water-affinitive polymer material that exhibits adhesive properties when dissolved in water or kelized by water. The ratio of agents is 1:0.3-3, and the actual ratio is 1:1-25 (
It is preferable to set it as the range of (weight ratio). If the blending amount of the plasticizer is outside the above range, it will be difficult to obtain appropriate flexibility and solubility.
このように水に溶解又は水でゲル化して粘着性を示す水
親和性高分子物質層の表面には、前記水溶性高分子物質
の群から選ばれた一種以上のを架橋してなる架橋物と可
塑剤とを必須成分とする水に非又は遅延溶解性の高分子
物質１曽が設けられる。In this way, on the surface of the water-affinity polymer material layer that exhibits adhesiveness when dissolved or gelled in water, a cross-linked material formed by cross-linking one or more types of water-soluble polymer materials selected from the group of water-soluble polymer materials mentioned above is used. A water-insoluble or delayed-solubility polymeric substance 1 is provided which contains a plasticizer and a plasticizer as essential components.
該高分子物質層は、前記水親和性高分子物質層を構成す
るのに用いた、前記水溶性高分子物質及び可塑剤から構
成される。各成分の配合割合は、前記水親和性高分子物
質層と同等の範囲で用いられる。The polymeric material layer is composed of the water-soluble polymeric material and plasticizer used to form the water-affinity polymeric material layer. The mixing ratio of each component is used within the same range as that of the water-affinity polymer material layer.
核高分子物質層を構成する架橋物は、前記水溶性高分子
物質を薬学的に許容し得る方法によって架橋することに
より得られる。The crosslinked material constituting the core polymeric substance layer is obtained by crosslinking the water-soluble polymeric substance by a pharmaceutically acceptable method.
架橋方法として１ｒｉ、水酸基を含□有する水溶性高分
子物質においては、多価カルボン酸とのエステル化反応
又は多官能インシアネートとのウレタン反応などによる
方法、カルボキシル基を含有する前記物質においては、
多価アルコールとのエステル化反応、多官能インシアネ
ートとのウレタン反応或いは２価以上の金属イオンとの
塩架橋などによる方法があり、その他活性水素を含有す
る前記物質とエポキサイドとのエポキシ反応或いは電子
線、過酸化物などによるラジカル反応などの方法でもよ
いものである。The crosslinking method is 1ri, for water-soluble polymer substances containing hydroxyl groups, a method such as esterification reaction with polyhydric carboxylic acid or urethane reaction with polyfunctional incyanate, and for the above substances containing carboxyl groups,
There are methods such as esterification reaction with polyhydric alcohol, urethane reaction with polyfunctional incyanate, salt crosslinking with divalent or higher metal ions, and epoxy reaction between the above substances containing active hydrogen and epoxide, or electron reaction. A method such as a radical reaction using a hydrogen ray or a peroxide may also be used.
し７かして、架橋方法としての簡便さ及び架橋反応の正
確性などから、カルボキシル基を含有する水溶性高分子
物質を用いて、２価以上の金属イオンで塩架橋する方法
が好ましいものである。かかる金属イオンとじては、薬
学的に許容し得る塩化力ルシュウム、塩化第１鉄、塩化
マグネシュウム、塩化アルミニーラムなどを挙げること
ができる。However, in view of the simplicity of the crosslinking method and the accuracy of the crosslinking reaction, it is preferable to use a water-soluble polymer substance containing a carboxyl group and salt crosslinking with metal ions of divalent or higher valence. be. Examples of such metal ions include pharmaceutically acceptable rhusium chloride, ferrous chloride, magnesium chloride, aluminum chloride, and the like.
前記水親和性高分子物質層と水に非又は遅延溶解性の高
分子物質層とは、予め夫々の層を離型ライナー上などに
形成し、これを重ね合せて積層して粘膜製剤とするのが
好ましいが、例えば水溶性高分子物質と可塑剤とからな
る水親和性高分子物質層を形成し、この一方の表面側を
前記手法により所定１！ｔみだけ架橋して水に非又は遅
延溶解性の高分子物質層としてもよいものである。The water-affinity polymer material layer and the water-insoluble or delayed-solubility polymer material layer are formed in advance on a release liner, etc., and then stacked on top of each other to form a mucosal preparation. Preferably, for example, a water-affinity polymer material layer made of a water-soluble polymer material and a plasticizer is formed, and one surface side of the layer is coated with a predetermined 1! It is also possible to form a layer of polymer material that is non- or delayed-soluble in water by crosslinking only by t.
なお水に非又は遅延溶解性の高分子物質層が多孔ｉ状で
水分全透過せしめ、不必快に水親和性高分子物質層の／
６解又はゲル化を早める恐れがあるときには、前記層又
は遅延溶解性の高分子物質層面に、さらに非多孔性の水
に非又は遅延溶解性柔軟フィルム層を設けてもよいもの
である。Note that the polymeric substance layer that is non- or delayed-soluble in water has a porous i-shape that allows all moisture to pass through, and unavoidably causes the water-affinity polymeric substance layer to pass through.
6. When there is a risk of accelerating dissolution or gelation, a non-porous, non-water-soluble or delayed-dissolving flexible film layer may be further provided on the surface of the above-mentioned layer or the delayed-dissolving polymer material layer.
本発明の粘；模製剤は水に対する親和性が良好で、しか
も水に溶解又は水でゲル化して粘着性を示す高分子物質
層と、柔軟性が良好で、しかも水に非又は遅延溶解性の
高分子物質層とで構成されているので、使用時に違和感
を与えることなく、口）杜の如き粘膜部位に適用するこ
とができ、しかもすぐれた粘着性を示すという特徴を有
する。The viscous imitation product of the present invention has a polymeric material layer that has good affinity for water and exhibits tackiness when dissolved or gelled in water, and has good flexibility and is non- or delayed-soluble in water. Since it is composed of a polymer material layer, it can be applied to mucous membrane areas such as the mouth without causing any discomfort during use, and has the characteristics of exhibiting excellent adhesiveness.
捷だ水に非又は遅延溶解性の高分子物質層の架橋度を調
整することによって、薬物の種類などに応じた＃解時間
即ち薬物の固定時間とすることができるものである。By adjusting the degree of cross-linking of the polymer material layer that is non-or delayed soluble in fresh water, the #resolution time, that is, the fixation time of the drug, can be adjusted depending on the type of drug.
以下本発明の実施例を示す。Examples of the present invention will be shown below.
実施例１
カルホキシメグールセルロース（ＯＭＯ）８９、グリセ
リン２０ｇ及び水３０ｇからなる混合物を充分に撹拌混
合し、この混合液を乾燥後の厚みが２００μｒｒＬとな
るようにポリエステルフィルム（禎面に塗布乾燥して、
水に溶解又は水でゲル化する水親和性高分子物質層（Ａ
）を得る。Example 1 A mixture consisting of 89 g of carboxymegol cellulose (OMO), 20 g of glycerin, and 30 g of water was thoroughly stirred and mixed, and this mixed solution was coated on a polyester film (on the surface and dried) so that the thickness after drying was 200 μrrL. do,
A water-affinity polymer material layer that dissolves in water or gels with water (A
).
−万、ポリアクリル酸ナトリコウム３ ｇ 、 ｅＭＣ
８１１グリセリン１５ｇ、塩化カルシュラム１ｇ及び水
１０ｆｊからなる混合液を充分に撹拌混合し、この水沼
液を乾燥後の厚みが１００μｍとなるようにポリツース
テルフィルム（功面に塗布乾燥し、さらにこｉｔを塩化
第１鉄５重量％水溶液に３０秒間浸漬して、多孔負夕・
ｒブの弁済解性の高分子物質層（Ｂ）を得る。-10,000, sodium polyacrylate 3 g, eMC
A mixed solution consisting of 15 g of 811 glycerin, 1 g of calcium chloride, and 10 fj of water was sufficiently stirred and mixed, and the water solution was coated on a polytuster film (coated and dried) so that the thickness after drying was 100 μm. was immersed in a 5% by weight ferrous chloride aqueous solution for 30 seconds to form a porous anode.
A resolvable polymeric material layer (B) of r-build is obtained.
該層（Ｂ）をフィルム（ｎ）面から剥離し、前記層（Ａ
）の表面に剥離面を介し７て貼り合せ、本発明の粘膜製
１１すを得た。The layer (B) is peeled off from the film (n) side, and the layer (A) is peeled off from the film (n) side.
) through the peeling surface 7 to obtain the mucous membrane 11 of the present invention.
該製剤をフィルム（Ａ’）面から剥離し、１０人のバネ
ラーのロバ・２粘膜面に施用したところ、平均で３０分
間に戸って良好に付着した。When the preparation was peeled off from the film (A') side and applied to the mucous membranes of 10 donkeys, it adhered well in an average of 30 minutes.
実施例２
実施例１ｆ得られた粘膜製剤の層（Ｂ）の表面に、非溶
解性高分子物質とし７てのコロジオン（日本薬局方）を
塗布乾燥し２て、非溶解性被覆を形成した粘膜製剤を得
た。Example 2 Example 1f Collodion (Japanese Pharmacopoeia) as a non-soluble polymer substance 7 was applied to the surface of the layer (B) of the obtained mucosal preparation and dried to form a non-soluble coating. A mucosal preparation was obtained.
実施例１と同様に測定したところ９０分間に亘って良好
に付着した。Measurements were made in the same manner as in Example 1, and good adhesion was observed for 90 minutes.
実施例３
ポリアクリル酸ナトリュウム３ｇ、ポリビニルアルコー
ル４９、アルギン酸、 ＋ ） ＩＪ ニウム７９、グ
リセリン２０９及び水２０ ｇからなる混合液を作り、
以下実施例１と同様の操作により、２００μｍのｒＦＩ
（Ａ）をフィルム（Ａ）面に形成した。Example 3 A mixed solution consisting of 3 g of sodium polyacrylate, 49 polyvinyl alcohol, alginic acid, 79 IJ nium, 209 glycerin, and 20 g of water was prepared,
Hereinafter, by the same operation as in Example 1, a 200 μm rFI
(A) was formed on the film (A) side.
一方、ポリアクリル酸ナトリュウム３．９ 、ポリビニ
ルアルコール４９、アルギン酸ナトリニウム７ｇ、グリ
セリン２０ｇ、塩化カルシュラム１ｇ及び水６０ｇから
なる混合液を作り、これをポリエステルフィルム（ｄ）
面に、乾燥後の厚みが２００μｍとなるように塗布乾燥
して、遅延冶解性の高分子物質層（Ｃ）を得る。On the other hand, a mixed solution consisting of 3.9 g of sodium polyacrylate, 49 g of polyvinyl alcohol, 7 g of sodium alginate, 20 g of glycerin, 1 g of calcium chloride, and 60 g of water was prepared, and this was used to form a polyester film (d).
It is coated on the surface and dried to a thickness of 200 μm after drying to obtain a delayed melting polymeric substance layer (C).
前記層（Ａ）と（０）とを貼り合せて粘膜製剤を得、パ
ネラ−のロバな粘膜面に、層（Ａ）を介して貼り付けた
ところ、平均で２０分間に亘って良好に付着した。When the above-mentioned layers (A) and (0) were bonded together to obtain a mucosal preparation, and it was attached to the mucous membrane surface of a panelist via layer (A), it adhered well for an average of 20 minutes. did.
実施例４
実施例３の粘膜製剤の層（Ｃ）の表面に、置換度２以上
の水不溶性エチルセルロース溶液を塗布乾燥して、非溶
解性被覆を形成した粘膜製剤は、平均で（５０分間に１
って良好に付着した。Example 4 A water-insoluble ethyl cellulose solution with a degree of substitution of 2 or more was applied to the surface of layer (C) of the mucosal preparation of Example 3 and dried to form an insoluble coating. 1
It adhered well.
実施例５
ポリアクリル酸ナトリュウム３９，０Ｍ０６９、グリセ
リン２５ｇ及び水３０．ｑからなる混合液を作り、ポリ
エステルフィルム面に乾燥後の厚みが４００μｍとなる
ように塗布乾”ｊ架して、ｌ？＊ （Ａ）を得る。Example 5 Sodium polyacrylate 39.0M069, glycerin 25g and water 30. A mixed solution consisting of q is prepared and applied onto a polyester film so that the thickness after drying is 400 μm.
この層（、Ａ）の表面に塩化マグネシーウ１０重量係水
ｆ６液を塗布乾燥して、該層（Ａ）の表層部分を架扁せ
しめ、この部分を遅延溶解性の層（Ｃ）とし、粘膜製剤
を得る。On the surface of this layer (A), a 10-weight water-containing F6 solution of magnesium chloride is applied and dried, and the surface layer of the layer (A) is stretched, and this portion is used as a slow-dissolving layer (C). Obtain the formulation.
この製剤の付着時間は平均で３０分間であった。The average deposition time for this formulation was 30 minutes.
実施例６
ヒドロキシエチルセルロース３０９．カルボキシビニル
ポリマー５．９及びプロピレングリコール５０ｇからな
る混合物を型に流し込み、プレス成型して厚さ３００μ
ｍの層（Ａ）を得る。Example 6 Hydroxyethyl cellulose 309. A mixture consisting of 5.9 g of carboxyvinyl polymer and 50 g of propylene glycol was poured into a mold and press-molded to a thickness of 300 μm.
m layers (A) are obtained.
一方、ポリアクリル酸１０ｇ、ポリビニルアルコール１
０ｇ、グリセリン１０．ｑ及び水７０９からなる混合液
を作り、ポリエステルフィルム（Ｂ） 面の表面に乾燥
後のノ９みが８０μｍとなるように塗布し、１１０℃で
１０分間加熱処理して架橋せしめ、層（０）を得る。On the other hand, 10 g of polyacrylic acid, 1 g of polyvinyl alcohol
0g, glycerin 10. q and water 709 was prepared, and applied to the surface of the polyester film (B) so that the thickness after drying was 80 μm, and was heat-treated at 110°C for 10 minutes to crosslink. ).
前記１＠（Ａ）を層（０）の表面に貼ね合せて粘膜製剤
を得、付着時間合狗鼠したところ平均で２０分間であっ
た。A mucosal preparation was obtained by laminating the above 1@(A) on the surface of layer (0), and the adhesion time was determined to be 20 minutes on average.
実施ｖｊ７
ヒドロキシプロピルセルロース１０９． ヒドロキシ
エチルセルロース３０ｇ及びプロピ１．／フグリコール
４０．９からなる混合物全プレス成型１７て。Implementation vj7 Hydroxypropyl cellulose 109. 30g of hydroxyethyl cellulose and 1. /Fuglycol 40.9 total press molding 17.
２００μｎＬ厚の層ＦＡ）を得る。A layer FA) of 200 μnL thickness is obtained.
一方、ポリアクリルａｋ ５．９ 、アルギン酸ナトリ
ニウム１０．９．グリセリン３０ ｇ、塩化カルシュラ
ム１．５９及び水７０．９からなる混合液を作り、ポリ
エステルフィルム（ｄ）面の表面に、乾燥後の厚みが１
５０μｍとカるように塗布乾燥し７て層（０）を得る。On the other hand, polyacrylic ak 5.9, sodium alginate 10.9. Prepare a mixed solution consisting of 30 g of glycerin, 1.59 g of calcium chloride, and 70.9 g of water, and apply it to the surface of the polyester film (d) so that the thickness after drying is 1.
It was coated to a thickness of 50 μm and dried to obtain layer (0).
前記１ｉ’Ｊ（Ａ）と（Ｇ）とを貼り合せて粘膜製剤を
得、付着時間を測定したとξろ平均で３０分間であった
。A mucosal preparation was obtained by pasting 1i'J (A) and (G) together, and the adhesion time was measured to be 30 minutes on average.
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)
れた一種以上と薬学的に許容し得る可塑剤とを必須成分
とする水に溶解又は水でゲル化して粘着性を示す水親和
性高分子物質層と、薬学的に許容し得る水溶性高分子物
質の群から選ばれた一種以上の架橋物と薬学的に許拝し
得る可塑剤とを必須成分とする水に非又は遅延溶解性の
高分子物質層とからなる粘膜製剤。 ２）水溶性高分子物質がポリアクリル酸及びその塩、カ
ルボキシメチルセルロース及びアルギン酸ナトリュウム
の群から選ばれた一種以上である特許請求の範囲第１項
記載の粘膜製剤。 ３）可塑剤がグリセリン、プロピレングリコールの群か
ら選ばれた一種以上である特許請求の範囲第１項記載の
粘膜製剤。 ４）架橋物がポリアクリル酸及びその塩、カルボキシメ
チルセルロース及びアルギン酸ナトリュウムの群から選
ばれた一種以上を架橋してなるものである特許請求の範
囲第１項記載の粘膜製剤。 ５）架橋物がカルボキシル基を含有する水溶性高分子物
質を薬学的に許容し得る２価以上の金属イオンで架橋し
たものである特許請求の範囲第１項記載の粘膜製剤。[Scope of Claims] 1) A product which is dissolved in water or gelled with water, and which contains as essential components one or more selected from the group of pharmaceutically acceptable water-bathable polymer substances and a pharmaceutically acceptable plasticizer. The essential ingredients include a water-friendly polymer material layer that exhibits adhesive properties, one or more crosslinked products selected from the group of pharmaceutically acceptable water-soluble polymer materials, and a pharmaceutically acceptable plasticizer. and a layer of a polymeric material that is non- or slowly soluble in water. 2) The mucous membrane preparation according to claim 1, wherein the water-soluble polymeric substance is one or more selected from the group of polyacrylic acid and its salts, carboxymethyl cellulose, and sodium alginate. 3) The mucosal preparation according to claim 1, wherein the plasticizer is one or more selected from the group of glycerin and propylene glycol. 4) The mucosal preparation according to claim 1, wherein the crosslinked product is formed by crosslinking one or more types selected from the group of polyacrylic acid and its salts, carboxymethyl cellulose, and sodium alginate. 5) The mucosal preparation according to claim 1, wherein the crosslinked product is a carboxyl group-containing water-soluble polymer substance crosslinked with a pharmaceutically acceptable metal ion having a valence of two or more.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP1129982A JPS58128314A (en) | 1982-01-26 | 1982-01-26 | Preparation for mucous membrane |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP1129982A JPS58128314A (en) | 1982-01-26 | 1982-01-26 | Preparation for mucous membrane |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS58128314A true JPS58128314A (en) | 1983-07-30 |
| JPS6125687B2 JPS6125687B2 (en) | 1986-06-17 |
Family
ID=11774109
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP1129982A Granted JPS58128314A (en) | 1982-01-26 | 1982-01-26 | Preparation for mucous membrane |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS58128314A (en) |
Cited By (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS60116631A (en) * | 1983-11-29 | 1985-06-24 | Nitto Electric Ind Co Ltd | Pharmaceutical preparation for oral cavity |
| JPS60116630A (en) * | 1983-11-29 | 1985-06-24 | Nitto Electric Ind Co Ltd | Pharmaceutical preparation for oral cavity |
| JPS60215622A (en) * | 1984-04-09 | 1985-10-29 | Toyobo Co Ltd | Sustained release preparation for mucosa in oral cavity |
| JPS60248609A (en) * | 1984-05-23 | 1985-12-09 | Toyobo Co Ltd | Gradually releasing preparation for oral mucosa |
| JPS6185315A (en) * | 1984-10-04 | 1986-04-30 | Teikoku Seiyaku Kk | Sheet-like preparation |
| JPS61280423A (en) * | 1985-06-05 | 1986-12-11 | Kiyuukiyuu Yakuhin Kogyo Kk | Mucosal application agent in oral cavity |
| JPS62135417A (en) * | 1985-12-09 | 1987-06-18 | Sato Seiyaku Kk | Filmy pharmaceutical |
| JPS63310818A (en) * | 1987-06-12 | 1988-12-19 | Sato Seiyaku Kk | Sheet preparation to be applied to oral mucosa |
| JPH0248525A (en) * | 1988-08-11 | 1990-02-19 | Lederle Japan Ltd | Remedy for peptic ulcer |
| JPH02300123A (en) * | 1989-03-27 | 1990-12-12 | Lederle Japan Ltd | Remedy for peptic ulcer |
| JPH05501880A (en) * | 1989-11-07 | 1993-04-08 | ダム，アンデルス | Nicotine-containing stimulant unit |
| EP0781546A1 (en) | 1995-12-26 | 1997-07-02 | Sanwa Kagaku Kenkyusho Co., Ltd. | A multi-layered film preparation |
| US5733574A (en) * | 1989-11-07 | 1998-03-31 | Dam; Anders | Nicotine containing stimulant unit |
| JP2007513916A (en) * | 2003-12-12 | 2007-05-31 | エルテーエス ローマン テラピー−ジステーメ アーゲー | Dosage forms based on cross-linked hydrophilic polymers |
| US10987321B2 (en) * | 2018-09-04 | 2021-04-27 | Babak Ghalili | Cannabinoid and anesthetic compositions and methods |
Citations (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS502006A (en) * | 1973-05-09 | 1975-01-10 | ||
| JPS5282715A (en) * | 1975-12-29 | 1977-07-11 | Sanyo Chem Ind Ltd | Long acting drug composition |
| JPS5315413A (en) * | 1976-07-28 | 1978-02-13 | Daikiyou Yakuhin Kougiyou Kk | Pap agent |
| JPS5492618A (en) * | 1977-12-30 | 1979-07-23 | Japan Synthetic Rubber Co Ltd | Poultice |
| JPS555488A (en) * | 1978-06-16 | 1980-01-16 | Bbc Brown Boveri & Cie | Operation method of gas turbine apparatus |
| JPS5562012A (en) * | 1978-11-06 | 1980-05-10 | Teijin Ltd | Slow-releasing preparation |
| JPS5584166A (en) * | 1978-12-20 | 1980-06-25 | Lion Hamigaki Kk | Band for spongy medicine |
| JPS5584167A (en) * | 1978-12-20 | 1980-06-25 | Lion Hamigaki Kk | Band for spongy medicine |
| JPS5592334U (en) * | 1978-12-20 | 1980-06-26 | ||
| JPS5758615A (en) * | 1980-09-26 | 1982-04-08 | Nippon Soda Co Ltd | Film agnent and its preparation |
-
1982
- 1982-01-26 JP JP1129982A patent/JPS58128314A/en active Granted
Patent Citations (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS502006A (en) * | 1973-05-09 | 1975-01-10 | ||
| JPS5282715A (en) * | 1975-12-29 | 1977-07-11 | Sanyo Chem Ind Ltd | Long acting drug composition |
| JPS5315413A (en) * | 1976-07-28 | 1978-02-13 | Daikiyou Yakuhin Kougiyou Kk | Pap agent |
| JPS5492618A (en) * | 1977-12-30 | 1979-07-23 | Japan Synthetic Rubber Co Ltd | Poultice |
| JPS555488A (en) * | 1978-06-16 | 1980-01-16 | Bbc Brown Boveri & Cie | Operation method of gas turbine apparatus |
| JPS5562012A (en) * | 1978-11-06 | 1980-05-10 | Teijin Ltd | Slow-releasing preparation |
| JPS5584166A (en) * | 1978-12-20 | 1980-06-25 | Lion Hamigaki Kk | Band for spongy medicine |
| JPS5584167A (en) * | 1978-12-20 | 1980-06-25 | Lion Hamigaki Kk | Band for spongy medicine |
| JPS5592334U (en) * | 1978-12-20 | 1980-06-26 | ||
| JPS5758615A (en) * | 1980-09-26 | 1982-04-08 | Nippon Soda Co Ltd | Film agnent and its preparation |
Cited By (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS60116630A (en) * | 1983-11-29 | 1985-06-24 | Nitto Electric Ind Co Ltd | Pharmaceutical preparation for oral cavity |
| JPS60116631A (en) * | 1983-11-29 | 1985-06-24 | Nitto Electric Ind Co Ltd | Pharmaceutical preparation for oral cavity |
| JPS60215622A (en) * | 1984-04-09 | 1985-10-29 | Toyobo Co Ltd | Sustained release preparation for mucosa in oral cavity |
| JPH0530808B2 (en) * | 1984-04-09 | 1993-05-11 | Toyo Boseki | |
| JPS60248609A (en) * | 1984-05-23 | 1985-12-09 | Toyobo Co Ltd | Gradually releasing preparation for oral mucosa |
| JPS6347687B2 (en) * | 1984-05-23 | 1988-09-26 | Toyo Boseki | |
| JPH0522685B2 (en) * | 1984-10-04 | 1993-03-30 | Teikoku Seiyaku Kk | |
| JPS6185315A (en) * | 1984-10-04 | 1986-04-30 | Teikoku Seiyaku Kk | Sheet-like preparation |
| JPS61280423A (en) * | 1985-06-05 | 1986-12-11 | Kiyuukiyuu Yakuhin Kogyo Kk | Mucosal application agent in oral cavity |
| JPH0260644B2 (en) * | 1985-06-05 | 1990-12-17 | Kyukyu Yakuhin Kogyo Kk | |
| JPS62135417A (en) * | 1985-12-09 | 1987-06-18 | Sato Seiyaku Kk | Filmy pharmaceutical |
| JPH044296B2 (en) * | 1987-06-12 | 1992-01-27 | ||
| JPS63310818A (en) * | 1987-06-12 | 1988-12-19 | Sato Seiyaku Kk | Sheet preparation to be applied to oral mucosa |
| JPH0248525A (en) * | 1988-08-11 | 1990-02-19 | Lederle Japan Ltd | Remedy for peptic ulcer |
| JPH02300123A (en) * | 1989-03-27 | 1990-12-12 | Lederle Japan Ltd | Remedy for peptic ulcer |
| JPH05501880A (en) * | 1989-11-07 | 1993-04-08 | ダム，アンデルス | Nicotine-containing stimulant unit |
| US5733574A (en) * | 1989-11-07 | 1998-03-31 | Dam; Anders | Nicotine containing stimulant unit |
| US6110495A (en) * | 1989-11-07 | 2000-08-29 | Dam; Anders | Nicotine containing stimulant unit |
| EP0781546A1 (en) | 1995-12-26 | 1997-07-02 | Sanwa Kagaku Kenkyusho Co., Ltd. | A multi-layered film preparation |
| US5914118A (en) * | 1995-12-26 | 1999-06-22 | Sanwa Kagaku Kenkyusho Co., Ltd. | Multi-layered drug containing film preparation having powder adhesive thereon |
| JP2007513916A (en) * | 2003-12-12 | 2007-05-31 | エルテーエス ローマン テラピー−ジステーメ アーゲー | Dosage forms based on cross-linked hydrophilic polymers |
| JP4943160B2 (en) * | 2003-12-12 | 2012-05-30 | エルテーエス ローマン テラピー−ジステーメ アーゲー | Dosage forms based on cross-linked hydrophilic polymers |
| US10987321B2 (en) * | 2018-09-04 | 2021-04-27 | Babak Ghalili | Cannabinoid and anesthetic compositions and methods |
Also Published As
| Publication number | Publication date |
|---|---|
| JPS6125687B2 (en) | 1986-06-17 |
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