JPS59186913A - Base to be applied to mucosa in oral cavity - Google Patents
Base to be applied to mucosa in oral cavityInfo
- Publication number
- JPS59186913A JPS59186913A JP6095783A JP6095783A JPS59186913A JP S59186913 A JPS59186913 A JP S59186913A JP 6095783 A JP6095783 A JP 6095783A JP 6095783 A JP6095783 A JP 6095783A JP S59186913 A JPS59186913 A JP S59186913A
- Authority
- JP
- Japan
- Prior art keywords
- base
- oral cavity
- gum
- vinyl acetate
- gluten
- 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
Abstract
Description
【発明の詳細な説明】
本発明はゼラチン又は寒天、グルテン、カルボキシビニ
ルポリマー、及び酢酸ビニル樹脂又はガム類を配合した
口腔粘膜貼付用基剤に関する。DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a base for application to oral mucosa containing gelatin or agar, gluten, carboxyvinyl polymer, and vinyl acetate resin or gums.
口腔用の徐放性製剤として従来よりトローチやバッカル
なでが知られている。Troches and buccal dabs have been known as sustained-release preparations for the oral cavity.
しかし、これらの製剤は固く、かつある程度の厚みを有
するため口腔内において異物感が大きい。そのため啄下
したりかみ砕いたりする衝動にかられ、長時間口腔内に
止めておくことは困難であシ、薬物を長時間にわたって
投与するための製剤としては適当でない。However, these preparations are hard and have a certain degree of thickness, so they feel like a foreign body in the oral cavity. Therefore, it is difficult to keep it in the oral cavity for a long time due to the urge to swallow or chew it, and it is not suitable as a preparation for administering drugs over a long period of time.
そこで、本発明者らは口腔に長時間保持しうる徐放性製
剤について種々検討した結果、ゼラチン又は寒天、グル
テン、カルボキシビニルポリマー、及び酢酸ビニル又は
ガム類を配合した基剤に薬物を添加し、シート状とした
後、歯肉粘膜に適用すると、その粘膜上の水分を吸収し
て歯肉に密着し、唾液の影響を受けることなく長時間口
腔内に保持することができ、薬物を徐々に放出し、局所
的ならびに全身的な薬物の長時間投与に適したシート製
剤とすることができることを見い出した。As a result of various studies on sustained-release preparations that can be retained in the oral cavity for a long period of time, the present inventors added a drug to a base containing gelatin or agar, gluten, carboxyvinyl polymer, and vinyl acetate or gums. When applied to the gingival mucosa after forming into a sheet, it absorbs the moisture on the mucosa and adheres closely to the gingiva, allowing it to be retained in the oral cavity for a long time without being affected by saliva, and gradually releasing the drug. We have found that it can be made into a sheet preparation suitable for long-term administration of drugs both locally and systemically.
本発明は上記知見に基づいて完成されたものである。The present invention was completed based on the above findings.
本発明の基剤において使用するグルテンは広く食品など
に利用されているもので、小麦から得られる蛋白質の混
合物である。Gluten used in the base of the present invention is widely used in foods and is a mixture of proteins obtained from wheat.
カルボキシビニルポリマーとしては、例えばポリアクリ
ル酸や、その一部を架橋したもの、例えばカーボポール
などの酸型のものがあげられる。Examples of carboxyvinyl polymers include polyacrylic acid and partially crosslinked polymers, such as acid type polymers such as carbopol.
酢酸ビニル樹脂とは酢酸ビニルを主成分とする合成樹脂
のことで、例えばポリ酢酸ビニルや酢酸ビニルを主成分
とする共重合体などがあげられる。Vinyl acetate resin refers to a synthetic resin whose main component is vinyl acetate, such as polyvinyl acetate or a copolymer whose main component is vinyl acetate.
ガム類としては例えば、グアーガム、天然チクル、キサ
ンタンガム、アラビアゴム、トラガカントゴム、カラヤ
ゴム、エコーガム、ローカストビーンガムなどの植物ガ
ム質があげられる。Examples of gums include vegetable gums such as guar gum, natural chicle, xanthan gum, gum arabic, gum tragacanth, gum karaya, echo gum, and locust bean gum.
酢酸ビニル樹脂やガム類はそれぞれ単独で用いてもよく
、又、両者を併用してもよい。Vinyl acetate resin and gums may be used alone or in combination.
本発明基剤中の各成分の使用割合はそれらの成分全量に
対し、ゼラチン又は寒天１〜７０ ｗ／ｗ％、好ましく
は４〜５０ｗ／ｗ％、さらに好ましくは５〜４ Ｑ ｗ
／ｗ％、グルテン１〜７Ｑｗ／ｗ％、好ましくは１０〜
５０ｗ／ｗ％、さらに好ましくは２０〜３８ｗ／ｗ％、
カルボキシビニルポリマー１〜５０ｗ／ｗ％、好ましく
は１０〜４０ｗ／ｗ％、さらに好ましくは２０〜３０
ｗ ／ ｗ％、酢酸ビニル樹脂又はガム類１〜７０ｗ／
ｗ％、好捷しくは１０〜５０Ｗ／ｗ％、さらに好寸しく
は１２〜３８ｗ／ｗａ；ｂ程度である。The proportion of each component used in the base of the present invention is gelatin or agar 1 to 70 w/w%, preferably 4 to 50 w/w%, more preferably 5 to 4 Q w %, based on the total amount of those components.
/w%, gluten 1-7Qw/w%, preferably 10-7%
50 w/w%, more preferably 20 to 38 w/w%,
Carboxyvinyl polymer 1 to 50 w/w%, preferably 10 to 40 w/w%, more preferably 20 to 30
w/w%, vinyl acetate resin or gums 1-70w/
w%, preferably about 10 to 50 W/w%, more preferably about 12 to 38 w/wa;b.
本発明の基剤にはパップ剤などに通常使用しつる基剤成
分、例えば水、グリセリン、グロピレングリコール、ポ
リエチレングリコール、■。The base of the present invention includes base components commonly used in poultices, such as water, glycerin, glopylene glycol, polyethylene glycol, and the like.
３−ブタンジオール、ソルビトールなどの多価アルコー
ル、メチルセルロース、エチルセルロース、プロピルセ
ルロース、エチルメチルセルロース、ヒドロキシエチル
セルロース、ヒドロキシグロビルセルロース、カルボキ
シメチルセルロース、セルロースアセテートフタレート
ナどのセルロース誘導体、ポリアクリル酸ナトリウム、
ポリビニルピロリドンなどを添加してもよい。その配合
割合は本発明の基剤に対し水ではＯ〜３０ ｗ ／ ｗ
％、好ましくは２〜２５ｗ／ｗ％程度であり、他の成分
では０〜１００ｗ／ｗ％、好ましくは３０〜８０’ｗ／
ｗ％程度である。Polyhydric alcohols such as 3-butanediol and sorbitol, cellulose derivatives such as methylcellulose, ethylcellulose, propylcellulose, ethylmethylcellulose, hydroxyethylcellulose, hydroxyglobil cellulose, carboxymethylcellulose, cellulose acetate phthalate, sodium polyacrylate,
Polyvinylpyrrolidone or the like may also be added. The mixing ratio of water to the base of the present invention is O~30 w/w
%, preferably about 2 to 25 w/w%, and 0 to 100 w/w%, preferably 30 to 80'w/w% for other components.
It is about w%.
本発明の基剤を用いて口腔粘膜用製剤を得るには、ゼラ
チンもしくは寒天、グルテン、カルボキシビニルポリマ
ー、及び酢酸ビニルもしくはガム類を精製水とともに加
温下撹拌してペースト状組成物とし、次いでこの組成物
に種々の薬物を添加して均一に混合した後、適当な支持
体上に展延塗布し、通常水分含量が０．５〜２０ｗ ／
ｗ％程度になるまで乾燥することにより、優れた口腔
粘膜貼付用製剤が得られる。To obtain a preparation for oral mucosa using the base of the present invention, gelatin or agar, gluten, carboxyvinyl polymer, and vinyl acetate or gums are stirred with purified water under heating to form a paste composition, and then After various drugs are added to this composition and mixed uniformly, it is spread and coated on a suitable support, and the water content is usually 0.5 to 20 w/w.
By drying to about w%, an excellent oral mucosal patch preparation can be obtained.
薬物としては特に制限ないが、例えばベタヒスチン、γ
−アミノ酪酸、クロルプロマジン、塩化スキザメトニウ
ム、エチレフリン、スコポラミン、トルブタミド、イミ
プラミンなどの水溶性の薬物が好ましい。There are no particular restrictions on the drugs, but for example, betahistine, γ
- Water soluble drugs such as aminobutyric acid, chlorpromazine, schizamethonium chloride, etilefrine, scopolamine, tolbutamide, imipramine are preferred.
本発明の基剤を用いた製剤は、薬物を徐々に放出すると
ともに使用後は製剤中に残存する薬物の量も少なく、又
、貼付部位の水分を吸収して貼付部位に充分に密着し、
使用中の保型性も良好で、８時間以上、必要ならば２４
時間程度貼付しておくことが可能なので、薬物の吸収率
も良好であり、かつ適度な柔軟性とともに厚さも１０〜
１０００μｍ程度まで薄くすることができるので使用感
も良好である。The formulation using the base of the present invention gradually releases the drug, has a small amount of drug remaining in the formulation after use, and also absorbs moisture from the application site and adheres well to the application site.
Good shape retention during use, more than 8 hours, 24 hours if necessary
It can be left on for about an hour, so the absorption rate of the drug is good, and the thickness is 10~10cm with moderate flexibility.
Since the thickness can be reduced to about 1000 μm, the usability is also good.
５−
次に本発明の基剤が優れた効果を有するものであること
を実験例により説明する。5- Next, the excellent effects of the base material of the present invention will be explained using experimental examples.
実施例
（１）試料の調製
ゼラチン１４１、グルテン８Ｊ１カルボキシビニルポリ
マー８１、酢酸ビニル樹脂６１を混合し、次いで精製水
３０ ｍｌを加え、加熱攪拌してペースト状とした後、
脱気する。このペースト状組成物を塩化ビニルフィルム
に５００ Ｐ／ｍ２の割合で展延塗布し、ついで３０℃
の恒温室にて水分含量が１５％になるまで乾燥した後、
所定のサイズ（３ｃｂ
た。Example (1) Preparation of sample Gelatin 141, Gluten 8J1 carboxyvinyl polymer 81, and vinyl acetate resin 61 were mixed, and then 30 ml of purified water was added and heated and stirred to form a paste.
Degas. This paste composition was spread and coated on a vinyl chloride film at a rate of 500 P/m2, and then heated at 30°C.
After drying in a constant temperature room until the moisture content reaches 15%,
Predetermined size (3cb).
（２）実験方法
試料をボランティア２名の歯肉粘膜に就寝前貼付し、そ
の接着性及び使用感を調べた。(2) Experimental method Samples were applied to the gingival mucosa of two volunteers before going to bed, and their adhesion and feeling of use were examined.
（３）結果
ボランティア２名に貼付した試料はいずれも起床時（８
時間後）においても剥離せず、密着していた。又、その
使用感も、ボランティア２６一
名のいずれも、気になるほどの違物感もなく良好であっ
た。(3) Results The samples affixed to the two volunteers were tested upon waking up (8
Even after several hours), the film remained in close contact with the film without peeling off. Moreover, the feeling of use was good, with none of the 26 volunteers feeling any strangeness that bothered them.
実施例１゜
ゼラチン４０部、グルテン２５部、カルボキシビニルポ
リマー２０部、グアーガム１５部を水５０部とともに均
一に練合しペースト状組成物を得る。Example 1 40 parts of gelatin, 25 parts of gluten, 20 parts of carboxyvinyl polymer, and 15 parts of guar gum are uniformly kneaded with 50 parts of water to obtain a paste composition.
次いでこのペースト状組成物に塩酸エチレン９フ１０部
を添加し、支持体上に塗布、水分が２０％になるまで乾
燥すると本発明の基剤を利用した製剤を得ることができ
る。Next, 9 parts of ethylene hydrochloride and 10 parts of ethylene hydrochloride are added to this paste-like composition, and the mixture is coated on a support and dried until the moisture content becomes 20% to obtain a preparation using the base of the present invention.
実施例２゜
寒天９部、グルテン３６部、カルボキシビニルポリマー
２４部、酢酸ビニル樹脂１８部、天然チクル１３部を水
１００部とともに加熱下撹拌してペースト状組成物を得
る。Example 2 9 parts of agar, 36 parts of gluten, 24 parts of carboxyvinyl polymer, 18 parts of vinyl acetate resin, and 13 parts of natural chicle were stirred with 100 parts of water under heat to obtain a paste composition.
次いで実施例１と同様にして本発明の基剤を利用した製
剤を得ることができる。Next, a preparation using the base of the present invention can be obtained in the same manner as in Example 1.
７− −８９＝7- −89=
Claims (1)
ポリマー、及び酢酸ビニル樹脂又はガム類を配合した口
腔粘膜貼付用基剤(1) Base for oral mucosa patch containing gelatin or agar, gluten, carboxyvinyl polymer, and vinyl acetate resin or gums
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP6095783A JPS59186913A (en) | 1983-04-08 | 1983-04-08 | Base to be applied to mucosa in oral cavity |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP6095783A JPS59186913A (en) | 1983-04-08 | 1983-04-08 | Base to be applied to mucosa in oral cavity |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPS59186913A true JPS59186913A (en) | 1984-10-23 |
Family
ID=13157383
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP6095783A Pending JPS59186913A (en) | 1983-04-08 | 1983-04-08 | Base to be applied to mucosa in oral cavity |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS59186913A (en) |
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2571253A1 (en) * | 1984-10-04 | 1986-04-11 | Nippon Kayaku Kk | SHEET-FORM PREPARATION |
| EP0200508A2 (en) * | 1985-04-27 | 1986-11-05 | Nitto Denko Corporation | Adhesive oral bandages and oral pharmaceutical preparations |
| EP0223524A2 (en) * | 1985-11-08 | 1987-05-27 | Nitto Denko Corporation | Use of adhesive dermal bandages and dermal percutaneous preparations |
| JPH02200624A (en) * | 1989-01-30 | 1990-08-08 | Nippon Kayaku Co Ltd | Dental dressing agent |
| JPH02202814A (en) * | 1989-01-31 | 1990-08-10 | Nitto Denko Corp | Plaster preparation for mucosa of oral cavity |
| US6585997B2 (en) | 2001-08-16 | 2003-07-01 | Access Pharmaceuticals, Inc. | Mucoadhesive erodible drug delivery device for controlled administration of pharmaceuticals and other active compounds |
| WO2015101907A1 (en) | 2013-12-30 | 2015-07-09 | Uluru, Inc. | Controlling the erosion rates of mucoadhesive devices that deliver actives and other compounds and providing increased and variable therapeutic blood levels |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS4950127A (en) * | 1972-09-22 | 1974-05-15 | ||
| JPS54117552A (en) * | 1978-03-03 | 1979-09-12 | Dai Ichi Seiyaku Co Ltd | Preparation of hydrated compound of vinyl acetate resin and poultice composition containing it |
| JPS5562012A (en) * | 1978-11-06 | 1980-05-10 | Teijin Ltd | Slow-releasing preparation |
-
1983
- 1983-04-08 JP JP6095783A patent/JPS59186913A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS4950127A (en) * | 1972-09-22 | 1974-05-15 | ||
| JPS54117552A (en) * | 1978-03-03 | 1979-09-12 | Dai Ichi Seiyaku Co Ltd | Preparation of hydrated compound of vinyl acetate resin and poultice composition containing it |
| JPS5562012A (en) * | 1978-11-06 | 1980-05-10 | Teijin Ltd | Slow-releasing preparation |
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2571253A1 (en) * | 1984-10-04 | 1986-04-11 | Nippon Kayaku Kk | SHEET-FORM PREPARATION |
| EP0200508A2 (en) * | 1985-04-27 | 1986-11-05 | Nitto Denko Corporation | Adhesive oral bandages and oral pharmaceutical preparations |
| US4772470A (en) * | 1985-04-27 | 1988-09-20 | Nitto Electric Industrial Co., Ltd. | Oral bandage and oral preparations |
| EP0223524A2 (en) * | 1985-11-08 | 1987-05-27 | Nitto Denko Corporation | Use of adhesive dermal bandages and dermal percutaneous preparations |
| JPH02200624A (en) * | 1989-01-30 | 1990-08-08 | Nippon Kayaku Co Ltd | Dental dressing agent |
| JPH02202814A (en) * | 1989-01-31 | 1990-08-10 | Nitto Denko Corp | Plaster preparation for mucosa of oral cavity |
| US6585997B2 (en) | 2001-08-16 | 2003-07-01 | Access Pharmaceuticals, Inc. | Mucoadhesive erodible drug delivery device for controlled administration of pharmaceuticals and other active compounds |
| WO2015101907A1 (en) | 2013-12-30 | 2015-07-09 | Uluru, Inc. | Controlling the erosion rates of mucoadhesive devices that deliver actives and other compounds and providing increased and variable therapeutic blood levels |
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