JPS61186309A - Composition applicable to mucosa of oral cavity - Google Patents
Composition applicable to mucosa of oral cavityInfo
- Publication number
- JPS61186309A JPS61186309A JP2732185A JP2732185A JPS61186309A JP S61186309 A JPS61186309 A JP S61186309A JP 2732185 A JP2732185 A JP 2732185A JP 2732185 A JP2732185 A JP 2732185A JP S61186309 A JPS61186309 A JP S61186309A
- Authority
- JP
- Japan
- Prior art keywords
- layer
- elution
- enzyme
- prolonging
- plaque
- 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)
- Cosmetics (AREA)
Abstract
Description
【発明の詳細な説明】
(産業上の利用分野)
本発明は歯垢のせ解並びに生成付着を抑制する作用を有
する組成物に関し、さらに詳しくは1口腔内粘膜に容易
に、且つ長時間接着し、デキストラナーゼ、ムタナーゼ
等の歯垢分解酵素の唾液への溶出が長時間持続する為に
、う蝕、歯肉炎、歯槽膿漏などの口腔内疾病の予防が効
率的に行われる口腔粘膜適用組成物に関する。DETAILED DESCRIPTION OF THE INVENTION (Field of Industrial Application) The present invention relates to a composition that has the effect of suppressing the decomposition of dental plaque and the formation and adhesion of dental plaque. , dextranase, mutanase, and other plaque-degrading enzymes elute into saliva for a long time, so oral diseases such as caries, gingivitis, and alveolar pyorrhea can be effectively prevented by application to the oral mucosa. Regarding the composition.
(従来の技術)
従来、う蝕、歯肉炎、歯槽膿漏などの口腔内疾病を予防
する為の検討は、ガムや歯磨等に於てなされてきた。(Prior Art) Conventionally, studies have been made on gums, toothpastes, etc. to prevent oral diseases such as dental caries, gingivitis, and alveolar pyorrhea.
(発明が解決しようとする問題点) しかし、ガム、歯磨ともに効力持続時間が短く。(Problem that the invention attempts to solve) However, both gum and toothpaste have a short duration of effectiveness.
さらに歯磨に於いては他成分による有効成分の失活等の
問題があって配合に制約があるという欠点を有している
。Furthermore, in toothpaste, there are problems such as deactivation of the active ingredient by other ingredients, and there are restrictions on the formulation.
(問題点を解決する九めの手段)
本発明の目的は、従来う蝕、歯肉炎、歯槽膿漏などの口
腔内疾病を予防する為の製品にみられる上記の欠点に鑑
み5口腔内粘膜に接着し、飲食。(Ninth Means for Solving the Problems) In view of the above-mentioned drawbacks of conventional products for preventing oral diseases such as dental caries, gingivitis, and alveolar pyorrhea, the purpose of the present invention is to Glue to food and drink.
会話などの通常の行動に際してもはがれず、異物感はな
く、デギストラナーゼ、ムタナーゼ等の歯垢分解酵素の
唾液への溶出が長時間持続する新しいタイプの口腔粘膜
適用組成物を提供することにある。The object of the present invention is to provide a new type of oral mucosal composition that does not peel off during normal activities such as conversation, does not give a foreign body sensation, and maintains the elution of plaque-degrading enzymes such as degistranase and mutanase into saliva for a long time. .
本発明者等は、上記目的の製品を得る為に鋭意工夫した
結果、デキストラナーゼ、ムタナーゼ等の歯垢分解酵素
の溶出を中程度に遅延する層(1)と高度に遅延する層
(「)の2層から成る製品で。As a result of intensive efforts to obtain the desired product, the present inventors discovered a layer (1) that moderately retards the elution of plaque-degrading enzymes such as dextranase and mutanase, and a layer (1) that highly retards the elution of plaque-degrading enzymes such as dextranase and mutanase. ) is a product consisting of two layers.
その目的が達せられることを見出し友。A friend who found that that purpose could be achieved.
すなわち本発明は1層(I)および層(II)の少なく
とも2層からなり、該層(I)がポリビニルピロリドン
、ポリビニルアルコール、アルギン酸およびその薬学的
に許容される塩、無水マレイン酸とメチルビニルエーテ
ルの交互共重合体からなる群から選ばれた1種又は2種
以上のポリマー成分。That is, the present invention consists of at least two layers, one layer (I) and one layer (II), and the layer (I) is composed of polyvinylpyrrolidone, polyvinyl alcohol, alginic acid and its pharmaceutically acceptable salt, maleic anhydride and methyl vinyl ether. One or more polymer components selected from the group consisting of alternating copolymers of
歯垢分解酵素、賦形剤および必要によりその他の添加剤
を含み、かつ該ポリマー成分が該層(I)の全組成物に
対して20〜50重11%であり、該層(II)がポリ
ビニルピロリドン、ポリビニルアルコール、アルギン酸
およびその薬学的に許容される塩、無水マレイン酸とメ
チルビニルエーテルの交互共重合体からなる群から選ば
れ次1種又は2種以上のポリマー成分(A)とポリアク
リル酸およびその薬学的に許容される塩からなる群から
選ばれた1種又は2種以上のポリマー成分(B)、歯垢
分解酵素および必要により賦形剤、その他の添加剤を含
み、かつポリマー成分(A)とポリマー成分(B)の重
量比が70=30〜95:5であることを特徴とする口
腔粘膜適用組成物である。The layer (II) contains a plaque-degrading enzyme, an excipient, and other additives if necessary, and the polymer component is 20 to 50% by weight based on the total composition of the layer (I). One or more polymer components (A) selected from the group consisting of polyvinylpyrrolidone, polyvinyl alcohol, alginic acid and its pharmaceutically acceptable salts, alternating copolymers of maleic anhydride and methyl vinyl ether, and polyacrylic Contains one or more polymer components (B) selected from the group consisting of acids and pharmaceutically acceptable salts thereof, a plaque-degrading enzyme, and if necessary excipients and other additives, and the polymer component This is a composition for application to oral mucosa, characterized in that the weight ratio of component (A) to polymer component (B) is 70=30 to 95:5.
上記層(I)、(I[)に用いられるポリマー成分、ポ
リビニルピロリドン、ポリビニルアルコール。Polyvinyl pyrrolidone, polyvinyl alcohol used in the above layers (I) and (I[).
アルギン酸及びその薬学的に許容される塩、無水マレイ
ン酸とメチルビニルエーテルの交互共重合体はその物理
化学的性質に影響しない限り、他の1種以上のモノマー
との2元以上の共重合体、適当な架橋剤で架橋された架
橋ポリマーもこの中に含まれる。物理化学的性質に影響
しない為には。Alginic acid and its pharmaceutically acceptable salts, alternating copolymers of maleic anhydride and methyl vinyl ether are copolymers of two or more elements with one or more other monomers, as long as they do not affect their physicochemical properties; Also included are crosslinked polymers crosslinked with suitable crosslinking agents. In order not to affect the physicochemical properties.
他の七ツマ−の共重合割合が30モ/I/%以下である
ことが望ましい。こ\で薬学的に許容される塩とは、ナ
トリウム塩、カリウム塩等のアルカリ金属塩、カルシウ
ム塩等のアルカリ土類金属塩、アンモニウム塩などをい
う。It is desirable that the copolymerization ratio of other heptamers is 30 mo/I/% or less. The pharmaceutically acceptable salts herein include alkali metal salts such as sodium salts and potassium salts, alkaline earth metal salts such as calcium salts, ammonium salts, and the like.
層(I[)に用いられる他のポリマー成分、ポリアクI
))し酸およびその薬学的に許容される塩の場合も、そ
れぞれホモポリマー、他の1種以上のモノマーとの2元
以上の共重合体、適当な架橋剤で架橋された架橋ポリマ
ー等がこの中に含まれ、ホモポリマーの物理化学的性質
に影響しない為に、共重合体である場合には、他のモノ
マーが30モル多以下の範囲で共重合されていることが
好まれる。Other polymer components used in layer (I[), Polyac I
)) In the case of acid and its pharmaceutically acceptable salts, homopolymers, copolymers of two or more elements with one or more other monomers, crosslinked polymers crosslinked with a suitable crosslinking agent, etc. In the case of a copolymer, it is preferable that other monomers are copolymerized in an amount of 30 moles or less so that it is included in this and does not affect the physicochemical properties of the homopolymer.
好適な例としてカーボポール934■、カーポポ−1v
940■、カーボポー/L’941■等の市販品を使用
することができる。Suitable examples include Carbopol 934■ and Carpopol 1v.
Commercially available products such as 940■ and CABOPO/L'941■ can be used.
本発明で使用する歯垢分解酵素とは歯垢の分解並びに生
成付着を抑制する能力を有する酵素のことであシ1例え
ばデキストラナーゼ、ムタナーゼ等が挙げられる。歯垢
分解酵素は層(I)又は層(II)の全組成物1f当シ
200〜10万酵素単位配合するのが合理的である。The plaque-degrading enzyme used in the present invention refers to an enzyme that has the ability to decompose dental plaque and inhibit its formation and adhesion. Examples include dextranase, mutanase, and the like. It is reasonable to include 200 to 100,000 units of plaque-degrading enzyme per 1f of the total composition of layer (I) or layer (II).
本発明で使用する賦形剤としては、デンプン。The excipient used in the present invention is starch.
結晶セルロース、デキストリン、am、マンニド−〜、
ソルビトール、無水リン酸カルシウム等がある。Crystalline cellulose, dextrin, am, mannide,
Examples include sorbitol and anhydrous calcium phosphate.
本発明で提供される口腔粘膜適用組成物の製造は、ポリ
ビニルピロリドン、ポリビニルアルコール、アルギン酸
及びその薬学的に許容される塩。The oral mucosal application composition provided by the present invention is manufactured using polyvinylpyrrolidone, polyvinyl alcohol, alginic acid, and a pharmaceutically acceptable salt thereof.
無水マレイン酸とメチルビニルエーテルの交互共重合体
からなる群から選ばれた1種ま九は2種以上のポリマー
成分および歯垢分解酵素および賦形剤、更には必要に応
じ外観あるいは臭味を良くするため、滑沢剤、結合剤、
矯味矯臭剤1着色剤の1種または2種以上とを十分に混
合し、均一な混金物を形成せしめ、これ等の適当量をパ
ンチ、ダイスおよびプレスを用いて直接加圧成形する方
法。One or more selected from the group consisting of alternating copolymers of maleic anhydride and methyl vinyl ether may contain two or more polymer components, plaque-degrading enzymes, excipients, and, if necessary, to improve appearance or odor. For this purpose, lubricants, binders,
A method in which a flavoring agent and one or more coloring agents are sufficiently mixed to form a uniform mixture, and an appropriate amount of the mixture is directly pressure-molded using a punch, die, or press.
あるいは適当な造粒工程を経て加圧成形する方法によυ
層(1)を成形し比後、ポリビニルピロリドン、ポリビ
ニルアルコール、アルギン酸及びその薬学的に許容され
る塩、無水マレイン酸とメチルビニルエーテルの交互共
重合体から成る群から選ばれた1@または2種以上のポ
リマー成分(A)とポリアクリル酸およびその薬学的に
許容される塩から成る群から選ばれた1種ま友は2種以
上のポリマー成分(B)と歯垢分解酵素、更には必要に
応じ滑沢剤、結合剤、賦形剤、矯味矯臭剤1M色剤の1
種又は2種以上を均一に混合した混合物を層(1)の上
にのせ、更に印加することにより容易に製造することが
できる。Alternatively, υ can be formed by pressure molding through an appropriate granulation process.
After forming the layer (1), one or two selected from the group consisting of polyvinylpyrrolidone, polyvinyl alcohol, alginic acid and its pharmaceutically acceptable salts, and alternating copolymers of maleic anhydride and methyl vinyl ether are added. One type selected from the group consisting of the above polymer component (A), polyacrylic acid, and a pharmaceutically acceptable salt thereof is two or more types of polymer component (B) and a plaque-degrading enzyme, and furthermore, necessary Lubricants, binders, excipients, flavorings, 1M coloring agent, depending on the requirements
It can be easily produced by placing a species or a mixture of two or more species uniformly on the layer (1) and applying further application.
本発明で提供される口腔粘膜適用組成物製造の他の方法
として層(I)、(II)のそれぞれを構成する成分を
別々に適当な溶媒溶液とした後、流延し、転属工程を経
て薄膜上に成形し、適当な接着剤により貼シ合せるか、
水その他の溶媒で湿らせて圧着するか、熱を用いて圧着
するかのいずれかの方法で2層錠を得ることができる。Another method for producing the composition for oral mucosa provided by the present invention is to separately dissolve the components constituting each of layers (I) and (II) in a suitable solvent, and then cast the solution and undergo a transfer step. Form it on a thin film and paste it with a suitable adhesive, or
Bilayer tablets can be obtained either by moistening with water or other solvents and pressing, or by applying heat.
また必要に応じ用いられる滑沢剤としては1例えばタル
ク、ステア・リン酸およびその塩、ワックス類などが挙
げられ、結合剤としては1例えばデンプン、デキストリ
ン、トフガント、ゼラチン。Examples of lubricants that may be used as necessary include talc, stearic acid and its salts, and waxes, and examples of binders include starch, dextrin, tofugant, and gelatin.
ヒドロキシプロピルセルロース等が挙げられ、賦形剤と
してはデンプン、結晶セルロース、デキストリン、 乳
fasマンニトール、ソルビトール、無水リン酸カルシ
ウム等が挙げられ、矯味矯臭剤としては、クエン酸、ツ
マ−〃酸、酒石酸、メントール、カンキツ香料等が挙げ
られる。Examples of excipients include starch, crystalline cellulose, dextrin, milk fas mannitol, sorbitol, anhydrous calcium phosphate, etc., and flavoring agents include citric acid, tumatric acid, tartaric acid, and menthol. , citrus flavor, etc.
本発明では層(I)又は層(I[)に殺菌剤、抗菌剤。In the present invention, layer (I) or layer (I[) contains a bactericidal agent or an antibacterial agent.
防腐剤等が含まれていてもよい。Preservatives etc. may be included.
本発明の製品の適用は特に限定されるものでは無く、歯
茎、内側の頬の粘膜に層(I[)側を貼付して行われる
。本発明の製品の層(1)側も粘着性ポリマーの存在に
よフ粘膜に対する接着性を有するが、これを例えば歯茎
の外側に層(n)側を接着させて適用し友場合1層(I
)側が頬粘膜に接着することがあるが、これは何ら支障
にならない。Application of the product of the present invention is not particularly limited, and the layer (I[) side is applied to the gums and inner cheek mucosa. The layer (1) side of the product of the present invention also has adhesive properties to the mucous membrane due to the presence of the adhesive polymer, but if this is applied, for example, by adhering the layer (n) side to the outside of the gums, then one layer ( I
) side may adhere to the buccal mucosa, but this does not pose any problem.
層(I)はポリビニルピロリドン、ポリビニルアルコー
ル、アルギン酸及びその薬学的に許容される塩、無水マ
レイン酸とメチルビニルエーテルの交互共重合体から成
る群から選ばれた1種taは2種以上のポリマー成分、
歯垢分解酵素および賦形剤を必須の構成成分とするもの
であり、歯垢分解酵素の放出を中程度に遅延する作用は
上記ポリマー成分によりもたらされる。この層の中には
上記ポリマー成分と歯垢分解酵素と賦形剤の他、必要に
応じてその他の添加物を含ませることができるが、薬物
の溶出が適度に遅延される為には、上記ポリマー成分が
層(1)中、全組成物の20重量%〜50重量%である
ことが必要である。上記ポリマー成分が20重量%に満
たない場合には歯垢分解酵素の溶出が速すぎ溶出を高度
に遅延する層と組合せても溶出が長時間持続されず、ま
九50重量%を超えると溶出が遅れる為に溶出を中程度
遅延する層としての役割を果し得ない。Layer (I) is one selected from the group consisting of polyvinylpyrrolidone, polyvinyl alcohol, alginic acid and its pharmaceutically acceptable salts, and alternating copolymers of maleic anhydride and methyl vinyl ether. ta is two or more polymer components. ,
It contains a plaque-degrading enzyme and an excipient as essential components, and the effect of moderately delaying the release of the plaque-degrading enzyme is brought about by the polymer component. In addition to the above-mentioned polymer components, plaque-degrading enzymes, and excipients, this layer can contain other additives as necessary, but in order to appropriately delay the elution of the drug, It is necessary that the above polymer component constitutes 20% to 50% by weight of the total composition in layer (1). If the above polymer component is less than 20% by weight, the elution of the plaque-degrading enzyme is too fast and the elution cannot be sustained for a long time even when combined with a layer that highly retards elution. Because of this delay, it cannot serve as a layer that moderately delays elution.
一方1層(I[)はポリビニルピロリドン、ポリビニル
アルコ−1v%アルギン酸およびその薬学的に許容され
る塩から成る群から選ばれf:、1種または2種以上の
ポリマー成分(A)と、ポリアクリル酸およびその薬学
的に許容される塩から成る群から選ばれた1種ま次は2
種以上のポリマー成分(B)。On the other hand, the first layer (I[) is selected from the group consisting of polyvinylpyrrolidone, polyvinylalco-1v% alginic acid, and pharmaceutically acceptable salts thereof; one or two selected from the group consisting of acrylic acid and its pharmaceutically acceptable salts;
More than one polymer component (B).
歯垢分解酵素の三成分を必須の構成成分とするものであ
り、歯垢分解酵素を高度に放出遅延する作用は、上記ポ
リマー成分(A)とポリマー成分(B)の組合せにより
もたらされる。ポリマー成分(A)のみでは放出遅延作
用が十分でなく、(B)成分のみでは放出遅延作用は十
分示すが、膨潤性が強すぎる為に異物感が強い。この観
点からポリマー成分(A)とポリマー成分(B)の重量
比が70=30〜95:5であることが必要である。ま
九層(II)中には必要に応じて賦形剤、その他の添加
物を加えることができるが、その効果を十分に発揮させ
る為には(A) 、 (B) 、歯垢分解酵素以外の添
加物は層(I[)中食組成物の20重量%以下、特に1
0重量%以下であることが好ましい。を九層(If)は
粘着性を有する(A)、(B)両ポリマー成分の存在に
より口腔粘膜に対する強い接着性を有している。The three components of the plaque-degrading enzyme are essential components, and the effect of highly delaying the release of the plaque-degrading enzyme is brought about by the combination of the polymer component (A) and the polymer component (B). The polymer component (A) alone does not have a sufficient release retardation effect, and the (B) component alone exhibits a sufficient release retardation effect, but the swelling property is too strong, resulting in a strong foreign body sensation. From this point of view, it is necessary that the weight ratio of the polymer component (A) and the polymer component (B) is 70=30 to 95:5. Excipients and other additives can be added to the layer (II) as necessary, but in order to fully demonstrate their effects, (A), (B), and plaque-degrading enzymes are required. Additives other than 20% by weight or less of the food composition in layer (I[), especially 1
It is preferably 0% by weight or less. The nine-layer (If) has strong adhesion to the oral mucosa due to the presence of both the adhesive polymer components (A) and (B).
(発明の効果)
上述し友ように1本発明は歯垢分解酵素の放出を中程度
に遅延する層(I)および高度に遅延する層(I[)の
少なくとも2層から成る口腔粘膜適用組成物であって、
歯垢分解酵素の長時間に亘る放出を示し1口腔粘膜に容
易に接着し、飲食、会話などの通常の行動に際しても容
易にはがれず、全く異物感の無い新しいタイプの口腔粘
膜適用組成物である。(Effects of the Invention) As mentioned above, the present invention provides a composition for application to oral mucosa comprising at least two layers: a layer (I) that moderately retards the release of plaque-degrading enzymes and a layer (I[) that highly retards the release of plaque-degrading enzymes. It is a thing,
A new type of oral mucosal composition that exhibits long-term release of plaque-degrading enzymes, easily adheres to the oral mucosa, does not come off easily during normal activities such as eating, drinking, and talking, and does not give any foreign body sensation. It is.
本発明の製品の最大の特徴は、歯垢分解酵素の唾液への
溶出速度が長時間に亘シ持続することであり、歯垢分解
酵素によろう蝕、歯肉炎、歯槽膿漏などの口腔内疾病の
予防効率を大巾に改善できることが期待される点にある
。The greatest feature of the product of the present invention is that the rate of elution of plaque-degrading enzymes into saliva is sustained over a long period of time. It is expected that the prevention efficiency of internal diseases can be greatly improved.
本発明の製品の第2の特徴は1口腔内粘膜に容易に接着
し、その接着性が4〜24時間にも亘シ。The second feature of the product of the present invention is that it easily adheres to the oral mucosa and remains adhesive for 4 to 24 hours.
持続することである。しかもこの接着性は飲酒。It is about sustaining. Moreover, this adhesiveness is drunk.
喫煙、喫茶、喫食、会話などの日常の口腔内運動に何ら
影響されることが無い。It is not affected by daily oral movements such as smoking, drinking coffee, eating, and talking.
本発明の製品の1g3の特徴は、成形品が口中で唾液に
より膨潤し、極めて柔軟になる為に異物感がほとんど無
いことである。The feature of 1g3 of the product of the present invention is that the molded product swells with saliva in the mouth and becomes extremely soft, so there is almost no foreign body sensation.
本発明の製品の第4の特徴は、歯垢分解酵素の溶出を中
程度に遅延する!fj (I)及び/ま九は高度に遅延
する層(π)中の組成を変えることにより。The fourth feature of the product of the invention is that it moderately retards the elution of plaque-degrading enzymes! fj (I) and /m by changing the composition in the highly retarded layer (π).
接着性、持続性の調節を任意に行えること、及び層(I
)と層(II)の量比を調節することにより歯垢分解酵
素の作用に応じ次最適の溶出性能を任意に得ることがで
きる点にある。Adhesion and durability can be adjusted arbitrarily, and the layer (I
) and layer (II), it is possible to arbitrarily obtain the next optimum elution performance depending on the action of the plaque-degrading enzyme.
(実施例)
以下、実施例により本発明を詳述するが1本発明はこれ
らにより限定されるものでは無い。実施例中、単に部あ
るいはチとあるのは重量部あるいは重量%を示す。(Examples) Hereinafter, the present invention will be explained in detail with reference to Examples, but the present invention is not limited thereto. In the examples, parts or q indicate parts by weight or % by weight.
試験方法1.歯垢分解酵素の溶出試験
実施例1に示す方法と同様に調製したトラックフィール
ド型錠剤の第π層側を水で微かに濡したのち100g/
のビーカーの底より3cf11の壁面に錠剤の中心が位
置するように押し付けて、短径が水面に平行になる様に
固定する。次いで、40℃の0.2M酢酸緩衝液(pH
5,5) 100震lをビーカーに入れ、攪拌を開始す
る。攪拌速度100 rpmとし40℃に試験液を保ち
ながら適時1回3 mlずつサンプリングを行い、サン
プリングの都度、同量の0.2M酢酸緩衝液(pH5,
5)を補充し、内容液は常時100g/を保つ。採取サ
ンプルはメンブランフィルタ−(孔径5μ)で濾過した
後、F液1 mlを検液とした。Test method 1. Elution test of dental plaque degrading enzyme After slightly wetting the π-layer side of a Trackfield-type tablet prepared in the same manner as shown in Example 1 with water, 100 g/
Press the tablet from the bottom of the beaker so that the center of the tablet is located on the wall of 3cf11, and fix it so that the short axis is parallel to the water surface. Then, 0.2M acetate buffer (pH
5,5) Pour 100 liters into a beaker and start stirring. While keeping the test solution at 40°C with a stirring speed of 100 rpm, sample 3 ml at a time, and for each sampling, add the same amount of 0.2 M acetate buffer (pH 5,
5) and keep the content at 100 g/l at all times. The collected sample was filtered with a membrane filter (pore size: 5 μm), and 1 ml of solution F was used as a test solution.
デキストラナーゼの場合はデキストランを、ムタナーゼ
の場合は、ムタンの懸濁液に高単位のデキストラン分解
酵素(市販品)を加え、400でムタン中のα−1,6
−グルコシド結合を切断させたムタンを0.2 M酢酸
緩衝液に0.5チになるよう溶解または懸濁させ友。In the case of dextranase, add dextran, and in the case of mutanase, add a high unit of dextran degrading enzyme (commercial product) to the suspension of mutan, and at 400% α-1,6 in mutan.
- Dissolve or suspend mutan whose glucoside bond has been cleaved in a 0.2 M acetate buffer to a concentration of 0.5%.
この液1 mlと検液を400で10分間反応させた後
、遊離し次還元糖をソモギー・ネルラン法で定量し理論
値を100%として溶出率を求めた。After reacting 1 ml of this solution with the test solution at 400° C. for 10 minutes, the released subreducing sugar was quantified by the Somogyi-Nerlan method and the elution rate was determined with the theoretical value as 100%.
実施例1゜
(I)層
ポリビニルピロリドン(分子量4万) 28.6
5%d−マンニドー/L’
66.85チデキストヲナーゼ(50万単位/P)
3%バニラパウダー
1%ステアリン酸マグネシウム
0.5%食用赤色3号
0.002%上記組成を均一に混合した後、打
錠し、(1)層を形成し友。Example 1゜(I) layer polyvinylpyrrolidone (molecular weight 40,000) 28.6
5% d-mannido/L'
66.85 Tidextowonase (500,000 units/P)
3% vanilla powder
1% Magnesium Stearate
0.5% food red No. 3
0.002% After uniformly mixing the above composition, it was compressed to form (1) a layer.
(I[)層
ポリアクリル酸 6.6
9%ポリビニルピロリドン(分子量36万) 88
.8:2%デキストラナーゼ(50万単位/P)
3%バニラパウダー
1%ステアリン酸マグネシウム
0.5%上記(I[)層組成を均一に混合した後、上
記(I)層の上に載せ、打錠して重量70■、厚さ1.
75鱈、長径B、Bar、短径4.4Hのトラックフィ
ールド型の2層錠を得た。(I[) layer polyacrylic acid 6.6
9% polyvinylpyrrolidone (molecular weight 360,000) 88
.. 8: 2% dextranase (500,000 units/P)
3% vanilla powder
1% Magnesium Stearate
0.5% After uniformly mixing the above (I[) layer composition, it was placed on the above (I) layer and compressed into tablets with a weight of 70 cm and a thickness of 1.5%.
A track field type two-layer tablet with a length of 75 cod, a major axis of B, a bar, and a minor axis of 4.4H was obtained.
得られ次製品を用い試験方法1に従って溶出試験を行つ
友。その結果を第1図に示す。Perform a dissolution test using the obtained product according to Test Method 1. The results are shown in FIG.
実施例2゜
(I)層
ポリビニルピロリドン(分子量4万) 29.2
5%d−マンニトール 68.
25%ムタナーゼ(10万単泣/2)
1チパニラパウダー
1%ステアリン酸マグネシウム 0
.5%食用赤色3号 0.
02%(II)層
ポリアクリル酸 6.
83%ポリビニルピロリドン(分子量36万) 9
0.68%ムタナーゼ(10万単位/2)
1チバニラパウダー
1%ステアリン酸マグネシウム
0.5%実施例1と同様の2層錠を得た。Example 2゜(I) layer polyvinylpyrrolidone (molecular weight 40,000) 29.2
5% d-mannitol 68.
25% mutanase (100,000 single tears/2)
1 Chipanilla powder
1% Magnesium Stearate 0
.. 5% food red No. 3 0.
02% (II) layer polyacrylic acid 6.
83% polyvinylpyrrolidone (molecular weight 360,000) 9
0.68% mutanase (100,000 units/2)
1 vanilla powder
1% Magnesium Stearate
A two-layer tablet similar to 0.5% Example 1 was obtained.
得られた製品を用い試験方法1に従って溶出試験を行っ
た。その結果を第2図に示す。A dissolution test was conducted using the obtained product according to Test Method 1. The results are shown in FIG.
比較例1. 本発明の(I)層のみょシ成る単層錠ポリ
ビニルピロリドン(分子量4万) 29%d
−マンニトール 68.5チ
バニラパウダー 1チ
ステアリン酸マグネシウム 00
5%デキストラナーゼ(100万単m/P)
1%上記組成を均一に混合した後、打錠し重量70キ
、厚さ1.751+1、長径8.8ff、短径4.4M
のトラックフィールド型の単層錠を得た。Comparative example 1. Monolayer tablet consisting of layer (I) of the present invention polyvinylpyrrolidone (molecular weight 40,000) 29%d
- Mannitol 68.5 Ti Vanilla Powder 1 Ti Magnesium Stearate 00
5% dextranase (1 million unit m/P)
1% After uniformly mixing the above composition, it was compressed into tablets, weight 70kg, thickness 1.751+1, major axis 8.8ff, minor axis 4.4M.
A truck field type single layer tablet was obtained.
得られた製品を用い試験方法1に準じて溶出試験を行っ
た。その結果を第1図に示す。A dissolution test was conducted using the obtained product according to Test Method 1. The results are shown in FIG.
実施例3゜
実施例1.2の2層錠製剤を1種につき2人づつの被検
者に対し異物感及び接着性の評価を行ったが、いずれも
8時間以上の接着性を示し、異物感を訴える被検者はな
かった。Example 3 The two-layer tablet formulation of Example 1.2 was evaluated for foreign body sensation and adhesiveness on two subjects per type, and both showed adhesiveness for 8 hours or more. None of the subjects complained of foreign body sensation.
第1図はデキストラナーゼを含有する実施例1および比
較例1の製品の溶出試験結果を示す。
第1図において−づつ−は実施例1.一番−は比較例1
を示す。
第2図はムタナーゼを含有する実施例2の製品の溶出試
験結果を示す。
第1 日
B’r P? (hrs、)
第2@
1間(hrs)FIG. 1 shows the elution test results of the products of Example 1 and Comparative Example 1 containing dextranase. In FIG. 1, - by - indicates Example 1. The first one is Comparative Example 1
shows. Figure 2 shows the elution test results for the product of Example 2 containing mutanase. 1st day B'rP? (hrs,) 2nd @ 1 interval (hrs)
Claims (1)
該層( I )がポリビニルピロリドン、ポリビニルアル
コール、アルギン酸およびその薬学的に許容される塩、
無水マレイン酸とメチルビニルエーテルの交互共重合体
からなる群から選ばれた1種又は2種以上のポリマー成
分、歯垢分解酵素、賦形剤および必要によりその他の添
加剤を含み、かつ該ポリマー成分が該層( I )の全組
成物に対して20〜50重量%であり、該層(II)がポ
リビニルピロリドン、ポリビニルアルコール、アルギン
酸およびその薬学的に許容される塩、無水マレイン酸と
メチルビニルエーテルの交互共重合体からなる群から選
ばれた1種又は2種以上のポリマー成分(A)とポリア
クリル酸およびその薬学的に許容される塩からなる群か
ら選ばれた1種又は2種以上のポリマー成分(B)、歯
垢分解酵素および必要により賦形剤、その他の添加剤を
含み、かつポリマー成分(A)とポリマー成分(B)の
重量比が70:30〜95:5であることを特徴とする
口腔粘膜適用組成物。Consisting of at least two layers, layer (I) and layer (II),
The layer (I) is polyvinylpyrrolidone, polyvinyl alcohol, alginic acid and a pharmaceutically acceptable salt thereof,
Contains one or more polymer components selected from the group consisting of alternating copolymers of maleic anhydride and methyl vinyl ether, a plaque-degrading enzyme, an excipient, and other additives if necessary, and the polymer component is 20 to 50% by weight based on the total composition of the layer (I), and the layer (II) contains polyvinylpyrrolidone, polyvinyl alcohol, alginic acid and its pharmaceutically acceptable salts, maleic anhydride and methyl vinyl ether. One or more polymer components selected from the group consisting of alternating copolymers of (A) and one or more polymer components selected from the group consisting of polyacrylic acid and pharmaceutically acceptable salts thereof. contains polymer component (B), plaque-degrading enzyme, and if necessary, excipients and other additives, and the weight ratio of polymer component (A) and polymer component (B) is 70:30 to 95:5. A composition for application to oral mucosa.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2732185A JPS61186309A (en) | 1985-02-13 | 1985-02-13 | Composition applicable to mucosa of oral cavity |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2732185A JPS61186309A (en) | 1985-02-13 | 1985-02-13 | Composition applicable to mucosa of oral cavity |
Publications (1)
Publication Number | Publication Date |
---|---|
JPS61186309A true JPS61186309A (en) | 1986-08-20 |
Family
ID=12217808
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2732185A Pending JPS61186309A (en) | 1985-02-13 | 1985-02-13 | Composition applicable to mucosa of oral cavity |
Country Status (1)
Country | Link |
---|---|
JP (1) | JPS61186309A (en) |
Cited By (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7122615B1 (en) * | 1998-09-10 | 2006-10-17 | Rutgers, The State University Of New Jersey | Polyanhydrides with therapeutically useful degradation products |
JP2010537008A (en) * | 2007-08-27 | 2010-12-02 | ユニヴァーシティー オブ トロント | Ultra-macropolymer composites that provide controlled nitric oxide release to heal wounds |
US8088405B2 (en) | 1999-12-07 | 2012-01-03 | Rutgers, The State University of New Jersery | Therapeutic compositions and methods |
US9782432B2 (en) | 2012-10-25 | 2017-10-10 | Rutgers, The State University Of New Jersey | Polymers and methods thereof for wound healing |
US9862672B2 (en) | 2013-05-29 | 2018-01-09 | Rutgers, The State University Of New Jersey | Antioxidant-based poly(anhydride-esters) |
US10023521B2 (en) | 2014-06-13 | 2018-07-17 | Rutgers, The State University Of New Jersey | Process and intermediates for preparing poly(anhydride-esters) |
US10092578B2 (en) | 2006-09-13 | 2018-10-09 | Polymerix Corporation | Active agents and their oligomers and polymers |
US10543162B2 (en) | 2015-04-10 | 2020-01-28 | Rutgers, The State University Of New Jersey | Kojic acid polymers |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS5625211A (en) * | 1979-08-08 | 1981-03-11 | Minolta Camera Co Ltd | Magnetic recording system |
JPS6347687A (en) * | 1986-08-14 | 1988-02-29 | Hitachi Medical Corp | Single photon emission ct |
-
1985
- 1985-02-13 JP JP2732185A patent/JPS61186309A/en active Pending
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS5625211A (en) * | 1979-08-08 | 1981-03-11 | Minolta Camera Co Ltd | Magnetic recording system |
JPS6347687A (en) * | 1986-08-14 | 1988-02-29 | Hitachi Medical Corp | Single photon emission ct |
Cited By (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7534852B2 (en) * | 1997-09-10 | 2009-05-19 | Rutgers, The State University Of New Jersey | Polyanhydrides with therapeutically useful degradation products |
US8017714B2 (en) | 1997-09-10 | 2011-09-13 | Rutgers, The State University Of New Jersey | Polyanhydrides with therapeutically useful degradation products |
US7122615B1 (en) * | 1998-09-10 | 2006-10-17 | Rutgers, The State University Of New Jersey | Polyanhydrides with therapeutically useful degradation products |
US8088405B2 (en) | 1999-12-07 | 2012-01-03 | Rutgers, The State University of New Jersery | Therapeutic compositions and methods |
US10092578B2 (en) | 2006-09-13 | 2018-10-09 | Polymerix Corporation | Active agents and their oligomers and polymers |
JP2010537008A (en) * | 2007-08-27 | 2010-12-02 | ユニヴァーシティー オブ トロント | Ultra-macropolymer composites that provide controlled nitric oxide release to heal wounds |
US9782432B2 (en) | 2012-10-25 | 2017-10-10 | Rutgers, The State University Of New Jersey | Polymers and methods thereof for wound healing |
US9862672B2 (en) | 2013-05-29 | 2018-01-09 | Rutgers, The State University Of New Jersey | Antioxidant-based poly(anhydride-esters) |
US10023521B2 (en) | 2014-06-13 | 2018-07-17 | Rutgers, The State University Of New Jersey | Process and intermediates for preparing poly(anhydride-esters) |
US10543162B2 (en) | 2015-04-10 | 2020-01-28 | Rutgers, The State University Of New Jersey | Kojic acid polymers |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
US4597959A (en) | Sustained release breath freshener, mouth and palate coolant wafer composition and method of use | |
US5780046A (en) | Oral formulations of S(+)-ibuprofen | |
Rassing | Chewing gum as a drug delivery system | |
AU2006322282B2 (en) | Foam wafer containing a polyvinyl alcohol-polyethyleneglycol-graft copolymer | |
CA2274910A1 (en) | Flat medicament preparation for the application and release of buprenorphine or a pharmacologically comparable substance in the buccal cavity, and method of producing the same | |
US4715369A (en) | Method of treating an injured part on the oral mucosa and the covering material for use thereof | |
JPS63161953A (en) | Denture stabilizer composition | |
AU711853B2 (en) | Oral formulations of S(+)-etodolac | |
US20070293587A1 (en) | Combating sinus, throat, and blood infections with xylitol delivered in the mouth | |
JP2007519745A (en) | Rapidly dissolving film for active substance delivery | |
WO2005039499A3 (en) | Rapidly disintegrating film | |
JPH07101856A (en) | Solid tablet form product to reduce oral cavity exrosis symptom | |
JPH01501472A (en) | Composition for prolonging the action of antiplaque agents | |
US20210259952A1 (en) | Oral compositions and mucoadhesive thin films formed therefrom | |
JPS61186309A (en) | Composition applicable to mucosa of oral cavity | |
WO2004047661A2 (en) | Appetite suppressant toothpaste | |
HU208488B (en) | Process for producing sucralfat-containing chewing tablet | |
JP2022132446A (en) | Methods and compositions for soft anticholinergic esters | |
JP2000063268A (en) | Oral mucosa adhesion-type controlled release troche and periodontal disease therapeutic agent | |
JP2000178185A (en) | Oral mucous membrane-adhering type sustained release tablet | |
JPH0513131B2 (en) | ||
JP2001163768A (en) | Slow-releasing stick-form preparation to be inserted between teeth | |
US20070248655A1 (en) | Lenticular shaped protective mouth sore discs | |
US20070248654A1 (en) | Protective mouth sore discs made with corn starch | |
JPS6115829A (en) | Sustained release nifedipine pharmaceutical for application to oral mucosa |