JPH01226823A - Oral mucosa plaster containing 'shikon' - Google Patents
Oral mucosa plaster containing 'shikon'Info
- Publication number
- JPH01226823A JPH01226823A JP63057052A JP5705288A JPH01226823A JP H01226823 A JPH01226823 A JP H01226823A JP 63057052 A JP63057052 A JP 63057052A JP 5705288 A JP5705288 A JP 5705288A JP H01226823 A JPH01226823 A JP H01226823A
- Authority
- JP
- Japan
- Prior art keywords
- adhesive layer
- shikon
- water
- extract
- tacky
- 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
- 210000002200 mouth mucosa Anatomy 0.000 title abstract description 9
- 239000011505 plaster Substances 0.000 title abstract 2
- 239000012790 adhesive layer Substances 0.000 claims abstract description 24
- 239000010410 layer Substances 0.000 claims abstract description 23
- 239000001856 Ethyl cellulose Substances 0.000 claims abstract description 12
- 229920002125 Sokalan® Polymers 0.000 claims abstract description 12
- 229920001249 ethyl cellulose Polymers 0.000 claims abstract description 12
- 235000019325 ethyl cellulose Nutrition 0.000 claims abstract description 12
- 239000004584 polyacrylic acid Substances 0.000 claims abstract description 12
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims abstract description 11
- 229920002678 cellulose Polymers 0.000 claims abstract description 8
- 239000001913 cellulose Substances 0.000 claims abstract description 8
- 229920000639 hydroxypropylmethylcellulose acetate succinate Polymers 0.000 claims abstract description 8
- 150000005215 alkyl ethers Chemical class 0.000 claims abstract description 6
- 150000003839 salts Chemical class 0.000 claims abstract description 6
- 239000000126 substance Substances 0.000 claims abstract description 6
- 239000000853 adhesive Substances 0.000 claims description 9
- 230000001070 adhesive effect Effects 0.000 claims description 9
- 239000004480 active ingredient Substances 0.000 claims description 3
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 3
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 3
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 3
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 3
- 239000003814 drug Substances 0.000 abstract description 6
- 229940079593 drug Drugs 0.000 abstract description 6
- 210000000214 mouth Anatomy 0.000 abstract description 6
- 230000003110 anti-inflammatory effect Effects 0.000 abstract description 4
- 239000004014 plasticizer Substances 0.000 abstract description 3
- 239000000758 substrate Substances 0.000 abstract 3
- 241001071917 Lithospermum Species 0.000 abstract 1
- 230000001747 exhibiting effect Effects 0.000 abstract 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 14
- 229920001296 polysiloxane Polymers 0.000 description 6
- -1 alkali metal salts Chemical class 0.000 description 5
- 230000000052 comparative effect Effects 0.000 description 4
- 238000002474 experimental method Methods 0.000 description 4
- 238000012360 testing method Methods 0.000 description 4
- 239000002202 Polyethylene glycol Substances 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- DOOTYTYQINUNNV-UHFFFAOYSA-N Triethyl citrate Chemical compound CCOC(=O)CC(O)(C(=O)OCC)CC(=O)OCC DOOTYTYQINUNNV-UHFFFAOYSA-N 0.000 description 3
- 210000004400 mucous membrane Anatomy 0.000 description 3
- 239000002674 ointment Substances 0.000 description 3
- 229920001223 polyethylene glycol Polymers 0.000 description 3
- 238000004080 punching Methods 0.000 description 3
- 239000001069 triethyl citrate Substances 0.000 description 3
- VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 description 3
- 235000013769 triethyl citrate Nutrition 0.000 description 3
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerol Natural products OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- 235000014113 dietary fatty acids Nutrition 0.000 description 2
- 239000000194 fatty acid Substances 0.000 description 2
- 229930195729 fatty acid Natural products 0.000 description 2
- 239000000796 flavoring agent Substances 0.000 description 2
- 235000013355 food flavoring agent Nutrition 0.000 description 2
- 235000011187 glycerol Nutrition 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- URAYPUMNDPQOKB-UHFFFAOYSA-N triacetin Chemical compound CC(=O)OCC(OC(C)=O)COC(C)=O URAYPUMNDPQOKB-UHFFFAOYSA-N 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- DEXFNLNNUZKHNO-UHFFFAOYSA-N 6-[3-[4-[2-(2,3-dihydro-1H-inden-2-ylamino)pyrimidin-5-yl]piperidin-1-yl]-3-oxopropyl]-3H-1,3-benzoxazol-2-one Chemical compound C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)C1CCN(CC1)C(CCC1=CC2=C(NC(O2)=O)C=C1)=O DEXFNLNNUZKHNO-UHFFFAOYSA-N 0.000 description 1
- 206010002091 Anaesthesia Diseases 0.000 description 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
- 241000699800 Cricetinae Species 0.000 description 1
- IMROMDMJAWUWLK-UHFFFAOYSA-N Ethenol Chemical compound OC=C IMROMDMJAWUWLK-UHFFFAOYSA-N 0.000 description 1
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 description 1
- 239000004354 Hydroxyethyl cellulose Substances 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- 208000025157 Oral disease Diseases 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 0.000 description 1
- 229920001800 Shellac Polymers 0.000 description 1
- DHKHKXVYLBGOIT-UHFFFAOYSA-N acetaldehyde Diethyl Acetal Natural products CCOC(C)OCC DHKHKXVYLBGOIT-UHFFFAOYSA-N 0.000 description 1
- 150000001241 acetals Chemical class 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 229910052783 alkali metal Inorganic materials 0.000 description 1
- 229920003144 amino alkyl methacrylate copolymer Polymers 0.000 description 1
- 150000003863 ammonium salts Chemical class 0.000 description 1
- 230000037005 anaesthesia Effects 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 239000004359 castor oil Substances 0.000 description 1
- 235000019438 castor oil Nutrition 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- CRVGKGJPQYZRPT-UHFFFAOYSA-N diethylamino acetate Chemical compound CCN(CC)OC(C)=O CRVGKGJPQYZRPT-UHFFFAOYSA-N 0.000 description 1
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 1
- 239000001087 glyceryl triacetate Substances 0.000 description 1
- 235000013773 glyceryl triacetate Nutrition 0.000 description 1
- 241000411851 herbal medicine Species 0.000 description 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 229920003132 hydroxypropyl methylcellulose phthalate Polymers 0.000 description 1
- 229940031704 hydroxypropyl methylcellulose phthalate Drugs 0.000 description 1
- 238000004898 kneading Methods 0.000 description 1
- 230000005923 long-lasting effect Effects 0.000 description 1
- 230000007721 medicinal effect Effects 0.000 description 1
- 229920003145 methacrylic acid copolymer Polymers 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 230000000877 morphologic effect Effects 0.000 description 1
- 208000030194 mouth disease Diseases 0.000 description 1
- 210000004877 mucosa Anatomy 0.000 description 1
- 201000001245 periodontitis Diseases 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000008055 phosphate buffer solution Substances 0.000 description 1
- XNGIFLGASWRNHJ-UHFFFAOYSA-N phthalic acid Chemical class OC(=O)C1=CC=CC=C1C(O)=O XNGIFLGASWRNHJ-UHFFFAOYSA-N 0.000 description 1
- 229920000728 polyester Polymers 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 159000000001 potassium salts Chemical class 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 210000003296 saliva Anatomy 0.000 description 1
- 239000004208 shellac Substances 0.000 description 1
- ZLGIYFNHBLSMPS-ATJNOEHPSA-N shellac Chemical compound OCCCCCC(O)C(O)CCCCCCCC(O)=O.C1C23[C@H](C(O)=O)CCC2[C@](C)(CO)[C@@H]1C(C(O)=O)=C[C@@H]3O ZLGIYFNHBLSMPS-ATJNOEHPSA-N 0.000 description 1
- 229940113147 shellac Drugs 0.000 description 1
- 235000013874 shellac Nutrition 0.000 description 1
- 208000017520 skin disease Diseases 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 239000004071 soot Substances 0.000 description 1
- 208000003265 stomatitis Diseases 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 208000004371 toothache Diseases 0.000 description 1
- 238000011200 topical administration Methods 0.000 description 1
- 229960002622 triacetin Drugs 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
Abstract
Description
【発明の詳細な説明】
産業上の利用分野
本発明はシコン含有口腔粘膜貼付剤、更に詳しくは、シ
コン含有粘着層および口腔粘膜に対して非粘着性の支持
体層から成り、口腔内の患部に貼付して抗炎症作用を長
時間にわたって発揮しうる口腔内製剤に関する。DETAILED DESCRIPTION OF THE INVENTION Field of Industrial Application The present invention is directed to an oral mucosal patch containing Sicon, more specifically, it comprises an adhesive layer containing Sicon and a support layer that is non-adhesive to the oral mucosa, and is applied to the affected area in the oral cavity. The present invention relates to an oral preparation that can be applied to the body and exert anti-inflammatory effects for a long period of time.
従来技術と発明の解決すべき課題
シコン（紫根）は古来より漢方薬として知られており、
たとえばムラサキ科植物の乾燥した根のエキスから軟膏
の「紫雲膏」が作られ、皮膚病。Prior art and problems to be solved by the invention Shikon (purple root) has been known as a Chinese herbal medicine since ancient times.
For example, an ointment called ``Shiun-yang'' is made from the extract of the dried roots of plants in the family Murasakiceae, and is used to treat skin diseases.
外傷などの妙薬として多用されている。It is often used as an elixir for injuries.
ところで、口腔内疾患、たとえば歯槽膿漏、口内炎、歯
痛に対する治療法として、各種の生理活性成分を含有し
た軟膏や液剤などの局所投与が行われているが、この方
法では、投与後項時間で唾液等に溶解して飲み下されて
しまい、患部に薬物を長時間滞めてお（ことが困難で、
薬効の持続時間を長く保てないという欠点がある。Incidentally, as a treatment for oral diseases such as alveolar pyorrhea, stomatitis, and toothache, topical administration of ointments and liquids containing various physiologically active ingredients is performed. It is difficult to keep the drug in the affected area for a long time because it dissolves in saliva and is swallowed.
The drawback is that the medicinal effect cannot be maintained for a long time.
本発明者らは、優れた抗炎症活性を持つシコンを用い、
優れた形態安定性を有し粘膜への製着性、柔軟性、薬効
持続性に優れる新規な口腔粘膜貼付剤を提供するため鋭
意研究を進めたところ、特定成分の粘着層および非粘着
支持体層から成る製剤において、その粘着層にシコンエ
キスを含有すれば、所期目的の口腔内貼付剤が得られる
ことを見出し、本発明を完成させるに至った。The present inventors used Shikone, which has excellent anti-inflammatory activity, to
In order to provide a new oral mucosal patch with excellent morphological stability, adhesion to mucous membranes, flexibility, and long-lasting medicinal efficacy, we conducted intensive research and found that an adhesive layer of specific ingredients and a non-adhesive support were developed. The present inventors have discovered that, in a preparation consisting of layers, if the adhesive layer contains Sicon extract, an intraoral patch for the intended purpose can be obtained, and the present invention has been completed.
すなわち、本発明は、セルロース低級アルキルエーテル
類とポリアクリル酸もしくはその医薬的に許容しうる塩
からなる粘Ｓ層、および水不溶性または水膨潤性高分子
物質からなる非粘着支持体層から成り、上記粘着層に生
理活性成分としてシコンエキスを含有したことを特徴と
するシコン含有口腔粘膜貼付剤を提供するものである。That is, the present invention consists of a viscous S layer made of cellulose lower alkyl ethers and polyacrylic acid or a pharmaceutically acceptable salt thereof, and a non-adhesive support layer made of a water-insoluble or water-swellable polymeric substance, The present invention provides an oral mucosa patch containing Shikon, characterized in that the adhesive layer contains Shikon extract as a physiologically active ingredient.
本発明における粘着層は、口腔粘膜に付着ｄ■能なフィ
ルム状のシコン含有層であって、患部に薬物を付与する
。ここで用いるセルロース低ｉフルキルエーテル頑とし
ては、たとえばメチルセルロース、エチルセルロース、
ヒドロキシエチルセルロース、ヒドロキシプロピルセル
ロース、ヒドロキシプロピルメチルセルロース、ヒドロ
キシプロピルメチルセルロースアセテートサクシネート
などが挙げられ、これらの少な（とも１種を使用に供ス
ル（特に、エチルセルロース、ヒドロキシプロピルメチ
ルセルロース、ヒドロキシプロピルメチルセルロースア
セテートサクシネートが好ましい）。またポリアクリル
酸の医薬的に許容しうる塩としては、ナトリウム塩、カ
リウム塩などのアルカリ金属塩やアンモニウム塩が挙げ
られる。The adhesive layer in the present invention is a film-like silicone-containing layer capable of adhering to the oral mucosa, and applies the drug to the affected area. Examples of the cellulose low i furkyl ether used here include methyl cellulose, ethyl cellulose,
Hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, hydroxypropylmethylcellulose acetate succinate, etc. (preferred). Pharmaceutically acceptable salts of polyacrylic acid include alkali metal salts such as sodium salts and potassium salts, and ammonium salts.
かかる粘着層は乾煤重置中、一般に口腔粘膜に対する付
着力やフィルム強度もしくは柔軟度等を考慮シて、セル
ロース低級アルキルエーテル＠５〜７０％（重量％、以
下同様）（好ましくは１０〜６０％）とポリアクリル酸
もしくはその医薬的に許容しうる塩１０〜９０％（好ま
しくは２０〜８５％）、これに５〜３０％の可塑剤（フ
タル酸エステル類、トリアセチン、プロピレングリコー
ル、ポリエチレングリコール、クエン酸トリエチルなど
）および０．５〜１０％のシコンエキスを含有する。こ
れ以外に、通常の賦形剤、着色剤、矯味剤、矯臭剤等が
適量配合されていてもよい。Such an adhesive layer is generally made of cellulose lower alkyl ether @ 5 to 70% (wt%, the same applies hereinafter) (preferably 10 to 60% by weight) during dry soot overlaying, taking into account the adhesion to the oral mucosa, film strength, flexibility, etc. %) and polyacrylic acid or a pharmaceutically acceptable salt thereof, 10-90% (preferably 20-85%), plus 5-30% of a plasticizer (phthalate esters, triacetin, propylene glycol, polyethylene glycol). , triethyl citrate, etc.) and 0.5-10% Sicon extract. In addition to these, appropriate amounts of ordinary excipients, coloring agents, flavoring agents, and flavoring agents may be added.
なお、かかる粘着層にあって、ポリアクリル酸とたとえ
ばアミノアルキルメタクリレートやポリ。In addition, in such an adhesive layer, polyacrylic acid and, for example, aminoalkyl methacrylate or polyester may be used.
ビニルアルコールなどの水溶性高分子物質との組合せで
は付着性（貼付性）に劣ることが認められる（後記比較
例１．２参照）。It is recognized that adhesion (stickability) is poor when used in combination with a water-soluble polymeric substance such as vinyl alcohol (see Comparative Example 1.2 below).
本発明における非粘着支持体層は、柔軟なフィルム状の
層であって、柔軟性および薬効持続性を付与する。主成
分である水不溶性または水膨潤性高分子物質としては、
たとえばセルロース低級アルキルエーテル類（エチルセ
ルロース、ヒドロキシプロピルメチルセルロースアセテ
ートサクシネート、ヒドロキシプロピルメチルセルロー
スフタレート、カルボキシメチルセルロース、カルボキ
シメチルエチルセルロースなど）、シェラツク、ポリビ
ニルアセタール、ジエチルアミノアセテート、メタクリ
ル酸コポリマーが挙げられ、これらの少な（とも１種を
使用に供する（特に、エチルセルロース、ヒドロキシプ
ロピルメチルセルロースアセテートサクシネートが好ま
しい）。これ以外にも、上記粘着層で例示した可塑剤や
他の配合成分を適量使用してもよい。The non-adhesive support layer in the present invention is a flexible film-like layer that provides flexibility and durability of drug efficacy. The water-insoluble or water-swellable polymeric substances that are the main components are:
Examples include cellulose lower alkyl ethers (ethyl cellulose, hydroxypropyl methylcellulose acetate succinate, hydroxypropyl methyl cellulose phthalate, carboxymethyl cellulose, carboxymethyl ethyl cellulose, etc.), shellac, polyvinyl acetal, diethylamino acetate, and methacrylic acid copolymers; One kind is used (Ethyl cellulose and hydroxypropyl methyl cellulose acetate succinate are particularly preferred).In addition to these, appropriate amounts of the plasticizers and other ingredients exemplified for the adhesive layer may be used.
本発明に係る口腔粘膜貼付剤は、常法に従って形成した
上記シコン含有粘着層および非粘着支持体層のフィルム
ラミネート層を、適当な形状（円形、楕円形、絢形）に
打抜くことにより得られる。各層の厚みは通常、粘着層
５０〜１５０μｍおよび支持体１１２０〜５０μｍに選
定すればよい。The oral mucosa patch according to the present invention can be obtained by punching the film laminate layer of the silicone-containing adhesive layer and the non-adhesive support layer formed according to a conventional method into an appropriate shape (circular, elliptical, or inky shape). It will be done. The thickness of each layer is usually selected to be 50 to 150 μm for the adhesive layer and 1120 to 50 μm for the support.
このようにして得られる本発明貼付剤は、たとえば直径
５〜１５ｍ＋、総厚７０〜２００μｍの円形片として供
されるので、口腔内への適用に非常にマツチすることが
でき、その需要度は極めて高いものといえる。しかも、
その薬効などの面においても以下の利点を奏することが
できる。The patch of the present invention obtained in this way is provided as a circular piece with a diameter of 5 to 15 m+ and a total thickness of 70 to 200 μm, so it is very suitable for application in the oral cavity, and its demand is high. This can be said to be extremely high. Moreover,
In terms of its medicinal efficacy, it also has the following advantages.
１、口１体粘膜に強固に長時間付着し、患部に対して適
確に直接、抗炎症作用を発揮する。1. It firmly adheres to the mucous membranes of the mouth and body for a long time, and exerts an anti-inflammatory effect directly and accurately on the affected area.
２、口腔内において特に溶解して流出せす、膨潤した形
態を比較的長時間にわたって保つ。2. It dissolves and flows out in the oral cavity and maintains its swollen form for a relatively long period of time.
３、製剤中のシコン含酸の変化によって所望の薬物ａｌ
′ｆが得られる他、厚みや付着面積を変えても所壜の薬
物酸を容易に得ることができる。3. Desired drug al
'f can be obtained, and even if the thickness and adhesion area are changed, the drug acid can be easily obtained in a specific bottle.
次に実施例および比較例を挙げて、本発明をより具体的
に説明する。なお、本発明はこれらの実施例に限定され
るものではない。Next, the present invention will be explained in more detail with reference to Examples and Comparative Examples. Note that the present invention is not limited to these examples.
実施例１
エチルセルロース０．６ｙ、ポリアクリル酸５ｙおよび
グリセリン脂肪酸エステル０．６２をエタノール４０ｙ
中で練合し、ペースト状とした後シコンエキス０．１ｙ
を加え、再度練合し、これを厚み７０＃ｎ となるよ
うに紙セパレーター上に展延、乾燥してシコン含有粘着
層を形成する。Example 1 0.6y of ethyl cellulose, 5y of polyacrylic acid and 0.62y of glycerin fatty acid ester were mixed with 40y of ethanol.
After kneading it in a paste and making it into a paste, add 0.1y of Sikon extract.
was added, kneaded again, and spread on a paper separator to a thickness of 70#n, and dried to form a silicone-containing adhesive layer.
さらに、この粘着層の片面にエチルセルロースとヒマシ
油のエタノール溶液を厚み３０μｍとなるように均一に
塗布、乾燥して非粘着支持体層を形成して、二層構造の
フィルムラミネート層を得、次いで直径１０ｆｌの円形
に打抜いて口腔粘膜貼付剤を邊る。Furthermore, an ethanol solution of ethyl cellulose and castor oil was uniformly coated on one side of this adhesive layer to a thickness of 30 μm, and dried to form a non-adhesive support layer to obtain a two-layer film laminate layer. Punch out a circle with a diameter of 10 fl and apply an oral mucosal patch.
実施例２ ＩＪＨ’ＤＩにおいて、エチルセルロース０．６ｙ。Example 2 In IJH'DI, ethylcellulose 0.6y.
ヒドロキシプロピルメチルセルロースアセテートサクシ
ネート５ｙ、ポリアクリル酸２．５ｙおよびクエン酸ト
リエチル２ｙをエタノール３０ｙ中、攪拌練合した後シ
コンエキス０．２ｙを加えたものを用いてシコン含有粘
着層を形成する以外は、同様にフィルムラミネート層の
形成、次いで打抜きを行い口腔粘膜貼付剤を得る。Except that 5y of hydroxypropyl methylcellulose acetate succinate, 2.5y of polyacrylic acid, and 2y of triethyl citrate were stirred and kneaded in 30y of ethanol, and then 0.2y of Siconium extract was added to form a Siconium-containing adhesive layer. Similarly, a film laminate layer is formed and then punched out to obtain an oral mucosal patch.
実施例３
エチルセルロース０．６ｙおよびクエン酸トリエチル２
ｙをエタノール７０ｙに溶解し、ヒドロキシプロピルメ
チルセルロース２．５２、ポリアクリル酸５ｙおよび水
１０ｙを加え、練合してペースト状とした後、シコンエ
キス０．１５ｙを加え、再度練合し、これを厚み７０μ
ｍとなるように均一に塗布、乾燥してシコン含有粘着層
を形成する。Example 3 Ethyl cellulose 0.6y and triethyl citrate 2
y was dissolved in 70 y of ethanol, 2.52 y of hydroxypropyl methylcellulose, 5 y of polyacrylic acid, and 10 y of water were added, kneaded to form a paste, then 0.15 y of Sicon extract was added, kneaded again, and this was thickened. 70μ
The adhesive layer is coated uniformly so as to have a thickness of m and dried to form a silicone-containing adhesive layer.
さらに、この粘着層の片面にエチルセルロース、ヒドロ
キシプロピルメチルセルロースアセテートサクシネート
およびグリセリン脂肪酸エステルのエタノール溶液を厚
み３０μｍとなるように展延、乾燥して非粘着支持体層
を形成して、二層構造のフィルムラミネート層を得、次
いで直径１０Ｕの円形に打抜いて口腔粘膜貼付剤を得る
。Furthermore, an ethanol solution of ethyl cellulose, hydroxypropyl methyl cellulose acetate succinate, and glycerin fatty acid ester was spread on one side of this adhesive layer to a thickness of 30 μm, and dried to form a non-adhesive support layer, resulting in a two-layer structure. A film laminate layer is obtained, and then a circular shape with a diameter of 10 U is punched out to obtain an oral mucosal patch.
比較例１
アミノアルキルメタアクリレートコポリマー３２、ポリ
アクリル酸４ｙおよびポリエチレングリコール３ｙをエ
タノール２０ｙ中に分散し、水５゜ｙを加え、ペースト
状とした後シコンエキス０．２２を加え、以下実施例１
と同様にしてシコン含有粘着層を形成させ、ついでフィ
ルムラミネート層の形成、次いで打抜きを行い口腔粘膜
貼付剤を得る。Comparative Example 1 Aminoalkyl methacrylate copolymer 32, polyacrylic acid 4y, and polyethylene glycol 3y were dispersed in 20y of ethanol, 5°y of water was added to make a paste, and 0.22% of Sicon extract was added.
A silicone-containing adhesive layer is formed in the same manner as above, and then a film laminate layer is formed, followed by punching to obtain an oral mucosa patch.
比較例２
ポリアクリル酸５ｙ、ポリエチレングリコール３ｙをエ
タノール１５ｙ中で混合し、ポリビニルア／Ｌｚｍ−ル
６ｙの、ｌＪ液ｓｏｙおよびシコンエキス０．２５ ｙ
を加え、これを用いて実施列１と同様にしてシコン含有
粘着層を形成させ、さらに、打抜き形状を長径１８ｍ、
４径６！ｏ１の楕円形とする以外は、同様にフィルムラ
ミネート層の形成、次いで打抜きを行い口腔粘膜貼付剤
を得る。Comparative Example 2 5 y of polyacrylic acid and 3 y of polyethylene glycol were mixed in 15 y of ethanol, and 6 y of polyvinyl alcohol/Lzm-al, 1J liquid soy and 0.25 y of Sicon extract were mixed.
was added and used to form a silicone-containing adhesive layer in the same manner as in Example 1, and further, the punched shape was cut into a shape with a major diameter of 18 m,
4 diameter 6! An oral mucosa patch is obtained by forming a film laminate layer and then punching out the film in the same manner, except that it is shaped into an oval shape.
これらの貼付剤について、その特徴的な性質をモデル的
に示すためＦ記の実験を行った。The experiment described in F was conducted to model the characteristic properties of these patches.
実験１（付着試験）
０．１Ｍ−リン酸塩緩衝溶液（ｐＨ７，４）を入れたビ
ーカー内の側面に、各貼付剤をそれぞれ８枚づつ貼付し
、マグネチツクスターラーで２０ｏｒｐｍにて攪拌しな
がら５時間後まで、その脱落状況を観察した。結果を表
１に示す。Experiment 1 (adhesion test) Eight sheets of each patch were pasted on the side of a beaker containing 0.1M phosphate buffer solution (pH 7,4), and the mixture was stirred with a magnetic stirrer at 20 orpm. The state of shedding was observed until 5 hours later. The results are shown in Table 1.
表” （ｎ＝８ ）実験２（
貼付試験）
各貼付剤をボランティア１０名のそれぞれの歯肉粘膜に
貼付し、自然に剥離するまでの時間を調べた。結果を表
２に示す。Table” (n=8) Experiment 2 (
Patch Test) Each patch was applied to the gingival mucosa of 10 volunteers, and the time required for it to peel off naturally was determined. The results are shown in Table 2.
表２ （。＝１０）
実験３（血管透過性亢進抑制試験）
実験動物としてハムスターを用い、軽麻酔下に１％Ｅｖ
ａｎ’ｓ ｂｌｕｅを静脈内に投与（Ｑ、 ５ ｍ
／１００Ｂｕ）Ｌ、直ちに右側煩袋を反転露出せしめ、
直径１０ｍのキシレン含浸フェルトで煩袋粘膜を３０秒
間判激した後、被試験試料を適用する（適用時間は１時
間および２時間とする）。所定時間径ｉ後、右側煩袋を
皮膚と共に切取り、青染部の長径と短径を測定し、その
積（−）を指数として用いた。結果を表３に示す。Table 2 (.=10) Experiment 3 (vascular hyperpermeability suppression test) Using hamsters as experimental animals, 1% Ev was used under light anesthesia.
an's blue administered intravenously (Q, 5 m
/100Bu) L, immediately invert and expose the right side bag,
After agitating the mucous membrane for 30 seconds with a xylene-impregnated felt having a diameter of 10 m, the test sample is applied (application times are 1 hour and 2 hours). After a predetermined time period i, the right side pouch was cut out together with the skin, the long axis and short axis of the blue-stained part were measured, and the product (-) was used as an index. The results are shown in Table 3.
表３ 注■）実施例３よりシコンエキスを除いたもの。Table 3 Note ■) Same as Example 3 with Shicon extract removed.
■）実施例３と同量のシコンエキスを含む軟膏。■) Ointment containing the same amount of Sicon extract as in Example 3.
特許出願人 帝国製薬株式会社Patent applicant Teikoku Seiyaku Co., Ltd.
Claims (1)
酸もしくはその医薬的に許容しうる塩からなる粘着層、
および水不溶性または水膨潤性高分子物質からなる非粘
着支持体層から成り、上記粘着層に生理活性成分として
シコンエキスを含有したことを特徴とするシコン含有口
腔粘膜貼付剤。 ２、セルロース低級アルキルエーテル類が、エチルセル
ロース、ヒドロキシプロピルメチルセルロースおよびヒ
ドロキシプロピルメチルセルロースアセテートサクシネ
ートの少なくとも１種である請求項第１項記載の貼付剤
。 ３、水不溶性または水膨潤性高分子物質が、エチルセル
ロースおよび／またはヒドロキシプロピルメチルセルロ
ースアセテートサクシネートである請求項第１項または
第２項記載の貼付剤。[Claims] 1. An adhesive layer comprising cellulose lower alkyl ethers and polyacrylic acid or a pharmaceutically acceptable salt thereof;
and a non-adhesive support layer made of a water-insoluble or water-swellable polymeric substance, and the adhesive layer contains Shicon extract as a physiologically active ingredient. 2. The patch according to claim 1, wherein the cellulose lower alkyl ether is at least one of ethylcellulose, hydroxypropylmethylcellulose, and hydroxypropylmethylcellulose acetate succinate. 3. The adhesive patch according to claim 1 or 2, wherein the water-insoluble or water-swellable polymeric substance is ethylcellulose and/or hydroxypropylmethylcellulose acetate succinate.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP63057052A JP2685055B2 (en) | 1988-03-08 | 1988-03-08 | Oral mucosa patch containing Sikon |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP63057052A JP2685055B2 (en) | 1988-03-08 | 1988-03-08 | Oral mucosa patch containing Sikon |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH01226823A true JPH01226823A (en) | 1989-09-11 |
| JP2685055B2 JP2685055B2 (en) | 1997-12-03 |
Family
ID=13044675
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP63057052A Expired - Lifetime JP2685055B2 (en) | 1988-03-08 | 1988-03-08 | Oral mucosa patch containing Sikon |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP2685055B2 (en) |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2002512950A (en) * | 1998-04-29 | 2002-05-08 | バイロテックス コーポレイション | Drug carrier device suitable for delivering drug compounds to mucosal surfaces |
| US7579019B2 (en) | 1996-10-18 | 2009-08-25 | Arius Two, Inc. | Pharmaceutical carrier device suitable for delivery of pharmaceutical compounds to mucosal surfaces |
| US9597288B2 (en) | 2006-07-21 | 2017-03-21 | Biodelivery Sciences International, Inc. | Transmucosal delivery devices with enhanced uptake |
| US9901539B2 (en) | 2011-12-21 | 2018-02-27 | Biodelivery Sciences International, Inc. | Transmucosal drug delivery devices for use in chronic pain relief |
| JP2019122702A (en) * | 2018-01-19 | 2019-07-25 | 東洋化学株式会社 | Oral cavity mucosa protective film |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5618912A (en) * | 1979-07-25 | 1981-02-23 | Lion Corp | Oral band |
| JPS5622720A (en) * | 1979-07-31 | 1981-03-03 | Lion Corp | Composition for oral cavity application |
| JPS5758613A (en) * | 1980-09-26 | 1982-04-08 | Lion Corp | Composition for oral cavity application |
| JPS60143737U (en) * | 1984-03-05 | 1985-09-24 | 小川 裕三 | oral patch |
-
1988
- 1988-03-08 JP JP63057052A patent/JP2685055B2/en not_active Expired - Lifetime
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5618912A (en) * | 1979-07-25 | 1981-02-23 | Lion Corp | Oral band |
| JPS5622720A (en) * | 1979-07-31 | 1981-03-03 | Lion Corp | Composition for oral cavity application |
| JPS5758613A (en) * | 1980-09-26 | 1982-04-08 | Lion Corp | Composition for oral cavity application |
| JPS60143737U (en) * | 1984-03-05 | 1985-09-24 | 小川 裕三 | oral patch |
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7579019B2 (en) | 1996-10-18 | 2009-08-25 | Arius Two, Inc. | Pharmaceutical carrier device suitable for delivery of pharmaceutical compounds to mucosal surfaces |
| JP2002512950A (en) * | 1998-04-29 | 2002-05-08 | バイロテックス コーポレイション | Drug carrier device suitable for delivering drug compounds to mucosal surfaces |
| JP2005325140A (en) * | 1998-04-29 | 2005-11-24 | Virotex Corp | Pharmaceutical carrier device suitable for delivery of pharmaceutical compound to mucosal surface |
| US9597288B2 (en) | 2006-07-21 | 2017-03-21 | Biodelivery Sciences International, Inc. | Transmucosal delivery devices with enhanced uptake |
| US9655843B2 (en) | 2006-07-21 | 2017-05-23 | Biodelivery Sciences International, Inc. | Transmucosal delivery devices with enhanced uptake |
| US9901539B2 (en) | 2011-12-21 | 2018-02-27 | Biodelivery Sciences International, Inc. | Transmucosal drug delivery devices for use in chronic pain relief |
| JP2019122702A (en) * | 2018-01-19 | 2019-07-25 | 東洋化学株式会社 | Oral cavity mucosa protective film |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2685055B2 (en) | 1997-12-03 |
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