JPS63201119A - Plaster composition - Google Patents
Plaster compositionInfo
- Publication number
- JPS63201119A JPS63201119A JP3389487A JP3389487A JPS63201119A JP S63201119 A JPS63201119 A JP S63201119A JP 3389487 A JP3389487 A JP 3389487A JP 3389487 A JP3389487 A JP 3389487A JP S63201119 A JPS63201119 A JP S63201119A
- Authority
- JP
- Japan
- Prior art keywords
- drug
- water
- composition
- drugs
- insoluble
- 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
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- 229940079593 drug Drugs 0.000 claims abstract description 41
- 239000003814 drug Substances 0.000 claims abstract description 41
- 239000007787 solid Substances 0.000 claims abstract description 20
- -1 nicotinic acid ester Chemical class 0.000 claims abstract description 12
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 11
- 239000000126 substance Substances 0.000 claims abstract description 9
- PVNIIMVLHYAWGP-UHFFFAOYSA-N nicotinic acid Natural products OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 claims abstract description 7
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 claims abstract description 6
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 claims abstract description 6
- 229940041616 menthol Drugs 0.000 claims abstract description 6
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 claims abstract description 6
- DSSYKIVIOFKYAU-XCBNKYQSSA-N (R)-camphor Chemical compound C1C[C@@]2(C)C(=O)C[C@@H]1C2(C)C DSSYKIVIOFKYAU-XCBNKYQSSA-N 0.000 claims abstract description 5
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- DNXIKVLOVZVMQF-UHFFFAOYSA-N (3beta,16beta,17alpha,18beta,20alpha)-17-hydroxy-11-methoxy-18-[(3,4,5-trimethoxybenzoyl)oxy]-yohimban-16-carboxylic acid, methyl ester Natural products C1C2CN3CCC(C4=CC=C(OC)C=C4N4)=C4C3CC2C(C(=O)OC)C(O)C1OC(=O)C1=CC(OC)=C(OC)C(OC)=C1 DNXIKVLOVZVMQF-UHFFFAOYSA-N 0.000 description 2
- SPCKHVPPRJWQRZ-UHFFFAOYSA-N 2-benzhydryloxy-n,n-dimethylethanamine;2-hydroxypropane-1,2,3-tricarboxylic acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O.C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 SPCKHVPPRJWQRZ-UHFFFAOYSA-N 0.000 description 2
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- PPBRXRYQALVLMV-UHFFFAOYSA-N Styrene Chemical compound C=CC1=CC=CC=C1 PPBRXRYQALVLMV-UHFFFAOYSA-N 0.000 description 2
- XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 description 2
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- 150000001298 alcohols Chemical class 0.000 description 2
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- NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 description 2
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- 239000000057 synthetic resin Substances 0.000 description 1
- 239000005061 synthetic rubber Substances 0.000 description 1
- 229960002180 tetracycline Drugs 0.000 description 1
- 229930101283 tetracycline Natural products 0.000 description 1
- 235000019364 tetracycline Nutrition 0.000 description 1
- 150000003522 tetracyclines Chemical class 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 229960000790 thymol Drugs 0.000 description 1
- HTJXMOGUGMSZOG-UHFFFAOYSA-N tiaramide Chemical compound C1CN(CCO)CCN1C(=O)CN1C(=O)SC2=CC=C(Cl)C=C21 HTJXMOGUGMSZOG-UHFFFAOYSA-N 0.000 description 1
- 229950010302 tiaramide Drugs 0.000 description 1
- 239000004408 titanium dioxide Substances 0.000 description 1
- 229960001017 tolmetin Drugs 0.000 description 1
- UPSPUYADGBWSHF-UHFFFAOYSA-N tolmetin Chemical compound C1=CC(C)=CC=C1C(=O)C1=CC=C(CC(O)=O)N1C UPSPUYADGBWSHF-UHFFFAOYSA-N 0.000 description 1
- KHPCPRHQVVSZAH-UHFFFAOYSA-N trans-cinnamyl beta-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OCC=CC1=CC=CC=C1 KHPCPRHQVVSZAH-UHFFFAOYSA-N 0.000 description 1
- 229960005294 triamcinolone Drugs 0.000 description 1
- GFNANZIMVAIWHM-OBYCQNJPSA-N triamcinolone Chemical compound O=C1C=C[C@]2(C)[C@@]3(F)[C@@H](O)C[C@](C)([C@@]([C@H](O)C4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 GFNANZIMVAIWHM-OBYCQNJPSA-N 0.000 description 1
- 229960002117 triamcinolone acetonide Drugs 0.000 description 1
- YNDXUCZADRHECN-JNQJZLCISA-N triamcinolone acetonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O YNDXUCZADRHECN-JNQJZLCISA-N 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 229920003169 water-soluble polymer Polymers 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
- 239000011787 zinc oxide Substances 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
Description
【発明の詳細な説明】
〔産業上の利用分野〕
本発明は貼付剤組成物、更に詳しくは薬効成分の経皮吸
収性に優れた貼付剤組成物に関する。DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The present invention relates to a patch composition, and more particularly to a patch composition with excellent percutaneous absorption of medicinal ingredients.
皮膚外用剤には、軟膏、クリーム剤、ダル剤等の半固型
製剤や液剤およびシラスター、ノqツデ剤等の貼付剤が
ある。これらの皮膚外用剤は、近年、局所作用を有する
薬物だけでなく、全身作用を期待する薬物が配合されて
いる〇一方、薬物の副作用に対する関心が高まっておシ
、上記の外用剤は内服薬に比べて副作用が認められ九場
合、ただちに取り除くことが可能である点有側である。External skin preparations include semi-solid preparations such as ointments, creams, and dals, liquid preparations, and patches such as Shirastar and Noqtsude preparations. In recent years, these external skin preparations have been formulated not only with drugs that have local effects, but also with drugs that are expected to have systemic effects.On the other hand, there has been increasing interest in the side effects of drugs, and the above-mentioned external preparations have been combined with drugs that are expected to have systemic effects. In contrast, if side effects are observed, they can be removed immediately.
就中、貼付剤は、多くの薬物を膏体中のマトリックスに
保持することが可能でToシ、薬物を長期間一定の速度
で放出することができ、持続性を必要とされる薬物の投
与にあ九っては有利であることから期待されている製剤
である。該貼付剤のうち、例えばシラスターはゴム系粘
着成分、粘着付与成分および軟化剤を基本成分とする基
剤に薬物を配合して得た膏体を塩化ビールフィルム等に
展着することにより製造されている。また、eツブ剤は
無機粉体を賦形剤とし、水m性高分子、保湿剤、水等に
薬物を練合して得たペースト状膏体を不織布等に塗布し
て製造されている。In particular, patches can hold a large amount of drugs in a matrix in the plaster, and can release drugs at a constant rate over a long period of time, making it possible to administer drugs that require sustained delivery. Niaku is a promising formulation due to its advantages. Among these patches, for example, Shirastar is manufactured by blending a drug into a base consisting of a rubber adhesive component, a tackifier component, and a softener, and then spreading the paste on a chlorinated beer film or the like. ing. In addition, e-tubes are manufactured by using inorganic powder as an excipient and applying a paste-like paste obtained by kneading drugs with water-based polymers, humectants, water, etc. onto non-woven fabrics, etc. .
しかしながら、従来の貼付剤では薬物は単に基剤に混合
されているにすぎず、薬物が水に不m性の固体である場
合には、前記期待通シに薬物が膏体から放出されず充分
な薬効を発揮することができない。このため膏体からの
薬物の放出性が曳好で生物学的利用率が高い貼付剤組成
物の開発が熱望されていた。However, in conventional patches, the drug is simply mixed into the base, and if the drug is a water-immiscible solid, the drug is not released from the plaster as expected and is not sufficient. cannot exert its medicinal effects. For this reason, there has been a strong desire to develop a patch composition that exhibits good drug release from the plaster and a high bioavailability.
本発明者らは、かかる従来の貼付剤の欠点を克服すぺ〈
鋭意研究を行った結果、水に不溶性の固体薬物を、これ
を溶解することのできる液状の特定の物質を用いて溶解
して貼付剤とすることにょ)、膏体からの薬物の放出性
および薬物の経皮吸収性が極めて向上することを見い出
し、本発明を完成した。The present inventors have developed a project to overcome the drawbacks of such conventional patches.
As a result of extensive research, we have discovered that solid drugs that are insoluble in water can be dissolved into patches using a specific liquid substance that can dissolve them, and that the release properties of drugs from plasters and The present invention was completed based on the discovery that the transdermal absorption of drugs is greatly improved.
すなわち、本発明はベンジルアルコール、クロタミトン
、ジフェンヒドラミン、ニコチン酸エステル、サリチル
酸エステル及びメントールとカンフルの混合物よりなる
群から選ばれた一種又は二種以上の物質及び水に不溶性
の固体薬物を含有すること1特徴とする貼付剤組成物を
提供するものである。That is, the present invention contains one or more substances selected from the group consisting of benzyl alcohol, crotamiton, diphenhydramine, nicotinic acid ester, salicylic acid ester, and a mixture of menthol and camphor, and a solid drug insoluble in water. The present invention provides a patch composition having the following characteristics.
本発明組成物に配合される水に不溶性の固体薬物として
は、局所作用、全身作用のどちらの効能を有する薬物を
も含み、例えば抗炎症剤、催眠鎮静剤、精神神経用剤、
抗生物質、強心剤等の薬物のうち水に不溶で固体のもの
が挙げられる。ここで固体とは、結晶状、粉末状及びフ
レーク状等のものを含むものである。The water-insoluble solid drugs that are incorporated into the composition of the present invention include drugs that have both local and systemic effects, such as anti-inflammatory agents, hypnotic sedatives, psychoneurotic agents,
Examples include solid drugs that are insoluble in water, such as antibiotics and cardiotonic drugs. Here, the term "solid" includes those in the form of crystals, powders, flakes, and the like.
抗炎症剤としては、非ステロイド系及びステロイド系の
抗炎症剤が、催眠鎮静剤としてはフェノパルピタール、
抱水りaラール、ゾアゼ、Qム等が、精神神経用剤とし
てはレセルピン、クロルゾアゼ?キシド、クロルゾキサ
ゾン等が、抗生物質としてはエリスロマイシン、テトラ
サイクリン、クロラムフェニコール等が、また強心剤と
してはゾギトキシン、ゾゴ中シン等が挙げられる0就中
、アセチルサリチル酸、アセトアミノフェン、アミノビ
リン、ベンタゾシン、メビリゾール、チアラミド、プフ
ェ午すマック、ナンドロン、ピロキシカム、フェニルブ
タシン、オキシフェンブタシン、スキシブシン、イブプ
ロフェン、ナfaキセン、ケトデクフェン、フラパイデ
ロフェン、フェノデクフェン、プラノプロ7エン、チア
ゾロフェン、フルルビシc!7エン、トルメチン、スリ
ンダク、シクロフェナック、アルクロフェナック、フェ
ンブフェン、メフェナム酸、フルフェナム酸、インドメ
タシン等の非ステロイド系の抗炎症剤や、プレドニゾロ
ン、コーチシン、トリアムシノロン、ペタメタシン、ハ
イドロコーチシン、酢酸ハイドロコーチシン、デキサメ
タシン、メチルプレドニゾロン、フルオシノaン、フル
オロメソロン、トリアムシノロンアセトニド、プレドナ
ジノクンアセトニド、デキサメタシンバレレート、ペタ
メタシンバレレート、ペタメタシンアセテート、ペタメ
タシンベンゾエート、フルメタシン、プレドニゾロンア
セテート、ハイドロコーチシンバレレート、ゾロピオン
駿ペタメタシン、ゾロピオン酸ベクロメタゾン等のステ
ロイド系抗炎症剤が好ましいO
これらの水に不溶性の固体薬物を溶解することのできる
液状物質は、ベンジルアルコール、・クロタミトン、ジ
フェンヒドラミン、ニコチン酸エステル、サリチル酸エ
ステル、及びメントールとカンフルの混合物から選ばれ
た一徨又は二重以上のものである。ここで、ニコチン酸
エステルトシテハ、Cm〜C・の−級アルコールとのエ
ステル、ベンジルアルコールとのエステル等が、またサ
リチル酸エステルとしては、CI〜C6のアルコールと
のエステル、エチレングリコール等ポリアルキレングリ
コールとのエステル等が挙げられる。またメントール及
びカンフルは、6体、7体、dj1体いずれでも用いる
ことができる。メントールとしては、ハツカ油、ユーカ
リ油等の植物抽出油をそのまま用いることもできる。Anti-inflammatory drugs include nonsteroidal and steroidal anti-inflammatory drugs, and hypnotic and sedative drugs include phenopalpital and
Aral hydrate, zoaze, Qmu, etc., but reserpine and chlorzoase as psychoneurotic agents? Antibiotics include erythromycin, tetracycline, chloramphenicol, etc., and cardiac drugs include zogitoxin, zogocin, etc. Among these, acetylsalicylic acid, acetaminophen, aminovirine, bentazocine, Mevirizole, Tiaramide, Puffet Nox Mac, Nandrone, Piroxicam, Phenylbutacin, Oxyphenbutacin, Sxibucin, Ibuprofen, Nafaxene, Ketodekufen, Frapaiderofen, Fenodekufen, Pranopro7ene, Thiazolofen, Flurubici c! Nonsteroidal anti-inflammatory drugs such as 7ene, tolmetin, sulindac, cyclofenac, alclofenac, fenbufen, mefenamic acid, flufenamic acid, and indomethacin, as well as prednisolone, corchicin, triamcinolone, petamethacin, hydrocortiscin, and hydrocortisone acetate. Syn, dexamethacin, methylprednisolone, fluorocino-a, fluorometholone, triamcinolone acetonide, prednazinocune acetonide, dexamethacin valerate, petamethacin valerate, petamethacin acetate, petamethacin benzoate, flumethacin, Steroidal anti-inflammatory agents such as prednisolone acetate, hydrococcin valerate, zolopion petamethacin, and beclomethasone zoropionate are preferred. Liquid substances capable of dissolving these water-insoluble solid drugs include benzyl alcohol, crotamiton, One or more members selected from diphenhydramine, nicotinic acid ester, salicylic acid ester, and a mixture of menthol and camphor. Here, nicotinic acid esters, esters with -grade alcohols of Cm to C, esters with benzyl alcohol, etc., and salicylic acid esters include esters with alcohols of CI to C6, polyalkylene glycols such as ethylene glycol, etc. Examples include esters of Further, menthol and camphor can be used in any of six forms, seven forms, and one dj form. As the menthol, vegetable extracted oils such as peppermint oil and eucalyptus oil can also be used as they are.
本発明組成物において水に不溶性の固体薬物の配合量は
、薬効、効力等によって異なるが例えばステロイド系抗
炎症剤の場合、0.01〜5.0重量−1特に0.05
〜3.0重量−が好ましぐ、非ステロイド系抗炎症剤の
場合、0.5〜5.0皇量チ、特に1.0〜3.0重量
%が好ましい。ま九該固体薬物を溶解することのできる
液状物質の配合量は、該固体薬物を溶解し得る量であれ
ば充分であるが、該固体薬物1重量部に対し、1〜10
重量部以上であることが好ましい。The amount of the water-insoluble solid drug in the composition of the present invention varies depending on the medicinal effect, potency, etc., but for example, in the case of a steroid anti-inflammatory agent, 0.01 to 5.0 weight -1, especially 0.05
-3.0% by weight is preferred; in the case of non-steroidal anti-inflammatory agents, 0.5-5.0% by weight, particularly 1.0-3.0% by weight is preferred. (9) The amount of the liquid substance that can dissolve the solid drug is sufficient as long as it can dissolve the solid drug, but it is 1 to 10 parts by weight per 1 part by weight of the solid drug.
It is preferable that it is at least part by weight.
本発明組成物を製造するには、あらかじめ本に不溶性の
固体薬物を前記液状物質に溶解し、その後貼付側基剤中
に加え練合することKよシ実施される。斯〈実施するこ
とによって、膏体中で薬物は析出することなく、該液状
物質に溶解した状態で存在することができる。ここで用
いる貼付剤基剤としては、従来貼付剤に用いられている
公知のものであれば特に制限されない。例えばシラスタ
ー及びテープ剤の基剤のうち、ゴム系粘着成分としては
、天然ゴム(NR)や、スチレン、プタゾエン共重合体
(SBB)、スチレン−イソプレン−スチレン共重合体
エラマドマー(S I S )、シリコンゴムなどの合
成ゴムが挙げられる。粘着付与成分としては、フィント
ン0(商品名、日本ゼオン社製、脂肪族系)、アルコン
0ビ商品名、荒用化学社製、脂JJI族系)などの石油
樹脂や、ロジン、水添aシン、エステルガムなどの樹脂
類が、軟化剤とじては?リプテン、流動ノqラフイン、
イソfcxビルンリステートの如き高級脂肪酸エステル
類、シリコンや植物油等が挙げられる0また、プラスタ
ーを製造する上で必要により加えられる基剤としては、
ブチルヒトミキシアニソール、グアヤコールエステル類
、シブチルヒドロキシトルエン、ノルゾヒドaグアイア
レチン酸等の酸化防止剤、チモール等の防腐剤等が挙げ
られるO
また、eツゾ剤の基剤のうち、賦形剤としては、カオリ
ン、メルク、ベントナイト、二酸化チタン、酸化亜鉛等
の無機粉体が挙げられ、水溶性高分子としてはゼラチン
、鍍すアクリル散、−リアクリル故ソーダ、?リピニル
アルコール、?リピニルビavyン、?リエチレンオキ
サイド、カルボ中ジメチルセルロース、ヒトaキシfo
ビルセルロース、アルギン酸ソーダ、天然ガム類等が挙
げられ、保湿剤としてはグリセリン、ソルビトール、?
リエチレングリコール等が挙げられる。To produce the composition of the present invention, a solid drug that is insoluble in liquid is dissolved in the liquid substance, and then added to the adhesive base and kneaded. By carrying out this procedure, the drug can exist in a state dissolved in the liquid substance without being precipitated in the paste. The patch base used here is not particularly limited as long as it is a publicly known patch base that has been conventionally used in patches. For example, among the bases of Shirastar and tape agents, rubber-based adhesive components include natural rubber (NR), styrene, putazoene copolymer (SBB), styrene-isoprene-styrene copolymer elamadomer (SI S), Examples include synthetic rubber such as silicone rubber. As tackifier components, petroleum resins such as Finton 0 (trade name, manufactured by Nippon Zeon Co., Ltd., aliphatic type), Alcon 0 Bi (trade name, manufactured by Arayo Kagaku Co., Ltd., fatty JJI group type), rosin, hydrogenated a Can resins such as synthetic resin and ester gum be used as softeners? Ripten, Fluid Noq Rough In,
Examples include higher fatty acid esters such as isofcx birne ristate, silicone, vegetable oil, etc.0 In addition, base materials that may be added as necessary in producing plaster include:
Antioxidants such as butyl human mixyanisole, guaiacol esters, sibutyl hydroxytoluene, norzohydro-guaiaretic acid, preservatives such as thymol, etc. Examples include inorganic powders such as kaolin, Merck, bentonite, titanium dioxide, and zinc oxide, and examples of water-soluble polymers include gelatin, acrylic powder, and lyacrylic soda. Lipinyl alcohol? Lipinylvin avyn? Liethylene oxide, dimethyl cellulose in carbo, human axy fo
Examples include cellulose, sodium alginate, and natural gums, and moisturizers include glycerin, sorbitol, and ?
Examples include lyethylene glycol.
本発明の貼付側組成物は、従来の貼付剤においては膏体
中に固体として存在していた水に不溶性の固体薬物が、
膏体中で溶解して存在している丸め、膏体からの薬物の
放出性及び経皮吸収性が極めて高く、優れた治療効果を
発揮する。また従来経皮吸収性が劣るため内服薬として
のみ投与されておシ、胃粘膜に対する刺激性に基づく副
作用が問題となっていた非ステロイド系抗炎症剤等の薬
物を本発明に適用することによシ、当該副作用を軽減す
ることが可能となった。In the patch composition of the present invention, the water-insoluble solid drug, which was present as a solid in the paste in conventional patches, is
The drug is dissolved in the paste and has extremely high drug release properties and transdermal absorption from the paste, and exhibits excellent therapeutic effects. Furthermore, by applying drugs such as non-steroidal anti-inflammatory drugs to the present invention, which have conventionally been administered only as oral drugs due to poor transdermal absorption, and which have had problems with side effects due to irritation to the gastric mucosa. It has become possible to reduce these side effects.
次に実施例を挙げて本発明の詳細な説明する。 Next, the present invention will be explained in detail with reference to Examples.
実施例1
組成: (重量−)■
インドメタシン 2.0
■ニコチン酸エチル 4.0
■?リプデン 10.0
■石油樹脂(日本ゼオン社製、フィントンU−185)
49.0■スチレン−イソプレ
/−スチレン・テレブロック共重合体樹脂
35.0(シェル化学社111 、カリフレックスTR
−1107”)製法:
■、■、■をトルエン適量に加え溶解し、あらかじめ■
に■を溶かした溶液を加えて均一に混合する。これを離
型ライナー上に塗布後トルエンを留去し、塩化ビニルフ
ィルムに展着し、インドメタシン含有プラスターを得た
。Example 1 Composition: (Weight-)■
Indomethacin 2.0 ■Ethyl nicotinate 4.0 ■? Lipden 10.0 ■Petroleum resin (manufactured by Nippon Zeon Co., Ltd., Finton U-185)
49.0■ Styrene-isoprene/-styrene-tereblock copolymer resin
35.0 (Shell Kagakusha 111, Cariflex TR
-1107") Manufacturing method: Add and dissolve ■, ■, and ■ in an appropriate amount of toluene, and
Add the solution containing ■ and mix evenly. After coating this on a mold release liner, the toluene was distilled off and spread on a vinyl chloride film to obtain an indomethacin-containing plaster.
実施例2
組成: (重t%)■酢酸
デキサメタシン 0.5■クロタミトン
5.0■ゼラチン
15,0■?リピニルアルコール 1.0
■−リアクリル酸ナトリウム 0.5(0,2チ水
溶液の粘度:400〜600 cps )■グリセリン
25.0■?リソルペート80
0.20酸化チタン
10.0■精製水 42.8製
法:
■を■の一部(30,0重量%)に湿潤させ、50’C
K加温して溶解する。■及び■を■の残シ(12,8重
量%)K溶解する。■及び■を■に加え混合攪拌する。Example 2 Composition: (wt%) ■ Dexamethacin acetate 0.5 ■ Crotamiton
5.0 ■ Gelatin
15,0■? Lipinyl alcohol 1.0
■-Sodium lyacrylate 0.5 (0.2% viscosity of aqueous solution: 400-600 cps)■Glycerin 25.0■? resolpate 80
0.20 titanium oxide
10.0 ■Purified water 42.8 Manufacturing method: Wet ■ with part of ■ (30.0% by weight) and heat at 50'C.
Heat to dissolve. (1) and (2) are dissolved in K (12.8% by weight) remaining in (2). Add ■ and ■ to ■ and mix.
これらの液を順々に万能攪拌機に投入し攪拌した後?リ
エチレン及びレーヨンよシなる不織布に均一に塗工しス
テロイド含有ノ9ツデ剤を得九。After pouring these liquids one by one into a multipurpose stirrer and stirring? A steroid-containing drug was obtained by uniformly coating a nonwoven fabric made of polyethylene and rayon.
実施例3
組成: (重量−
)■レセルピン 0.05■ニコチ
ン酸ペンシル O,S■グリセリン
20.0■酸化チタン −4,0
■tos、teリピニルアルコール水溶液 20.0■
ゼラチン 10.0■10−ジア
ルデヒド澱粉水溶液 4.0■水
バランス製法:
■、■、■を均一に攪拌・混合し、40°〜50℃に保
つ。一方■を■に加え、溶解したのち上記混合液に加え
、攪拌する。これに■を■に溶解したものを加え、混合
して■を加える。Example 3 Composition: (Weight -
)■Reserpine 0.05■Nicotinic acid pencil O,S■Glycerin
20.0 ■ Titanium oxide -4,0 ■ tos, te lipinyl alcohol aqueous solution 20.0 ■
Gelatin 10.0 ■ 10-dialdehyde starch aqueous solution 4.0 ■ Water
Balance manufacturing method: Stir and mix (1), (2), and (2) uniformly and keep at 40° to 50°C. On the other hand, add (2) to (2) and dissolve, then add to the above mixture and stir. Add ■ dissolved in ■ to this, mix, and add ■.
さらに混合攪拌した後、得られたペースト状膏体を?リ
エチレンーレーヨンよりなる不織布に塗工しノ9ツデ剤
を得た。After further mixing and stirring, the resulting paste-like paste? A nonwoven agent was obtained by coating on a nonwoven fabric made of polyethylene-rayon.
実施例4
組成: (重量
%)■アセトアミノフェン 2.0■ニコチ
ン酸エチル 10.0■ゼラチ7
10.0■カオリン
10.0■グリセリン 15.0■
10S/リピニルアルコール 20.0■5Oqh
ゾアルデヒド澱粉水溶液 2.0■水
バランス製法:
■、■、■を混合−攪拌し、40〜50℃に保つ。これ
に■を■1cilかしたものを加え、攪拌し、さらに■
を■に溶解しこものを加えて混合し、■を加える。さら
に混合攪拌して得られ九ペースト状の膏体を?リエチレ
ンーレーヨンよりなる不織布に塗工し、/Qツゾ剤を得
た。Example 4 Composition: (% by weight) ■Acetaminophen 2.0■Ethyl nicotinate 10.0■Gelachi 7
10.0 ■ Kaolin
10.0 ■ Glycerin 15.0 ■
10S/lipinyl alcohol 20.0■5Oqh
Zoaldehyde starch aqueous solution 2.0 ■ water
Balance manufacturing method: Mix and stir ①, ② and ② and keep at 40-50°C. Add 1 cil of ■ to this, stir, and then add ■
Dissolve the ingredients in ■, add the mushrooms, mix, and add ■. Further mixing and stirring yields a paste-like paste? It was coated on a nonwoven fabric made of polyethylene-rayon to obtain a /Q agent.
実施例5
実施例11Cて製造したインドメタシン含有プラスター
の膏体を図−1に示し九構造を有する放出試験器を用い
、膏体からのインドメタシンの放出量を測定した。測定
は図−1のサンプル抜き取り口より経時的に50 pi
の液を抜き取つ死後、高速液体クロマトグラフィにより
行なつ九。比較品としては、実施例1の組成からニコチ
ン酸エチルを除き、?リプテンにおきかえたものを用い
九〇その結果を図−2に示す。本発明組成物は比較品に
比べて膏体からのインドメタシンの放出量が極めて高い
ものであった。Example 5 The indomethacin-containing plaster prepared in Example 11C was used to measure the amount of indomethacin released from the plaster using a release tester having a structure shown in Figure 1. Measurements were taken over time at 50 pi from the sample extraction port in Figure 1.
After death, the fluid is extracted using high-performance liquid chromatography. As a comparison product, ethyl nicotinate was removed from the composition of Example 1, and ? The results are shown in Figure 2. The composition of the present invention released an extremely high amount of indomethacin from the plaster as compared to the comparative product.
実施例6
実施例4にて製造したアセトアミノフェン含有ノ9ツゾ
剤(14X103)を用いて、経皮吸収性を検討した。Example 6 Using the acetaminophen-containing drug (14X103) produced in Example 4, transdermal absorption was investigated.
腹部を毛刈りし、あおむけに固定し九体重約3Ktの雄
性家兎(n−5)の腹部に、eツゾ剤を貼付し九〇貼付
後経時的に採血し、血中のアセトアミノ7工ン濃度を測
定した。表お、比較品としては、実施例4の組成からニ
コチン酸エチルを除き、水でバランスしたものを用いた
。結果を図−3に示す。本発明、Qツブ剤貼付により、
極めて高い血中7セトアミノ7工ン濃度が得られ、本発
明組成物は優れた放出性及び経皮吸収性を有することが
わかる。The abdomen of a male rabbit (n-5) was shaved and fixed on its back, weighing approximately 3Kt. E-Tsuzo agent was applied to the abdomen of a male rabbit (n-5). The ion concentration was measured. As a comparative product, the composition of Example 4 except that ethyl nicotinate was removed and the composition was balanced with water was used. The results are shown in Figure 3. By applying the present invention and the Q-tube agent,
It can be seen that an extremely high blood concentration of 7cetaminocane was obtained, indicating that the composition of the present invention has excellent release properties and transdermal absorption properties.
図−1は、実施例5において使用した放出試験器を模式
的に示した説明図でToシ、図−2は実施例5の放出性
試験の結果得られたインドメタシン放出量と経過時間と
の関係を示す図面である。図−3は実施例6の試験の結
果得られた血中アセトアミノフェン濃度と、Qツブ剤貼
付後の時間との関係を示す図面である。
以上
図−1
1−・−膏体
2、−寸うンラ・ノフ′
3−・ニトロでルロース8冥(ス/7T’ウンλ1工り
4、−、スクープ−と°−ス
ロー″Tンフー11染舎耳スリロ
図−2
経過一時間(h「]
×−一−−本光明
・−一比l東品Figure 1 is an explanatory diagram schematically showing the release tester used in Example 5. Figure 2 shows the relationship between the amount of indomethacin released and the elapsed time obtained as a result of the release test in Example 5. It is a drawing showing the relationship. FIG. 3 is a drawing showing the relationship between the blood acetaminophen concentration obtained as a result of the test of Example 6 and the time after application of QTub. Above figure-1 1-・-Glue body 2,-Sun La Nof' 3-・Nitro and Reulose 8 Megumi (Su/7T'un λ1 Machining 4,-,Scoop-and°-Slow''Tnfu 11 Dyesha Mimi Suriro Figure-2 Elapsed 1 hour (h ``]
Claims (1)
ラミン、ニコチン酸エステル、サリチル酸エステル及び
メントールとカンフルの混合物よりなる群から選ばれた
一種又は二種以上の物質及び水に不溶性の固体薬物を含
有することを特徴とする貼付剤組成物。1. It is characterized by containing one or more substances selected from the group consisting of benzyl alcohol, crotamiton, diphenhydramine, nicotinic acid ester, salicylic acid ester, and a mixture of menthol and camphor, and a solid drug insoluble in water. Patch composition.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP3389487A JPS63201119A (en) | 1987-02-17 | 1987-02-17 | Plaster composition |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP3389487A JPS63201119A (en) | 1987-02-17 | 1987-02-17 | Plaster composition |
Publications (1)
Publication Number | Publication Date |
---|---|
JPS63201119A true JPS63201119A (en) | 1988-08-19 |
Family
ID=12399235
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP3389487A Pending JPS63201119A (en) | 1987-02-17 | 1987-02-17 | Plaster composition |
Country Status (1)
Country | Link |
---|---|
JP (1) | JPS63201119A (en) |
Cited By (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH0482828A (en) * | 1990-07-26 | 1992-03-16 | Dia Seiyaku Kk | Percutaneous absorption-type patching agent containing indomethacin |
JPH04193826A (en) * | 1990-11-27 | 1992-07-13 | Shirogane Seiyaku Kk | Sodium dichlofenac-containing percutaneous absorption type antiinflammatory-analgesic patch |
JPH04230212A (en) * | 1990-06-25 | 1992-08-19 | Lts Lohmann Therapie Syst Gmbh & Co Kg | Plaster high in content of softened internal substance |
WO1993024129A1 (en) * | 1992-05-25 | 1993-12-09 | Toko Yakuhin Kogyo Kabushiki Kaisha | Composition for treating acne vulgaris |
JPH05331064A (en) * | 1992-05-26 | 1993-12-14 | Sekisui Chem Co Ltd | Anti-inflammatory analgesic plaster |
FR2721515A1 (en) * | 1994-06-28 | 1995-12-29 | Fabre Pierre Cosmetique | Pharmaceutical compsn. for topical application |
WO1996015776A1 (en) * | 1994-11-18 | 1996-05-30 | Hisamitsu Pharmaceutical Co., Inc. | Percutaneously absorbable patch |
WO2000002563A1 (en) * | 1998-07-10 | 2000-01-20 | Hisamitsu Pharmaceutical Co., Inc. | Steroid-containing cataplasms and process for producing the same |
JP2004115525A (en) * | 2002-09-27 | 2004-04-15 | Alpharx Inc | Carrier for locally carrying anti-inflammatory compound |
JP2008137936A (en) * | 2006-12-01 | 2008-06-19 | Taisho Pharmaceutical Co Ltd | Adapalene-containing composition for external use |
WO2011074567A1 (en) * | 2009-12-15 | 2011-06-23 | 帝國製薬株式会社 | Transdermal preparation containing basic anti-inflammatory agent |
US9206190B2 (en) | 2008-12-08 | 2015-12-08 | Euro-Celtique S.A. | Dihydroetorphines and their preparation |
US10898479B2 (en) | 2013-05-30 | 2021-01-26 | Euro-Celtique S.A. | Dihydroetorphine for the provision of pain relief and anaesthesia |
-
1987
- 1987-02-17 JP JP3389487A patent/JPS63201119A/en active Pending
Cited By (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH04230212A (en) * | 1990-06-25 | 1992-08-19 | Lts Lohmann Therapie Syst Gmbh & Co Kg | Plaster high in content of softened internal substance |
JPH0482828A (en) * | 1990-07-26 | 1992-03-16 | Dia Seiyaku Kk | Percutaneous absorption-type patching agent containing indomethacin |
JPH04193826A (en) * | 1990-11-27 | 1992-07-13 | Shirogane Seiyaku Kk | Sodium dichlofenac-containing percutaneous absorption type antiinflammatory-analgesic patch |
WO1993024129A1 (en) * | 1992-05-25 | 1993-12-09 | Toko Yakuhin Kogyo Kabushiki Kaisha | Composition for treating acne vulgaris |
JPH05331064A (en) * | 1992-05-26 | 1993-12-14 | Sekisui Chem Co Ltd | Anti-inflammatory analgesic plaster |
FR2721515A1 (en) * | 1994-06-28 | 1995-12-29 | Fabre Pierre Cosmetique | Pharmaceutical compsn. for topical application |
WO1996015776A1 (en) * | 1994-11-18 | 1996-05-30 | Hisamitsu Pharmaceutical Co., Inc. | Percutaneously absorbable patch |
US6432431B1 (en) | 1998-07-10 | 2002-08-13 | Hisamitsu Pharmaceutical Co., Inc. | Steroid-containing cataplasms and process for producing the same |
WO2000002563A1 (en) * | 1998-07-10 | 2000-01-20 | Hisamitsu Pharmaceutical Co., Inc. | Steroid-containing cataplasms and process for producing the same |
JP2004115525A (en) * | 2002-09-27 | 2004-04-15 | Alpharx Inc | Carrier for locally carrying anti-inflammatory compound |
JP2008137936A (en) * | 2006-12-01 | 2008-06-19 | Taisho Pharmaceutical Co Ltd | Adapalene-containing composition for external use |
US9206190B2 (en) | 2008-12-08 | 2015-12-08 | Euro-Celtique S.A. | Dihydroetorphines and their preparation |
US9481681B2 (en) | 2008-12-08 | 2016-11-01 | Euro-Celtique S.A. | Dihydroetorphines and their preparation |
US10745406B2 (en) | 2008-12-08 | 2020-08-18 | Euro-Celtique S.A. | Dihydroetorphines and their preparation |
WO2011074567A1 (en) * | 2009-12-15 | 2011-06-23 | 帝國製薬株式会社 | Transdermal preparation containing basic anti-inflammatory agent |
JPWO2011074567A1 (en) * | 2009-12-15 | 2013-04-25 | 帝國製薬株式会社 | Percutaneous absorption preparation containing basic anti-inflammatory analgesic |
JP5677680B2 (en) * | 2009-12-15 | 2015-02-25 | 帝國製薬株式会社 | Percutaneous absorption preparation containing basic anti-inflammatory analgesic |
US10898479B2 (en) | 2013-05-30 | 2021-01-26 | Euro-Celtique S.A. | Dihydroetorphine for the provision of pain relief and anaesthesia |
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