JP5842304B2 - External patch - Google Patents
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- JP5842304B2 JP5842304B2 JP2011253250A JP2011253250A JP5842304B2 JP 5842304 B2 JP5842304 B2 JP 5842304B2 JP 2011253250 A JP2011253250 A JP 2011253250A JP 2011253250 A JP2011253250 A JP 2011253250A JP 5842304 B2 JP5842304 B2 JP 5842304B2
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- 229940107700 pyruvic acid Drugs 0.000 description 1
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 1
- GRWFGVWFFZKLTI-UHFFFAOYSA-N rac-alpha-Pinene Natural products CC1=CCC2C(C)(C)C1C2 GRWFGVWFFZKLTI-UHFFFAOYSA-N 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 230000000717 retained effect Effects 0.000 description 1
- 239000010668 rosemary oil Substances 0.000 description 1
- 229940058206 rosemary oil Drugs 0.000 description 1
- 239000010670 sage oil Substances 0.000 description 1
- 229910052710 silicon Inorganic materials 0.000 description 1
- 239000010703 silicon Substances 0.000 description 1
- 150000003377 silicon compounds Chemical class 0.000 description 1
- 239000013464 silicone adhesive Substances 0.000 description 1
- JGMJQSFLQWGYMQ-UHFFFAOYSA-M sodium;2,6-dichloro-n-phenylaniline;acetate Chemical compound [Na+].CC([O-])=O.ClC1=CC=CC(Cl)=C1NC1=CC=CC=C1 JGMJQSFLQWGYMQ-UHFFFAOYSA-M 0.000 description 1
- 241000894007 species Species 0.000 description 1
- TUHBEKDERLKLEC-UHFFFAOYSA-N squalene Natural products CC(=CCCC(=CCCC(=CCCC=C(/C)CCC=C(/C)CC=C(C)C)C)C)C TUHBEKDERLKLEC-UHFFFAOYSA-N 0.000 description 1
- 229940038774 squalene oil Drugs 0.000 description 1
- 229920003048 styrene butadiene rubber Polymers 0.000 description 1
- 229920000468 styrene butadiene styrene block copolymer Polymers 0.000 description 1
- 229920003051 synthetic elastomer Polymers 0.000 description 1
- 239000005061 synthetic rubber Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- TUNFSRHWOTWDNC-HKGQFRNVSA-N tetradecanoic acid Chemical compound CCCCCCCCCCCCC[14C](O)=O TUNFSRHWOTWDNC-HKGQFRNVSA-N 0.000 description 1
- 229920001169 thermoplastic Polymers 0.000 description 1
- 229920002803 thermoplastic polyurethane Polymers 0.000 description 1
- 229920005992 thermoplastic resin Polymers 0.000 description 1
- 239000004416 thermosoftening plastic Substances 0.000 description 1
- 239000010678 thyme oil Substances 0.000 description 1
- 229960000790 thymol Drugs 0.000 description 1
- OGIDPMRJRNCKJF-UHFFFAOYSA-N titanium oxide Inorganic materials [Ti]=O OGIDPMRJRNCKJF-UHFFFAOYSA-N 0.000 description 1
- 229940042585 tocopherol acetate Drugs 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- VLPFTAMPNXLGLX-UHFFFAOYSA-N trioctanoin Chemical compound CCCCCCCC(=O)OCC(OC(=O)CCCCCCC)COC(=O)CCCCCCC VLPFTAMPNXLGLX-UHFFFAOYSA-N 0.000 description 1
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- 239000000341 volatile oil Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
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- 229960001296 zinc oxide Drugs 0.000 description 1
- CPYIZQLXMGRKSW-UHFFFAOYSA-N zinc;iron(3+);oxygen(2-) Chemical compound [O-2].[O-2].[O-2].[O-2].[Fe+3].[Fe+3].[Zn+2] CPYIZQLXMGRKSW-UHFFFAOYSA-N 0.000 description 1
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical class OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
本発明は、外用貼付剤に関し、より詳しくは、支持体と、薬物及び粘着剤を含有する膏体層とを備える外用貼付剤に関する。 The present invention relates to an external patch, and more particularly, to an external patch comprising a support and a plaster layer containing a drug and an adhesive.
従来から、支持体と、抗炎症薬等の薬物を含有する膏体層と、剥離ライナーとから順に構成された外用貼付剤が広く知られ、製造販売されている。一般的に外用貼付剤は、膏体層の含有基剤成分によって、概略、含水系製剤であるパップ剤と、非含水系製剤であるテープ剤とに分類される。外用貼付剤で使用されている支持体のほとんどは、不織布や編布(ニット)などの布基材である。 Conventionally, external patches comprising a support, a paste layer containing a drug such as an anti-inflammatory drug, and a release liner have been widely known and manufactured and sold. In general, external patches are roughly classified into a cataplasm, which is a hydrous preparation, and a tape, which is a non-hydrous preparation, depending on the base component contained in the plaster layer. Most of the supports used in external patches are cloth base materials such as nonwoven fabric and knitted fabric (knit).
一方、貼付時の目立ちにくさ等の観点から、支持体としてポリウレタンフィルムが用いられた貼付剤も知られている。例えば、特開2006−104174号公報(特許文献1)には、ウレタン樹脂層と繊維シート層とを積層してなる支持体と、含水性膏体とを備えた貼付剤が開示されている。特公平7−116023号公報(特許文献2)には、厚み40〜150μmのポリウレタンフィルムを支持体とし、薬物を含有するアクリル系粘着剤層が設けられた貼付剤が開示されている。 On the other hand, a patch using a polyurethane film as a support is also known from the viewpoint of conspicuousness at the time of sticking. For example, JP 2006-104174 A (Patent Document 1) discloses a patch comprising a support formed by laminating a urethane resin layer and a fiber sheet layer, and a hydrous plaster. Japanese Patent Publication No. 7-116023 (Patent Document 2) discloses a patch having a polyurethane film having a thickness of 40 to 150 μm as a support and provided with an acrylic pressure-sensitive adhesive layer containing a drug.
特許文献1で開示されている貼付剤はパップ剤であって、テープ剤と比べて厚みがあることにより、曲げ伸ばしを繰り返すような膝や肘などの関節部に貼付する場合や、寝具や衣類との擦れが起こりうるような就寝中などに使用する場合に、貼付剤が皮膚に十分密着できずにはがれやすくなるなど、使用性の面で問題があった。特許文献2で開示されている貼付剤は、支持体としてある程度の厚みを有するポリウレタンフィルムを用いているため、貼付感(違和感)の観点で十分満足できないなどの問題があり、更なる改善が望まれていた。 The patch disclosed in Patent Document 1 is a poultice and has a thickness compared to a tape, so that it is applied to joints such as knees and elbows where bending and stretching are repeated, bedding and clothing When it is used while sleeping such that it can rub against the skin, there is a problem in terms of usability, such as the patch is not sufficiently adhered to the skin and is easily peeled off. Since the patch disclosed in Patent Document 2 uses a polyurethane film having a certain thickness as a support, there is a problem that it cannot be sufficiently satisfied from the viewpoint of sticking feeling (uncomfortable feeling), and further improvement is desired. It was rare.
また、外用貼付剤は、膏体層中で抗炎症薬等の薬物を均一に含有させるため、場合によってはその薬物を溶解するための溶解剤を用いる必要がある。例えば、支持体にポリウレタンフィルムを用いる場合、その溶解剤を多量に用いれば、ポリウレタンフィルムが溶解したり変形したりする等の劣化の恐れがある。特に、フィルムが薄ければ薄いほどその劣化の恐れは顕著である。また、膏体層中に含まれる薬物等の影響によっても、ポリウレタンフィルムが少なからず劣化する恐れがある。製剤の性状安定性の観点で問題があり、更なる改善が望まれていた。 Further, since the external patch contains a drug such as an anti-inflammatory drug uniformly in the plaster layer, it is necessary to use a dissolving agent for dissolving the drug in some cases. For example, when a polyurethane film is used for the support, if a large amount of the dissolving agent is used, there is a risk of deterioration such as dissolution or deformation of the polyurethane film. In particular, the thinner the film, the more prominent the deterioration. Moreover, there is a possibility that the polyurethane film is deteriorated to some extent due to the influence of a drug or the like contained in the plaster layer. There was a problem in terms of the stability of the properties of the preparation, and further improvement was desired.
本発明は、上記事情に鑑みなされたものであり、皮膚に十分密着してはがれにくく、貼付感のよい(違和感のない)、かつ支持体の劣化を抑制できる等の製剤の性状安定性に優れる外用貼付剤を提供することを目的とする。 The present invention has been made in view of the above circumstances, and is excellent in property stability of a preparation such as being sufficiently peeled off to the skin, having a good sticking feeling (no discomfort), and capable of suppressing deterioration of the support. An object is to provide an external patch.
本発明者らは、以上の目的を達成するために鋭意研究を行ったところ、支持体としてポリウレタンフィルムを用いること、そして、薬物、及び粘着剤を含有する膏体層に、モノテルペン類を配合することで、皮膚に十分密着してはがれにくく、貼付感のよい(違和感のない)、かつ支持体の劣化を抑制できる等の製剤の性状安定性に優れる外用貼付剤を提供できることを見出し、本発明を完成するに至った。具体的には、本発明は以下のようなものを提供する。 The inventors of the present invention conducted intensive research to achieve the above-mentioned object. As a result, a polyurethane film was used as a support, and monoterpenes were blended into a plaster layer containing a drug and an adhesive. It has been found that the present invention can provide an external patch excellent in property stability of a preparation that is difficult to peel off sufficiently to adhere to the skin, has a good feeling of sticking (no discomfort), and can suppress deterioration of the support. The invention has been completed. Specifically, the present invention provides the following.
(1) 支持体と、この支持体上に積層された膏体層とを備え、
前記支持体は、ポリウレタンフィルムであり、
前記膏体層は、薬物、モノテルペン類、及び粘着剤を含有することを特徴とする外用貼付剤。
(2) 前記支持体は、厚み5〜30μmのポリウレタンフィルムである(1)に記載の外用貼付剤。
(3) 前記支持体と前記膏体層との合計厚みは、10〜60μmである(1)又は(2)に記載の外用貼付剤。
(4) 前記粘着剤は、ゴム系粘着剤、アクリル系粘着剤、及びシリコーン系粘着剤から選択される少なくとも1種である(1)〜(3)のいずれかに記載の外用貼付剤。
(5) 前記粘着剤は、ゴム系粘着剤である(4)に記載の外用貼付剤。
(6) 前記ゴム系粘着剤は、スチレン−イソプレン−スチレンブロック共重合体である(5)に記載の外用貼付剤。
(7) 前記薬物は、非ステロイド性抗炎症剤である(1)〜(6)のいずれかに記載の外用貼付剤。
(8) 前記非ステロイド性抗炎症剤は、フェルビナク、ジクロフェナク、ロキソプロフェン、ケトプロフェン、及びこれらの薬理学的に許容できる塩からなる群から選択される少なくとも1種である(7)に記載の外用貼付剤。
(9) 支持体と、この支持体上に積層された膏体層とを備え、
前記支持体は、厚み5〜30μmのポリウレタンフィルムであり、
前記支持体と前記膏体層との合計厚みは、10〜60μmであり、
前記膏体層は、薬物、l−メントール、及びスチレン−イソプレン−スチレンブロック共重合体を含有し、
前記薬物は、フェルビナク、ジクロフェナク、ロキソプロフェン、ケトプロフェン、及びこれらの薬理学的に許容できる塩からなる群から選択される少なくとも1種であることを特徴とする外用貼付剤。(1) A support and a plaster layer laminated on the support,
The support is a polyurethane film;
The external patch, wherein the paste layer contains a drug, monoterpenes, and an adhesive.
(2) The external patch according to (1), wherein the support is a polyurethane film having a thickness of 5 to 30 μm.
(3) The external patch according to (1) or (2), wherein the total thickness of the support and the plaster layer is 10 to 60 μm.
(4) The adhesive for external use according to any one of (1) to (3), wherein the adhesive is at least one selected from a rubber adhesive, an acrylic adhesive, and a silicone adhesive.
(5) The adhesive for external use according to (4), wherein the adhesive is a rubber adhesive.
(6) The external patch according to (5), wherein the rubber-based adhesive is a styrene-isoprene-styrene block copolymer.
(7) The external patch according to any one of (1) to (6), wherein the drug is a non-steroidal anti-inflammatory agent.
(8) The external patch according to (7), wherein the non-steroidal anti-inflammatory agent is at least one selected from the group consisting of felbinac, diclofenac, loxoprofen, ketoprofen, and pharmacologically acceptable salts thereof. Agent.
(9) A support and a plaster layer laminated on the support,
The support is a polyurethane film having a thickness of 5 to 30 μm,
The total thickness of the support and the plaster layer is 10 to 60 μm,
The plaster layer contains a drug, l-menthol, and a styrene-isoprene-styrene block copolymer,
The external patch, wherein the drug is at least one selected from the group consisting of felbinac, diclofenac, loxoprofen, ketoprofen, and pharmacologically acceptable salts thereof.
本発明によれば、皮膚に十分密着してはがれにくく、貼付感のよい(違和感のない)、かつ支持体の劣化を抑制できる等の製剤の性状安定性に優れる外用貼付剤を提供することができる。 According to the present invention, it is possible to provide an external patch excellent in property stability of a preparation, such as being sufficiently close to the skin and not easily peeled off, having a good patch feeling (no discomfort), and capable of suppressing deterioration of a support. it can.
[外用貼付剤]
本発明の外用貼付剤は、皮膚に貼付するための医薬品、医薬部外品または化粧品として利用できる貼付剤であって、支持体と、この支持体上に積層された膏体層とを備える外用貼付剤である。一般的に、外用貼付剤は、膏体層の含有基剤成分によって、概略、含水系製剤であるパップ剤と、非含水系製剤であるテープ剤に分類できるが、本発明の外用貼付剤は、膏体層の厚みによる皮膚密着性及び貼付性の観点から、テープ剤であることが好ましい。[External patch]
The external patch of the present invention is a patch that can be used as a pharmaceutical, a quasi-drug, or a cosmetic for applying to the skin, and comprises a support and a plaster layer laminated on the support. It is a patch. In general, external patches can be roughly classified into a cataplasm, which is a hydrous preparation, and a tape, which is a non-hydrous preparation, depending on the base component contained in the plaster layer. From the viewpoints of skin adhesion and adhesiveness depending on the thickness of the plaster layer, a tape is preferable.
[支持体]
本発明の支持体には、ポリウレタンフィルムが用いられる。ポリウレタンフィルムは、ジイソシアネートとポリオールとを反応させることによって生成されるポリウレタンエラストマーをフィルム状に成形したものであり、公知の製造方法により製造したものを用いることができる。ポリウレタンフィルムの厚みは、5〜30μmとすることが好ましい。5μmを下まわると、フィルムの製造が困難であったり、支持体として強度が不十分であるからであり、また、30μmを超えると、貼付感(違和感)の観点で十分満足できないからである。本発明の支持体に用いられるポリウレタンフィルムとしては、市販品を用いることができ、例えば、モビロンフィルム(商品名:日清紡ケミカル株式会社)、クランジール(商品名:倉敷紡績株式会社)が挙げられる。このようなウレタンフィルムを用いることで、皮膚に十分密着してはがれにくく、貼付感のよい(違和感のない)外用貼付剤を得ることができる。また、本発明の外用貼付剤は、防水性等の利便性を有し、簡単な入浴も可能となる。[Support]
A polyurethane film is used for the support of the present invention. The polyurethane film is obtained by forming a polyurethane elastomer produced by reacting diisocyanate and polyol into a film, and can be produced by a known production method. The thickness of the polyurethane film is preferably 5 to 30 μm. If the thickness is less than 5 μm, it is difficult to produce a film or the strength is insufficient as a support, and if it exceeds 30 μm, the film cannot be sufficiently satisfied from the viewpoint of sticking feeling (uncomfortable feeling). Commercially available products can be used as the polyurethane film used in the support of the present invention, and examples include Mobilon film (trade name: Nisshinbo Chemical Co., Ltd.) and Klanger (trade name: Kurashiki Spinning Co., Ltd.). By using such a urethane film, it is possible to obtain an external patch with good adhesion feeling (no discomfort) that is not easily peeled off sufficiently to the skin. In addition, the external patch of the present invention has convenience such as waterproofness, and allows simple bathing.
[キャリア層]
なお、本発明の外用貼付剤は、支持体の製膜性、貼付剤の取扱性、被着体への貼付性を向上させる目的で、支持体であるポリウレタンフィルムの片面上に、キャリア層などの付加的な層を設けることができる。この場合、「キャリア層/支持体/膏体層/ライナー」の積層構成を有する貼付剤として作成することができる。キャリア層は、例えば、ポリウレタン、ポリエチレン、ポリプロピレン、アイオノマー、ポリアミド、ポリ塩化ビニル、ポリ塩化ビニリデン、エチレン酢酸ビニル共重合体、熱可塑性ポリエステル、ポリテトラフルオロエチレンなどの各種熱可塑性樹脂からなるフィルムを用いて形成することが好ましい。各種フィルムは、紙にラミネートされた状態のものでもよい。これらのキャリア層は、ポリウレタンエラストマー層に比べて、厚みが厚いか、腰の強いものとすることが望ましい。キャリアの厚みは、適宜設定できるが、通常、10μm以上、好ましくは20μm以上であり、その上限値は500μm程度である。支持体と膏体層とが強固に接着しているため、キャリア層は、使用時に容易に剥離することができる。[Carrier layer]
The external patch of the present invention is a carrier layer or the like on one side of a polyurethane film as a support for the purpose of improving the film forming property of the support, the handleability of the patch, and the adherence to an adherend. Additional layers can be provided. In this case, it can be prepared as a patch having a laminated structure of “carrier layer / support / plaster layer / liner”. For the carrier layer, for example, films made of various thermoplastic resins such as polyurethane, polyethylene, polypropylene, ionomer, polyamide, polyvinyl chloride, polyvinylidene chloride, ethylene vinyl acetate copolymer, thermoplastic polyester, polytetrafluoroethylene, etc. are used. It is preferable to form them. Various films may be laminated on paper. These carrier layers are desirably thicker or stronger than the polyurethane elastomer layer. The thickness of the carrier can be appropriately set, but is usually 10 μm or more, preferably 20 μm or more, and the upper limit is about 500 μm. Since the support and the paste layer are firmly bonded, the carrier layer can be easily peeled off during use.
[膏体層]
本発明の膏体層は、薬物、モノテルペン類、及び粘着剤を含有する。[Plaster layer]
The plaster layer of the present invention contains a drug, monoterpenes, and an adhesive.
[薬物]
本発明に用いる薬物としては、外用剤として使用できる薬物であれば、特に限定されない。例えば、フェルビナク、ジクロフェナク、ロキソプロフェン、ケトプロフェン、インドメタシン、フルルビプロフェン、ピロキシカム、メロキシカム、ケトロラック、フェニルブタゾン、アセチルサリチル酸、フルフェナム酸、メフェナム酸、イブプロフェン、アンフェナク、フェンブフェン、またはこれらの薬理学的に許容できる塩である非ステロイド性抗炎症剤が挙げられる。また、その他の薬物として例えば、酢酸コルチゾン、酢酸デキサメタゾン、デキサメタゾン、酢酸ヒドロコルチゾン、ヒドロコルチゾン、酢酸プレドニゾロン、プレドニゾロン、酪酸ヒドロコルチゾン、吉草酸酢酸プレドニゾロン、塩酸イソチペンジル、クロルフェニラミン、マレイン酸クロルフェニラミン、ジフェンヒドラミン、塩酸ジフェンヒドラミン、クロタミトン、グリチルリチン酸(及びその塩類)、グリチルレチン酸、サリチル酸グリコール、サリチル酸メチル、アラントイン、イソプロピルメチルフェノール、塩化ベンザルコニウム、塩化ベンゼトニウム、カラミン、酸化亜鉛、アミノ安息香酸エチル、オキシポリエトキシドデカン、ジブカイン、塩酸ジブカイン、リドカイン、塩酸リドカイン、アンモニア水、トコフェロール、酢酸トコフェロール、またはパンテノールが挙げられる。好ましくは、前記非ステロイド性抗炎症剤であり、その中でもより好ましくは、フェルビナク、ジクロフェナク、ロキソプロフェン、ケトプロフェン、及びこれらの薬理学的に許容できる塩からなる群より選ばれる少なくとも一種である。薬物の含有量は、特に限定されないが、一般的には膏体全体に対して0.1〜20重量%である。[Drug]
The drug used in the present invention is not particularly limited as long as it can be used as an external preparation. For example, felbinac, diclofenac, loxoprofen, ketoprofen, indomethacin, flurbiprofen, piroxicam, meloxicam, ketorolac, phenylbutazone, acetylsalicylic acid, flufenamic acid, mefenamic acid, ibuprofen, ampenac, fenbufen, or pharmacologically acceptable thereof Non-steroidal anti-inflammatory agents that are possible salts. Other drugs include, for example, cortisone acetate, dexamethasone acetate, dexamethasone, hydrocortisone acetate, hydrocortisone, prednisolone acetate, prednisolone, hydrocortisone butyrate, prednisolone acetate valerate, istipendyl hydrochloride, chlorpheniramine hydrochloride, chlorpheniramine maleate, diphenhydramine, hydrochloric acid Diphenhydramine, crotamiton, glycyrrhizic acid (and its salts), glycyrrhetinic acid, glycol salicylate, methyl salicylate, allantoin, isopropylmethylphenol, benzalkonium chloride, benzethonium chloride, calamine, zinc oxide, ethyl aminobenzoate, oxypolyethoxydodecane, Dibucaine, dibucaine hydrochloride, lidocaine, lidocaine hydrochloride, aqueous ammonia, tocophero , And tocopherol acetate or panthenol, it is. Preferably, the non-steroidal anti-inflammatory agent, more preferably at least one selected from the group consisting of felbinac, diclofenac, loxoprofen, ketoprofen, and pharmacologically acceptable salts thereof. The content of the drug is not particularly limited, but is generally 0.1 to 20% by weight with respect to the entire plaster.
[モノテルペン類]
本発明に係る外用貼付剤は、膏体層にモノテルペン類が含有されている。モノテルペン類を配合することで、薬物及びその溶解剤等の影響によるポリウレタンフィルムの劣化を抑制することができ、さらに、膏体層中で薬物を均一に含有させることができる。すなわち、モノテルペン類を配合することで、薬物を溶解するための溶解剤の使用量を少なくすることができ、さらに、モノテルペン類が薬物の溶解補助剤としても使用可能となるため、ポリウレタンフィルムの劣化が抑制できると同時に、膏体層中の薬物等の析出化を抑制できる。このことにより、製剤の性状安定性に優れる外用貼付剤とすることができる。[Monoterpenes]
The external patch according to the present invention contains monoterpenes in the plaster layer. By blending monoterpenes, the deterioration of the polyurethane film due to the influence of the drug and its solubilizer can be suppressed, and the drug can be uniformly contained in the plaster layer. That is, by blending monoterpenes, the amount of solubilizer used to dissolve the drug can be reduced, and furthermore, the monoterpenes can be used as a drug solubilizing agent. Can be prevented, and at the same time, the precipitation of drugs and the like in the plaster layer can be suppressed. By this, it can be set as the external patch which is excellent in the property stability of a formulation.
本発明に用いるモノテルペン類は、通常医薬品、医薬部外品、化粧品において用いられるモノテルペン類であれば特に制限されないが、例えば、メントール、カンフル、ボルネオール、オイゲノール、シネオール、チモール、ビサボロール、α−ピネン、またはリモネンを例示することができる。好ましくはメントールまたはカンフル、より好ましくはメントールである。これらのモノテルペン類は、天然品、合成品のいずれも利用することができ、d体、l体又はdl体のいずれでもよい。なかでも、l−メントールが好ましい。これらのモノテルペン類は、モノテルペン類を含有する精油として外用貼付剤に使用することもでき、例えば、ユーカリ油、ハッカ油、チョウジ油、ケイヒ油、ペパーミント油、ミント油、ティーツリー油、カモミール油、ローズマリー油、レモン油、オレンジ油、タイム油、セージ油、クローブ油等を例示することができる。好ましくはユーカリ油、ハッカ油またはティーツリー油であり、より好ましくはユーカリ油またはハッカ油等として、外用貼付剤に使用してもよい。これらのモノテルペン類は1種又は2種以上組合わせて用いることもできる。モノテルペン類の含有量は、膏体全重量に対して通常0.001〜20重量%、好ましくは0.001〜10重量%、特に好ましくは0.01〜5重量%の範囲で用いることができる。 Monoterpenes used in the present invention are not particularly limited as long as they are monoterpenes usually used in pharmaceuticals, quasi drugs, and cosmetics. For example, menthol, camphor, borneol, eugenol, cineol, thymol, bisabolol, α- Pinene or limonene can be exemplified. Menthol or camphor is preferable, and menthol is more preferable. These monoterpenes can be used as natural products or synthetic products, and may be d-form, l-form or dl-form. Of these, l-menthol is preferable. These monoterpenes can also be used for external patches as essential oils containing monoterpenes, such as eucalyptus oil, mint oil, clove oil, cinnamon oil, peppermint oil, mint oil, tea tree oil, chamomile Examples thereof include oil, rosemary oil, lemon oil, orange oil, thyme oil, sage oil, and clove oil. Eucalyptus oil, mint oil or tea tree oil is preferable, and eucalyptus oil or mint oil may be used in external patches. These monoterpenes can be used alone or in combination of two or more. The content of monoterpenes is usually 0.001 to 20% by weight, preferably 0.001 to 10% by weight, particularly preferably 0.01 to 5% by weight, based on the total weight of the plaster. it can.
[粘着剤]
本発明に用いる粘着剤としては、ゴム系粘着剤、アクリル系粘着剤、シリコーン系粘着剤等が挙げられる。ゴム系粘着剤としては、天然ゴム、合成ゴム、スチレン−イソプレン−スチレンブロック共重合体、イソプレンゴム、ポリイソブチレン、スチレン−ブタジエン−スチレンブロック共重合体、スチレン−ブタジエンゴム、ポリブテン等が挙げられる。アクリル系粘着剤としては、(メタ)アクリル酸エステルの単独重合体または共重合体及び/又は前記(メタ)アクリル酸アルキルエステルとその他の官能性モノマーとの共重合体等が挙げられる。なお、本明細書においては、「(メタ)アクリル酸」という用語は、アクリル酸又はメタアクリル酸(メタクリル酸)という意味で使用される。したがって、例えば、前記した(メタ)アクリル酸エステルという用語は、アクリル酸エステル又はメタアクリル酸エステルという意味である。シリコーン系粘着剤としては、ポリジメチルシロキサンなどを主成分とするものが挙げられる。これらの粘着剤の中でも、性状、製造時のコスト、品質設計の容易さや、再現性等を考慮して、ゴム系粘着剤が好ましく、その中でもより好ましくは、スチレン−イソプレン−スチレンブロック共重合体である。これらの粘着剤は1種を単独で用いてもよく、2種以上を組み合わせて用いても良い。また、粘着剤の配合量は、膏体層の形成および有効成分の皮膚への透過性を考慮して、膏体層の組成全体の重量を基準として10〜80重量%であることが好ましく、さらに好ましくは20〜40重量%である。[Adhesive]
Examples of the pressure-sensitive adhesive used in the present invention include a rubber-based pressure-sensitive adhesive, an acrylic pressure-sensitive adhesive, and a silicone-based pressure-sensitive adhesive. Examples of the rubber-based pressure-sensitive adhesive include natural rubber, synthetic rubber, styrene-isoprene-styrene block copolymer, isoprene rubber, polyisobutylene, styrene-butadiene-styrene block copolymer, styrene-butadiene rubber, and polybutene. Examples of the acrylic pressure-sensitive adhesive include homopolymers or copolymers of (meth) acrylic acid esters and / or copolymers of the above (meth) acrylic acid alkyl esters and other functional monomers. In the present specification, the term “(meth) acrylic acid” is used to mean acrylic acid or methacrylic acid (methacrylic acid). Thus, for example, the term (meth) acrylic acid ester means acrylic acid ester or methacrylic acid ester. Examples of the silicone-based pressure-sensitive adhesive include those containing polydimethylsiloxane as a main component. Among these pressure-sensitive adhesives, rubber-based pressure-sensitive adhesives are preferable in consideration of properties, manufacturing costs, ease of quality design, reproducibility, etc., and among them, styrene-isoprene-styrene block copolymers are more preferable. It is. These pressure-sensitive adhesives may be used alone or in combination of two or more. The amount of the pressure-sensitive adhesive is preferably 10 to 80% by weight based on the weight of the entire composition of the paste layer in consideration of the formation of the paste layer and the permeability of the active ingredient to the skin. More preferably, it is 20 to 40% by weight.
なお、前記スチレン−イソプレン−スチレンブロック共重合体としては、TR−2000、TR−2003、SIS−5002、5200(商品名:JSR株式会社)、クインタック3421、3520、3530、3570C(商品名:日本ゼオン株式会社)、クレイトンD−KX401CS、D−1107CP、D−1161JP、D−6117(商品名:JSRクレイトンエラストマー株式会社)、ソルプレン428(商品名:フィリップペトロリアム株式会社)等が挙げられ、1種又は2種以上を組合せて使用することができる。 In addition, as said styrene-isoprene-styrene block copolymer, TR-2000, TR-2003, SIS-5002, 5200 (trade name: JSR Corporation), Quintac 3421, 3520, 3530, 3570C (trade name: Zeon Corporation), Clayton D-KX401CS, D-1107CP, D-1161JP, D-6117 (trade name: JSR Kraton Elastomer Co., Ltd.), Sorprene 428 (trade name: Philippe Petroleum Corporation), etc. Species or a combination of two or more can be used.
[厚み]
本発明の支持体と膏体層との合計厚みは、10〜60μmとすることが好ましい。10μmを下まわると、支持体の厚みとの兼ね合いから、膏体層をうまく形成できない問題もあり、また、60μmを超えると、貼付感(違和感)の観点で十分満足できないからである。[Thickness]
The total thickness of the support and plaster layer of the present invention is preferably 10 to 60 μm. If the thickness is less than 10 μm, there is a problem that the plaster layer cannot be formed satisfactorily due to the balance with the thickness of the support, and if it exceeds 60 μm, it is not satisfactory from the viewpoint of sticking feeling (uncomfortable feeling).
[任意成分]
また、本発明の貼付剤の膏体層には、任意成分として、薬物の溶解剤、経皮吸収促進剤、粘着付与剤、可塑剤、賦形剤、抗酸化剤、香料、着色料、水等を含有することができる。[Optional ingredients]
In the plaster layer of the patch of the present invention, as an optional component, a drug solubilizer, a transdermal absorption accelerator, a tackifier, a plasticizer, an excipient, an antioxidant, a fragrance, a colorant, water Etc. can be contained.
(薬物の溶解剤、経皮吸収促進剤)
本発明に用いられる薬物の溶解剤や経皮吸収促進剤としては、脂肪族カルボン酸(酢酸、プロピオン酸、オレイン酸、リノール酸、リノレン酸、イソステアリン酸、ミリスチン酸、ラウリン酸、クエン酸(無水クエン酸を含む)、イソ酪酸、カプロン酸、カプリル酸、乳酸、マレイン酸、ピルビン酸、シュウ酸、コハク酸、酒石酸等)等の有機酸、ポリエチレングリコール(マクロゴールともいう)(平均分子量は200〜30000)、グリセリン、エチレングリコール、ジエチレングリコール等の多価アルコール類、ミリスチン酸イソプロピル、パルミチン酸イソプロピル、アジピン酸ジイソプロピル、セバシン酸ジエチル等の脂肪酸エステル、カプリル酸モノグリセリド、カプリル酸トリグリセリド、ソルビタン脂肪酸エステル等の脂肪酸多価アルコールエステル、N−メチル−2−ピロリドン、クロタミトン等が挙げられる。これらの溶解剤や経皮吸収促進剤は、支持体であるポリウレタンフィルムの劣化に影響する恐れがあるため、できるだけ少ない含有量とすることが好ましい。例えば、10重量%以下とすることが好ましい。(Drug dissolution agent, transdermal absorption enhancer)
Examples of drug solubilizers and transdermal absorption enhancers used in the present invention include aliphatic carboxylic acids (acetic acid, propionic acid, oleic acid, linoleic acid, linolenic acid, isostearic acid, myristic acid, lauric acid, citric acid (anhydrous anhydride). (Including citric acid), organic acids such as isobutyric acid, caproic acid, caprylic acid, lactic acid, maleic acid, pyruvic acid, oxalic acid, succinic acid, tartaric acid), polyethylene glycol (also referred to as macrogol) (average molecular weight is 200) To 30000), polyhydric alcohols such as glycerin, ethylene glycol, diethylene glycol, fatty acid esters such as isopropyl myristate, isopropyl palmitate, diisopropyl adipate, diethyl sebacate, caprylic acid monoglyceride, caprylic acid triglyceride, sorbitan fatty acid ester, etc. Fat Acid polyhydric alcohol ester, N- methyl-2-pyrrolidone, and a crotamiton. Since these solubilizers and percutaneous absorption enhancers may affect the deterioration of the polyurethane film as a support, it is preferable to make the content as small as possible. For example, it is preferably 10% by weight or less.
(粘着付与剤)
本発明に用いられる粘着付与剤としては、特に限定されないが、テルペン樹脂、脂環式飽和炭化水素樹脂(合成石油樹脂)、ロジンエステル誘導体、フェノール樹脂等が挙げられる。テルペン系樹脂としては、例えば、YSレジンPX−1150N(商品名:ヤスハラケミカル株式会社)が挙げられる。脂環式飽和炭化水素樹脂としては、例えば、アルコンP−100(商品名:荒川化学工業株式会社)が挙げられる。ロジンエステル誘導体としては、例えば、エステルガムH(商品名:荒川化学工業株式会社)、KE−311(商品名:荒川化学工業株式会社)、KE−100(商品名:荒川化学工業株式会社)が挙げられる。本発明に用いられる粘着付与剤としては、例えば、これらの1種又は2種以上を選択して使用できる。粘着付与剤の含有量は、特に限定されないが、膏体全体に対して10〜35質量%であることが好ましい。(Tackifier)
Although it does not specifically limit as a tackifier used for this invention, A terpene resin, an alicyclic saturated hydrocarbon resin (synthetic petroleum resin), a rosin ester derivative, a phenol resin, etc. are mentioned. Examples of the terpene resin include YS resin PX-1150N (trade name: Yasuhara Chemical Co., Ltd.). Examples of the alicyclic saturated hydrocarbon resin include Alcon P-100 (trade name: Arakawa Chemical Industries, Ltd.). Examples of rosin ester derivatives include ester gum H (trade name: Arakawa Chemical Industries, Ltd.), KE-311 (trade name: Arakawa Chemical Industries, Ltd.), and KE-100 (trade name: Arakawa Chemical Industries, Ltd.). Can be mentioned. As a tackifier used for this invention, these 1 type (s) or 2 or more types can be selected and used, for example. Although content of a tackifier is not specifically limited, It is preferable that it is 10-35 mass% with respect to the whole plaster.
(可塑剤)
本発明に用いられる可塑剤としては、特に限定されず、例えば、流動パラフィン、オクチルドデカノール等の高級アルコール、スクワラン、スクワレン、ひまし油等が挙げられる。好ましくは、流動パラフィンである。可塑剤の含有量は、特に限定されないが、一般的に膏体全体に対して20〜60重量%である。(Plasticizer)
The plasticizer used in the present invention is not particularly limited, and examples thereof include higher alcohols such as liquid paraffin and octyldodecanol, squalane, squalene and castor oil. Preferably, it is a liquid paraffin. Although content of a plasticizer is not specifically limited, Generally it is 20 to 60 weight% with respect to the whole plaster.
(賦形剤)
本発明に用いられる賦形剤としては、例えば、タルク、無水ケイ酸、軽質無水ケイ酸、含水ケイ酸等のケイ素化合物、エチルセルロース、メチルセルロース、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等のセルロース誘導体、ポリビニルアルコール等の水溶性高分子、乾燥水酸化アルミニウムゲル、含水ケイ酸アルミニウム等のアルミニウム化合物、カオリン、酸化チタン等が挙げられる。(Excipient)
Examples of the excipient used in the present invention include silicon compounds such as talc, silicic anhydride, light anhydrous silicic acid, and hydrous silicic acid, cellulose derivatives such as ethyl cellulose, methyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, and polyvinyl alcohol. Water-soluble polymers such as dry aluminum hydroxide gel, hydrated aluminum silicate such as aluminum silicate, kaolin, titanium oxide and the like.
(抗酸化剤)
本発明に用いられる抗酸化剤としては、例えば、ジブチルヒドロキシトルエン、アスコルビン酸、トコフェロール、トコフェロールエステル誘導体、ブチルヒドロキシアニソール等が挙げられる。(Antioxidant)
Examples of the antioxidant used in the present invention include dibutylhydroxytoluene, ascorbic acid, tocopherol, tocopherol ester derivatives, butylhydroxyanisole and the like.
[ライナー]
本発明の外用貼付剤は、ポリウレタンフィルムである支持体と、この支持体上に膏体が積層された膏体層とを備えるが、通常、膏体層上に剥離可能なライナーを備えた形態で提供される。剥離可能なライナーとしては、ポリエチレン、ポリプロピレン、エチレン酢酸ビニル共重合体、塩化ビニル等のフィルム、アルミニウム蒸着の金属性のフィルム等が使用できる。更に、ライナー表面にシリコン処理等の剥離処理が施されたものを使用してもよい。また、剥離が容易となる点で、ライナーに直線又は曲線状等の切り込み部が設けられていることが好ましく、切れ込み部の設置方式としては、2つの切り込み線を設置して3分割のライナーとしてもよい。[liner]
The external patch of the present invention comprises a support that is a polyurethane film and a paste layer in which a paste is laminated on the support, and usually includes a peelable liner on the paste layer. Provided in. As the releasable liner, polyethylene, polypropylene, ethylene vinyl acetate copolymer, vinyl chloride film, aluminum-deposited metallic film, or the like can be used. Further, a liner surface that has been subjected to a peeling treatment such as a silicon treatment may be used. Moreover, it is preferable that the liner is provided with a cut portion such as a straight line or a curved shape in terms of easy peeling. As the installation method of the cut portion, two cut lines are provided to form a three-part liner. Also good.
[製造方法]
本発明の外用貼付剤の製造方法としては、薬物および基剤成分等膏体層に含ませる成分を加熱溶融させ、この溶融物を剥離ライナー上に展膏し、膏体層を形成した後、支持体を貼り合わせることによって外用貼付剤を得る方法、すなわちホットメルト法を用いることが好ましい。例えば、薬物および基剤成分等膏体層に含ませる成分を酢酸エチル、ヘキサン、トルエン等の有機溶媒に溶解させ、この溶解物を剥離ライナー上に展膏し、該溶解物中の溶媒を留去させ膏体層を形成した後、支持体を貼り合わせることによって外用貼付剤を得る方法、すなわち溶剤法と比べて、膏体層中に、揮発性成分であるモノテルペン類を含有させることが容易であるからである。[Production method]
As a method for producing an external patch of the present invention, the components to be included in the paste layer such as the drug and base component are heated and melted, and the melt is spread on a release liner to form a paste layer. It is preferable to use a method of obtaining an external patch by laminating a support, that is, a hot melt method. For example, the components to be included in the paste layer such as the drug and base component are dissolved in an organic solvent such as ethyl acetate, hexane, and toluene, and this dissolved product is spread on a release liner, and the solvent in the dissolved product is retained. After forming the plaster layer, the method for obtaining an external patch by pasting the support, that is, compared to the solvent method, the plaster layer may contain monoterpenes that are volatile components. This is because it is easy.
以下に実施例を挙げて本発明を具体的に説明するが、本発明はこれらに限定されるものではない。 EXAMPLES The present invention will be specifically described below with reference to examples, but the present invention is not limited to these examples.
以下の組成及び製法により、外用貼付剤を製造した。
(組成)
(1)フェルビナク 3.5重量%
(2)l−メントール 3.0重量%
(日局)
(3)ジブチルヒドロキシトルエン 0.5重量%
(薬添規)
(4)タルク 2.5重量%
(日局)
(5)スチレン−イソプレン−スチレンブロック共重合体 30.0重量%
(薬添規)
(6)テルペン樹脂 17.0重量%
(薬添規)
(7)流動パラフィン 43.5重量%
(日局)
(製法)
前記組成(1)及び(2)を除く各成分を加熱溶融させ、次に(1)及び(2)を加えて混合撹拌し、均一な溶融物とした。この溶融物を1gあたり70cm2の割合でライナー(PETフィルム)に均一に展膏し膏体層を形成した。その後、この膏体層にポリウレタンフィルム(厚さ8μm)を貼り合わせ、本発明の外用貼付剤を得た。なお、ポリウレタンフィルムと膏体層との合計厚みは、20μmであった。An external patch was produced by the following composition and production method.
(composition)
(1) Felbinac 3.5% by weight
(2) 3.0% by weight of 1-menthol
(JP)
(3) Dibutylhydroxytoluene 0.5% by weight
(Medicine regulations)
(4) Talc 2.5% by weight
(JP)
(5) Styrene-isoprene-styrene block copolymer 30.0% by weight
(Medicine regulations)
(6) Terpene resin 17.0% by weight
(Medicine regulations)
(7) Liquid paraffin 43.5% by weight
(JP)
(Manufacturing method)
Each component except the compositions (1) and (2) was heated and melted, and then (1) and (2) were added and mixed and stirred to obtain a uniform melt. This melt was uniformly spread on a liner (PET film) at a rate of 70 cm 2 per gram to form a paste layer. Thereafter, a polyurethane film (thickness: 8 μm) was bonded to the plaster layer to obtain an external patch of the present invention. The total thickness of the polyurethane film and the plaster layer was 20 μm.
以下の処方で上記実施例1の製造方法に準じて本発明の外用貼付剤を製造した。
(1)ケトプロフェン 2.0重量%
(2)l−メントール 2.0重量%
(日局)
(3)ジブチルヒドロキシトルエン 0.5重量%
(薬添規)
(4)スチレン−イソプレン−スチレンブロック共重合体 33.0重量%
(薬添規)
(5)テルペン樹脂 16.0重量%
(薬添規)
(6)スクワラン 3.5重量%
(外原規)
(7)セバシン酸ジエチル 0.5重量%
(薬添規)
(8)流動パラフィン 42.5重量%
(日局)An external patch of the present invention was produced according to the production method of Example 1 with the following formulation.
(1) Ketoprofen 2.0% by weight
(2) 2.0% by weight of 1-menthol
(JP)
(3) Dibutylhydroxytoluene 0.5% by weight
(Medicine regulations)
(4) Styrene-isoprene-styrene block copolymer 33.0% by weight
(Medicine regulations)
(5) Terpene resin 16.0% by weight
(Medicine regulations)
(6) Squalane 3.5% by weight
(External rule)
(7) Diethyl sebacate 0.5 wt%
(Medicine regulations)
(8) Liquid paraffin 42.5% by weight
(JP)
以下の組成及び製法により、外用貼付剤を製造した。
(組成)
(1)ジクロフェナクナトリウム 1.0重量%
(2)l−メントール 2.0重量%
(日局)
(3)ジブチルヒドロキシトルエン 0.5重量%
(薬添規)
(4)スチレン−イソプレン−スチレンブロック共重合体 33.0重量%
(薬添規)
(5)テルペン樹脂 19.0重量%
(薬添規)
(6)合成スクワラン 3.7重量%
(外原規)
(7)タルク 2.5重量%
(日局)
(8)イソステアリン酸 5.0重量%
(薬添規)
(9)流動パラフィン 33.3重量%
(日局)
(製法)
前記組成(1)及び(2)を除く各成分を加熱溶融させ、次に(1)及び(2)を加えて混合撹拌し、均一な溶融物とした。この溶融物を1.5gあたり70cm2の割合でライナー(PETフィルム)に均一に展膏し膏体層を形成した。その後、この膏体層にポリウレタンフィルム(厚さ8μm)を貼り合わせ、本発明の外用貼付剤を得た。なお、ポリウレタンフィルムと膏体層との合計厚みは、20μmであった。An external patch was produced by the following composition and production method.
(composition)
(1) Diclofenac sodium 1.0% by weight
(2) 2.0% by weight of 1-menthol
(JP)
(3) Dibutylhydroxytoluene 0.5% by weight
(Medicine regulations)
(4) Styrene-isoprene-styrene block copolymer 33.0% by weight
(Medicine regulations)
(5) Terpene resin 19.0% by weight
(Medicine regulations)
(6) Synthetic squalane 3.7% by weight
(Norimoto)
(7) Talc 2.5% by weight
(JP)
(8) Isostearic acid 5.0% by weight
(Medicine regulations)
(9) Liquid paraffin 33.3% by weight
(JP)
(Manufacturing method)
Each component except the compositions (1) and (2) was heated and melted, and then (1) and (2) were added and mixed and stirred to obtain a uniform melt. This melt was uniformly spread on a liner (PET film) at a rate of 70 cm 2 per 1.5 g to form a paste layer. Thereafter, a polyurethane film (thickness: 8 μm) was bonded to the plaster layer to obtain an external patch of the present invention. The total thickness of the polyurethane film and the plaster layer was 20 μm.
以下の処方で上記実施例1の製造方法に準じて本発明の外用貼付剤を製造した。
(1)ロキソプロフェンナトリウム2水和物 5.67重量%
(2)l−メントール 3.00重量%
(日局)
(3)イソステアリン酸 5.00重量%
(薬添規)
(4)ジブチルヒドロキシトルエン 0.20重量%
(薬添規)
(5)タルク 2.50重量%
(日局)
(6)スチレン−イソプレン−スチレンブロック共重合体 30.00重量%
(薬添規)
(7)テルペン樹脂 18.00重量%
(薬添規)
(8)流動パラフィン 35.63重量%
(日局)An external patch of the present invention was produced according to the production method of Example 1 with the following formulation.
(1) Loxoprofen sodium dihydrate 5.67% by weight
(2) l-Menthol 3.00% by weight
(JP)
(3) Isostearic acid 5.00% by weight
(Medicine regulations)
(4) Dibutylhydroxytoluene 0.20% by weight
(Medicine regulations)
(5) Talc 2.50% by weight
(JP)
(6) Styrene-isoprene-styrene block copolymer 30.00% by weight
(Medicine regulations)
(7) Terpene resin 18.00% by weight
(Medicine regulations)
(8) Liquid paraffin 35.63 wt%
(JP)
以下の処方で上記実施例1の製造方法に準じて本発明の外用貼付剤を製造した。
(1)ロキソプロフェンナトリウム2水和物 5.67重量%
(2)l−メントール 3.00重量%
(日局)
(3)イソステアリン酸 5.00重量%
(薬添規)
(4)マクロゴール300 2.50重量%
(薬添規)
(5)ジブチルヒドロキシトルエン 0.20重量%
(薬添規)
(6)タルク 2.50重量%
(日局)
(7)スチレン−イソプレン−スチレンブロック共重合体 30.00重量%
(薬添規)
(8)テルペン樹脂 18.00重量%
(薬添規)
(9)流動パラフィン 33.13重量%
(日局)An external patch of the present invention was produced according to the production method of Example 1 with the following formulation.
(1) Loxoprofen sodium dihydrate 5.67% by weight
(2) l-Menthol 3.00% by weight
(JP)
(3) Isostearic acid 5.00% by weight
(Medicine regulations)
(4) Macrogol 300 2.50% by weight
(Medicine regulations)
(5) Dibutylhydroxytoluene 0.20% by weight
(Medicine regulations)
(6) Talc 2.50% by weight
(JP)
(7) Styrene-isoprene-styrene block copolymer 30.00% by weight
(Medicine regulations)
(8) Terpene resin 18.00% by weight
(Medicine regulations)
(9) Liquid paraffin 33.13 wt%
(JP)
以下の処方で上記実施例1の製造方法に準じて本発明の外用貼付剤を製造した。
(1)ロキソプロフェンナトリウム2水和物 5.67重量%
(2)l−メントール 3.00重量%
(日局)
(3)イソステアリン酸 5.00重量%
(薬添規)
(4)セバシン酸ジイソプロピル 5.00重量%
(薬添規)
(5)ジブチルヒドロキシトルエン 0.50重量%
(薬添規)
(6)タルク 2.50重量%
(日局)
(7)スチレン−イソプレン−スチレンブロック共重合体 32.00重量%
(薬添規)
(8)テルペン樹脂 19.00重量%
(薬添規)
(9)流動パラフィン 27.33重量%
(日局)An external patch of the present invention was produced according to the production method of Example 1 with the following formulation.
(1) Loxoprofen sodium dihydrate 5.67% by weight
(2) l-Menthol 3.00% by weight
(JP)
(3) Isostearic acid 5.00% by weight
(Medicine regulations)
(4) Diisopropyl sebacate 5.00% by weight
(Medicine regulations)
(5) Dibutylhydroxytoluene 0.50% by weight
(Medicine regulations)
(6) Talc 2.50% by weight
(JP)
(7) Styrene-isoprene-styrene block copolymer 32.00% by weight
(Medicine regulations)
(8) Terpene resin 19.00% by weight
(Medicine regulations)
(9) Liquid paraffin 27.33% by weight
(JP)
<比較例1>
l−メントールを加えず、流動パラフィンを46.5重量%配合したことを除き、実施例1と同様の手順で外用貼付剤を製造した。<Comparative Example 1>
An external patch was prepared in the same procedure as in Example 1 except that 1-menthol was not added and 46.5% by weight of liquid paraffin was blended.
<比較例2>
l−メントールを加えず、N−メチル−2−ピロリドンを10重量%配合し、流動パラフィンを36.5重量%配合したことを除き、実施例1と同様の手順で外用貼付剤を製造した。<Comparative Example 2>
An external patch was produced in the same manner as in Example 1 except that 10% by weight of N-methyl-2-pyrrolidone was added and 16.5% by weight of liquid paraffin was added without adding 1-menthol.
<比較例3>
支持体として、ポリウレタンフィルムのかわりに、厚み500μm、目付100g/m2のポリエステル編布を用いたことを除き、実施例3と同様の手順で外用貼付剤を製造した。<Comparative Example 3>
An external patch was produced in the same procedure as in Example 3, except that a polyester knitted fabric having a thickness of 500 μm and a weight per unit area of 100 g / m 2 was used in place of the polyurethane film.
<評価>
上記実施例1、実施例3、及び比較例1〜3で製造した外用貼付剤について、製剤の性状安定性(膏体層、支持体)、密着性、使用感を評価した。<Evaluation>
About the external patch manufactured in the said Example 1, Example 3, and Comparative Examples 1-3, the property stability (plaster layer, support body), adhesiveness, and usability | use_condition of a formulation were evaluated.
[試験例1(製剤の性状安定性(膏体層))]
実施例1及び比較例1で製造した外用貼付剤(7×10cm)を、直ちにアルミラミネート包装袋に密封したのち、40℃で10日間保存した。その後、下記基準に基づいて、膏体層中の析出物の有無を目視で観察評価した。この結果を表1に示す。
「析出物有無の評価基準」
○:析出物無し。
×:析出物有り。[Test Example 1 (Property stability of formulation (plaster layer))]
The external patch (7 × 10 cm) produced in Example 1 and Comparative Example 1 was immediately sealed in an aluminum laminate packaging bag and then stored at 40 ° C. for 10 days. Thereafter, the presence or absence of precipitates in the plaster layer was visually observed and evaluated based on the following criteria. The results are shown in Table 1.
"Evaluation criteria for the presence or absence of precipitates"
○: No precipitate.
X: Precipitation exists.
[試験例2(製剤の性状安定性(支持体))]
実施例1及び比較例2で製造した外用貼付剤(7×10cm)を、直ちにアルミラミネート包装袋に密封したのち、40℃で10日間保存した。その後、各外用貼付剤を被験者の腕に貼付した。下記基準に基づいて、支持体(ポリウレタンフィルム)の劣化の有無を目視で観察評価した。この結果を表2に示す。
「支持体の劣化有無の評価基準」
○:問題なく貼付できた。
×:貼付剤が破れて貼付できなかった。[Test Example 2 (Property stability of preparation (support))]
The external patch (7 × 10 cm) produced in Example 1 and Comparative Example 2 was immediately sealed in an aluminum laminate packaging bag and then stored at 40 ° C. for 10 days. Thereafter, each external patch was applied to the subject's arm. Based on the following criteria, the presence or absence of deterioration of the support (polyurethane film) was visually observed and evaluated. The results are shown in Table 2.
"Evaluation criteria for deterioration of support"
○: Attached without problems.
X: The patch was torn and could not be applied.
[試験例3(密着性、使用感)]
実施例3及び比較例3で製造した外用貼付剤(7×10cm)を、被験者の膝に8時間貼付した(勤務時間中において、膝の曲げ伸ばしの制限なし)。下記基準に基づいて、密着性、使用感を評価した。この結果を表3に示す。
「密着性、使用感の評価基準」
○:貼付剤が皮膚表面になじんで、違和感を感じなかった。
×:貼付剤が皮膚表面になじまず、違和感を感じた。[Test Example 3 (Adhesion, Usability)]
The external patch (7 × 10 cm) produced in Example 3 and Comparative Example 3 was applied to the subject's knee for 8 hours (no restriction on bending and stretching of the knee during working hours). Based on the following criteria, adhesion and usability were evaluated. The results are shown in Table 3.
"Evaluation criteria for adhesion and usability"
○: The patch was familiar with the skin surface and did not feel uncomfortable.
X: The patch did not conform to the skin surface, and a sense of incongruity was felt.
本発明の外用貼付剤は、皮膚に十分密着してはがれにくく、貼付感のよい(違和感のない)、かつ支持体の劣化を抑制できる等の製剤の性状安定性に優れる製剤であることから、外用医薬品として好適に利用可能である。 The external patch of the present invention is a preparation that is excellent in property stability of the preparation, such as it is difficult to peel off sufficiently to the skin, has a good sticking feeling (no discomfort), and can suppress deterioration of the support. It can be suitably used as an external medicine.
Claims (2)
前記支持体は、厚み5〜30μmのポリウレタンフィルムであり、The support is a polyurethane film having a thickness of 5 to 30 μm,
前記支持体と前記膏体層との合計厚みは、10〜60μmであり、The total thickness of the support and the plaster layer is 10 to 60 μm,
前記膏体層は、薬物、l−メントール、及びスチレン−イソプレン−スチレンブロック共The plaster layer comprises a drug, 1-menthol, and a styrene-isoprene-styrene block. 重合体を含有し、Containing a polymer,
前記薬物は、フェルビナク、ジクロフェナク、ロキソプロフェン、ケトプロフェン、及びThe drugs are felbinac, diclofenac, loxoprofen, ketoprofen, and これらの薬理学的に許容できる塩からなる群から選択される少なくとも1種であることをIt is at least one selected from the group consisting of these pharmacologically acceptable salts. 特徴とする外用貼付剤。A featured external patch.
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JP2011253250A JP5842304B2 (en) | 2011-11-01 | 2011-11-01 | External patch |
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US8158145B2 (en) * | 2002-02-19 | 2012-04-17 | Hisamitsu Pharmaceutical Co., Inc. | Percutaneous absorption type plaster |
JP3668728B2 (en) * | 2002-08-26 | 2005-07-06 | 祐徳薬品工業株式会社 | External patch and method for inhibiting esterification of drug in external patch |
JP4650613B2 (en) * | 2004-10-08 | 2011-03-16 | ライオン株式会社 | Patch |
JP5581080B2 (en) * | 2009-03-19 | 2014-08-27 | 共立薬品工業株式会社 | External patch |
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