JPH04244019A - Patch for medical application - Google Patents
Patch for medical applicationInfo
- Publication number
- JPH04244019A JPH04244019A JP3184891A JP3184891A JPH04244019A JP H04244019 A JPH04244019 A JP H04244019A JP 3184891 A JP3184891 A JP 3184891A JP 3184891 A JP3184891 A JP 3184891A JP H04244019 A JPH04244019 A JP H04244019A
- Authority
- JP
- Japan
- Prior art keywords
- support
- moisture permeability
- patch
- laminated
- medical patch
- 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
- 239000000463 material Substances 0.000 claims abstract description 49
- 239000003814 drug Substances 0.000 claims abstract description 31
- 230000035699 permeability Effects 0.000 claims abstract description 31
- 239000000126 substance Substances 0.000 claims abstract description 17
- 238000010521 absorption reaction Methods 0.000 claims abstract description 15
- 229940079593 drug Drugs 0.000 claims description 28
- 239000002998 adhesive polymer Substances 0.000 claims description 16
- 239000008280 blood Substances 0.000 abstract description 11
- 210000004369 blood Anatomy 0.000 abstract description 11
- 229920000642 polymer Polymers 0.000 abstract description 3
- 230000007794 irritation Effects 0.000 abstract description 2
- 239000000758 substrate Substances 0.000 abstract 1
- 239000010410 layer Substances 0.000 description 25
- 210000003491 skin Anatomy 0.000 description 19
- 206010040880 Skin irritation Diseases 0.000 description 10
- 239000000853 adhesive Substances 0.000 description 10
- 230000001070 adhesive effect Effects 0.000 description 10
- 230000036556 skin irritation Effects 0.000 description 10
- 231100000475 skin irritation Toxicity 0.000 description 10
- 230000000694 effects Effects 0.000 description 7
- 238000010030 laminating Methods 0.000 description 6
- 238000000034 method Methods 0.000 description 6
- 230000000144 pharmacologic effect Effects 0.000 description 6
- -1 polytetrafluoroethylene Polymers 0.000 description 6
- 229920003169 water-soluble polymer Polymers 0.000 description 5
- 239000004372 Polyvinyl alcohol Substances 0.000 description 4
- MOYKHGMNXAOIAT-JGWLITMVSA-N isosorbide dinitrate Chemical compound [O-][N+](=O)O[C@H]1CO[C@@H]2[C@H](O[N+](=O)[O-])CO[C@@H]21 MOYKHGMNXAOIAT-JGWLITMVSA-N 0.000 description 4
- 239000002861 polymer material Substances 0.000 description 4
- 229920002451 polyvinyl alcohol Polymers 0.000 description 4
- 238000002360 preparation method Methods 0.000 description 4
- ZFXYFBGIUFBOJW-UHFFFAOYSA-N theophylline Chemical compound O=C1N(C)C(=O)N(C)C2=C1NC=N2 ZFXYFBGIUFBOJW-UHFFFAOYSA-N 0.000 description 4
- 208000010201 Exanthema Diseases 0.000 description 3
- NIXOWILDQLNWCW-UHFFFAOYSA-N acrylic acid group Chemical group C(C=C)(=O)O NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 3
- 229910001429 cobalt ion Inorganic materials 0.000 description 3
- XLJKHNWPARRRJB-UHFFFAOYSA-N cobalt(2+) Chemical compound [Co+2] XLJKHNWPARRRJB-UHFFFAOYSA-N 0.000 description 3
- 238000002845 discoloration Methods 0.000 description 3
- 229920001971 elastomer Polymers 0.000 description 3
- 201000005884 exanthem Diseases 0.000 description 3
- 229920001343 polytetrafluoroethylene Polymers 0.000 description 3
- 239000004810 polytetrafluoroethylene Substances 0.000 description 3
- 206010037844 rash Diseases 0.000 description 3
- 239000005060 rubber Substances 0.000 description 3
- 230000001225 therapeutic effect Effects 0.000 description 3
- GOXQRTZXKQZDDN-UHFFFAOYSA-N 2-Ethylhexyl acrylate Chemical compound CCCCC(CC)COC(=O)C=C GOXQRTZXKQZDDN-UHFFFAOYSA-N 0.000 description 2
- 229920002799 BoPET Polymers 0.000 description 2
- KAKZBPTYRLMSJV-UHFFFAOYSA-N Butadiene Chemical compound C=CC=C KAKZBPTYRLMSJV-UHFFFAOYSA-N 0.000 description 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- 239000012790 adhesive layer Substances 0.000 description 2
- 229920000233 poly(alkylene oxides) Polymers 0.000 description 2
- 229920000139 polyethylene terephthalate Polymers 0.000 description 2
- 239000005020 polyethylene terephthalate Substances 0.000 description 2
- 229920001296 polysiloxane Polymers 0.000 description 2
- 210000000434 stratum corneum Anatomy 0.000 description 2
- 229960000278 theophylline Drugs 0.000 description 2
- 238000002560 therapeutic procedure Methods 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 description 1
- HFCUBKYHMMPGBY-UHFFFAOYSA-N 2-methoxyethyl prop-2-enoate Chemical compound COCCOC(=O)C=C HFCUBKYHMMPGBY-UHFFFAOYSA-N 0.000 description 1
- ROGIWVXWXZRRMZ-UHFFFAOYSA-N 2-methylbuta-1,3-diene;styrene Chemical compound CC(=C)C=C.C=CC1=CC=CC=C1 ROGIWVXWXZRRMZ-UHFFFAOYSA-N 0.000 description 1
- 244000215068 Acacia senegal Species 0.000 description 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 description 1
- 239000005977 Ethylene Substances 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- 229920000084 Gum arabic Polymers 0.000 description 1
- 244000043261 Hevea brasiliensis Species 0.000 description 1
- 239000004952 Polyamide Substances 0.000 description 1
- 239000004698 Polyethylene Substances 0.000 description 1
- 229920002367 Polyisobutene Polymers 0.000 description 1
- 229920001328 Polyvinylidene chloride Polymers 0.000 description 1
- 229920002125 Sokalan® Polymers 0.000 description 1
- XTXRWKRVRITETP-UHFFFAOYSA-N Vinyl acetate Chemical compound CC(=O)OC=C XTXRWKRVRITETP-UHFFFAOYSA-N 0.000 description 1
- QYKIQEUNHZKYBP-UHFFFAOYSA-N Vinyl ether Chemical compound C=COC=C QYKIQEUNHZKYBP-UHFFFAOYSA-N 0.000 description 1
- 239000000205 acacia gum Substances 0.000 description 1
- 235000010489 acacia gum Nutrition 0.000 description 1
- 229920000800 acrylic rubber Polymers 0.000 description 1
- 229940035674 anesthetics Drugs 0.000 description 1
- 230000000954 anitussive effect Effects 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 230000003474 anti-emetic effect Effects 0.000 description 1
- 230000003556 anti-epileptic effect Effects 0.000 description 1
- 230000003276 anti-hypertensive effect Effects 0.000 description 1
- 229940088710 antibiotic agent Drugs 0.000 description 1
- 239000001961 anticonvulsive agent Substances 0.000 description 1
- 239000000935 antidepressant agent Substances 0.000 description 1
- 229940005513 antidepressants Drugs 0.000 description 1
- 229940125683 antiemetic agent Drugs 0.000 description 1
- 239000002111 antiemetic agent Substances 0.000 description 1
- 229960003965 antiepileptics Drugs 0.000 description 1
- 229940121375 antifungal agent Drugs 0.000 description 1
- 229940125715 antihistaminic agent Drugs 0.000 description 1
- 239000000739 antihistaminic agent Substances 0.000 description 1
- 239000002220 antihypertensive agent Substances 0.000 description 1
- 229940030600 antihypertensive agent Drugs 0.000 description 1
- 239000002246 antineoplastic agent Substances 0.000 description 1
- 239000003434 antitussive agent Substances 0.000 description 1
- 229940124584 antitussives Drugs 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 238000005266 casting Methods 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- GVPFVAHMJGGAJG-UHFFFAOYSA-L cobalt dichloride Chemical compound [Cl-].[Cl-].[Co+2] GVPFVAHMJGGAJG-UHFFFAOYSA-L 0.000 description 1
- 229920001577 copolymer Polymers 0.000 description 1
- 239000003218 coronary vasodilator agent Substances 0.000 description 1
- 239000003246 corticosteroid Substances 0.000 description 1
- 229960001334 corticosteroids Drugs 0.000 description 1
- 238000004132 cross linking Methods 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 239000002934 diuretic Substances 0.000 description 1
- 229940030606 diuretics Drugs 0.000 description 1
- 238000002651 drug therapy Methods 0.000 description 1
- 239000002532 enzyme inhibitor Substances 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 239000003193 general anesthetic agent Substances 0.000 description 1
- 239000003163 gonadal steroid hormone Substances 0.000 description 1
- 230000036571 hydration Effects 0.000 description 1
- 238000006703 hydration reaction Methods 0.000 description 1
- 229960000201 isosorbide dinitrate Drugs 0.000 description 1
- 229920000126 latex Polymers 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 230000005923 long-lasting effect Effects 0.000 description 1
- 239000002184 metal Substances 0.000 description 1
- 229910052751 metal Inorganic materials 0.000 description 1
- 239000000178 monomer Substances 0.000 description 1
- 229920003052 natural elastomer Polymers 0.000 description 1
- 229920001194 natural rubber Polymers 0.000 description 1
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 229920000058 polyacrylate Polymers 0.000 description 1
- 239000004584 polyacrylic acid Substances 0.000 description 1
- 229920002647 polyamide Polymers 0.000 description 1
- 229920000728 polyester Polymers 0.000 description 1
- 229920000573 polyethylene Polymers 0.000 description 1
- 229920002338 polyhydroxyethylmethacrylate Polymers 0.000 description 1
- 229920001195 polyisoprene Polymers 0.000 description 1
- 238000006116 polymerization reaction Methods 0.000 description 1
- 229920000098 polyolefin Polymers 0.000 description 1
- 229920001184 polypeptide Polymers 0.000 description 1
- 229920002635 polyurethane Polymers 0.000 description 1
- 239000004814 polyurethane Substances 0.000 description 1
- 229920000915 polyvinyl chloride Polymers 0.000 description 1
- 239000004800 polyvinyl chloride Substances 0.000 description 1
- 239000005033 polyvinylidene chloride Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 230000003449 preventive effect Effects 0.000 description 1
- 102000004196 processed proteins & peptides Human genes 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- 238000007127 saponification reaction Methods 0.000 description 1
- 230000001932 seasonal effect Effects 0.000 description 1
- 239000013464 silicone adhesive Substances 0.000 description 1
- 229920002379 silicone rubber Polymers 0.000 description 1
- 239000004945 silicone rubber Substances 0.000 description 1
- 239000002356 single layer Substances 0.000 description 1
- 229920006132 styrene block copolymer Polymers 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 229920003051 synthetic elastomer Polymers 0.000 description 1
- 239000005061 synthetic rubber Substances 0.000 description 1
- 239000003204 tranquilizing agent Substances 0.000 description 1
- 230000002936 tranquilizing effect Effects 0.000 description 1
- 230000005068 transpiration Effects 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 230000002087 whitening effect Effects 0.000 description 1
Abstract
Description
【０００１】0001
【産業上の利用分野】本発明は医療用貼付剤に関し、詳
しくは皮膚貼付時の皮膚刺激を軽減しつつ、薬物を効率
よく経皮吸収できる医療用貼付剤に関する。BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a medical patch, and more particularly to a medical patch that can efficiently absorb drugs transdermally while reducing skin irritation when applied to the skin.
【０００２】0002
【従来の技術】近年、薬物を生体内に投与する製剤とし
て経皮吸収投与製剤が種々開発されており、その中でも
取扱い性や厳格な投与量の管理の点から貼付剤が注目さ
れている。貼付剤は薬物の血中濃度が有効治療域内に長
時間維持できること（効果の持続性）が他の製剤と比べ
て優れた特徴の一つである。また、薬物治療においては
血中濃度が速やかに有効治療領域内に到達すること（速
効性）も重要な要求特性ではあるが、上記持続性と速効
性を兼備する貼付剤の開発品が数少ないのが実情である
。BACKGROUND OF THE INVENTION In recent years, various transdermal absorption preparations have been developed as preparations for administering drugs into living bodies, and among these, patches have attracted attention from the viewpoint of ease of handling and strict control of dosage. One of the superior features of patches compared to other preparations is that the blood concentration of the drug can be maintained within the effective therapeutic range for a long period of time (durability of effect). In addition, in drug therapy, an important characteristic required is that the blood concentration quickly reach the effective therapeutic range (fast-acting), but there are only a few developed patches that have both the above-mentioned long-lasting and quick-acting properties. is the reality.
【０００３】上記貼付剤の基本構造は通常、不透湿性の
支持体と薬物を含有する粘着性の高分子物質層との積層
体であり、支持体の積層による密封包帯療法（ＯＤＴ）
にて薬物の経皮吸収性を向上させている。しかしながら
、ＯＤＴは所謂、皮膚面をムレさせて皮膚の角質層をル
ーズさせる療法であるので皮膚面に刺激が生じやすくな
り、薬物の経皮吸収性は良好となるが皮膚刺激を起こし
やすくなるという問題を有する。[0003] The basic structure of the above-mentioned patch is usually a laminate of a moisture-impermeable support and an adhesive polymer layer containing a drug, and occlusive dressing therapy (ODT) is achieved by laminating the support.
This improves the transdermal absorption of drugs. However, ODT is a therapy that loosens the stratum corneum of the skin by making the skin stuffy, so it tends to irritate the skin, and although the transdermal absorption of the drug is good, it tends to cause skin irritation. have a problem
【０００４】一方、支持体を透湿性の高い支持体として
皮膚刺激を抑制する製剤も提案されているが、ＯＤＴが
充分に行えないこともあり、速効性を期待できない場合
があり、時には有効治療域の薬物の血中濃度に達しない
こともある。On the other hand, preparations that suppress skin irritation by using a support with high moisture permeability have been proposed, but ODT may not be able to be performed sufficiently, and quick effects may not be expected, and sometimes effective treatment may not be possible. The blood concentration of the drug within the range may not be reached.
【０００５】[0005]
【発明が解決しようとする課題】従って、本発明は上記
従来の薬物を経皮吸収させるための貼付剤が有する欠点
を解決し、薬物をできるだけ速やかに生体内に移行させ
て長期間にわたって持続的に薬物の有効血中濃度を維持
でき、しかも皮膚に対する刺激を抑制できる医療用貼付
剤を提供することを目的とする。SUMMARY OF THE INVENTION Therefore, the present invention solves the above-mentioned drawbacks of conventional patches for transdermal absorption of drugs, and allows drugs to be transferred into the body as quickly as possible to maintain a sustained state over a long period of time. An object of the present invention is to provide a medical patch that can maintain an effective blood concentration of a drug and suppress irritation to the skin.
【０００６】[0006]
【課題を解決するための手段】そこで、本発明者らは上
記目的を達成するために鋭意検討を重ねた結果、特定の
透湿度以上を有する支持体に薬物を含有した粘着性高分
子物質層を形成し、上記支持体の他面に透湿性の低いカ
バー材を剥離が容易な状態で積層することによって、上
記目的が達成できることを見いだし、本発明を完成する
に至った。[Means for Solving the Problems] Therefore, the present inventors have made extensive studies to achieve the above object, and as a result, have developed an adhesive polymer material layer containing a drug on a support having a moisture permeability above a specific level. The inventors have discovered that the above object can be achieved by laminating a cover material with low moisture permeability on the other surface of the support in an easily peelable state, and have completed the present invention.
【０００７】即ち、本発明は高透湿性を有する支持体の
片面に経皮吸収用薬物を含有する粘着性高分子物質層が
積層され、他面には透湿度が２５０ｇ／ｍ２ ／２４ｈ
以下の低透湿性カバー材が剥離容易な状態にて積層され
ていることを特徴とする医療用貼付剤を提供するもので
ある。That is, in the present invention, an adhesive polymer material layer containing a drug for transdermal absorption is laminated on one side of a support having high moisture permeability, and the other side has a moisture permeability of 250 g/m2/24 h.
The present invention provides a medical patch characterized in that the following low moisture permeability cover material is laminated in an easily peelable state.
【０００８】本発明に用いる支持体は比較的高い透湿性
を有するものであって、皮膚面の動きに対する追従性の
点からは柔軟性を有するものが好ましい。このような支
持体の材質としては、例えばポリオレフィン、ポリエス
テル、ポリビニルアルコール、ポリウレタン、ポリ塩化
ビニル、ポリ塩化ビニリデン、ポリアミド、ポリテトラ
フルオロエチレンなどが挙げられ、フィルム状や織物状
、不織布状、多孔質状にして用いる。これらの支持体は
単層でも積層してもよく、また、金属蒸着体としてもよ
い。なお、支持体の材質自体に高い透湿性がない場合は
、穿孔処理を施すなどして支持体としての透湿性を付与
することもできる。また、支持体の厚みも高い透湿性を
有するものであれば、特に制限はないが、通常５〜１０
００μｍ程度とする。[0008] The support used in the present invention has relatively high moisture permeability, and is preferably flexible in terms of its ability to follow the movement of the skin surface. Examples of the material for such a support include polyolefin, polyester, polyvinyl alcohol, polyurethane, polyvinyl chloride, polyvinylidene chloride, polyamide, polytetrafluoroethylene, etc.; It is used in the form of These supports may be a single layer or a laminate, or may be a metal vapor deposited body. Note that if the material of the support itself does not have high moisture permeability, perforation treatment may be performed to impart moisture permeability to the support. In addition, the thickness of the support is not particularly limited as long as it has high moisture permeability, but it is usually 5 to 10
It is set to about 00 μm.
【０００９】上記支持体の片面に形成される粘着性高分
子物質層は、生体内へ投与する経皮吸収用の薬物を含有
保持するものであって、薬物を貯蔵・保持する機能と、
薬物を皮膚面に放出する機能、皮膚面への接着機能を兼
ね備えたものである。この層を形成する高分子物質は例
えば、シリコーンゴム、ポリイソブチレンゴム、ポリイ
ソプレンゴム、スチレン−イソプレン（またはブタジエ
ン）−スチレンブロック共重合体ゴム、アクリルゴム、
アラビアゴムのような合成ゴムや天然ゴム類、（メタ）
アクリル酸アルキルエステルを主成分モノマーとして重
合したアクリル系粘着剤、ビニルエーテル系粘着剤、シ
リコーン系粘着剤などの粘着剤を用いることができる。
さらに、これらの粘着剤には凝集力の調整のために各種
液状物質を添加したり、これに架橋処理を施すなどの手
段を講じてもよい。The adhesive polymer material layer formed on one side of the support contains and retains a drug for transdermal absorption to be administered into a living body, and has the function of storing and retaining the drug;
It has both the function of releasing drugs to the skin surface and the function of adhesion to the skin surface. Examples of the polymeric substances forming this layer include silicone rubber, polyisobutylene rubber, polyisoprene rubber, styrene-isoprene (or butadiene)-styrene block copolymer rubber, acrylic rubber,
Synthetic rubbers such as gum arabic and natural rubbers, (meth)
Adhesives such as acrylic adhesives, vinyl ether adhesives, silicone adhesives, etc., which are polymerized using an acrylic acid alkyl ester as a main monomer can be used. Furthermore, measures such as adding various liquid substances to these adhesives or subjecting them to crosslinking treatment may be taken in order to adjust the cohesive force.
【００１０】経皮吸収用薬物としては、生体内に薬物を
経皮投与して各種疾患の治療や予防効果を発揮するもの
であって、その種類には限定されない。例えば薬理効果
別に例示すると、コルチコステロイド類、消炎鎮痛剤、
催眠鎮静剤、精神安定剤、抗高血圧剤、降圧利尿剤、抗
生物質、麻酔剤、抗真菌剤、ビタミン剤、抗てんかん剤
、冠血管拡張剤、抗ヒスタミン剤、鎮咳剤、性ホルモン
剤、抗鬱剤、脳循環改善剤、制吐剤、抗腫瘍剤、酵素阻
害剤、生体医薬（ポリペプチド）などを用いることがで
きる。上記高分子物質層中でのこれらの薬物の含有量は
、薬理効果や使用目的に応じて任意に設定できる。[0010] Drugs for transdermal absorption are drugs that are administered transdermally into living bodies to exert therapeutic or preventive effects on various diseases, and are not limited to the type. Examples of pharmacological effects include corticosteroids, anti-inflammatory analgesics,
Hypnosedatives, tranquilizers, antihypertensives, antihypertensive diuretics, antibiotics, anesthetics, antifungals, vitamins, antiepileptics, coronary vasodilators, antihistamines, antitussives, sex hormones, antidepressants, brain Circulation improvers, antiemetics, antitumor agents, enzyme inhibitors, biomedicines (polypeptides), and the like can be used. The content of these drugs in the polymeric material layer can be arbitrarily set depending on the pharmacological effect and purpose of use.
【００１１】本発明の医療用貼付剤においては、上記支
持体の片面に経皮吸収用薬物を含有する粘着性高分子物
質層が積層された状態の貼付剤は透湿性が高く、皮膚刺
激を抑制するうえで重要な役割を果たす。この構成の貼
付剤としての透湿度は、好ましくは３５０ｇ／ｍ２ ／
２４ｈ以上、さらに好ましくは５００ｇ／ｍ２ ／２４
ｈ以上とすることが、皮膚面へ長時間貼付した際の皮膚
刺激を低減する上で好ましい。[0011] In the medical patch of the present invention, the patch in which an adhesive polymer material layer containing a drug for transdermal absorption is laminated on one side of the support has high moisture permeability and does not cause skin irritation. plays an important role in suppressing The moisture permeability of a patch with this configuration is preferably 350 g/m2/
24 hours or more, more preferably 500g/m2/24
It is preferable to set it to h or more in order to reduce skin irritation when it is attached to the skin surface for a long time.
【００１２】本発明の医療用貼付剤は上記構成の貼付剤
の支持体の他面に、透湿度が２５０ｇ／ｍ２ ／２４ｈ
以下の低透湿性カバー材を剥離容易な状態にて積層され
てなるものである。つまり、上記支持体の他面、即ち背
面に低透湿性カバー材を設けることによって、まず皮膚
面に本発明の医療用貼付剤を貼付した場合、初期にＯＤ
Ｔを行うことができ、適用皮膚面の角質層をルーズ化さ
せることができる。従って、経皮吸収用薬物を短時間で
経皮吸収することができ、速効性が期待できるのである
。
しかし、この状態が長時間にわたって続くと皮膚刺激を
生じるようになるので、本発明においては皮膚面へ貼付
後適当な時期に上記カバー材を剥離し、貼付剤に透湿性
を与え、皮膚刺激の軽減化を図ると共に、薬理効果の持
続性を発揮させるようにする。The medical patch of the present invention has a moisture permeability of 250 g/m2/24h on the other side of the patch support having the above structure.
It is made by laminating the following low moisture permeability cover materials in an easily peelable state. In other words, by providing a low moisture permeable cover material on the other surface of the support, that is, on the back surface, when the medical patch of the present invention is first applied to the skin surface, the OD
T can be performed to loosen the stratum corneum on the applied skin surface. Therefore, drugs for transdermal absorption can be absorbed transdermally in a short period of time, and rapid efficacy can be expected. However, if this condition continues for a long period of time, skin irritation will occur, so in the present invention, the covering material is peeled off at an appropriate time after application to the skin surface, giving moisture permeability to the patch and preventing skin irritation. In addition to reducing the effects of the drug, efforts are made to maintain the pharmacological effect.
【００１３】このようなカバー材は、ＯＤＴを行うため
にはその透湿度を２５０ｇ／ｍ２ ／２４ｈ以下の値を
有するもので、厚みが５〜１０００μｍ程度のものを採
用することがよく、低透湿度を有するものであればその
材質は特に限定されず、前記支持体にて例示したものを
採用することができる。また、このようなカバー材は支
持体と剥離可能な状態にて積層するが、少なくとも粘着
性高分子物質層と支持体との接着力よりも小さな接着力
にて支持体に接着する必要がある。剥離可能に積層する
ための具体的な方法としては、支持体背面に剥離処理を
施し粘着剤を介しててカバー剤を積層する方法、弱粘着
性の粘着剤層を介在させて積層する方法、ゴムラテック
ス粒子を介在させて積層する方法、熱圧着によって積層
する方法などが挙げられる。[0013] In order to perform ODT, such a cover material should have a moisture permeability value of 250 g/m2/24 h or less and a thickness of about 5 to 1000 μm, and should have a low permeability. The material is not particularly limited as long as it has humidity, and the materials exemplified for the support can be used. In addition, such a cover material is laminated to the support in a releasable state, but it must be adhered to the support with at least an adhesive force that is smaller than the adhesive force between the adhesive polymer material layer and the support. . Specific methods for removably laminating include a method in which the back surface of the support is subjected to a release treatment and a cover material is laminated via an adhesive, a method in which a weakly adhesive adhesive layer is interposed, and a cover material is laminated. Examples include a method of laminating with rubber latex particles interposed therebetween, a method of laminating by thermocompression bonding, and the like.
【００１４】上記カバー材はＯＤＴが充分にかかったと
きに剥離することが好ましいが、皮膚面からの水分の蒸
散は個人差があり、また、同一個体であっても、例えば
日内変動や季節変動を生じ、さらに、風呂あがりでは皮
膚の水和量が多く、ＯＤＴ効果は比較的早い時期に現れ
るようになる。そこで、一定のＯＤＴ効果が現れたとき
にカバー材を剥離するようにするためには、例えば本発
明の医療用貼付剤中に湿度の変化によって変色する物質
を含有させておくと、剥離時期の認識が容易となる。含
有量は特に限定されないが、通常、変色物質を含有する
層の総重量に対して０．１〜２０重量％、好ましくは１
〜１０重量％程度とする。[0014] It is preferable that the above-mentioned cover material is peeled off when sufficient ODT is applied, but the transpiration of moisture from the skin surface varies from person to person, and even in the same individual, for example, diurnal fluctuations and seasonal fluctuations occur. Furthermore, the amount of hydration in the skin is large after taking a bath, and the ODT effect appears relatively early. Therefore, in order to peel off the cover material when a certain ODT effect appears, for example, if the medical patch of the present invention contains a substance that changes color due to changes in humidity, it is possible to Easy to recognize. Although the content is not particularly limited, it is usually 0.1 to 20% by weight, preferably 1% by weight based on the total weight of the layer containing the color-changing substance.
~10% by weight.
【００１５】このような物質としては、例えばコバルト
イオンが挙げられる。コバルトイオンは湿気を吸収しな
いときは青系統に呈色しており、湿気を吸収すると赤系
統に変色する。従って、コバルトイオンは皮膚面から蒸
散して貼付剤中に吸収された水分（湿気）によって変色
するので、変色したのちにカバー剤を剥離すると本発明
の効果を最大限に発揮することができる。[0015] Examples of such substances include cobalt ions. Cobalt ions have a blue color when not absorbing moisture, and change to a red color when they absorb moisture. Therefore, since cobalt ions evaporate from the skin surface and change color due to water (moisture) absorbed into the patch, the effect of the present invention can be maximized by peeling off the cover material after the color change occurs.
【００１６】上記変色物質は本発明の医療用貼付剤を構
成する支持体、粘着性高分子物質層、カバー材の少なく
とも一つに含有させればよいが、好ましくは支持体もし
くはカバー材中、さらに好ましくはカバー材中に含有さ
せる。ただし、カバー材中に含有させる場合はカバー材
背面側から浸透する大気中の水分の影響を受けないよう
にする必要があり、非透湿性フィルムでオーバーコート
するか非透湿化処理を施すことが好ましい。また、カバ
ー材に変色物質を含有させた場合、支持体を白色化する
ことによって変色の程度を容易に認識できて好ましい。The above-mentioned color-changing substance may be contained in at least one of the support, the adhesive polymer layer, and the cover material constituting the medical patch of the present invention, but preferably in the support or the cover material, More preferably, it is contained in the cover material. However, when incorporating it into the cover material, it is necessary to prevent it from being affected by atmospheric moisture that penetrates from the back side of the cover material, so it must be overcoated with a non-moisture-permeable film or treated to make it non-moisture-permeable. is preferred. Further, it is preferable that the cover material contains a discoloration substance, since the degree of discoloration can be easily recognized by whitening the support.
【００１７】また、変色物質は上記層内にかならず含有
させる必要はなく、医療用貼付剤中であればよく、例え
ば水溶性ポリマー中に含有させてカバー材と支持体の間
や支持体と粘着性高分子物質層との間に介在させること
もできる。水溶性ポリマーを用いることによって吸収さ
れた皮膚面からの水分は速やかに変色物質に到達するの
で、変色反応（応答）が敏感に起こる。水溶性ポリマー
としては高ケン化度ポリビニルアルコール、ポリアルキ
レンオキサイド、セルロースなどの結晶性を有する水溶
性ポリマー、ポリビニルピロリドンやポリアルキレンオ
キサイドあるいはポリアルキルエーテルの架橋体、ポリ
ヒドロキシエチルメタクリレート、ゼラチン架橋体、ポ
リアクリル酸系架橋体などの水溶性ポリマー架橋体など
が好ましく用いることができる。[0017] Furthermore, the color-changing substance does not necessarily have to be contained in the above-mentioned layer, but may be contained in a medical patch; for example, it can be contained in a water-soluble polymer and placed between the cover material and the support, or between the support and the adhesive. It can also be interposed between a polymer material layer and a polymer material layer. By using a water-soluble polymer, water absorbed from the skin surface quickly reaches the color-changing substance, so a color change reaction (response) occurs sensitively. Water-soluble polymers include highly saponified polyvinyl alcohol, polyalkylene oxide, crystalline water-soluble polymers such as cellulose, polyvinylpyrrolidone, polyalkylene oxide, or polyalkyl ether crosslinked products, polyhydroxyethyl methacrylate, gelatin crosslinked products, Water-soluble polymer crosslinked products such as polyacrylic acid crosslinked products can be preferably used.
【００１８】[0018]
【実施例】以下に実施例を示し、本発明の医療用貼付剤
について具体的に説明する。[Example] The medical patch of the present invention will be explained in detail with reference to Examples below.
【００１９】実施例１
アクリル酸２−エチルヘキシルエステル９５重量部とア
クリル酸５重量部とを共重合して得た粘着性高分子物質
に、含有量が２０重量％となるようにイソソルビドジニ
トレート（以下、ＩＳＤＮと略す）を含有させて、経皮
吸収用薬物を含有する粘着性高分子物質層（４０μｍ厚
）を形成した。Example 1 A sticky polymer material obtained by copolymerizing 95 parts by weight of acrylic acid 2-ethylhexyl ester and 5 parts by weight of acrylic acid was added with isosorbide dinitrate (20% by weight). (hereinafter abbreviated as ISDN) to form an adhesive polymer material layer (40 μm thick) containing a drug for transdermal absorption.
【００２０】次に、９μｍ厚のポリエチレンテレフタレ
ート（以下、ＰＥＴと略す）フィルムと３０μｍ厚のエ
チレン／酢酸ビニル共重合体（以下、ＥＶＡと略す）フ
ィルムとの積層支持体のＥＶＡ面に上記高分子物質層を
積層して貼付剤とした。この貼付剤には穿孔処理を支持
体に施すことによって透湿度を３５０ｇ／ｍ２ ／２４
ｈ以上となるように調整した。なお、ＰＥＴフィルムは
背面にシリコーン処理を施したものを使用した。Next, the above polymer was applied to the EVA side of a laminated support consisting of a 9 μm thick polyethylene terephthalate (hereinafter abbreviated as PET) film and a 30 μm thick ethylene/vinyl acetate copolymer (hereinafter abbreviated as EVA) film. The material layers were laminated to form a patch. This patch has a moisture permeability of 350g/m2/24 by perforating the support.
It was adjusted so that it was more than h. The PET film used had its back surface treated with silicone.
【００２１】一方、上記と同じＰＥＴフィルムに上記に
て共重合した粘着性高分子物質を１０μｍ厚にて積層し
、これを粘着シート状の低透湿性カバー材（透湿度７０
ｇ／ｍ２ ／２４ｈ）として、上記にて作製した貼付剤
の支持体面上に貼着し、図１に示すような本発明の医療
用貼付剤を得た。On the other hand, the adhesive polymer material copolymerized above is laminated to a thickness of 10 μm on the same PET film as above, and this is used as an adhesive sheet-like low moisture permeable cover material (moisture permeability 70
g/m2/24h) and adhered to the support surface of the patch prepared above to obtain a medical patch of the present invention as shown in FIG.
【００２２】この医療用貼付剤を３０ｍｍφに切断して
５人の被験者の胸部皮膚面に３時間貼付したのち、カバ
ー材を剥離して貼付を続けたところ、ＩＳＤＮは有効血
中濃度域に早期に達し、かつ４８時間にわたって有効血
中濃度を維持することができ薬理効果が確認できた。ま
た、皮膚面の刺激（かぶれ）も観察されなかった。[0022] This medical patch was cut into pieces of 30 mm in diameter and applied to the chest skin of five subjects for 3 hours, and then the cover material was peeled off and the application was continued. The effective blood concentration was maintained for 48 hours, confirming the pharmacological effect. Furthermore, no skin irritation (rash) was observed.
【００２３】実施例２
一方、ケン化度９９．５モル％、平均重合度約１７００
のポリビニルアルコール（以下、ＰＶＡと略す）１５重
量部と塩化コバルト１重量部とから調製された変色物質
含有層（２０μｍ厚）を、ポリテトラフルオロエチレン
（以下、ＰＴＦＥと略す）からなる多孔質支持体（６０
μｍ厚、透湿度４０００ｇ／ｍ２ ／２４ｈ）上にキャ
スティング法にて積層した。なお、支持体と変色物質含
有層とは剥離容易な状態にて積層されていた。Example 2 On the other hand, the degree of saponification was 99.5 mol%, the average degree of polymerization was about 1700
A color-changing substance-containing layer (20 μm thick) prepared from 15 parts by weight of polyvinyl alcohol (hereinafter abbreviated as PVA) and 1 part by weight of cobalt chloride was placed on a porous support made of polytetrafluoroethylene (hereinafter abbreviated as PTFE). Body (60
(μm thickness, moisture permeability 4000g/m2/24h) by a casting method. Note that the support and the color-changing substance-containing layer were laminated in such a manner that they could be easily peeled off.
【００２４】次いで、実施例１にて用いた低透湿性カバ
ー材を上記積層体の変色物質含有層側に貼着し、さらに
実施例１にて用いたと同様のＩＳＤＮを含有する粘着性
高分子物質層を上記積層体の支持体側に貼着して図２に
示すような本発明の医療用貼付剤を得た。なお、支持体
と粘着性高分子物質層との積層体での透湿度は１４００
ｇ／ｍ２ ／２４ｈであった。Next, the low moisture permeability cover material used in Example 1 was adhered to the discoloration substance-containing layer side of the laminate, and the same ISDN-containing adhesive polymer as used in Example 1 was then applied. A material layer was attached to the support side of the laminate to obtain a medical patch of the present invention as shown in FIG. The moisture permeability of the laminate of the support and the adhesive polymer material layer is 1400.
g/m2/24h.
【００２５】この医療用貼付剤を４５ｍｍφに切断して
５人の被験者の胸部皮膚面に貼付したところ、貼付前に
は全面が青色であった貼付剤が徐々に変色し、平均約２
時間後に全面がピンク色に変色した。そののちカバー材
を剥離して貼付を続けたところ、ＩＳＤＮは有効血中濃
度域に早期に達し、かつ４８時間にわたって有効血中濃
度を維持することができ薬理効果が確認できた。また、
皮膚面の刺激（かぶれ）も観察されなかった。[0025] When this medical patch was cut into 45 mm diameter pieces and applied to the chest skin of five subjects, the entire surface of the patch, which was blue before application, gradually changed color, with an average of about 2.
After some time, the entire surface turned pink. Thereafter, when the cover material was peeled off and the application was continued, ISDN quickly reached the effective blood concentration range, and the effective blood concentration was maintained for 48 hours, confirming the pharmacological effect. Also,
No skin irritation (rash) was observed.
【００２６】実施例３
アクリル酸２−エチルヘキシルエステル５５重量部とア
クリル酸２−メトキシエチルエステル２５重量部、酢酸
ビニル２０重量部とを共重合して得た粘着性高分子物質
に、含有量が２０重量％となるようにテオフィリンを含
有させて、経皮吸収用薬物を含有する粘着性高分子物質
層（８０μｍ厚）を形成した。Example 3 A sticky polymer substance obtained by copolymerizing 55 parts by weight of 2-ethylhexyl acrylate, 25 parts by weight of 2-methoxyethyl acrylate, and 20 parts by weight of vinyl acetate contained Theophylline was contained in an amount of 20% by weight to form an adhesive polymer material layer (80 μm thick) containing a drug for transdermal absorption.
【００２７】次に、１２μｍ厚のポリエチレン製の多孔
質支持体（透湿度３０００ｇ／ｍ２ ／２４ｈ）の片面
に上記高分子物質層を積層して貼付剤とした。なお、こ
の支持体は背面にシリコーン処理を施したものを使用し
た。Next, the above-mentioned polymer material layer was laminated on one side of a 12 μm thick polyethylene porous support (moisture permeability 3000 g/m 2 /24 h) to prepare a patch. The back surface of this support was treated with silicone.
【００２８】一方、実施例１にて用いた低透湿性カバー
材を上記にて作製した貼付剤の支持体面上に貼着し、本
発明の医療用貼付剤を得た。On the other hand, the low moisture permeability cover material used in Example 1 was adhered to the support surface of the patch prepared above to obtain a medical patch of the present invention.
【００２９】この医療用貼付剤を３０ｍｍφに切断して
５人の被験者の胸部皮膚面に２時間貼付したのち、カバ
ー材を剥離して貼付を続けたところ、テオフィリンは有
効血中濃度域に早期に達し、かつ２４時間にわたって有
効血中濃度を維持することができ薬理効果が確認できた
。また、皮膚面の刺激（かぶれ）も観察されなかった。[0029] This medical patch was cut into 30 mm diameter pieces and applied to the chest skin of five subjects for 2 hours, and then the cover material was peeled off and the application continued. As a result, theophylline quickly reached the effective blood concentration range. The effective blood concentration was maintained for 24 hours, confirming the pharmacological effect. Furthermore, no skin irritation (rash) was observed.
【００３０】[0030]
【発明の効果】以上のように、本発明の医療用貼付剤は
特定の透湿度以上を有する支持体に薬物を含有した粘着
性高分子物質層を形成し、上記支持体の他面に透湿性の
低い裏打部材を剥離が容易な状態で積層した構成である
ので、含有する薬物が速やかに生体内に移行し、かつ長
期間にわたって持続的に薬物の有効血中濃度が維持でき
るという効果を発揮するものである。Effects of the Invention As described above, the medical patch of the present invention has a drug-containing adhesive polymer material layer formed on a support having a moisture permeability above a specific level, and a transparent adhesive layer on the other side of the support. Because it has a structure in which a backing member with low moisture content is laminated in a state that is easy to peel off, the drug contained therein is quickly transferred into the body, and the effective blood concentration of the drug can be continuously maintained over a long period of time. It is something that can be demonstrated.
【図１】実施例１にて得た本発明の医療用貼付剤を示す
断面図である。FIG. 1 is a cross-sectional view showing the medical patch of the present invention obtained in Example 1.
【図２】実施例２にて得た本発明の医療用貼付剤を示す
断面図である。FIG. 2 is a cross-sectional view showing the medical patch of the present invention obtained in Example 2.
１ 経皮吸収用薬物を含有する粘着性高分子物質層２
支持体
３ 低透湿性カバー材
４ 変色物質含有層1 Adhesive polymer material layer containing drug for transdermal absorption 2
Support 3 Low moisture permeability cover material 4 Color-changing substance-containing layer
Claims (3)
吸収用薬物を含有する粘着性高分子物質層が積層され、
他面には透湿度が２５０ｇ／ｍ２ ／２４ｈ以下の低透
湿性カバー材が剥離容易な状態にて積層されていること
を特徴とする医療用貼付剤。Claim 1: An adhesive polymer material layer containing a drug for transdermal absorption is laminated on one side of a support having high moisture permeability,
A medical patch characterized in that a low moisture permeable cover material having a moisture permeability of 250 g/m2/24 h or less is laminated on the other side in an easily peelable state.
状態における透湿度が３５０ｇ／ｍ２ ／２４ｈ以上で
ある請求項１記載の医療用貼付剤。2. The medical patch according to claim 1, wherein the support and the adhesive polymer material layer have a moisture permeability of 350 g/m2/24 h or more in a laminated state.
別可能に変色する物質が含有されている請求項１または
２記載の医療用貼付剤。3. The medical patch according to claim 1, wherein the medical patch contains a substance that visibly changes color due to changes in humidity.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP3031848A JP3071839B2 (en) | 1991-01-30 | 1991-01-30 | Medical patch |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP3031848A JP3071839B2 (en) | 1991-01-30 | 1991-01-30 | Medical patch |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH04244019A true JPH04244019A (en) | 1992-09-01 |
| JP3071839B2 JP3071839B2 (en) | 2000-07-31 |
Family
ID=12342477
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP3031848A Expired - Lifetime JP3071839B2 (en) | 1991-01-30 | 1991-01-30 | Medical patch |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP3071839B2 (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000062763A3 (en) * | 1999-04-15 | 2001-01-04 | Acutek Internat | Carrier patch for the delivery of agents to the skin |
| JP2006025847A (en) * | 2004-07-12 | 2006-02-02 | Nichiei:Kk | Sheet body for make-up |
| EP2548551A1 (en) | 2011-07-20 | 2013-01-23 | Nitto Denko Corporation | Patch preparation |
| EP2702968A1 (en) | 2012-08-31 | 2014-03-05 | Nitto Denko Corporation | A patch comprising a three layer support |
-
1991
- 1991-01-30 JP JP3031848A patent/JP3071839B2/en not_active Expired - Lifetime
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000062763A3 (en) * | 1999-04-15 | 2001-01-04 | Acutek Internat | Carrier patch for the delivery of agents to the skin |
| JP2006025847A (en) * | 2004-07-12 | 2006-02-02 | Nichiei:Kk | Sheet body for make-up |
| JP4632705B2 (en) * | 2004-07-12 | 2011-02-16 | 株式会社ニチエイ | Cosmetic sheet body |
| EP2548551A1 (en) | 2011-07-20 | 2013-01-23 | Nitto Denko Corporation | Patch preparation |
| US8758312B2 (en) | 2011-07-20 | 2014-06-24 | Nitto Denko Corporation | Patch preparation |
| EP2702968A1 (en) | 2012-08-31 | 2014-03-05 | Nitto Denko Corporation | A patch comprising a three layer support |
| US9345670B2 (en) | 2012-08-31 | 2016-05-24 | Nitto Denko Corporation | Patch preparation |
Also Published As
| Publication number | Publication date |
|---|---|
| JP3071839B2 (en) | 2000-07-31 |
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