JPH08291055A - Shape memory plaster - Google Patents
Shape memory plasterInfo
- Publication number
- JPH08291055A JPH08291055A JP7092860A JP9286095A JPH08291055A JP H08291055 A JPH08291055 A JP H08291055A JP 7092860 A JP7092860 A JP 7092860A JP 9286095 A JP9286095 A JP 9286095A JP H08291055 A JPH08291055 A JP H08291055A
- Authority
- JP
- Japan
- Prior art keywords
- shape memory
- patch
- weight
- plaster
- shape
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Landscapes
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Treatments For Attaching Organic Compounds To Fibrous Goods (AREA)
- Nonwoven Fabrics (AREA)
Abstract
Description
【0001】[0001]
【産業上の利用分野】本発明はケトプロフェン貼付剤こ
とに形状記憶性素材からなる貼付剤及び全身効果並びに
従来の局所的効果を目的とした貼付剤の投薬法に係る。BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a ketoprofen patch, and more particularly to a patch made of a shape memory material and a method for administering a patch for systemic effects and conventional local effects.
【0002】[0002]
【従来技術】ケトプロフェンは、我国では本発明者等に
より経口、注射剤として、解熱鎮痛目的に研究開発され
(日薬誌70,543頁、1974年)、局所的鎮痛剤(筋肉痛
等)としては軟膏剤、パップ剤が古くから使用されてい
る(1979年イタリヤ薬局方INFORMATORE FARMACEUTICO 4
66 頁、特公平2-28572 号、特公平6-62401 号等)。ま
た、最近では吸収性が良好で疾患状況、年齢、性別、体
重、皮膚表皮面積、貼付時間が管理コントロールしやす
い貼付基剤について、各種薬剤を対象に研究が行われて
いる(特公平4-50291 号等)。2. Description of the Related Art Ketoprofen has been researched and developed by the present inventors in Japan as an oral or injectable drug for the purpose of antipyretic analgesia (Japanese Pharmacopoeia 70, 543 pages, 1974), and as a local analgesic (muscle pain, etc.), ointment. Agents and poultices have been used for a long time (1979 INFORMATORE FARMACEUTICO 4
66 pages, Japanese Patent Publication No. 2-28572, Japanese Patent Publication No. 6-62401, etc.). In addition, recently, studies have been conducted on various drugs for patch bases that have good absorbability and are easy to control and control disease status, age, sex, weight, skin epidermal area, and patching time (Patent Publication 4- No. 50291).
【0003】全身作用効果を目的とした経皮吸収による
投薬方法は、肝分解の抑制、副作用発生の抑制等各種の
利点があることが予測される事から、近年脚光をあび、
本出願人会社等により各種製剤が上市されている(治験
医師薬情報238 頁 医事出版社1992)。Since a transdermal drug administration method for the purpose of systemic effect is expected to have various advantages such as suppression of liver degradation and occurrence of side effects, it has recently been highlighted.
Various formulations have been put on the market by the applicant company, etc. (Investigator Information, page 238, Medical Affairs Publisher, 1992).
【0004】形状記憶性材質については、金属、プラス
チック繊維を利用したものや、リンアミド系素材を付着
させたもの等最近衣服類にその応用がはかられている
が、医薬品についての応用はカテーテル等にその利用が
見られるが貼付剤や軟膏基剤そのものについての研究は
ほとんど見られない。(特開平5-44128,5-51853,5-7893
2 号等)Shape memory materials have recently been applied to clothes such as those using metal or plastic fiber, and those to which phosphorus amide material is attached, but catheters are applicable to pharmaceutical products. However, there is almost no research on patches and ointment bases themselves. (JP-A-5-44128,5-51853,5-7893
No. 2 etc.)
【0005】[0005]
【発明が解決しようとする問題点及び課題】貼付剤は貼
付後数時間経過すると体温、吸湿等により型崩れが発生
しやすく、粗悪なものは膏剤が流出したり、気泡が皮膚
面に発生したりして剥がれやすくなる点がかねてから指
摘されている。[Problems and problems to be solved by the invention] The patch is likely to lose its shape due to body temperature, moisture absorption, etc. several hours after the patch is applied, and if the patch is poor, the plaster may flow out or bubbles may be generated on the skin surface. It has been pointed out that it is easy to peel it off.
【0006】経皮吸収による投薬方法、貼付剤ことにパ
ップ剤、テープ剤による経皮吸収方法は、乳幼児、老齢
者のように経口、注射投与ができない者や、肝分解の抑
制、副作用発生の抑制等各種の利点があり、非常に理想
的な投薬方法である。ところが、前述のような型崩れの
問題があり、吸収性と投薬コントロール方法が困難な事
からイソソルバイド、ニトログリセリン、クロニジン等
の吸収性の良い微量活性薬剤をパップ剤、テープ剤とし
て使用する方法に限られていた。[0006] The method of administration by percutaneous absorption, the patch, and the method of percutaneous absorption by patches and tapes are used for those who cannot be administered orally or by injection, such as infants and the elderly, and the suppression of liver degradation and the occurrence of side effects. It has various advantages such as suppression and is a very ideal dosing method. However, there is a problem of shape loss as described above, and it is difficult to control absorption and dosing, so it is recommended to use a small amount of a well-absorbed active agent such as isosorbide, nitroglycerin, or clonidine as a patch or tape. It was limited.
【0007】ケトプロフェンは副作用がインドメタシン
等の類似薬剤と比較して少なく、注射剤、経口剤、カプ
セル剤、坐剤形態のものが解熱鎮痛剤として使用されて
いる。ところがパップ剤、テープ剤形態のものは接着
性、放出性等の管理コントロールが困難である事から局
所の鎮痛消炎目的としてしか使用されていない。[0007] Ketoprofen has fewer side effects than similar drugs such as indomethacin, and injections, oral preparations, capsules, and suppository forms are used as antipyretic analgesics. However, it is difficult to control the adhesiveness, release property, and the like of the form of a poultice or tape, and therefore, it is used only for the purpose of local analgesic and anti-inflammatory.
【0008】また、ケトプロフェンの経口使用は乳幼児
や消化性潰瘍経験者には投薬上注意が必要であり、不快
感、胃痛、食欲不振、嘔吐、悪心、下痢等が副作用とし
て報告されており、管理コントロールが容易な貼付剤の
開発が望まれていた。[0008] In addition, oral use of ketoprofen requires caution in administration to infants and people who have experienced peptic ulcer, and discomfort, stomach pain, loss of appetite, vomiting, nausea, diarrhea, etc. have been reported as side effects, and management It was desired to develop a patch that is easy to control.
【0009】本発明者等はすでに経皮投与に適する理想
的な軟膏基剤を開発していたが、この軟膏基剤を使用し
てケトプロフェンの上述の問題点を解決すべく検討を試
みた結果、伸縮通気性を有する支持体に、膏体量に対し
てケトプロフェン{2−(m−ベンゾイルフェニル)プ
ロピオン酸}0.3 〜3重量%と、溶解剤としてヒマシ油
0.5 〜2重量%と、保形・保湿剤として、ポリアクリル
酸あるいはその塩を2〜10重量%、水酸化アルミナマグ
ネシウムを0.2 〜3重量%、ソルビトールを20〜50重量
%含有し、吸収促進及び芳香剤としてカンファーあるい
はメントール0.5 〜2重量%を含有させた製剤が、形状
記憶性が向上することにより皮膚接着性と伸縮性に富
み、吸収管理コントロールが比較的容易である事を発見
し、本発明を完成するに至った。The present inventors have already developed an ideal ointment base suitable for transdermal administration. As a result of trying to solve the above-mentioned problems of ketoprofen by using this ointment base , Stretchable and breathable support, ketoprofen {2- (m-benzoylphenyl) propionic acid} 0.3-3 wt% relative to the amount of plaster, and castor oil as a solubilizer
0.5 to 2% by weight, and 2 to 10% by weight of polyacrylic acid or its salt as a shape-retaining / humidifying agent, 0.2 to 3% by weight of magnesium alumina hydroxide and 20 to 50% by weight of sorbitol to promote absorption. And, it was discovered that a formulation containing 0.5 to 2% by weight of camphor or menthol as an fragrance has improved shape memory properties, is rich in skin adhesiveness and elasticity, and is relatively easy to control absorption, The present invention has been completed.
【0010】なお、本発明は局所の消炎鎮痛目的と言う
従来のケトプロフェン貼付剤の効果と共に、幼児等の経
口投与を嫌う患者等に対しても、例えば解熱鎮痛剤とし
ての使用可能性を提案するものであり、経口投与に代わ
る理想的なケトプロフェン経皮吸収製剤を提供するもの
でもある。In addition to the effects of the conventional ketoprofen patch for the purpose of local antiphlogistic and analgesia, the present invention proposes the possibility of using it as an antipyretic analgesic even for patients who dislike oral administration such as infants. It also provides an ideal ketoprofen transdermal drug delivery alternative to oral administration.
【0011】また、局所の消炎鎮痛目的であっても、薬
剤の放出に優れ、形状記憶性に富んだ軟基剤を使用する
事によりケトプロフェンの投薬量を正確にコントロール
できる製剤となり、さらには錠剤の割引に代わる切り取
り線を添付する工夫により乳幼児、衰弱者、老齢者に対
しても、安全に使用できる製剤を提供するものである。Even for the purpose of local antiphlogistic and analgesia, a soft base having excellent drug release and a good shape memory property can be used to obtain a formulation in which the dose of ketoprofen can be accurately controlled, and further tablets. It is intended to provide a preparation that can be safely used by infants, debilitated people, and elderly people by devising a cutting line instead of the discount.
【0012】本発明は形状記憶性を有する事から、上記
投薬量のコントロールの他に運動時の伸縮性、加圧性、
体温における膏剤の硬度変化に耐えることができる。こ
のため長時間使用しても形が崩れず、接着性に優れ、運
動時に適度の脱着、接着を繰り返しても空気だまりの発
生を抑制でき、投薬量を正確にコントロールする事が可
能となる。Since the present invention has a shape memory property, in addition to the above-mentioned dosage control, elasticity during exercise, pressurization,
Can withstand changes in hardness of plasters at body temperature. For this reason, the shape does not collapse even when used for a long time, the adhesiveness is excellent, and the occurrence of air pockets can be suppressed even when repeated proper desorption and adhesion during exercise, and the dosage can be accurately controlled.
【0013】形状記憶膏体並びに形状記憶支持体あるい
はこの組み合わせからなる貼付剤としては、経皮吸収性
医薬の大部分に本発明方法は利用する事ができる。例え
ば、本発明実施例のケトプロフェンの他、インドメサシ
ン、フルルビプロフェン等の解熱性消炎鎮痛剤、ステロ
イド系、ペプタイド系ホルモン類、ニトログリセリン、
クロニジン、硝酸イソソルバイド等の循環作用薬、フマ
ル酸フォルモテール、リン酸ジモルファン、クエン酸カ
ルベタペンタン、塩酸プロカテロール等の抗喘息薬等へ
の応用が可能である。また、従来皮膚接着性のコントロ
ールができないために、経皮的薬剤として利用できなか
った薬剤に応用する事もできる。As a patch comprising a shape memory plaster and a shape memory support or a combination thereof, the method of the present invention can be used for most of transdermal medicines. For example, in addition to ketoprofen of the examples of the present invention, indomethacin, antipyretic anti-inflammatory analgesics such as flurbiprofen, steroids, peptide hormones, nitroglycerin,
It can be applied to circulatory agents such as clonidine and isosorbide dinitrate, and anti-asthma agents such as formotere fumarate, dimorphan phosphate, carbetapentane citrate, and procaterol hydrochloride. In addition, it can be applied to a drug that could not be used as a transdermal drug because it is impossible to control the skin adhesiveness.
【0014】[0014]
【課題を解決するための手段及び方法】本発明は伸縮通
気性を有する好ましくは形状記憶性を有する支持体に、
膏体量に対してケトプロフェン{2−(m−ベンゾイル
フェニル)プロピオン酸}0.3 〜3重量%と、溶解剤と
してヒマシ油0.5 〜2重量%と、保形・保湿剤として、
ポリアクリル酸あるいはその塩を2〜10重量%、水酸化
アルミナマグネシウムを0.2 〜3重量%、ソルビトール
を20〜50重量%含有し、吸収促進及び芳香剤としてカン
ファーあるいはメントール0.5 〜2重量%を含有する事
を特徴とするケトプロフェンパップ剤を基本としてお
り、支持体を形状記憶合金繊維を用いた織布あるいは不
織布としたものの他、解熱鎮痛剤としての全身作用を目
的とする場合は、投薬量を正確に調製するために、ライ
ナー(剥離紙)あるいは膏薬の裏面に断線あるいはハサ
ミで切断できるような切断線が印刷されている形状のも
のを含む。The present invention relates to a support having stretchable and breathable property, preferably shape memory property.
Ketoprofen {2- (m-benzoylphenyl) propionic acid} 0.3-3% by weight, castor oil 0.5-2% by weight as a solubilizer, and a shape-retaining / humectant, relative to the amount of plaster.
Containing 2 to 10% by weight of polyacrylic acid or its salt, 0.2 to 3% by weight of alumina magnesium hydroxide, 20 to 50% by weight of sorbitol, and containing 0.5 to 2% by weight of camphor or menthol as an absorption accelerating and aromatic agent. Based on a ketoprofen poultice, which is characterized by the fact that the support is a woven or non-woven fabric using shape memory alloy fibers, in addition to the systemic action as an antipyretic analgesic, the dosage is For accurate preparation, a liner (release paper) or a plaster having a shape in which a cutting line that can be cut with scissors is printed on the back surface of the plaster is included.
【0015】実際の使用に当たっては、全身作用を目的
とする場合は対象患者の疾患状況、年齢、性別、体重、
皮膚表皮面積から貼付時間を算出して、投薬コントロー
ルする事により正確な薬理効果を期待する事ができる。In actual use, in the case of aiming at systemic action, the disease status, age, sex, weight of the target patient,
An accurate pharmacological effect can be expected by calculating the application time from the skin epidermal area and controlling the medication.
【0016】また、局所の作用目的のためには患者の状
態、年齢、性別、体重、皮膚表皮面積から貼付剤を切断
して使用する方法をとる事もできる。For the purpose of local action, a method of cutting the patch from the patient's condition, age, sex, body weight, and skin epidermis area can be used.
【0017】本発明によるケトプロフェン貼付剤は溶解
剤、吸収促進剤としてヒマシ油、メントール、カンファ
ーを使用して、ケトプロフェンを半溶解状態で形状記憶
性基剤に拡散、分散させる方法で経時的放出性を保持
し、さらには運動時の接着性を良好に保つ目的で形状記
憶性基剤として、ゼラチン、グリコール、ポリアクリル
酸類、ソルビトール、ソルビタン類等を組み合わせた素
材が選択される。The ketoprofen patch according to the present invention uses a castor oil, menthol and camphor as a dissolution agent and an absorption enhancer to diffuse and disperse ketoprofen in a shape-memory base in a semi-dissolved state. For the purpose of retaining the above properties and further maintaining good adhesiveness during exercise, a material in which gelatin, glycol, polyacrylic acid, sorbitol, sorbitan, etc. are combined is selected as a shape memory base.
【0018】本発明に使用される形状記憶膏剤支持体と
してはリンアミド系化合物を付着させた蛋白繊維糸、コ
ポリエステル繊維/熱融着性バインダー繊維積層体、Ni
/Ti等の形状記憶合金繊維糸等体温での形状記憶機能を
有するように比較的加工な容易な繊維材質を利用する事
ができる。以下実施例をあげ本発明をさらに詳細に説明
する。As the shape memory plaster support used in the present invention, a protein fiber thread to which a phosphorus amide compound is attached, a copolyester fiber / heat-fusible binder fiber laminate, Ni
It is possible to use a relatively easy-to-process fiber material having a shape memory function at body temperature, such as a shape memory alloy fiber thread such as / Ti. Hereinafter, the present invention will be described in more detail with reference to examples.
【0019】[0019]
製剤例1(形状記憶基剤使用パップ剤) 貼付剤1枚あたり(膏体10g、10×14cm)、以下処方を
有するパップ剤を調製した。 Formulation Example 1 (Shape memory base patch) A patch having the following formulation was prepared per patch (paste 10 g, 10 × 14 cm).
【0020】製剤例2(形状記憶基剤使用パップ剤) 貼付剤1枚あたり(膏体10g、10×14cm)、以下処方を
有するパップ剤を調製した。 Formulation Example 2 (Shape patch using shape memory base) A patch having the following formulation was prepared per patch (paste 10 g, 10 × 14 cm).
【0021】製剤例3 コポリエステル型形状記憶織布(ユニチカ製)を支持体
として用い製造例1記載の膏体を貼付した製剤を調製し
た。Formulation Example 3 A formulation was prepared by applying the plaster of Production Example 1 using a copolyester type shape memory woven fabric (made by Unitika) as a support.
【0022】製剤例4 リンアミド型形状記憶織布(日東紡製)を支持体として
用い製造例2記載の膏体を貼付した製剤を調製した。Formulation Example 4 A formulation was prepared in which the plaster described in Production Example 2 was applied using a phosphoramide type shape memory woven fabric (manufactured by Nitto Boseki) as a support.
【0023】製剤例5(比較例1) Formulation Example 5 (Comparative Example 1)
【0024】製剤例6(比較例2) 膏体 ケトプロフェン 0.30 水酸化アルミナマグネシウム 0.01 カオリン 0.05 ソルビトール 3.00 ゼラチン 0.06 ポリビニルアルコール 0.04 グリセリン 2.50 ハッカ油 0.01 ヒドロキシメトキシベンゾフェノン0.01 ジヒドロキシトルエン 0.03精製水 適 量 全 量 10.0g 支持体 不織布 ライナー ポリプロピレンFormulation Example 6 (Comparative Example 2) Paste Ketoprofen 0.30 Alumina magnesium hydroxide 0.01 Kaolin 0.05 Sorbitol 3.00 Gelatin 0.06 Polyvinyl alcohol 0.04 Glycerin 2.50 Mint oil 0.01 Hydroxymethoxybenzophenone 0.01 Dihydroxytoluene 0.03 Purified water Appropriate amount Total 10.0g Support Non-woven fabric Liner Polypropylene
【0025】試験例1(形状記憶度および製剤材質試
験) 試験方法 形状記憶性試験 1)中央部変形状態の改善性試験 室温を35度Cに保ち製剤10cm×14cmの周辺部1cm四方を
固定し、中央部に20g のオモリを乗せ、6時間経過後に
オモリを取り除き、中央部の変形状態の改善性を検討し
た。Test Example 1 (Shape Memory Test and Formulation Material Test) Test Method Shape Memory Test 1) Improvement test of central deformed state Maintain room temperature at 35 ° C and fix 1cm square around 10cm × 14cm formulation Then, 20 g of weight was placed on the central part, and the weight was removed after 6 hours, and the improvement of the deformed state of the central part was examined.
【0026】2)引張り試験 製剤10cm×14cmの片方周辺部1cmを固定し、一方向に3
cm引き延ばした後、6時間経過後に取り外し復帰性を検
討した。2) Tensile test 1 cm of the peripheral part of the formulation 10 cm × 14 cm is fixed and 3 in one direction
After the stretching of cm, the recovery property after removal was examined 6 hours later.
【0027】3)圧縮試験 製剤10cm×14cmを鉄板上に乗せ、さらにその上面に2Kg
の鉄板を乗せて6時間経過後に加圧に伴う製剤四方から
の膏剤の染出状況について検討した。3) Compression test 10 cm × 14 cm of the preparation is placed on an iron plate, and 2 kg is placed on the upper surface.
6 hours after the iron plate was placed, the exuding state of the plaster from the four sides of the preparation due to pressurization was examined.
【0028】切取り試験 ボランティアにより製剤中央部を剥離紙と共に同一ハサ
ミで切断してもらい、1分あたりの切断枚数、ハサミの
刃部分への膏体の付着性にアンケート調査した。Cutout Test A volunteer was asked to cut the central part of the preparation together with release paper with the same scissors, and a questionnaire survey was conducted on the number of cuts per minute and the adhesiveness of the plaster to the blade part of the scissors.
【0029】結果は以下表1に示すように、製剤例1〜
4の製剤が形状記憶性に優れ、ハサミの刃部分への膏体
の付着性も少なく、切断しやすい製剤である事が判明し
た。The results are shown in Table 1 below.
It was found that the preparation of No. 4 was excellent in shape memory, had less adhesiveness of the plaster to the blade portion of the scissors, and was easy to cut.
【0030】[0030]
【表1】 本発明製剤1〜2 3〜4 比較製剤(5〜6) 形状記憶 1)中央部変形 やや変形 変形なし 変形(回復不能) 2)引張り 変形なし 変形なし 変形(回復不能) 3)圧縮試験 膏剤溶出なし 膏剤溶出なし 膏剤溶出発生 切取 1分間あたりの切断枚数 25枚以上 16枚前後 4枚前後 (比較品については膏体がハサミに付着するため、付着した膏体を取り除く必 要がある事が判明)[Table 1] Formulations 1 to 2 of the present invention 3 to 4 Comparative formulations (5 to 6) Shape memory 1) Deformation in central part Some deformation No deformation Deformation (non-recoverable) 2) Tensile deformation No deformation No deformation (non-recoverable) 3) Compression test No plaster elution No plaster elution Occurrence of plaster elution Cut out Number of cuts per minute 25 or more 16 or more About 4 4 sheets It turns out that it is necessary)
【0031】試験例2(経皮吸収性試験) 本発明製剤による解熱鎮痛効果について検定した。ラッ
トの背部を除毛し、1群5匹とし、20% ビール酵母10mg
/kg を皮下投与し、16時間後に本発明製剤を2.16cm四方
(4.7cm2 )に切断し(ケトプロフェンとして10mg含有)
除毛部に接着、固定し経皮投与群とした。さらに経口投
与群としてケトプロフェン(ケト)5mg/kgを経口投与
し、直腸温をサーミスター温度計を用いて1時間毎に6
時間迄6回測定し、経皮投与群と経口投与群の対象群に
対する各投与群の温度差の各時間値の総計(6回合計)
を解熱係数とした。結果は以下表2に示すように、本発
明製剤例4が最も優れている事が判明した。Test Example 2 (Transdermal Absorption Test) The antipyretic and analgesic effect of the preparation of the present invention was tested. The back of the rat is dehaired to make 5 mice per group, 20% brewer's yeast 10 mg
/ kg was subcutaneously administered, and 16 hours later, the preparation of the present invention was 2.16 cm square.
Cut to (4.7 cm 2 ) (containing 10 mg as ketoprofen)
It was adhered and fixed to the hair-removed part to make a transdermal administration group. Furthermore, 5 mg / kg of ketoprofen (keto) was orally administered as an oral administration group, and the rectal temperature was measured every 6 hours using a thermistor thermometer.
Measured 6 times up to the time, and summed up the time difference of the temperature difference of each administration group between the dermal administration group and the oral administration group (total of 6 times)
Was taken as the antipyretic coefficient. As a result, as shown in Table 2 below, it was found that Formulation Example 4 of the present invention was the most excellent.
【0032】[0032]
【表2】 [Table 2]
【0033】試験例3(使用感の評価) 本発明製剤を筋肉痛の20人のパネラーに協力してもらい
各5名つづ製剤例3、4の製剤並びに対照としてモーラ
ス(久光製薬商標)および製剤例6を適時使用してもら
い使用感を評価した。 使用感の評価:消炎鎮痛効果、接着性、密着性、伸縮
性、皮膚の状態(かゆみ、発赤他)等についてアンケー
ト調査した。 結果は以下表3に記載のごとく、本発明製剤については
好評を得た。Test Example 3 (Evaluation of feeling of use) The formulation of the present invention was asked by 20 panelists with myalgia to cooperate with each of the five formulations of Formulation Examples 3 and 4 as well as Morus (Hisami Pharmaceutical Co., Ltd.) and the formulation as controls. Example 6 was used in a timely manner and the feeling of use was evaluated. Evaluation of feeling of use: A questionnaire survey was conducted on the anti-inflammatory and analgesic effect, adhesiveness, adhesiveness, elasticity, and skin condition (itch, redness, etc.). The results are shown in Table 3 below, and the formulations of the present invention were well received.
【0034】[0034]
【表3】 本発明品 対照品 製剤例3 製剤例4 モーラス 製剤例6 a)消炎鎮痛効果 良好 5 5 5 0 b)貼付時における接着性 良好 5 5 3 0 c)貼付中の気泡発生 有り 0 0 3 5 d)貼付中のかゆみ 発生 0 0 2 2 e)運動時伸縮性 良好 5 5 2 0 f)運動後の剥がれ 発生 0 0 2 5 g)密着性 一度剥がしても数回接着可能 5 5 1 0 h)剥離後の貼付部分の状態 かゆみ発生 0 0 1 2 発赤 0 1 1 3 粘着剤の付着 0 0 1 5 i)使用感(剥離後数日間の知見) 皮膚の変化 かさついた 0 0 2 5 発赤 0 0 0 2 かゆみ発生 0 0 0 2[Table 3] Inventive product Control product Formulation example 3 Formulation example 4 Morus Formulation example 6 a) Anti-inflammatory and analgesic effect is good 5 5 5 0 b) Adhesiveness at the time of application is good 5 5 3 0 c) Air bubbles are generated during application 0 0 3 5 d) Occurrence of itch during application 0 0 2 2 e) Good stretchability during exercise 5 5 20 f) Peeling after exercise occurs 0 0 2 5 g) Adhesiveness Can be attached several times even if peeled off 5 5 10 h) State of pasted part after peeling Occurrence of itch 0 0 1 2 Redness 0 1 1 3 Adhesion of adhesive 0 0 1 5 i) Feel of use (discovery for several days after peeling) Change of skin Hot 0 0 25 Redness 0 0 0 2 Itching occurred 0 0 0 2
【0035】[0035]
【発明の効果】皮膚接着性が高く、貼付時における接着
不良空間の発生が少なく、使用中の運動伸縮性に富み、
数回にわたる接着〜剥離環境に耐える事ができる。また
刺激性、炎症性もなく、使用感の良い製剤である。断線
あるいは切断線をつける事により投薬量のコントロール
が可能となり、乳幼児、衰弱者、高齢者向け薬剤として
の応用もはかることができる。EFFECTS OF THE INVENTION High skin adhesiveness, little occurrence of defective adhesion space at the time of application, and excellent motion elasticity during use,
It can withstand several adhesion-peeling environments. It is also a non-irritating and non-irritating preparation that is easy to use. It is possible to control the dosage by breaking or adding a breaking line, and it can be applied as a drug for infants, debilitated people, and elderly people.
【図面の簡単な説明】[Brief description of drawings]
【図1】本発明による形状記憶製剤の一実施例外観図で
ある。FIG. 1 is an external view of an example of the shape memory preparation according to the present invention.
1〜投薬量調節のための断線が印刷あるいは刻印された
剥離紙 2〜投薬量調節のための断線が刻印された膏体を付着さ
せた形状記憶不織布 3〜ケトプロフェン含有形状記憶膏体1-Release paper with disconnection printed or engraved for dosage adjustment 2 Shape memory non-woven fabric to which paste with engraved disconnection for dosage adjustment 3 attached-Shape memory plaster containing ketoprofen
─────────────────────────────────────────────────────
─────────────────────────────────────────────────── ───
【手続補正書】[Procedure amendment]
【提出日】平成7年4月20日[Submission date] April 20, 1995
【手続補正1】[Procedure Amendment 1]
【補正対象書類名】明細書[Document name to be amended] Statement
【補正対象項目名】0011[Correction target item name] 0011
【補正方法】変更[Correction method] Change
【補正内容】[Correction content]
【0011】また、局所の消炎鎮痛目的であっても、薬
剤の放出に優れ、形状記憶性に富んだ軟膏基剤を使用す
る事によりケトプロフェンの投薬量を正確にコントロー
ルできる製剤となり、さらには錠剤の割引に代わる切り
取り線を添付する工夫により乳幼児、衰弱者、老齢者に
対しても、安全に使用できる製剤を提供するものであ
る。Further, even for the purpose of local anti-inflammatory and analgesia, a formulation capable of accurately controlling the dosage of ketoprofen by using an ointment base which is excellent in drug release and has a good shape memory property, and further tablets It is intended to provide a preparation that can be safely used by infants, debilitated people, and elderly people by devising a cutting line instead of the discount.
【手続補正2】[Procedure Amendment 2]
【補正対象書類名】明細書[Document name to be amended] Statement
【補正対象項目名】0013[Correction target item name] 0013
【補正方法】変更[Correction method] Change
【補正内容】[Correction content]
【0013】形状記憶膏体並びに形状記憶支持体あるい
はこの組み合わせからなる貼付剤としては、経皮吸収性
医薬の大部分に本発明方法は利用する事ができる。例え
ば、本発明実施例のケトプロフェンの他、インドメタシ
ン、フルルビプロフェン等の解熱性消炎鎮痛剤、ステロ
イド系、ペプタイド系ホルモン類、ニトログリセリン、
クロニジン、硝酸イソソルバイド等の循環作用薬、フマ
ル酸フォルモテール、リン酸ジモルファン、クエン酸カ
ルベタペンタン、塩酸プロカテロール等の抗喘息薬等へ
の応用が可能である。また、従来皮膚接着性のコントロ
ールができないために、経皮的薬剤として利用できなか
った薬剤に応用する事もできる。As a patch comprising a shape memory plaster and a shape memory support or a combination thereof, the method of the present invention can be used for most of transdermal medicines. For example, in addition to ketoprofen of the present invention examples, indomethacin, antipyretic anti-inflammatory analgesics such as flurbiprofen, steroids, peptide hormones, nitroglycerin,
It can be applied to circulatory agents such as clonidine and isosorbide dinitrate, and anti-asthma agents such as formotere fumarate, dimorphan phosphate, carbetapentane citrate, and procaterol hydrochloride. In addition, it can be applied to a drug that could not be used as a transdermal drug because it is impossible to control the skin adhesiveness.
【手続補正3】[Procedure 3]
【補正対象書類名】明細書[Document name to be amended] Statement
【補正対象項目名】0018[Correction target item name] 0018
【補正方法】変更[Correction method] Change
【補正内容】[Correction content]
【0018】本発明に使用される形状記憶膏剤支持体と
してはリンアミド系化合物を付着させた蛋白繊維糸、コ
ポリエステル繊維/熱融着性バインダー繊維積層体、Ni
/Ti等の形状記憶合金繊維糸等体温での形状記憶機能を
有するように比較的加工容易な繊維材質を利用する事が
できる。以下実施例をあげ本発明をさらに詳細に説明す
る。As the shape memory plaster support used in the present invention, a protein fiber thread to which a phosphorus amide compound is attached, a copolyester fiber / heat-fusible binder fiber laminate, Ni
It is possible to use a fiber material that is relatively easy to process so as to have a shape memory function at body temperature, such as a shape memory alloy fiber thread such as / Ti. Hereinafter, the present invention will be described in more detail with reference to examples.
【手続補正4】[Procedure amendment 4]
【補正対象書類名】明細書[Document name to be amended] Statement
【補正対象項目名】0028[Correction target item name] 0028
【補正方法】変更[Correction method] Change
【補正内容】[Correction content]
【0028】切取り試験 ボランティアにより製剤中央部を剥離紙と共に同一ハサ
ミで切断してもらい、1分あたりの切断枚数、ハサミの
刃部分への膏体の付着性についてアンケート調査した。Cut-off test A volunteer was asked to cut the central part of the preparation together with release paper with the same scissors, and a questionnaire survey was conducted on the number of cuts per minute and the adhesiveness of the plaster to the blade part of the scissors.
【手続補正5】[Procedure Amendment 5]
【補正対象書類名】明細書[Document name to be amended] Statement
【補正対象項目名】0035[Correction target item name] 0035
【補正方法】変更[Correction method] Change
【補正内容】[Correction content]
【0035】[0035]
【発明の効果】皮膚接着性が高く、貼付時における接着
不良空間の発生が少なく、使用中の運動伸縮性に富み、
数回にわたる接着〜剥離環境に耐える事ができる。また
刺激性、炎症性もなく、使用感の良い製剤である。投薬
量のコントロールが比較的正確に出来ることから、乳幼
児、衰弱者、高齢者向け薬剤としての応用もはかること
ができる。EFFECTS OF THE INVENTION High skin adhesiveness, little occurrence of defective adhesion space at the time of application, and excellent motion elasticity during use,
It can withstand several adhesion-peeling environments. It is also a non-irritating and non-irritating preparation that is easy to use. Since the dosage can be controlled relatively accurately, it can be applied as a drug for infants, debilitated people, and elderly people.
【手続補正6】[Procedure correction 6]
【補正対象書類名】明細書[Document name to be amended] Statement
【補正対象項目名】図面の簡単な説明[Name of item to be corrected] Brief description of the drawing
【補正方法】変更[Correction method] Change
【補正内容】[Correction content]
【図面の簡単な説明】[Brief description of drawings]
【図1】本発明による形状記憶製剤の一実施例外観図で
ある。FIG. 1 is an external view of an example of the shape memory preparation according to the present invention.
【図2】本発明による形状記憶繊維布を支持体として用
いた一実施例外観図である。FIG. 2 is an external view of an example in which the shape memory fiber cloth according to the present invention is used as a support.
【符号の説明】 1〜投薬量調節のための断線が印刷あるいは刻印された
剥離紙 2〜ケトプロフェン含有形状記憶膏体 3〜投薬量調節のための断線が刻印された膏体を付着さ
せた形状記憶不織布 4〜剥離紙 5〜膏体 6〜形状記憶繊維布 7〜不織布[Explanation of Codes] 1-Release paper printed or engraved with disconnection lines for dose adjustment 2 Ketoprofen-containing shape memory plaster 3 -Shape to which paste with engraved disconnection lines for dose adjustment is attached Memory nonwoven fabric 4 ~ Release paper 5 ~ Paste 6 ~ Shape memory fiber cloth 7 ~ Nonwoven fabric
【手続補正7】[Procedure Amendment 7]
【補正対象書類名】図面[Document name to be corrected] Drawing
【補正対象項目名】図1[Name of item to be corrected] Figure 1
【補正方法】変更[Correction method] Change
【補正内容】[Correction content]
【図1】 FIG.
【手続補正8】[Procedure Amendment 8]
【補正対象書類名】図面[Document name to be corrected] Drawing
【補正対象項目名】図2[Name of item to be corrected] Figure 2
【補正方法】追加[Correction method] Added
【補正内容】[Correction content]
【図2】 [Fig. 2]
───────────────────────────────────────────────────── フロントページの続き (51)Int.Cl.6 識別記号 庁内整理番号 FI 技術表示箇所 A61K 31/19 ABE A61K 31/19 ABE 47/02 47/02 F 47/10 47/10 F D04H 1/54 D04H 1/54 H D06M 13/44 D06M 13/44 ─────────────────────────────────────────────────── ─── Continuation of the front page (51) Int.Cl. 6 Identification number Reference number within the agency FI Technical display area A61K 31/19 ABE A61K 31/19 ABE 47/02 47/02 F 47/10 47/10 F D04H 1/54 D04H 1/54 H D06M 13/44 D06M 13/44
Claims (5)
はこの組み合わせからなる形状記憶機能を有する貼付
剤。1. A patch having a shape memory function, which comprises a shape memory plaster and a shape memory support or a combination thereof.
繊維布、リンアミド系化合物を付着させた蛋白繊維糸あ
るいはコポリエステル繊維/熱融着性バインダー繊維積
層体からなり、体温下での形状記憶機能を有する事を特
徴とした貼付剤。2. A stretchable and breathable support comprising a shape memory alloy fiber cloth, a protein fiber thread to which a phosphorus amide compound is attached, or a copolyester fiber / heat-fusible binder fiber laminate, and the shape at body temperature. A patch characterized by having a memory function.
としてのポリアクリル酸あるいはその塩、水酸化アルミ
ナマグネシウム、ソルビトールと吸収促進及び芳香剤か
らなり、体温下での形状記憶機能を有する事を特徴とし
た貼付剤。3. A plaster comprises a dissolving agent for the main drug, polyacrylic acid or a salt thereof as a shape-retaining / moisturizing agent, magnesium alumina hydroxide, sorbitol and an absorption-promoting and fragrance agent, which has a shape-memory function at body temperature. A patch characterized by having.
してケトプロフェン{2−(m−ベンゾイルフェニル)
プロピオン酸}0.3 〜3重量%と、溶解剤としてヒマシ
油0.5 〜2重量%と、保形・保湿剤として、ポリアクリ
ル酸あるいはその塩を2〜10重量%、水酸化アルミナマ
グネシウムを0.2 〜3重量%、ソルビトールを20〜50重
量%含有し、吸収促進及び芳香剤としてカンファーある
いはメントール0.5 〜2重量%を含有する事を特徴とす
る形状記憶性ケトプロフェン貼付剤。4. A support having stretchable and breathable properties, wherein ketoprofen {2- (m-benzoylphenyl) is used with respect to the amount of paste.
0.3 to 3% by weight of propionic acid, 0.5 to 2% by weight of castor oil as a solubilizer, 2 to 10% by weight of polyacrylic acid or a salt thereof as a shape-retaining / moisturizing agent, and 0.2 to 3 of magnesium alumina hydroxide. A shape memory ketoprofen patch characterized by containing 20% to 50% by weight of sorbitol and 0.5% to 2% by weight of camphor or menthol as an absorption accelerating and aromatic agent.
皮面積から貼付剤を切断して使用する事を特徴とした、
請求項1〜4記載の、断線付きあるいはライナー部分に
切取線が印刷されたケトプロフェン貼付剤。5. The patch is used by cutting from the subject's disease, age, sex, weight and skin-epidermal area before use.
The ketoprofen patch according to claim 1, wherein the ketoprofen patch is provided with a disconnection line or a cutout line printed on the liner portion.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP7092860A JPH08291055A (en) | 1995-04-18 | 1995-04-18 | Shape memory plaster |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP7092860A JPH08291055A (en) | 1995-04-18 | 1995-04-18 | Shape memory plaster |
Publications (1)
Publication Number | Publication Date |
---|---|
JPH08291055A true JPH08291055A (en) | 1996-11-05 |
Family
ID=14066194
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP7092860A Pending JPH08291055A (en) | 1995-04-18 | 1995-04-18 | Shape memory plaster |
Country Status (1)
Country | Link |
---|---|
JP (1) | JPH08291055A (en) |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7635416B1 (en) * | 2002-03-04 | 2009-12-22 | Beyond Borders, LLC | Three-dimensional reconfigurable wall adornment system |
WO2024075082A1 (en) * | 2021-10-19 | 2024-04-11 | Heather Sloan | Menthol- and magnesium-infused kinesiology tape |
-
1995
- 1995-04-18 JP JP7092860A patent/JPH08291055A/en active Pending
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7635416B1 (en) * | 2002-03-04 | 2009-12-22 | Beyond Borders, LLC | Three-dimensional reconfigurable wall adornment system |
WO2024075082A1 (en) * | 2021-10-19 | 2024-04-11 | Heather Sloan | Menthol- and magnesium-infused kinesiology tape |
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