JPH08165244A - Dermatosis therapeutic agent - Google Patents
Dermatosis therapeutic agentInfo
- Publication number
- JPH08165244A JPH08165244A JP7261918A JP26191895A JPH08165244A JP H08165244 A JPH08165244 A JP H08165244A JP 7261918 A JP7261918 A JP 7261918A JP 26191895 A JP26191895 A JP 26191895A JP H08165244 A JPH08165244 A JP H08165244A
- Authority
- JP
- Japan
- Prior art keywords
- agent
- formulated
- therapeutic agent
- local anesthetic
- skin
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
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- 235000010350 erythorbic acid Nutrition 0.000 description 1
- 239000004318 erythorbic acid Substances 0.000 description 1
- RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 1
- 229960001617 ethyl hydroxybenzoate Drugs 0.000 description 1
- 235000010228 ethyl p-hydroxybenzoate Nutrition 0.000 description 1
- 239000004403 ethyl p-hydroxybenzoate Substances 0.000 description 1
- NUVBSKCKDOMJSU-UHFFFAOYSA-N ethylparaben Chemical compound CCOC(=O)C1=CC=C(O)C=C1 NUVBSKCKDOMJSU-UHFFFAOYSA-N 0.000 description 1
- 235000019197 fats Nutrition 0.000 description 1
- 210000000245 forearm Anatomy 0.000 description 1
- LPLVUJXQOOQHMX-UHFFFAOYSA-N glycyrrhetinic acid glycoside Natural products C1CC(C2C(C3(CCC4(C)CCC(C)(CC4C3=CC2=O)C(O)=O)C)(C)CC2)(C)C2C(C)(C)C1OC1OC(C(O)=O)C(O)C(O)C1OC1OC(C(O)=O)C(O)C(O)C1O LPLVUJXQOOQHMX-UHFFFAOYSA-N 0.000 description 1
- UYRUBYNTXSDKQT-UHFFFAOYSA-N glycyrrhizic acid Natural products CC1(C)C(CCC2(C)C1CCC3(C)C2C(=O)C=C4C5CC(C)(CCC5(C)CCC34C)C(=O)O)OC6OC(C(O)C(O)C6OC7OC(O)C(O)C(O)C7C(=O)O)C(=O)O UYRUBYNTXSDKQT-UHFFFAOYSA-N 0.000 description 1
- 229960004949 glycyrrhizic acid Drugs 0.000 description 1
- 235000019410 glycyrrhizin Nutrition 0.000 description 1
- LPLVUJXQOOQHMX-QWBHMCJMSA-N glycyrrhizinic acid Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@@H]1C([C@H]2[C@]([C@@H]3[C@@]([C@@]4(CC[C@@]5(C)CC[C@@](C)(C[C@H]5C4=CC3=O)C(O)=O)C)(C)CC2)(C)CC1)(C)C)C(O)=O)[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O LPLVUJXQOOQHMX-QWBHMCJMSA-N 0.000 description 1
- 239000002554 heparinoid Substances 0.000 description 1
- 150000003840 hydrochlorides Chemical class 0.000 description 1
- 230000009610 hypersensitivity Effects 0.000 description 1
- 150000007529 inorganic bases Chemical class 0.000 description 1
- 229940026239 isoascorbic acid Drugs 0.000 description 1
- 229940074928 isopropyl myristate Drugs 0.000 description 1
- NFIDBGJMFKNGGQ-UHFFFAOYSA-N isopropylmethylphenol Natural products CC(C)CC1=CC=CC=C1O NFIDBGJMFKNGGQ-UHFFFAOYSA-N 0.000 description 1
- 229960003517 isothipendyl Drugs 0.000 description 1
- OQJBSDFFQWMKBQ-UHFFFAOYSA-N isothipendyl Chemical compound C1=CN=C2N(CC(C)N(C)C)C3=CC=CC=C3SC2=C1 OQJBSDFFQWMKBQ-UHFFFAOYSA-N 0.000 description 1
- 229940119170 jojoba wax Drugs 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 150000004667 medium chain fatty acids Chemical class 0.000 description 1
- 229960002409 mepivacaine Drugs 0.000 description 1
- INWLQCZOYSRPNW-UHFFFAOYSA-N mepivacaine Chemical compound CN1CCCCC1C(=O)NC1=C(C)C=CC=C1C INWLQCZOYSRPNW-UHFFFAOYSA-N 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 1
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 description 1
- 229960002216 methylparaben Drugs 0.000 description 1
- 239000004200 microcrystalline wax Substances 0.000 description 1
- 235000019808 microcrystalline wax Nutrition 0.000 description 1
- RZRNAYUHWVFMIP-UHFFFAOYSA-N monoelaidin Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC(O)CO RZRNAYUHWVFMIP-UHFFFAOYSA-N 0.000 description 1
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 1
- GOQYKNQRPGWPLP-UHFFFAOYSA-N n-heptadecyl alcohol Natural products CCCCCCCCCCCCCCCCCO GOQYKNQRPGWPLP-UHFFFAOYSA-N 0.000 description 1
- 229930014626 natural product Natural products 0.000 description 1
- 239000002736 nonionic surfactant Substances 0.000 description 1
- XMLQWXUVTXCDDL-UHFFFAOYSA-N oleyl alcohol Natural products CCCCCCC=CCCCCCCCCCCO XMLQWXUVTXCDDL-UHFFFAOYSA-N 0.000 description 1
- 229940055577 oleyl alcohol Drugs 0.000 description 1
- 239000004006 olive oil Substances 0.000 description 1
- 235000008390 olive oil Nutrition 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 235000010292 orthophenyl phenol Nutrition 0.000 description 1
- 239000004306 orthophenyl phenol Substances 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
- 210000005259 peripheral blood Anatomy 0.000 description 1
- 239000011886 peripheral blood Substances 0.000 description 1
- 235000019271 petrolatum Nutrition 0.000 description 1
- 150000003904 phospholipids Chemical class 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920001451 polypropylene glycol Polymers 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 229960001807 prilocaine Drugs 0.000 description 1
- MVFGUOIZUNYYSO-UHFFFAOYSA-N prilocaine Chemical compound CCCNC(C)C(=O)NC1=CC=CC=C1C MVFGUOIZUNYYSO-UHFFFAOYSA-N 0.000 description 1
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 description 1
- 229960003415 propylparaben Drugs 0.000 description 1
- 239000001397 quillaja saponaria molina bark Substances 0.000 description 1
- 238000005070 sampling Methods 0.000 description 1
- 229930182490 saponin Natural products 0.000 description 1
- 150000007949 saponins Chemical class 0.000 description 1
- 229920002545 silicone oil Polymers 0.000 description 1
- 231100000475 skin irritation Toxicity 0.000 description 1
- 230000036556 skin irritation Effects 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 210000000434 stratum corneum Anatomy 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 229940126585 therapeutic drug Drugs 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 229960000790 thymol Drugs 0.000 description 1
- 229940042585 tocopherol acetate Drugs 0.000 description 1
- ZIBGPFATKBEMQZ-UHFFFAOYSA-N triethylene glycol Chemical compound OCCOCCOCCO ZIBGPFATKBEMQZ-UHFFFAOYSA-N 0.000 description 1
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 description 1
- 239000003871 white petrolatum Substances 0.000 description 1
Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【0001】[0001]
【産業上の利用分野】本発明は、アトピー性皮膚炎、乾
皮症等の皮膚疾患による痒みを伴う皮膚疾患治療剤に関
するものである。BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a therapeutic agent for skin diseases accompanied by itching caused by skin diseases such as atopic dermatitis and xerosis.
【0002】[0002]
【従来の技術】アトピー性皮膚炎等の痒みを伴う皮膚湿
疹の治療には、現在のところ根本的な治療方法はなく、
ステロイド外用剤および鎮痒剤の内服薬が対処療法的に
用いられている。また、根本的な治療にならないまで
も、尿素を配合した外用製剤がアトピー性湿疹の治療薬
として皮膚科領域では汎用されている。2. Description of the Related Art At present, there is no fundamental treatment method for the treatment of skin eczema associated with itching such as atopic dermatitis.
Topical steroids and antipruritic drugs are used as coping therapy. Further, even if it is not a fundamental treatment, an external preparation containing urea is widely used in the dermatological field as a therapeutic drug for atopic eczema.
【0003】[0003]
【発明が解決しようとする課題】アトピー性皮膚炎は慢
性の湿疹であることから、薬物を継続的に使用する必要
がある。しかしながら、ステロイド剤を過剰に摂取する
と顔面などに脂肪沈着し、いわゆる満月様顔貌となり、
多毛症、皮膚裂線などの副作用が生じる。したがって、
外用ステロイド剤を継続的に使用することは困難であ
る。また、尿素を配合した外用製剤では、皮膚湿疹によ
る痒みを抑えることは困難であり、さらに角質の水分保
持量を増加させるため、高濃度の尿素を用いることから
疼痛、紅斑、落屑、過敏症状などの副作用を生じること
がある。Since atopic dermatitis is a chronic eczema, it is necessary to continuously use the drug. However, excessive intake of steroids causes fat deposits on the face, resulting in a so-called full moon-like face,
Side effects such as hirsutism and skin tears occur. Therefore,
Continuous use of topical steroids is difficult. In addition, it is difficult to prevent itching due to skin eczema with an external preparation containing urea, and since it increases the water retention of the keratin, it is necessary to use a high concentration of urea, so pain, erythema, desquamation, hypersensitivity, etc. May cause side effects.
【0004】[0004]
【課題を解決するための手段】かかる事情に鑑み、本発
明者らは継続的に使用しても副作用が少なく、しかも痒
みを抑えて、乾燥した肌に適度な水分を補給する製剤に
ついて鋭意検討した結果、局所麻酔薬、吸収促進剤およ
びムコ多糖の多硫酸エステルを配合した製剤がアトピー
性皮膚炎の症状を改善できることを見いだし、本発明を
完成したものである。In view of such circumstances, the present inventors have diligently studied a preparation which has few side effects even if it is continuously used, suppresses itch, and replenishes dry skin with an appropriate amount of water. As a result, they have found that a preparation containing a local anesthetic, an absorption enhancer and a polysulfate of mucopolysaccharide can improve the symptoms of atopic dermatitis, and completed the present invention.
【0005】すなわち本発明は、局所麻酔薬、経皮吸収
促進剤およびムコ多糖の多硫酸エステルを配合したこと
を特徴とする皮膚疾患治療剤である。That is, the present invention is a therapeutic agent for skin diseases, which comprises a local anesthetic, a percutaneous absorption enhancer and a polysulfate of mucopolysaccharide.
【0006】本発明において使用する局所麻酔薬として
は、リドカイン、ジブカイン、ブピバカイン、プリロカ
イン、メピバカインおよびこれらの塩酸塩があげられ
る。より好ましい局所麻酔薬としては、リドカインおよ
びその塩酸塩であり、その配合量は0.1〜5重量%が
望ましい。経皮吸収促進剤としては、メントール、オレ
イン酸、オクチルドデカノール、ミリスチン酸オクチル
ドデシル、プロピレングリコールに局所麻酔薬の顕著な
吸収促進効果があり、その配合量としては1〜10重量
%が望ましい。The local anesthetics used in the present invention include lidocaine, dibucaine, bupivacaine, prilocaine, mepivacaine and their hydrochlorides. More preferable local anesthetics are lidocaine and its hydrochloride, and its compounding amount is preferably 0.1 to 5% by weight. As a percutaneous absorption enhancer, menthol, oleic acid, octyldodecanol, octyldodecyl myristate, and propylene glycol have a remarkable effect of promoting absorption of a local anesthetic, and the compounding amount thereof is preferably 1 to 10% by weight.
【0007】また、本発明に使用するムコ多糖の多硫酸
エステル(以下MPSと略す)は、動物の臓器より抽出
したヘパリノイド物質であり、抗トロンビン作用、抗血
液凝固作用および抹消血液の循環促進作用とともに、優
れた保湿作用を有することも知られており、その配合量
としては0.01〜0.5重量%が望ましい。The polysulfate of mucopolysaccharide (hereinafter abbreviated as MPS) used in the present invention is a heparinoid substance extracted from the organs of animals, and has antithrombin action, anticoagulant action and peripheral blood circulation promoting action. At the same time, it is also known that it has an excellent moisturizing action, and its content is preferably 0.01 to 0.5% by weight.
【0008】本発明の皮膚疾患治療剤には、上述の成分
に加えて、グリチルリチン、グリチルリチン酸ジカリウ
ム、グリチルレチン酸などの消炎剤、ジフェンヒドラミ
ン、塩酸イソチペンジルなどの抗ヒスタミン剤などを配
合することができる。また、保湿剤としてグリセリン、
ポリエチレングリコール、1,3−ブチレングリコー
ル、エチレングリコール、ジエチレングリコール、トリ
エチレングリコール、ポリプロピレングリコール、ポリ
グリセリン、ソルビトール水溶液が用いることができる
が、皮膚刺激性の点からグリセリン、1,3−ブチレン
グリコールが好適である。これらの保湿剤の配合量は
0.5〜20重量%、好ましくは1〜10重量%配合さ
れる。In addition to the above components, the therapeutic agent for skin diseases of the present invention may contain anti-inflammatory agents such as glycyrrhizin, dipotassium glycyrrhizinate and glycyrrhetinic acid, and antihistamines such as diphenhydramine and isothipendyl hydrochloride. Also, glycerin as a moisturizer,
Polyethylene glycol, 1,3-butylene glycol, ethylene glycol, diethylene glycol, triethylene glycol, polypropylene glycol, polyglycerin, and sorbitol aqueous solution can be used, but glycerin and 1,3-butylene glycol are preferable from the viewpoint of skin irritation. Is. The amount of these moisturizers is 0.5 to 20% by weight, preferably 1 to 10% by weight.
【0009】本発明の皮膚疾患治療組成物はゲル剤、ク
リーム剤、ローション剤、乳液剤等の各種の外用剤とす
ることができる。以下に本発明の基剤成分について更に
詳細に説明する。The composition for treating skin diseases of the present invention can be used as various external preparations such as gels, creams, lotions and emulsions. The base component of the present invention will be described in more detail below.
【0010】ゲル剤の場合には、カルボキシビニルポリ
マーの配合量は、ゲル剤の物理的熱安定性、透明性、稠
度および使用感などから、0.1〜5重量%、好ましく
は0.3〜1.5重量%配合する。pH調節剤として
は、水酸化ナトリウム、水酸化カリウム、アンモニア水
などの無機塩基、トリエタノールアミン、ジエタノール
アミン、ジイソプロパノールアミン、トリイソプロパノ
ールアミン、アルギニンなどの有機塩基があげられる
が、有機塩基が特に好ましい。これらのpH調節剤の配
合量は、製剤のpHが3〜9、好ましくは6〜8になる
ように0.02〜3重量%の範囲で添加する。水の配合
量は他の基剤に合わせて適宜増減するが、20〜70重
量%、好ましくは35〜55重量%配合する。In the case of a gel, the blending amount of carboxyvinyl polymer is 0.1 to 5% by weight, preferably 0.3, from the viewpoint of physical heat stability, transparency, consistency and feeling of use of the gel. -1.5 wt% is compounded. Examples of the pH adjusting agent include inorganic bases such as sodium hydroxide, potassium hydroxide and aqueous ammonia, and organic bases such as triethanolamine, diethanolamine, diisopropanolamine, triisopropanolamine and arginine, and organic bases are particularly preferable. . The pH adjusting agent is added in an amount of 0.02 to 3% by weight so that the pH of the preparation is 3 to 9, preferably 6 to 8. The amount of water to be added may be appropriately adjusted depending on the other base, but it is 20 to 70% by weight, preferably 35 to 55% by weight.
【0011】クリーム剤の油分としては、天然から合成
のものまで幅広く選択できるが、例えば、白色ワセリ
ン、流動パラフィン、固形パラフィン、セレシン、マイ
クロクリスタリンワックス、コレステロール、スクワラ
ン、オリーブ油、ミンク油、ホホバ油、硬化ヒマシ油、
硬化ヤシ油、ミツロウ、ステアリン酸、パルミチン酸、
ラウリン酸、ステアリルアルコール、セチルアルコー
ル、ラウリルアルコール、オレイルアルコール、ミリス
チン酸イソプロピル、モノステアリン酸グリセリン、モ
ノオレイン酸プロピレングリコール、モノオレイン酸グ
リセリン、モノカプリン酸ソルビタン、クエン酸モノス
テアリン酸グリセリン、ジステアリン酸ジグリセリン、
モノラウリン酸デカグリセリル、シリコーンオイルなど
があげられ、これらは単独または任意の混合物として使
用することができる。これらの油分の配合量は0.5〜
60重量%、好ましくは1〜40重量%配合する。The oil component of the cream agent can be selected from a wide range of natural to synthetic ones. For example, white petrolatum, liquid paraffin, solid paraffin, ceresin, microcrystalline wax, cholesterol, squalane, olive oil, mink oil, jojoba oil, Hydrogenated castor oil,
Hydrogenated coconut oil, beeswax, stearic acid, palmitic acid,
Lauric acid, stearyl alcohol, cetyl alcohol, lauryl alcohol, oleyl alcohol, isopropyl myristate, glyceryl monostearate, propylene glycol monooleate, glyceryl monooleate, sorbitan monocaprate, glyceryl monostearate, distearate distearate Glycerin,
Decaglyceryl monolaurate, silicone oil and the like can be mentioned, and these can be used alone or as an arbitrary mixture. The amount of these oil components is 0.5-
The amount is 60% by weight, preferably 1 to 40% by weight.
【0012】クリーム剤、ローション剤に用いる界面活
性剤としては、ポリオキシエチレン脂肪酸エステル、ポ
リオキシエチレンソルビタン脂肪酸エステル、ポリグリ
セリンアルキルフェニルエーテル、ポリオキシエチレン
グリセリン脂肪酸エステル、ポリオキシエチレン硬化ヒ
マシ油などの非イオン性界面活性剤、あるいはカゼイ
ン、サポニン、リン脂質、糖ペプチドなどの天然物由来
の界面活性剤などがあげられ、これらは単独または任意
の混合物として使用することができる。これら界面活性
剤の配合量としては0.1〜25重量%である。水の配
合量には特に限定はないが、ローション剤の場合には4
0〜96重量%、クリーム剤の場合には20〜40重量
%配合する。Surfactants used in creams and lotions include polyoxyethylene fatty acid ester, polyoxyethylene sorbitan fatty acid ester, polyglycerin alkyl phenyl ether, polyoxyethylene glycerin fatty acid ester, polyoxyethylene hydrogenated castor oil and the like. Examples thereof include nonionic surfactants and surfactants derived from natural products such as casein, saponin, phospholipids and glycopeptides, and these can be used alone or as an arbitrary mixture. The content of these surfactants is 0.1 to 25% by weight. The amount of water to be added is not particularly limited, but in the case of a lotion, it is 4
0 to 96% by weight, and 20 to 40% by weight in the case of cream.
【0013】また本発明の組成物には、これらの基剤成
分に加えて防腐剤、抗酸化剤などの補助成分を適宜配合
することができる。防腐剤としては、メチルパラベン、
エチルパラベン、プロピルパラベン、ブチルパラベン、
チモール、クロルクレゾール、オルトフェニルフェノー
ル、イソプロピルメチルフェノールなどがあげられる。
抗酸化剤としては、ジブチルヒドロキシトルエン、エリ
ソルビン酸、酢酸トコフェロールなどがあげられる。In addition to these base components, auxiliary components such as antiseptics and antioxidants can be appropriately added to the composition of the present invention. As a preservative, methylparaben,
Ethylparaben, propylparaben, butylparaben,
Examples include thymol, chlorcresol, orthophenylphenol, and isopropylmethylphenol.
Examples of antioxidants include dibutylhydroxytoluene, erythorbic acid, and tocopherol acetate.
【0014】[0014]
【発明の効果】本発明で得られる局所麻酔薬、経皮吸収
促進剤およびMPSを配合した皮膚疾患治療薬は、痒み
の抑制と優れた保湿効果により、慢性難治性の皮膚疾患
であるアトピー性皮膚炎や乾皮症の治療剤として有用で
ある。EFFECTS OF THE INVENTION A therapeutic agent for skin diseases containing a local anesthetic, a percutaneous absorption enhancer and MPS obtained by the present invention is an atopic skin disease that is a chronic refractory skin disease due to the suppression of itch and an excellent moisturizing effect. It is useful as a therapeutic agent for dermatitis and xerosis.
【0015】[0015]
【実施例】以下に実施例および試験例をあげ、本発明を
具体的に説明する。EXAMPLES The present invention will be specifically described with reference to Examples and Test Examples.
【0016】実施例1〜11、比較例 表1に示す成分をそれぞれ配合して、第一二改正日本薬
局方ローション剤の製法に準じて調製した。Examples 1 to 11 and Comparative Example Each of the components shown in Table 1 was blended and prepared according to the manufacturing method of the Japanese Pharmacopoeia Lotion of the First and Second Amendments.
【0017】[0017]
【表1】 [Table 1]
【0018】実施例12 以下の各成分をそれぞれ配合して、上述の実施例に準じ
て調製した。 リドカイン 3 (重量%) MPS 0.3 塩酸ジフェンヒドラミン 1 レシチン 2 ニッコールTS−10 1 流動パラフィン 5 グリセリン 3 1,3−ブチレングリコール 3 オクチルドデカノール 3 カルボキシビニルポリマー 0.1 精製水 全100gとなるように調製。Example 12 The following components were each mixed and prepared according to the above-mentioned example. Lidocaine 3 (wt%) MPS 0.3 Diphenhydramine hydrochloride 1 Lecithin 2 Nikkor TS-10 1 Liquid paraffin 5 Glycerin 3 1,3-Butylene glycol 3 Octyldodecanol 3 Carboxyvinyl polymer 0.1 Purified water Total 100 g Preparation.
【0019】実施例13 以下の各成分をそれぞれ配合して、上述の実施例に準じ
て調製した。 リドカイン 1 (重量%) MPS 0.3 塩酸ジフェンヒドラミン 2 レシチン 1 ニッコールTS−10 1 スクワラン 5 オレイン酸 3 1,3−ブチレングリコール 10 カルボキシビニルポリマー 0.1 精製水 全100gとなるように調製。Example 13 The following components were each mixed and prepared according to the above-mentioned example. Lidocaine 1 (wt%) MPS 0.3 Diphenhydramine hydrochloride 2 Lecithin 1 Nikkor TS-10 1 Squalane 5 Oleic acid 3 1,3-butylene glycol 10 Carboxyvinyl polymer 0.1 Prepared to a total of 100 g of purified water.
【0020】実施例14 以下の各成分をそれぞれ配合して、上述の実施例に準じ
て調製した。 リドカイン 3 (重量%) MPS 0.3 塩酸ジフェンヒドラミン 1 グリチルリチン酸ジカリウム 1 メントール 0.5 中鎖脂肪酸トリグリセリド 3.5 グリセリン 5 1,3−ブチレングリコール 5 カルボキシビニルポリマー 0.2 ステアリン酸 0.5 精製水 全100gとなるように調製。Example 14 The following components were each mixed and prepared according to the above-mentioned example. Lidocaine 3 (wt%) MPS 0.3 Diphenhydramine hydrochloride 1 Dipotassium glycyrrhizinate 1 Menthol 0.5 Medium-chain fatty acid triglyceride 3.5 Glycerin 5 1,3-butylene glycol 5 Carboxyvinyl polymer 0.2 Stearic acid 0.5 Purified water Prepared to be 100g.
【0021】試験例1 実施例1〜11および比較例の製剤について、ヘアレス
ラットの腹部摘出皮膚を用いリドカインの皮膚透過試験
を行った。2チャンバー拡散セルに摘出皮膚を挟み、開
放した角質層側に製剤20μlを塗布し、精製水3ml
を入れた受容槽から、経時的にサンプリングしてそのリ
ドカイン量を定量した。吸収促進剤1成分を配合した結
果を図1に、吸収促進剤2成分を配合した結果を図2に
示す。7時間後の累積透過量を比較例と比べてみると、
図1の実施例1〜5では2.8〜4.5倍の促進効果
が、図2では実施例11が6.6倍と最も優れた促進効
果を示した。Test Example 1 With respect to the preparations of Examples 1 to 11 and Comparative Example, a skin permeation test of lidocaine was carried out using the skin of the abdomen of hairless rats. The excised skin is sandwiched between two-chamber diffusion cells, 20 μl of the preparation is applied to the open stratum corneum, and 3 ml of purified water is applied.
The amount of lidocaine was quantified by sampling over time from the receiving tank containing the. FIG. 1 shows the result of blending the absorption enhancer 1 component, and FIG. 2 shows the result of blending the absorption enhancer 2 component. Comparing the cumulative transmission amount after 7 hours with the comparative example,
In Examples 1 to 5 of FIG. 1, the accelerating effect was 2.8 to 4.5 times, and in FIG. 2, Example 11 was 6.6 times, which was the most excellent accelerating effect.
【0022】試験例2 実施例6、11および比較例の製剤について、ヒトにお
ける局所麻酔効力試験を行った。前腕屈側に製剤を10
μl/8cm2塗布して、皮膚を刺激したときの痛みの
感覚を評価した。痛み評価はプッシュプルゲージ(AIKO
H CPU GAUGE 14978)の円錐状の先端を皮膚に5gの力
で押して、そのときの痛みの感覚を点数化して行った。
測定は製剤塗布前と塗布直後から30分毎に4時間まで
行った。なお、痛みの感覚は、強い痛みを1点、弱い痛
みを0.5点、無痛を0点とし1箇所につき10回測定
しそれを合計した。結果は図3に示すように、局所麻酔
効果は試験例1の皮膚透過試験結果と相関し、特に実施
例11は優れた局所麻酔効果を示した。Test Example 2 The preparations of Examples 6 and 11 and Comparative Example were subjected to a local anesthetic efficacy test in humans. 10 preparations on flexion side of forearm
It was applied in an amount of μl / 8 cm 2 and the sensation of pain when the skin was stimulated was evaluated. Pain is evaluated by push-pull gauge (AIKO
The conical tip of H CPU GAUGE 14978) was pressed against the skin with a force of 5 g, and the pain sensation at that time was scored.
The measurement was performed every 30 minutes up to 4 hours from before and immediately after the application of the preparation. As for the sensation of pain, strong pain was 1 point, weak pain was 0.5 point, and no pain was 0 point, which was measured 10 times at one place and totaled. As shown in FIG. 3, the results show that the local anesthetic effect correlates with the results of the skin permeation test of Test Example 1, and particularly Example 11 showed an excellent local anesthetic effect.
【図1】図1は実施例1〜5および比較例の製剤につい
て、ヘアレスラットの腹部摘出皮膚を用いてリドカイン
の皮膚透過を測定した結果である。FIG. 1 shows the results of measuring the skin permeation of lidocaine using the abdominal excised skin of hairless rats for the formulations of Examples 1 to 5 and Comparative Example.
【図2】図2は実施例6〜11および比較例の製剤につ
いて、ヘアレスラットの腹部摘出皮膚を用いてリドカイ
ンの皮膚透過を測定した結果である。FIG. 2 shows the results of measuring the skin permeation of lidocaine using the skin of the abdomen of hairless rats for the preparations of Examples 6 to 11 and Comparative Example.
【図3】図3は実施例6、11および比較例の製剤につ
いて、ヒトにおける局所麻酔効力を測定した結果であ
る。FIG. 3 shows the results of measuring the local anesthetic efficacy in humans for the formulations of Examples 6 and 11 and Comparative Example.
───────────────────────────────────────────────────── フロントページの続き (72)発明者 漆崎 文男 東京都豊島区高田3丁目24番1号 大正製 薬株式会社内 ─────────────────────────────────────────────────── ─── Continuation of the front page (72) Inventor Fumio Urushizaki 3-24-1 Takada, Toshima-ku, Tokyo Taisho Pharmaceutical Co., Ltd.
Claims (2)
ルを配合したことを特徴とする皮膚疾患治療剤。1. A therapeutic agent for skin diseases, which comprises a local anesthetic and a polysulfate of mucopolysaccharide.
ール、オレイン酸、オクチルドデカノール、ミリスチン
酸オクチルドデシル、プロピレングリコールの1種また
は2種以上を添加してなる請求項1記載の皮膚疾患治療
剤。2. A skin disease according to claim 1, wherein one or more of menthol, oleic acid, octyldodecanol, octyldodecyl myristate, and propylene glycol are added as a percutaneous absorption enhancer of a local anesthetic. Therapeutic agent.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP7261918A JPH08165244A (en) | 1994-10-12 | 1995-10-11 | Dermatosis therapeutic agent |
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP6-245946 | 1994-10-12 | ||
JP24594694 | 1994-10-12 | ||
JP7261918A JPH08165244A (en) | 1994-10-12 | 1995-10-11 | Dermatosis therapeutic agent |
Publications (1)
Publication Number | Publication Date |
---|---|
JPH08165244A true JPH08165244A (en) | 1996-06-25 |
Family
ID=26537490
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP7261918A Pending JPH08165244A (en) | 1994-10-12 | 1995-10-11 | Dermatosis therapeutic agent |
Country Status (1)
Country | Link |
---|---|
JP (1) | JPH08165244A (en) |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2001501609A (en) * | 1996-09-27 | 2001-02-06 | ヘキスト・アクチエンゲゼルシヤフト | Antifungal gel with high active compound release |
JP2002505272A (en) * | 1998-03-06 | 2002-02-19 | スコーティア・ホールディングス・ピー・エル・シー | Oil-in-water topical composition comprising a galactolipid substance as emulsifier and having a sustained action of the introduced active substance |
JP2003321347A (en) * | 2002-05-07 | 2003-11-11 | Rohto Pharmaceut Co Ltd | Gel ointment |
EP1669064A1 (en) * | 2004-12-10 | 2006-06-14 | Bionics Pharma Gmbh | Composition and method of a topical therapy of neurodermatitis |
-
1995
- 1995-10-11 JP JP7261918A patent/JPH08165244A/en active Pending
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2001501609A (en) * | 1996-09-27 | 2001-02-06 | ヘキスト・アクチエンゲゼルシヤフト | Antifungal gel with high active compound release |
JP2002505272A (en) * | 1998-03-06 | 2002-02-19 | スコーティア・ホールディングス・ピー・エル・シー | Oil-in-water topical composition comprising a galactolipid substance as emulsifier and having a sustained action of the introduced active substance |
JP2003321347A (en) * | 2002-05-07 | 2003-11-11 | Rohto Pharmaceut Co Ltd | Gel ointment |
JP4549006B2 (en) * | 2002-05-07 | 2010-09-22 | ロート製薬株式会社 | Gel ointment |
EP1669064A1 (en) * | 2004-12-10 | 2006-06-14 | Bionics Pharma Gmbh | Composition and method of a topical therapy of neurodermatitis |
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