JP2010254645A - Oral ultraviolet resistance enhancer - Google Patents
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- JP2010254645A JP2010254645A JP2009109044A JP2009109044A JP2010254645A JP 2010254645 A JP2010254645 A JP 2010254645A JP 2009109044 A JP2009109044 A JP 2009109044A JP 2009109044 A JP2009109044 A JP 2009109044A JP 2010254645 A JP2010254645 A JP 2010254645A
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Abstract
Description
本発明は、経口摂取により、皮膚の紫外線抵抗性を向上させる経口紫外線抵抗性向上剤に関する。 The present invention relates to an oral ultraviolet resistance improver that improves the ultraviolet resistance of skin by oral ingestion.
近年、オゾン層の減少が一要因となり、紫外線による皮膚障害が問題になっている。例えば、慢性的な紫外線の暴露により、皮膚の紅班や浮腫が発生したり、しわやたるみ、しみやそばかすの形成が顕著となったり、皮膚の弾力性の低下、皮膚の黒化、黄ばみの増加、角質水分量の減少等が誘導される。 In recent years, a decrease in the ozone layer has become a factor, and skin damage due to ultraviolet rays has become a problem. For example, chronic UV exposure may cause erythema and edema of the skin, wrinkles, sagging, spots and freckles, and skin elasticity, skin darkening, yellowing Increase, decrease in keratin water content, etc. are induced.
従来、紫外線による皮膚へのダメージを改善する手段としては、紫外線散乱剤や紫外線吸収剤を配合したいわゆる日焼け止めを用いることや、メラニン産生抑制作用等を有する美白剤を用いることが主に行われているが、これらのほとんどは皮膚外用剤として使用した際に得られる作用を期待したものである。 Conventionally, as means for improving damage to the skin due to ultraviolet rays, so-called sunscreens containing ultraviolet scattering agents and ultraviolet absorbers have been mainly used, and whitening agents having a melanin production inhibitory effect and the like have been mainly used. However, most of these are expected to have an effect obtained when used as a skin external preparation.
しかしながら、近年、ホリスティック皮膚制御に基づくアプローチから、紫外線に強い身体をつくることが理想的であるとされ、経口摂取によって、皮膚の紫外線に対する抵抗力を向上させることが試みられている。例えば、ラクトバチルス属菌を経口摂取した場合に紫外線照射による皮膚バリア機能の損傷を抑制すること（特許文献１）、カロチノイドにエラスチンやセラミドを配合した組成物を経口摂取した場合に、紫外線に誘発される皮膚の紅斑を効果的に抑制し得ることが報告されている（特許文献２）。 However, in recent years, from an approach based on holistic skin control, it is considered ideal to create a body resistant to ultraviolet rays, and attempts have been made to improve the resistance of skin to ultraviolet rays by ingestion. For example, when Lactobacillus sp is orally ingested, it suppresses damage to the skin barrier function due to UV irradiation (Patent Document 1). It has been reported that the erythema of the skin to be able to be suppressed effectively (patent document 2).
メシル酸ガベキサートは、セリンプロテアーゼ阻害剤で、トリプシン、カリクレイン、プラスミン等の阻害効果を持ち、膵炎、汎発性血管内血液凝固症、皮膚ビラン、潰瘍の治療薬として用いられている医薬品であるが、皮膚に塗布した場合に美白効果を発揮することが報告されている（特許文献３）。
しかしながら、メシル酸ガベキサートに、皮膚の紫外線に対する抵抗性を改善する作用があることはこれまで知られていない。
Gabexate mesylate is a serine protease inhibitor, which has inhibitory effects on trypsin, kallikrein, plasmin, etc., and is used as a therapeutic agent for pancreatitis, generalized intravascular blood coagulation, skin bilane, and ulcer. It has been reported that whitening effect is exhibited when applied to the skin (Patent Document 3).
However, it has not been known so far that gabexate mesylate has an effect of improving the resistance of the skin to ultraviolet rays.
本発明は、経口摂取により、皮膚の紫外線に対する抵抗力を高め、紫外線の暴露により生じる皮膚のダメージを軽減又は抑制できる、紫外線抵抗性向上剤を提供することに関する。 The present invention relates to providing an ultraviolet resistance improver that can increase the skin's resistance to ultraviolet rays and reduce or suppress skin damage caused by exposure to ultraviolet rays by oral ingestion.
本発明者らは、皮膚の紫外線抵抗性を向上させる経口摂取可能な素材について検討したところ、メシル酸ガベキサートを経口摂取した場合に、紫外線暴露による皮膚紅斑の発症が有意に抑制でき、これが紫外線抵抗性向上剤として有用であることを見出した。 The present inventors examined an orally ingestible material that improves the ultraviolet resistance of the skin, and when orally ingesting gabexate mesylate, the onset of skin erythema due to ultraviolet exposure can be significantly suppressed, which is It was found useful as a property improver.
すなわち本発明は、以下の１）〜３）に係るものである。
１）メシル酸ガベキサートを有効成分とする経口紫外線抵抗性向上剤。
２）紫外線暴露により誘発される皮膚障害を軽減又は抑制する上記１）の経口紫外線抵抗性向上剤。
３）紫外線暴露により誘発される皮膚障害が、皮膚の炎症又は皮膚老化である上記２）の経口紫外線抵抗性向上剤。
That is, the present invention relates to the following 1) to 3).
1) An oral ultraviolet resistance improver comprising gabexate mesylate as an active ingredient.
2) The oral ultraviolet resistance improver of 1) above, which reduces or suppresses skin damage induced by ultraviolet exposure.
3) The oral ultraviolet resistance improver according to 2) above, wherein the skin disorder induced by ultraviolet exposure is skin inflammation or skin aging.
本発明の紫外線抵抗性向上剤は、例えば、皮膚への紫外線の暴露によって生じる、紅班や浮腫等の皮膚の炎症、しわやたるみの形成、しみやそばかすの形成、皮膚の弾力性の低下、皮膚の黒化、黄ばみの増加、角質水分量の減少といったいわゆる皮膚老化又は皮膚劣化等の皮膚のダメージの軽減又は抑制に有効である。 The ultraviolet resistance improver of the present invention is, for example, skin inflammation such as erythema or edema caused by exposure to ultraviolet rays on the skin, formation of wrinkles and sagging, formation of spots and freckles, reduction of skin elasticity, It is effective for reducing or suppressing skin damage such as so-called skin aging or skin deterioration such as skin blackening, yellowing increase and keratin water content reduction.
本発明の紫外線抵抗性向上剤において用いられるメシル酸ガベキサートは、下記化学構造式で表されるものである。 The gabexate mesylate used in the ultraviolet resistance improver of the present invention is represented by the following chemical structural formula.
メシル酸ガベキサートは、公知の方法により製造できるが、市販品を購入して使用することもできる。 Although gabexate mesylate can be produced by a known method, a commercially available product can also be purchased and used.
後記実施例に示すように、メシル酸ガベキサートをマウスに経口摂取した後に、紫外線照射した場合、当該紫外線による皮膚紅斑の発症が有意に抑制された。すなわち、メシル酸ガベキサートは、皮膚の紫外線に対する抵抗力を高める紫外線抵抗性向上剤として使用することができ、また、当該紫外線抵抗性向上剤を製造するために使用することができる。
従って、本発明の経口紫外線抵抗性向上剤は、紫外線暴露によって誘発される、皮膚の紅班や浮腫等の皮膚の炎症、しわやたるみの形成、しみやそばかすの形成、皮膚の弾力性の低下、皮膚の黒化、黄ばみの増加、角質水分量の減少といった皮膚老化又は皮膚劣化等の皮膚障害を軽減又は抑制するための経口医薬品若しくは医薬部外品又は食品として有用である。
As shown in Examples described later, when gabexate mesylate was orally ingested into mice and then irradiated with ultraviolet rays, the development of skin erythema due to the ultraviolet rays was significantly suppressed. That is, gabexate mesylate can be used as an ultraviolet resistance improver that enhances the skin's resistance to ultraviolet light, and can be used to produce the ultraviolet resistance improver.
Therefore, the oral ultraviolet resistance improver of the present invention is induced by exposure to ultraviolet rays, skin inflammation such as erythema and edema of the skin, formation of wrinkles and sagging, formation of spots and freckles, reduction of skin elasticity. It is useful as an oral drug or quasi-drug or food for reducing or suppressing skin aging such as skin aging or skin deterioration such as skin blackening, yellowing increase, and decrease in keratin water content.
本発明の経口紫外線抵抗性向上剤の剤型は、固形製剤又は液体製剤の何れでもよく、具体的には、錠剤、被覆錠剤、カプセル剤、顆粒剤、散剤、粉剤、徐放性製剤、懸濁液、エマルジョン剤、内服液、糖衣錠、丸剤、細粒剤、シロップ剤、エリキシル剤等が挙げられる。 The dosage form of the oral ultraviolet resistance improver of the present invention may be either a solid preparation or a liquid preparation. Specifically, tablets, coated tablets, capsules, granules, powders, powders, sustained-release preparations, suspensions. Suspensions, emulsions, oral liquids, dragees, pills, fine granules, syrups, elixirs and the like can be mentioned.
上記製剤には、メシル酸ガベキサートに、薬学的に許容される担体を配合することができる。斯かる担体としては、例えば、賦形剤、結合剤、崩壊剤、滑沢剤、希釈剤、浸透圧調整剤、流動性促進剤、吸収助剤、ｐＨ調整剤、乳化剤、防腐剤、安定化剤、酸化防止剤、着色剤、紫外線吸収剤、湿潤剤、増粘剤、光沢剤、活性増強剤、抗炎症剤、殺菌剤、矯味剤、矯臭剤、増量剤、界面活性剤、分散剤、緩衝剤、保存剤、固着剤、香料、被膜剤等が挙げられる。また、当該製剤には、ビタミンＣ、ビタミンＥ、カロチノイド等の薬効成分を適宜配合することもできる。 In the above preparation, a pharmaceutically acceptable carrier can be added to gabexate mesylate. Such carriers include, for example, excipients, binders, disintegrants, lubricants, diluents, osmotic pressure regulators, fluidity promoters, absorption aids, pH adjusters, emulsifiers, preservatives, stabilization. Agent, antioxidant, colorant, UV absorber, wetting agent, thickener, brightener, activity enhancer, anti-inflammatory agent, bactericidal agent, flavoring agent, flavoring agent, extender, surfactant, dispersant, Buffering agents, preservatives, fixing agents, fragrances, coating agents and the like can be mentioned. In addition, medicinal ingredients such as vitamin C, vitamin E, carotenoid and the like can be appropriately blended in the preparation.
上記製剤におけるメシル酸ガベキサートの含有量は、通常、製剤全質量の０．００１〜９０質量％であり、０．０１〜６０質量％が好ましい。 The content of gabexate mesylate in the above preparation is usually 0.001 to 90 mass%, preferably 0.01 to 60 mass%, based on the total mass of the preparation.
本発明の紫外線抵抗性向上剤を各種食品として使用する場合、一般飲食品のほか、紫外線によって生じる、皮膚の紅班や浮腫、しわやたるみの形成、しみやそばかすの形成、皮膚の弾力性の低下、皮膚の黒化等の皮膚のダメージを軽減又は抑制することをコンセプトとし、必要に応じてその旨表示した美容食品、病者用食品、栄養機能食品又は特定保健用食品等の機能性食品に応用できる。 When using the ultraviolet resistance improver of the present invention as various foods, in addition to general food and drink, erythema and edema of the skin, wrinkles and sagging, spots and freckles, and skin elasticity caused by ultraviolet rays. Functional foods such as beauty foods, foods for the sick, functional nutritional foods or foods for specified health, with the concept of reducing or suppressing skin damage such as reduction and skin blackening, as necessary It can be applied to.
食品の形態は、固形、半固形または液状であり得る。食品の例としては、パン類、麺類、クッキー等の菓子類、ゼリー類、乳製品、冷凍食品、インスタント食品、でんぷん加工製品、加工肉製品、その他加工食品、コーヒー飲料等の飲料、スープ類、調味料、栄養補助食品等、及びそれらの原料が挙げられる。また、上記の経口投与製剤と同様、錠剤形態、丸剤形態、カプセル形態、液剤形態、シロップ形態、粉末形態、顆粒形態等であってもよい。 The form of the food product can be solid, semi-solid or liquid. Examples of food include confectionery such as breads, noodles, cookies, jelly, dairy products, frozen foods, instant foods, processed starch products, processed meat products, other processed foods, coffee beverages, soups, Examples include seasonings, dietary supplements, and the like, and raw materials thereof. Further, like the above-mentioned oral administration preparation, it may be in tablet form, pill form, capsule form, liquid form, syrup form, powder form, granule form and the like.
斯かる形態の食品は、メシル酸ガベキサートの他、他の飲食品材料や、溶剤、軟化剤、油、乳化剤、防腐剤、香科、安定剤、着色剤、紫外線吸収剤、酸化防止剤、保湿剤、増粘剤、固着剤、分散剤、湿潤剤等を適宜組み合わせて配合し、調製することができる。 In addition to gabexate mesylate, foods of this form include other food and drink materials, solvents, softeners, oils, emulsifiers, preservatives, fragrances, stabilizers, colorants, UV absorbers, antioxidants, and moisturizers. An agent, a thickener, a sticking agent, a dispersant, a wetting agent, and the like can be blended and prepared as appropriate.
また、飲食品中におけるメシル酸ガベキサートの含有量は、その使用形態により異なるが、通常、０．０００１〜５０質量％であり、０．００１〜１０質量％が好ましい。 Moreover, although content of gabexate mesylate in food / beverage products changes with the usage forms, it is 0.0001-50 mass% normally, and 0.001-10 mass% is preferable.
本発明の紫外線抵抗性向上剤を医薬品として使用する場合の投与量は、患者の状態、体重、性別、年齢又はその他の要因に従って変動し得るが、経口投与の場合の成人１人当たりの１日の投与量は、通常、メシル酸ガベキサートとして０．００１〜１００ｇが好ましい。また、上記製剤は、任意の投与計画に従って投与され得るが、１日１回〜数回に分け、数週間〜数ヶ月間継続して投与することが好ましい。 The dosage when the UV resistance improver of the present invention is used as a pharmaceutical may vary according to the patient's condition, body weight, sex, age or other factors, but the daily dose per adult for oral administration The dose is usually preferably 0.001 to 100 g as gabexate mesylate. Moreover, although the said formulation can be administered according to arbitrary administration schedules, it is preferable to divide once to several times a day, and to administer continuously for several weeks to several months.
実施例１ 紫外線による皮膚紅斑発症抑制作用
（１）方法
ヘアレスマウスHR-1(雌性、7週齢)(日本SLC)を1週間以上予備飼育後、コントロール群、メシル酸ガベキサート投与群とに分けた。試験期間中、飼料および水は自由摂取させ、温度23±1℃、湿度50±1％、照明時間7:00−19:00の条件下で飼育した。
メシル酸ガベキサート投与群は、100mg/kg体重 を、投与量が0.1mL/10g体重 になるように調製し、メシル酸ガベキサート（和光純薬工業（株））をエマルジョン形態で、1日1回2週間、胃ゾンデを用いて強制経口投与した。コントロール群は、メシル酸ガベキサートを除いたものでエマルジョンとし、同様に経口投与した。
経口投与2週後に、ペントバルビタール麻酔下にて、マウス背部に0.6cm×1.0cmの部位を近接して2列×3行＝6ヶ所設定し、1mW/cm2のUVB照射線量で、0秒間(0mJ)と40秒間(40mJ)照射した(各3ヶ所)。照射48時間後の紅斑の程度を、目視による5段階評価(−；反応なし、±(最小紅斑)；軽度または部分的紅斑、＋；明らかな全面紅斑、＋＋；紅斑と浮腫、＋＋＋；紅斑と浮腫と水疱)と、色彩色差計OFC-300A(日本電色工業)を用いて皮膚色(a*値)測定を行った。a*値は皮膚色の赤味を表す指標であり、a*値が大きいほど皮膚が赤色に変化、すなわち紅斑が生じていることを示している。
Example 1 Skin Erythema Inhibition Action by Ultraviolet Light (1) Method Hairless mouse HR-1 (female, 7 weeks old) (Japan SLC) was preliminarily raised for 1 week or more and then divided into a control group and a gabexate mesylate administration group. . During the test period, food and water were freely consumed, and the animals were raised under conditions of a temperature of 23 ± 1 ° C., a humidity of 50 ± 1%, and a lighting time of 7: 00-19: 00.
In the gabexate mesilate group, 100 mg / kg body weight was prepared so that the dosage would be 0.1 mL / 10 g body weight, and gabexate mesilate (Wako Pure Chemical Industries, Ltd.) Weekly, gavage was performed using a stomach tube. The control group was an emulsion except for gabexate mesylate, and was orally administered in the same manner.
Two weeks after oral administration, under pentobarbital anesthesia, a 0.6 cm x 1.0 cm site was placed close to the back of the mouse, 2 rows x 3 rows = 6 locations, and a UVB irradiation dose of 1 mW / cm 2 for 0 sec. (0 mJ) and 40 seconds (40 mJ) were irradiated (each at 3 locations). Grade of erythema 48 hours after irradiation was evaluated on a five-point scale (-; no response, ± (minimal erythema); mild or partial erythema, +; clear erythema, ++; erythema and edema, +++; erythema) Skin color (a * value) was measured using an edema and blisters) and a color difference meter OFC-300A (Nippon Denshoku Industries Co., Ltd.). The a * value is an index representing the redness of the skin color, and the larger the a * value, the more the skin changes to red, that is, erythema occurs.
（２）結果
結果を表1(目視による評価)、表2(a*値)に示した。コントロール群と比較してメシル酸ガベキサート投与群において、UVB照射によるa*値の上昇を抑制する効果が見出され、目視による評価によっても紅斑を抑制することが明らかにされた。
(2) Results The results are shown in Table 1 (visual evaluation) and Table 2 (a * value). Compared to the control group, the gabexate mesylate administration group was found to have an effect of suppressing an increase in a * value due to UVB irradiation, and visual evaluation revealed that erythema was also suppressed.
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| JPH0193509A (en) * | 1987-10-02 | 1989-04-12 | Shiseido Co Ltd | Skin drug for external use |
| JPH07285879A (en) * | 1994-02-24 | 1995-10-31 | Nippon Chemiphar Co Ltd | Synthetic peptide preparation for oral administration |
| WO2007062469A1 (en) * | 2005-12-01 | 2007-06-07 | Flinders Technologies Pty Ltd | Methods and compositions for preventing and/or treating pancreatitis |
| JP2007535546A (en) * | 2004-04-29 | 2007-12-06 | グラクソスミスクライン・イストラジヴァッキ・センタル・ザグレブ・ドルズバ・ゼー・オメイェノ・オドゴヴォルノスティオ | Oral formulation containing bone morphogenetic protein for treating metabolic bone disease |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH0193509A (en) * | 1987-10-02 | 1989-04-12 | Shiseido Co Ltd | Skin drug for external use |
| JPH07285879A (en) * | 1994-02-24 | 1995-10-31 | Nippon Chemiphar Co Ltd | Synthetic peptide preparation for oral administration |
| JP2007535546A (en) * | 2004-04-29 | 2007-12-06 | グラクソスミスクライン・イストラジヴァッキ・センタル・ザグレブ・ドルズバ・ゼー・オメイェノ・オドゴヴォルノスティオ | Oral formulation containing bone morphogenetic protein for treating metabolic bone disease |
| WO2007062469A1 (en) * | 2005-12-01 | 2007-06-07 | Flinders Technologies Pty Ltd | Methods and compositions for preventing and/or treating pancreatitis |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| JP2013170158A (en) * | 2012-02-22 | 2013-09-02 | Kao Corp | Oral ultraviolet light resistance improver |
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