JP5921664B2 - 皮膚の乾燥予防または改善用経口剤 - Google Patents
皮膚の乾燥予防または改善用経口剤 Download PDFInfo
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- JP5921664B2 JP5921664B2 JP2014265536A JP2014265536A JP5921664B2 JP 5921664 B2 JP5921664 B2 JP 5921664B2 JP 2014265536 A JP2014265536 A JP 2014265536A JP 2014265536 A JP2014265536 A JP 2014265536A JP 5921664 B2 JP5921664 B2 JP 5921664B2
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- Prior art keywords
- citrulline
- preventing
- skin
- oral preparation
- salt
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- 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
- 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
- 239000000118 hair dye Substances 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 235000013402 health food Nutrition 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 235000001050 hortel pimenta Nutrition 0.000 description 1
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- 206010021198 ichthyosis Diseases 0.000 description 1
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- 150000002632 lipids Chemical class 0.000 description 1
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- 159000000003 magnesium salts Chemical class 0.000 description 1
- 230000014759 maintenance of location Effects 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- 235000010755 mineral Nutrition 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 230000001333 moisturizer Effects 0.000 description 1
- WWZKQHOCKIZLMA-UHFFFAOYSA-M octanoate Chemical compound CCCCCCCC([O-])=O WWZKQHOCKIZLMA-UHFFFAOYSA-M 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 235000019198 oils Nutrition 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
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- 235000008390 olive oil Nutrition 0.000 description 1
- 239000006186 oral dosage form Substances 0.000 description 1
- 229960003104 ornithine Drugs 0.000 description 1
- 239000007800 oxidant agent Substances 0.000 description 1
- 239000002304 perfume Substances 0.000 description 1
- 229940066842 petrolatum Drugs 0.000 description 1
- 235000019271 petrolatum Nutrition 0.000 description 1
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Chemical class OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 description 1
- 235000008729 phenylalanine Nutrition 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
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- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 235000019422 polyvinyl alcohol Nutrition 0.000 description 1
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 1
- 235000013324 preserved food Nutrition 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 238000007788 roughening Methods 0.000 description 1
- 239000008159 sesame oil Substances 0.000 description 1
- 235000011803 sesame oil Nutrition 0.000 description 1
- 239000002453 shampoo Substances 0.000 description 1
- 229920002545 silicone oil Polymers 0.000 description 1
- 210000004927 skin cell Anatomy 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 235000010413 sodium alginate Nutrition 0.000 description 1
- 239000000661 sodium alginate Substances 0.000 description 1
- 229940005550 sodium alginate Drugs 0.000 description 1
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 description 1
- 235000010234 sodium benzoate Nutrition 0.000 description 1
- 239000004299 sodium benzoate Substances 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 239000003549 soybean oil Substances 0.000 description 1
- 235000012424 soybean oil Nutrition 0.000 description 1
- 235000013599 spices Nutrition 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 230000002194 synthesizing effect Effects 0.000 description 1
- QEMXHQIAXOOASZ-UHFFFAOYSA-N tetramethylammonium Chemical compound C[N+](C)(C)C QEMXHQIAXOOASZ-UHFFFAOYSA-N 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 230000008719 thickening Effects 0.000 description 1
- 210000000689 upper leg Anatomy 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
- 239000007762 w/o emulsion Substances 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 150000003751 zinc Chemical class 0.000 description 1
Classifications
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- A61K31/00—Medicinal preparations containing organic active ingredients
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- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
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- A—HUMAN NECESSITIES
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- A23K—FODDER
- A23K20/00—Accessory food factors for animal feeding-stuffs
- A23K20/10—Organic substances
- A23K20/142—Amino acids; Derivatives thereof
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- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
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- A23K50/00—Feeding-stuffs specially adapted for particular animals
- A23K50/50—Feeding-stuffs specially adapted for particular animals for rodents
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
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- A23L33/175—Amino acids
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
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- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
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- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
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Description
(1)シトルリンまたはその塩を有効成分として含有する皮膚の乾燥予防または改善用経口剤。
(2)シトルリンまたはその塩の有効量を、必要とする対象に経口投与することを含む、皮膚の乾燥予防または改善方法。
(3)皮膚の乾燥予防または改善用経口剤の製造のための、シトルリンまたはその塩の使用。
シトルリンは、化学的に合成する方法、発酵生産する方法等により取得することができる。また、シトルリンは、市販品を購入することにより取得することもできる。
シトルリンを化学的に合成する方法としては、例えば、J. Biol. Chem. 122, 477 (1938)、J. Org. Chem. 6, 410 (1941)に記載の方法があげられる。
また、L-シトルリンおよびD-シトルリンは、シグマ−アルドリッチ社等より購入することもできる。
シトルリンの塩としては、酸付加塩、金属塩、アンモニウム塩、有機アミン付加塩、アミノ酸付加塩等があげられる。
金属塩としては、ナトリウム塩、カリウム塩等のアルカリ金属塩、マグネシウム塩、カルシウム塩等のアルカリ土類金属塩、アルミニウム塩、亜鉛塩等があげられる。
有機アミン付加塩としては、モルホリン、ピペリジン等の塩があげられる。
アミノ酸付加塩としては、グリシン、フェニルアラニン、リジン、アスパラギン酸、グルタミン酸等の塩があげられる。
本発明の皮膚の乾燥予防または改善用経口剤には、シトルリンまたはその塩に加え、適宜、各用途に適した添加剤を含有させることができる。
本発明の皮膚の乾燥予防または改善用経口剤を投与または摂取することにより皮膚の水分含量が上昇することから、皮膚の乾燥状態を予防または改善することができる。
肌荒れとは、乾燥により角質層がガサガサになる、肌の表面に触れたときにしっとりとした感覚がなくなる等の症状をいう。
手荒れとは、角質細胞間脂質が少ないなど、もともと体質的に皮膚が乾燥しやすい人が、炊事や洗濯等の水仕事を行ったり、シャンプーや毛染め液等の化学物質を繰り返し扱うことにより手に刺激が加わることにより生ずる、手肌における上記症状をいう。
皮膚の乾燥予防または改善用経口剤の剤形としては、錠剤、散剤、顆粒剤、乳剤、シロップ剤、カプセル剤等があげられる。
剤形がシロップ剤等の液体調製物である場合は、水、蔗糖、ソルビトール、果糖等の糖類、ポリエチレングリコール、プロピレングリコール等のグリコール類、ごま油、オリーブ油、大豆油等の油類、p−ヒドロキシ安息香酸エステル類等の防腐剤、ストロベリーフレーバー、ペパーミント等のフレーバー類などを添加して、製剤化することができる。
本発明の皮膚の乾燥予防または改善用経口剤の投与量は、投与形態、投与される者の年齢、体重等に応じて異なるが、通常成人に対し一日あたりシトルリンまたはその塩として、100〜10000mg、好ましくは100〜2000mg、特に好ましくは200〜1000mgであり、1日に1回または数回に分けて投与する。投与期間は、特に限定はないが、通常は1日間〜1年間、好ましくは1週間〜3ケ月間である。
試験例1
試験には、HOS:HR−1マウス(オス、5週齢、チャールズ・リバー社より購入)を用いた。飼育条件は、室温22±2℃、湿度35±15%、飼料および水は自由摂取とした。
各飼料の給餌開始1週間後から5週間後まで1週間毎に、各マウスの背側大腿部上部の皮膚表面の水分含量をSKICON−200(IBS社製)を用いて測定した。測定は1匹のマウスあたり10回行ってその個体の平均値を求め、さらに各試験群の平均値を算出した。
相対表皮水分含量(%)=(A2/A1)×100
A1:第1群の表皮水分含量
A2:第2群の表皮水分含量
結果を図1に示す。
シトルリンを含有する錠剤を、常法により製造する。すなわち、下記の各成分を均一に混合し、この混合物を単発式打錠機にて打錠し、直径5mm、重量15mgの錠剤を得る。
成分 量
L-シトルリン 10.0g
乳糖 90.0g
乾燥コーンスターチ 2.0g
タルク 1.8g
ステアリン酸マグネシウム 0.2g
実施例1で得られる錠剤を粉砕、製粒し、篩別して20−50メッシュの顆粒剤を得る。
シトルリンを含有する飲料を、下記の各成分を均一に攪拌溶解し、精製水を加えて全量を1000mlとすることにより製造する。なお、下記成分中の適量とは、香料、色素に関しては、通常の飲料の製造に用いられる量であり、精製水に関しては、他の成分に加え、全量として1000mlにするために必要な量のことをいう。
成分 量
L-シトルリン 5.0g
安息香酸ナトリウム 1.0g
果糖 10.0g
香料 適量
色素 適量
精製水 適量
下記の各成分からなるシトルリンを含有する飴を、常法により製造する。
成分 量
L-シトルリン 1.00g
粉末ソルビトール 98.75g
香料 0.20g
ソルビトールシード 0.05g
下記の各成分からなるシトルリンを含有する動物飼料を、常法により製造する。
成分 量
L-シトルリン 1.0g
ラード 5.0g
コーン油 1.0g
ショ糖 20.0g
セルロース 5.0g
塩化コリン 0.2g
ビタミン混合物 1.0g
ミネラル混合物 3.5g
コーンスターチ 44.3g
Claims (3)
- 有効成分としてはシトルリンまたはその塩のみを含有し、液体調製物である、皮膚の乾燥予防または改善用経口剤(ただし、農水産物およびそれらの加工品を除く)。
- 液体調製物が乳剤およびシロップ剤からなる群より選択される剤形である、請求項1に記載の皮膚の乾燥予防または改善用経口剤(ただし、農水産物およびそれらの加工品を除く)。
- 有効成分としてのシトルリンまたはその塩を含有し、乳剤およびシロップ剤からなる群より選択される剤形の液体調製物である、皮膚の乾燥予防または改善用経口剤(ただし、農水産物およびそれらの加工品を除く)。
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JPWO2008105384A1 (ja) * | 2007-02-26 | 2010-06-03 | 協和発酵バイオ株式会社 | シトルリン含有錠剤 |
US8466187B2 (en) * | 2007-09-18 | 2013-06-18 | Thermolife International, Llc | Amino acid compositions |
EP2215915B1 (en) * | 2007-11-16 | 2017-04-05 | Kyowa Hakko Bio Co., Ltd. | Citrulline-containing beverage |
JP5745751B2 (ja) * | 2009-04-22 | 2015-07-08 | 森永製菓株式会社 | ドライシンドロームの改善用組成物 |
US20120253014A1 (en) * | 2009-12-10 | 2012-10-04 | Lotte Company, Ltd. | Preventive agent for atopic dermatitis |
EP2696865B1 (en) | 2011-04-13 | 2016-12-21 | Thermolife International, LLC | N-acetyl beta alanine methods of use |
US9833426B2 (en) | 2012-06-29 | 2017-12-05 | Kyowa Hakko Bio Co., Ltd. | Agent for preventing deterioration in vascular endothelial function or improving vascular endothelial function |
MX2021002838A (es) * | 2018-09-24 | 2021-05-27 | Tastes Natural Llc | Proceso para aislar modificadores de sabor. |
US11865139B2 (en) | 2020-11-12 | 2024-01-09 | Thermolife International, Llc | Method of treating migraines and headaches |
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JPS57163488A (en) | 1981-04-02 | 1982-10-07 | Ajinomoto Co Inc | Production of l-citrulline through fermentation process |
US5702688A (en) * | 1986-12-23 | 1997-12-30 | Tristrata Technology, Inc. | Amphoteric compositions and polymeric forms of alpha hydroxyacids, and their therapeutic use |
DE4341000A1 (de) | 1993-12-02 | 1995-06-08 | Beiersdorf Ag | Verwendung von L-Arginin, L-Ornithin oder L-Citrullin und topischen Zubereitungen mit diesen Stoffen |
JP3843298B2 (ja) * | 2001-02-05 | 2006-11-08 | 国立大学法人 奈良先端科学技術大学院大学 | シトルリンを含有する活性酸素消去剤 |
WO2004082645A1 (ja) * | 2003-03-19 | 2004-09-30 | Kanebo Cosmetics Inc. | 油性メイクアップ化粧料 |
JP2003300895A (ja) * | 2002-04-05 | 2003-10-21 | Masaki Shibuta | 蜂蜜入りスイカ糖及びその製造方法 |
US20030211133A1 (en) * | 2002-05-10 | 2003-11-13 | Special Ops Nutrition, L.L.C. | Ingestible composition for enhancing athletic performance |
EP1459736A1 (en) | 2003-03-14 | 2004-09-22 | The Procter & Gamble Company | Skin care composition that increase and repair skin barrier function |
CN100418548C (zh) * | 2003-05-18 | 2008-09-17 | 漆又毛 | 一种药用组合物及其用途 |
JP2005306831A (ja) | 2004-04-20 | 2005-11-04 | Sakamoto Yakusoen:Kk | 皮膚外用剤 |
WO2005105126A1 (ja) * | 2004-04-30 | 2005-11-10 | National University Corporation NARA Institute of Science and Technology | 野生種スイカ抽出物を含有する活性酸素消去剤ならびに保湿剤 |
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CN101340905B (zh) | 2012-05-16 |
JPWO2007066642A1 (ja) | 2009-05-21 |
WO2007066642A1 (ja) | 2007-06-14 |
US20100004335A1 (en) | 2010-01-07 |
US8153692B2 (en) | 2012-04-10 |
CN101340905A (zh) | 2009-01-07 |
JP5697835B2 (ja) | 2015-04-08 |
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