JPH04243825A - Remedy for pigmentation - Google Patents

Remedy for pigmentation

Info

Publication number
JPH04243825A
JPH04243825A JP3023770A JP2377091A JPH04243825A JP H04243825 A JPH04243825 A JP H04243825A JP 3023770 A JP3023770 A JP 3023770A JP 2377091 A JP2377091 A JP 2377091A JP H04243825 A JPH04243825 A JP H04243825A
Authority
JP
Japan
Prior art keywords
pigmentation
hyperpigmentation
acid
ascorbic acid
tranexamic acid
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
Application number
JP3023770A
Other languages
Japanese (ja)
Inventor
Fumio Kita
北 史男
Kazuo Matsumoto
一男 松本
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
SSP Co Ltd
Original Assignee
SSP Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by SSP Co Ltd filed Critical SSP Co Ltd
Priority to JP3023770A priority Critical patent/JPH04243825A/en
Publication of JPH04243825A publication Critical patent/JPH04243825A/en
Priority to CA002086565A priority patent/CA2086565A1/en
Pending legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/02Preparations for care of the skin for chemically bleaching or whitening the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
    • A61K31/375Ascorbic acid, i.e. vitamin C; Salts thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/44Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67Vitamins
    • A61K8/676Ascorbic acid, i.e. vitamin C
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

PURPOSE:To provide the subject medicine capable of effectively curing pigmentation by a short period administration. CONSTITUTION:A medicine for internal use for pigmentation, containing tranexamic acid and ascorbic acid or salts thereof.

Description

【発明の詳細な説明】[Detailed description of the invention]

【0001】0001

【産業上の利用分野】本発明は色素沈着症に対して優れ
た効果を有する内服型の色素沈着症治療剤に関する。
BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an internally administered agent for treating hyperpigmentation which has excellent effects on hyperpigmentation.

【0002】0002

【従来の技術】色素沈着症は、一般に、遺伝的素因、ホ
ルモンの異常、日光の紫外線刺激、光力学的物質等の皮
膚刺激、アレルギー性接触皮膚炎の悪化等により、皮膚
内にメラニンが異常沈着することによっておこるものと
考えられている。このような色素沈着症の治療法として
は、従来、ハイドロキノン、ビタミンC誘導体、コウジ
酸、トラネキサム酸等を含有する外用剤;ビタミンC、
L−システイン、グルタチオン、トラネキサム酸等を含
有する内服剤が提案され、そのうちのあるものは実際に
市場に提供されているが、ハイドロキノン製剤以外には
、短期間に充分な効果が認められるものはない。しかし
ながら、ハイドロキノン製剤は副作用が強いために、本
邦ではほとんど使用されていない。
[Prior Art] Hyperpigmentation is generally caused by abnormal melanin in the skin due to genetic predisposition, hormonal abnormalities, ultraviolet stimulation from sunlight, skin irritation from photodynamic substances, exacerbation of allergic contact dermatitis, etc. It is thought that this is caused by deposition. Conventional treatments for such hyperpigmentation include topical preparations containing hydroquinone, vitamin C derivatives, kojic acid, tranexamic acid, etc.;
Oral preparations containing L-cysteine, glutathione, tranexamic acid, etc. have been proposed, and some of them are actually available on the market, but other than hydroquinone preparations, there are no drugs that have been shown to be sufficiently effective in a short period of time. do not have. However, hydroquinone preparations are rarely used in Japan because of their strong side effects.

【0003】0003

【発明が解決しようとす課題】従って、本発明は、副作
用がなく安定性が高く、短期間の投与で充分な効果が期
待できる色素沈着症治療剤を提供することを目的とする
ものである。
[Problems to be Solved by the Invention] Therefore, it is an object of the present invention to provide a therapeutic agent for hyperpigmentation that has no side effects, is highly stable, and can be expected to be sufficiently effective when administered for a short period of time. .

【0004】0004

【課題を解決するための手段】斯かる実情において、本
発明者は鋭意研究を行った結果、単独の内服でもある程
度の治療効果が認められるトラネキサム酸に、単独では
あまり効果が認められないアスコルビン酸又はその塩を
配合することにより、色素沈着症の治療効果が相乗的に
増大し、短期間の投与で優れた効果が得られることを見
出し、本発明を完成した。
[Means for Solving the Problem] Under these circumstances, the present inventor has conducted intensive research and found that tranexamic acid, which has some therapeutic effect even when taken alone, and ascorbic acid, which has little effect when taken alone. The present invention has been completed based on the discovery that the therapeutic effect of hyperpigmentation can be synergistically increased by incorporating a pigment or a salt thereof, and that excellent effects can be obtained with short-term administration.

【0005】すなわち、本発明は、トラネキサム酸、及
びアスコルビン酸又はその塩を含有する内服薬形態の色
素沈着症治療剤を提供するものである。
[0005] That is, the present invention provides a therapeutic agent for hyperpigmentation in the form of an internal medicine containing tranexamic acid and ascorbic acid or a salt thereof.

【0006】本発明治療剤の一成分であるトラネキサム
酸は抗プラスミン剤として用いられているもので、LD
50が5g/kg以上(イヌの経口)と極めて毒性の低
いものである。また、アスコルビン酸もLD50が5g
/kg以上(イヌの経口)の極めて毒性の低いものであ
る。アスコルビン酸の塩としては、ナトリウム塩、カル
シウム塩等が挙げられる。
Tranexamic acid, which is one of the components of the therapeutic agent of the present invention, is used as an anti-plasmin agent and is effective against LD.
50 has an extremely low toxicity of 5 g/kg or more (orally for dogs). Also, ascorbic acid has an LD50 of 5g.
/kg or more (orally administered to dogs), which has extremely low toxicity. Salts of ascorbic acid include sodium salts, calcium salts, and the like.

【0007】本発明の色素沈着症治療剤は、トラネキサ
ム酸、及びアスコルビン酸又はその塩が、共にそれぞれ
1日量として、500 〜1,500mg、特に1,0
00 〜1,500mg になるように、1日に1〜数
回、特に3回に分けて投与するのが好ましい。
The therapeutic agent for pigmentation of the present invention contains tranexamic acid and ascorbic acid or a salt thereof in a daily dose of 500 to 1,500 mg, particularly 1,0
It is preferable to administer 00 to 1,500 mg once to several times a day, particularly in 3 divided doses.

【0008】本発明の色素沈着症治療剤は経口投与の形
態、例えば顆粒剤、細粒剤、散剤、カプセル剤、錠剤、
液剤等の種々の製剤とすることができる。これらの製剤
を製造するには、上記必須成分のほかに、かかる場合に
一般に使用されている助剤及び他の薬剤等を使用するこ
とができ、その製法は自体公知の方法によって行われる
The therapeutic agent for hyperpigmentation of the present invention can be administered in the form of oral administration, such as granules, fine granules, powders, capsules, tablets, etc.
It can be made into various preparations such as liquid preparations. To manufacture these preparations, in addition to the above-mentioned essential ingredients, auxiliary agents and other drugs commonly used in such cases can be used, and the preparation is carried out by methods known per se.

【0009】[0009]

【実施例】次に実施例を挙げて説明する。[Example] Next, an example will be given and explained.

【0010】実施例1 アスコルビン酸                  
  1000mgトラネキサム酸          
          1000mg粉糖       
                       24
75mg軽質無水ケイ酸              
        25mg以上の成分から常法によって
顆粒剤を製造し、これを3包に分包し、1日分とした。
Example 1 Ascorbic acid
1000mg tranexamic acid
1000mg powdered sugar
24
75mg light silicic anhydride
Granules were produced from 25 mg or more of the ingredients by a conventional method, and the granules were divided into three packages for one day's worth.

【0011】試験例1 下記に示す3種の顆粒剤、すなわち実施例1で調製した
薬剤(A)、トラネキサム酸単味剤(B)及びアスコル
ビン酸単味剤(C)を、色素沈着症の1種である肝斑患
者(全て女性)に1回1包、1日3回、2ケ月間経口投
与し、投与前後の色素沈着の程度を比較する単純比較臨
床試験を行った。〔1日量(3包)中〕薬剤     
                 (A)    (
B)    (C) アスコルビン酸            1000mg
      − 1000mgトラネキサム酸    
        1000mg    1500mg−
  粉糖                     
 2475mg    2975mg    3475
mg 軽質無水ケイ酸              25mg
      25mg25mgそのときの、薬剤の投与
前後の症状変化は表1〔(A)投与群〕、表2〔(B)
投与群〕及び表3〔(C)投与群〕のとおりであり、こ
れに基づいて評価した色素沈着症の改善度は表4に示す
とおりである。
Test Example 1 The following three types of granules, namely the drug (A) prepared in Example 1, tranexamic acid monotherapy (B) and ascorbic acid monotherapy (C), were used to treat pigmentation disorders. A simple comparative clinical trial was conducted in which the drug was orally administered to patients with melasma, a type of melasma (all women), three times a day for two months, and the degree of pigmentation before and after administration was compared. [Daily dose (3 packages)] Drugs
(A) (
B) (C) Ascorbic acid 1000mg
- 1000mg tranexamic acid
1000mg 1500mg-
powdered sugar
2475mg 2975mg 3475
mg Light anhydrous silicic acid 25mg
Table 1 [(A) administration group] and Table 2 [(B)
Administration Group] and Table 3 [(C) Administration Group], and the degree of improvement in pigmentation that was evaluated based on this is as shown in Table 4.

【0012】0012

【表1】[Table 1]

【0013】[0013]

【表2】[Table 2]

【0014】[0014]

【表3】[Table 3]

【0015】[0015]

【表4】[Table 4]

【0016】[0016]

【発明の効果】本発明の色素沈着症治療剤は副作用がな
く、経口投与によって、短期間に色素沈着症を有効に治
療することができる。
EFFECTS OF THE INVENTION The agent for treating hyperpigmentation of the present invention has no side effects and can effectively treat hyperpigmentation within a short period of time by oral administration.

Claims (1)

【特許請求の範囲】[Claims] 【請求項1】  トラネキサム酸、及びアスコルビン酸
又はその塩を含有する内服薬形態の色素沈着症治療剤。
1. A therapeutic agent for hyperpigmentation in the form of an oral medication containing tranexamic acid and ascorbic acid or a salt thereof.
JP3023770A 1991-01-25 1991-01-25 Remedy for pigmentation Pending JPH04243825A (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP3023770A JPH04243825A (en) 1991-01-25 1991-01-25 Remedy for pigmentation
CA002086565A CA2086565A1 (en) 1991-01-25 1992-12-31 Pharmaceutical composition for treating pigmentation

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP3023770A JPH04243825A (en) 1991-01-25 1991-01-25 Remedy for pigmentation
CA002086565A CA2086565A1 (en) 1991-01-25 1992-12-31 Pharmaceutical composition for treating pigmentation

Publications (1)

Publication Number Publication Date
JPH04243825A true JPH04243825A (en) 1992-08-31

Family

ID=25675787

Family Applications (1)

Application Number Title Priority Date Filing Date
JP3023770A Pending JPH04243825A (en) 1991-01-25 1991-01-25 Remedy for pigmentation

Country Status (2)

Country Link
JP (1) JPH04243825A (en)
CA (1) CA2086565A1 (en)

Cited By (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10101522A1 (en) * 1997-07-08 2002-07-25 Rath Matthias Composition for treating collagenase-linked degenerative diseases, e.g. atherosclerosis, cancer and infections, comprises ascorbate and a fibrinolysis inhibitor
JP2004091473A (en) * 2002-07-12 2004-03-25 Tadayasu Takada Therapeutic agent for improving chromatosis
WO2004060364A1 (en) 2002-12-27 2004-07-22 Daiichi Pharmaceutical Co., Ltd. Skin lightening composition
US6974833B2 (en) 2001-01-16 2005-12-13 Matthias Rath Synergistic compositions comprising ascobate and lysine for states related to extra cellular matrix degeneration
WO2006003965A1 (en) * 2004-06-30 2006-01-12 Daiichi Sankyo Healthcare Co., Ltd. Skin-whitening compositions
JP2008508275A (en) * 2004-07-30 2008-03-21 ザノダイン ファーマシューティカルズ,インコーポレーテッド Tranexamic acid preparation
WO2010016509A1 (en) 2008-08-06 2010-02-11 第一三共ヘルスケア株式会社 Stable pharmaceutical composition containing tranexamic acid and ascorbic acid
WO2010027010A1 (en) 2008-09-05 2010-03-11 第一三共ヘルスケア株式会社 Pharmaceutical solid preparation having active ingredients separated by boundary therein
WO2010029930A1 (en) 2008-09-12 2010-03-18 第一三共ヘルスケア株式会社 Stable pharmaceutical formulation with limited discoloration
US7947739B2 (en) 2004-03-04 2011-05-24 Ferring B.V. Tranexamic acid formulations
US8022106B2 (en) 2004-03-04 2011-09-20 Ferring B.V. Tranexamic acid formulations
US8273795B2 (en) 2004-03-04 2012-09-25 Ferring B.V. Tranexamic acid formulations
US8957113B2 (en) 2004-03-04 2015-02-17 Ferring B.V. Tranexamic acid formulations
US8968777B2 (en) 2003-07-31 2015-03-03 Ferring B.V. Tranexamic acid formulations with reduced adverse effects

Cited By (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10101522B4 (en) * 1997-07-08 2007-02-22 Rath, Matthias, Dr. New pharmaceutical use of a combination of ascorbate and at least one fibrinolytic inhibitor
DE10101522A1 (en) * 1997-07-08 2002-07-25 Rath Matthias Composition for treating collagenase-linked degenerative diseases, e.g. atherosclerosis, cancer and infections, comprises ascorbate and a fibrinolysis inhibitor
US6974833B2 (en) 2001-01-16 2005-12-13 Matthias Rath Synergistic compositions comprising ascobate and lysine for states related to extra cellular matrix degeneration
JP2004091473A (en) * 2002-07-12 2004-03-25 Tadayasu Takada Therapeutic agent for improving chromatosis
JP4667875B2 (en) * 2002-12-27 2011-04-13 第一三共ヘルスケア株式会社 Whitening composition
JPWO2004060364A1 (en) * 2002-12-27 2006-05-11 第一製薬株式会社 Whitening composition
KR101107754B1 (en) * 2002-12-27 2012-01-20 다이이찌 산쿄 헬스케어 가부시키가이샤 Composition for preventing or treating pigmentations
WO2004060364A1 (en) 2002-12-27 2004-07-22 Daiichi Pharmaceutical Co., Ltd. Skin lightening composition
US8968777B2 (en) 2003-07-31 2015-03-03 Ferring B.V. Tranexamic acid formulations with reduced adverse effects
US7947739B2 (en) 2004-03-04 2011-05-24 Ferring B.V. Tranexamic acid formulations
US8487005B2 (en) 2004-03-04 2013-07-16 Ferring B.V. Tranexamic acid formulations
US9060939B2 (en) 2004-03-04 2015-06-23 Ferring B.V. Tranexamic acid formulations
US8809394B2 (en) 2004-03-04 2014-08-19 Ferring B.V. Tranexamic acid formulations
US8791160B2 (en) 2004-03-04 2014-07-29 Ferring B.V. Tranexamic acid formulations
US8957113B2 (en) 2004-03-04 2015-02-17 Ferring B.V. Tranexamic acid formulations
US8273795B2 (en) 2004-03-04 2012-09-25 Ferring B.V. Tranexamic acid formulations
US8022106B2 (en) 2004-03-04 2011-09-20 Ferring B.V. Tranexamic acid formulations
WO2006003965A1 (en) * 2004-06-30 2006-01-12 Daiichi Sankyo Healthcare Co., Ltd. Skin-whitening compositions
JP2011168596A (en) * 2004-07-30 2011-09-01 Ferring Bv Tranexamic acid formulation
JP2008508275A (en) * 2004-07-30 2008-03-21 ザノダイン ファーマシューティカルズ,インコーポレーテッド Tranexamic acid preparation
JP2014193878A (en) * 2004-07-30 2014-10-09 Ferring Bv Tranexamic acid formulations
JP2008508276A (en) * 2004-07-30 2008-03-21 ザノダイン ファーマシューティカルズ,インコーポレーテッド Tranexamic acid preparation
WO2010016509A1 (en) 2008-08-06 2010-02-11 第一三共ヘルスケア株式会社 Stable pharmaceutical composition containing tranexamic acid and ascorbic acid
WO2010027010A1 (en) 2008-09-05 2010-03-11 第一三共ヘルスケア株式会社 Pharmaceutical solid preparation having active ingredients separated by boundary therein
KR20110057145A (en) 2008-09-05 2011-05-31 다이이찌 산쿄 헬스케어 가부시키가이샤 Pharmaceutical solid preparation having active ingredients separated by boundary therein
JP5498387B2 (en) * 2008-09-12 2014-05-21 第一三共ヘルスケア株式会社 Stable pharmaceutical formulation with suppressed discoloration
WO2010029930A1 (en) 2008-09-12 2010-03-18 第一三共ヘルスケア株式会社 Stable pharmaceutical formulation with limited discoloration

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