CA2086565A1 - Pharmaceutical composition for treating pigmentation - Google Patents

Pharmaceutical composition for treating pigmentation

Info

Publication number
CA2086565A1
CA2086565A1 CA002086565A CA2086565A CA2086565A1 CA 2086565 A1 CA2086565 A1 CA 2086565A1 CA 002086565 A CA002086565 A CA 002086565A CA 2086565 A CA2086565 A CA 2086565A CA 2086565 A1 CA2086565 A1 CA 2086565A1
Authority
CA
Canada
Prior art keywords
cheeks
improved
pharmaceutical composition
forehead
pigmentation
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.)
Abandoned
Application number
CA002086565A
Other languages
French (fr)
Inventor
Fumio Kita
Kazuo Matsumoto
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
Priority to JP3023770A priority Critical patent/JPH04243825A/en
Application filed by SSP Co Ltd filed Critical SSP Co Ltd
Priority to CA002086565A priority patent/CA2086565A1/en
Publication of CA2086565A1 publication Critical patent/CA2086565A1/en
Abandoned 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Birds (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

ABSTRACT OF THE DISCLOSURE
A pharmaceutical composition for treating pigmentation for internal use which contains tranexamic acid and ascorbic acid or a salt thereof is disclosed. The composition is useful for treating pigmentation in a short time when orally administered.

Description

20g~

PHARMACEUTICAL COMPOSITION FOR TREATING PIGMENTATION

FIELD OF THE INVENTION
This invention relates to a pharmaceutical composition for internal use having a remarkable effect on pigmentation.
BACKGROUND OF THE INVENTION
Pigmentation is considered to ensue from chromatism of melanin in the skin generally caused by heredity, endocrinosis, stimulation by ultraviolet rays of sunlight, skin irritation by photodynamic substances, etc., aggravation of allergodermia, and so on.
Conventionally proposed treatment for pigmentation includes drugs for external use containing hydroquinone, vitamin C
derivatives, kojic acid, tranexamic acid, etc. and drugs for internal use containing vitamin C, L-cysteine, glutathione, tranexamic acid, etc. Some of these drugs have already been on the market, but no drugs except hydroquinone preparations shows a sufficient effect in a short time. However, hydroquinone preparations have hardly been used due to their strong side effects.
SUMMARY OF THE INVENTION
Accordingly, an object of the present invention is to provide a pharmaceutical composition for treating pigmentation which is of high safety with freedom from side effects and is expected to produce a sufficient effect through short-term administration.

- 2as6,~J~

In the light of the above-mentioned circumstances, the inventors have conducted extensive investigations and, as a result, have found that a combination of tranexamic acid which is noted to have efficacy to some extent when orally administered alone and ascorbic acid or a salt thereof which has no discernible effect when administered alone exerts a synergistically enhanced effect in the treatment of pigmentation and produces high therapeutic effects through short-term administration.
The present invention provides a pigmentation treating pharmaceutical composition for internal use which comprises tranexamic acid and ascorbic acid or a salt thereof. ~-DETAILED DESCRIPTION OF THE INVENTION
Tranexamic acid, one of the essential ingredients of the pharmaceutical composition of the present invention, is used as an antiplasmin agent and has such very low toxicity as having an LD50 of not less than 5 g~kg in dogs (p.o.).
Ascorbic acid, the other ingredient, is also of low toxicity as having an LD50 Of not less than 5 g/kg in doqs ~ -(p.o.). Suitable salts of ascorbic acid include a sodium salt and a calcium salt. -~
In the pharmaceutical composition of the present invention, ascorbic acid is contained in an amount of 0.3 to 2 parts by weight, preferably 0.5 to 2 parts by weight, per part by weight of tranexamic acid.

~` ` ~ ''' ~;!.!' ` . , ~ 2~62)65 The pigmentation treating composition of the present invention is preferably orally administered so that each of tranexamic acid and ascorbic acid or its salt be administered at a dose of from 500 to lS00 mg, particularly from 1000 to 1500 mg, per day in a single dose or several divided doses, particularly three divided doses.
The pigmentation treating composition may be formulated into various preparation forms for oral administration, such as granules, particles, powders, capsules, tablets, solutions, and the like together with a pharmaceutically acceptable carrier.
These preparations can be prepared in a usual manner from the above-mentioned essential ingredients, if necessary in ,. .... . .
con~unction with ad~uvants commonly employed in the art and other drugs.
The present invention is now illustrated in greater detail -with reference to Examples, but it should be understood that the present invention is not deemed to be limited thereto.
EXAMPLE 1 - ;
Ascorbic acid 1000 mg Tranexamic acid 1000 mg Powder sugar 2475 mg Light anhydrous silicic acid 25 mg Granules were prepared from the above ingredients in a usual manner and divided into three doses for one day.
2~8~

A simple comparative clinical test was carried out as follows.
The medication prepared in Example 1 (A), tranexamic acid alone (B), or ascorbic acid alone (C) was orally administered to patients (all female) suffering from chloasma, a kind of pigmentation, three times a day for 2 months, and the degrees of pigmentation before and after the administration were ~ ~
compared. ~ :
Inaredients of Daily Dose (3 doses):

Medication _ Inaredient (A) (B~ (C) Ascorbic acid 1000 mg - 1000 mg ~ .
Tranexamic acid1000 mg1500 mg Powder sugar 2475 mg 2975 mg 3475 mg Light anhydrous2S mg 25 mg 25 mg silicic acid The changes in the clinical picture after the administration of the medication are shown in Tables 1 (group ~ : `-`.
on (A)), 2 (group on (B)), and 3 (group on (C)), and the -. - -:: -- .-. ~
ameliorating effect of each medication on pigmentation judged from these clinical pictures is shown in Table 4.
The clinical pictures were allocated in accordance with the following five levels. : .
4: bad (observed through heavy makeup) 3: baddish (covered by heavy makeup) .
2: slight (covered by normal makeup) ?
208G~

1: very slight (covered by light makeup) 0: none In Tables 1 through 3, the degree of improvement was evaluated as follows.
markedly improved: the symptom at any level was improved up to 0 (4~0, 3~0, 2~0, 1~0).
improved: the level of clinical picture was raised by two or three steps (4~2, 4~1, 3~1). .
slightly improved: the level of clinical picture was raised by one step (4~3, 3~2, 2~
unchanged: the clinical picture was unchanged (4~4, 3~3, 2~2, 1~
aggravated: the clinical picture got worse (3~4; 2~3 or 4;
1~2, 3 or 4; 0~1,2,3 or 4) ';

_ 5 _ 2a~&~us Patient GrouP on ~A!
Degree of Case Aqe Sites _Improvement 1 39 forehead, right cheekmarkedly improved 2 39 cheeks, below nose 3 45 cheeks, below nose 4 41 cheeks improved S 31 cheeks ~ :-6 38 cheeks, eyelids ~ `
7 49 cheeks, eyelids -:.
8 40 upper lip 9 40 forehead slightly improved ~;
right cheek improved ..
ll 50 cheeks unchanged 12 47 forehead, cheeksslightly improved 13 52 cheeks unchanged 14 45 forehead, cheeksslightly improved 39 cheeks 16 40 forehead, cheeks improved 17 43 forehead, cheeksslightly improved 18 30 forehead, cheeks improved 19 41 entire face 51 cheeks "

. - - - , , i ~ ~

. ' ~ .
'~ ~
:` ' ' ` ~ :
' " ' .'' I ' , " ~

2v8~ ~

Patient Grou~ on (B) Degree of Case Aqe _ Sites ImProvement 21 45 cheeks improved 22 53 che~ks unchanged 23 58 forehead, left cheekslightly improved 24 43 forehead, cheeks ~
forehead, cheeks improved 26 35 cheeks markedly improved `~
27 38 cheeks improved 28 40 cheeks 29 50 right cheek slightly improved 39 forehead, cheeks improved 31 47 forehead, cheeks unchanged 32 45 cheeks 33 39 cheeks improved 34 40 forehead, cheeks 37 cheeks slightly improved 36 30 forehead improved 37 41 entire face unchanged 38 33 cheeks improved 39 40 cheeks "
37 cheeks slightly improved ,:

-2 0 ~ C~3 Patient GrouP on (C~
Degree of Case Aqe Sites Improvement 41 46 cheeks unchanged ~ . ~
42 43 cheeks 43 38 cheeks slightly improved ~ ~
44 49 forehead, cheeks unchanged - ; -forehead, cheeks 46 37 forehead slightly improved 47 35 cheeks "
48 51 entire face unchanged 49 53 forehead, cheeks 46 cheeks improved :~
51 48 cheeks unchanged :
52 37 right cheek 53 33 forehead slightly improved :
54 39 cheeks, below noseunchanged 37 cheeks improved 56 41 cheeks unchanged ::
57 38 cheeks slightly improved 58 40 left cheek unchanged 59 42 forehead, cheeks 39 forehead, cheeks :, . .

:, ~ - i . ' ~ :,,, ' `

2 9 8 ~ .S

Medication '. ;
Marked Improvement 3 1 0 -Improvement 10 10 2 :
Slight Improvement 5 5 5 : -~
. , :
No Change 2 4 13 Aggravation 0 0 0 _______________________________________________________ Total 20 20 20 Percent Improvement (%) 65.0 55.0 10.0 (90.0~) (80.0~) (35.0 Note: * The value in the parentheses is the percent improvement inclusive of slight improvement.
As described and demonstrated above, the pigmentation treating aqent according to the present invention has high efficacy in treating pigmentation through short-term oral administration without causing any adverse side effect.
While the invention has been described in detail and with reference to specific examples thereof, it will be apparent to one skilled in the art that various changes and modifications can be made therein without departing from the spirit and scope :
thereof.
.

_ g , ~...

Claims (3)

1. A pharmaceutical composition for treating pigmentation for internal use which comprises tranexamic acid and ascorbic acid or a salt thereof both in an effective amount for treating pigmentation and a pharmaceutically acceptable carrier.
2. The pharmaceutical composition according to claim 1, wherein ascorbic acid or a salt thereof is contained in an amount of 0.3 to 2 parts by weight per part by weight of tranexamic acid.
3. The use of tranexamic acid and ascorbic acid or a salt thereof for preparation of a pharmaceutical composition for treating pigmentation.
CA002086565A 1991-01-25 1992-12-31 Pharmaceutical composition for treating pigmentation Abandoned CA2086565A1 (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
CA2086565A1 true CA2086565A1 (en) 1994-07-01

Family

ID=25675787

Family Applications (1)

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

Country Status (2)

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

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004006908A1 (en) * 2002-07-12 2004-01-22 Hideyasu Takada Remedies for pigmentation
WO2004060364A1 (en) 2002-12-27 2004-07-22 Daiichi Pharmaceutical Co., Ltd. Skin lightening composition
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

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1068868A3 (en) * 1997-07-08 2001-01-31 Rath, Matthias, Dr. med. Synergistic compositions comprising ascorbate and lysine for states related to extracellular matrix degeneration
CH694549A5 (en) 2001-01-16 2005-03-31 Dr Matthias Rath A composition comprising an ascorbate and a fibrinolysis inhibitor for treating diseases associated with extracellular matrix degradation e.g. arteriosclerosis, cancer, inflammations and infections
JPWO2006003965A1 (en) * 2004-06-30 2008-04-17 第一三共ヘルスケア株式会社 Whitening composition
WO2006023001A1 (en) * 2004-07-30 2006-03-02 Xanodyne Pharmaceuticals, Inc. Tranexamic acid formulations
CN102105143B (en) 2008-08-06 2013-03-20 第一三共健康事业株式会社 Stable pharmaceutical composition containing tranexamic acid and ascorbic acid
KR101640958B1 (en) 2008-09-05 2016-07-19 다이이찌 산쿄 헬스케어 가부시키가이샤 Pharmaceutical solid preparation having active ingredients separated by boundary therein
MX340436B (en) * 2008-09-12 2016-07-08 Daiichi Sankyo Healthcare Co Ltd Stable pharmaceutical formulation with limited discoloration.

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004006908A1 (en) * 2002-07-12 2004-01-22 Hideyasu Takada Remedies for pigmentation
WO2004060364A1 (en) 2002-12-27 2004-07-22 Daiichi Pharmaceutical Co., Ltd. Skin lightening composition
CN100335048C (en) * 2002-12-27 2007-09-05 第一制药株式会社 Skin-whitening 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
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
US8487005B2 (en) 2004-03-04 2013-07-16 Ferring B.V. Tranexamic acid formulations
US8791160B2 (en) 2004-03-04 2014-07-29 Ferring B.V. Tranexamic acid formulations
US8809394B2 (en) 2004-03-04 2014-08-19 Ferring B.V. Tranexamic acid formulations
US8957113B2 (en) 2004-03-04 2015-02-17 Ferring B.V. Tranexamic acid formulations
US9060939B2 (en) 2004-03-04 2015-06-23 Ferring B.V. Tranexamic acid formulations

Also Published As

Publication number Publication date
JPH04243825A (en) 1992-08-31

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