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JPS61130205A - Aqueous composition containing stabilized ascorbic acid - Google Patents

Aqueous composition containing stabilized ascorbic acid

Info

Publication number
JPS61130205A
JPS61130205A JP59254595A JP25459584A JPS61130205A JP S61130205 A JPS61130205 A JP S61130205A JP 59254595 A JP59254595 A JP 59254595A JP 25459584 A JP25459584 A JP 25459584A JP S61130205 A JPS61130205 A JP S61130205A
Authority
JP
Japan
Prior art keywords
ascorbic acid
acid
aqueous composition
composition
cosmetics
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.)
Granted
Application number
JP59254595A
Other languages
Japanese (ja)
Other versions
JPS6245202B2 (en
Inventor
Seiichi Iida
誠一 飯田
Kazuyoshi Kita
一吉 喜多
Hidehiko Otsuki
秀彦 大槻
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.)
Sunstar Inc
Original Assignee
Sunstar Inc
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 Sunstar Inc filed Critical Sunstar Inc
Priority to JP59254595A priority Critical patent/JPS61130205A/en
Publication of JPS61130205A publication Critical patent/JPS61130205A/en
Publication of JPS6245202B2 publication Critical patent/JPS6245202B2/ja
Granted legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides 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
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36Carboxylic acids; Salts or anhydrides thereof
    • A61K8/362Polycarboxylic acids
    • 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
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/52Stabilizers

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Birds (AREA)
  • Chemical & Material Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Dermatology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Emergency Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Preparation And Processing Of Foods (AREA)
  • Non-Alcoholic Beverages (AREA)
  • Furan Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Cosmetics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

PURPOSE:An aqueous composition that is prepared by adding a dicarboxylic acid such as adipic or pimeric acid as a stabilizer, thus stabilizing ascorbic acid in an aqueous composition used in medicines, chemicals for nonmedical purposes, cosmetics or foods. CONSTITUTION:The objective aqueous composition is prepared by adding ascorbic acid or its derivative which is a nutrient as vitamin C and used as a skin color-lightening, medicines, cosmetics and foods and 0.1-10wt%, based on the total weight of the composition, of a dicarboxylic acid of 6-10 carbon atoms such as suberic, azelaic or sebacic acid whereby the ascorbic acid is stabilized.

Description

【発明の詳細な説明】 発明の分野 本発明はアスコルビン酸を安定に配合した水系の医薬品
、医薬部外品、化粧料、食品のごとき組成物に関する。
DETAILED DESCRIPTION OF THE INVENTION Field of the Invention The present invention relates to compositions such as aqueous pharmaceuticals, quasi-drugs, cosmetics, and foods that stably contain ascorbic acid.

発明の背景 アスコルビン酸はビタミンCとしての栄養効果をはじめ
、皮膚美白効果やその他、医薬品、医薬部外品、化粧料
および食品にとって有用な種々の効果を示す物質で、こ
れらの組成物の有効成分の1つとして汎用されている。
Background of the Invention Ascorbic acid is a substance that exhibits nutritional effects as vitamin C, skin whitening effects, and various other useful effects for pharmaceuticals, quasi-drugs, cosmetics, and foods, and is an active ingredient in these compositions. It is widely used as one of the

しかしながら、アスコルビン酸は非常に不安定な物質で
、それ自体水溶性であるものの、ことに水系組成物中で
は不安定となりやすく、その組成物への配合に際しては
従来から種々の安定化策が採用されている。例えば、リ
ン酸、硫酸、脂肪酸等のエステル誘導体としたり、シク
ロデキストリンやりポゾーム、その他油脂類で包んだり
、グリセリン等の多価アルコールの非水系水溶性基剤に
配合したりしている。
However, ascorbic acid is a very unstable substance, and although it is water-soluble itself, it tends to become unstable particularly in aqueous compositions, and various stabilization measures have traditionally been adopted when incorporating it into such compositions. has been done. For example, they are made into ester derivatives of phosphoric acid, sulfuric acid, fatty acids, etc., wrapped in cyclodextrin, posomes, or other fats and oils, or blended into non-aqueous water-soluble bases of polyhydric alcohols such as glycerin.

しかしなから、これらの安定化策は、アスコルビン酸か
安定化されても、その活性か発現されなかったり、また
、用途が制限されたりする場合があり、必ずしも満足す
べきものではない。
However, these stabilization measures are not necessarily satisfactory because even if ascorbic acid is stabilized, its activity may not be expressed or its uses may be limited.

本発明者らはアスコルビン酸の安定化について鋭意研究
をつつける間に、意外にも、炭素数6〜10のジカルボ
ン酸を少量併用することにより、水系の組成物において
もアスコルビン酸か安定化できることを見出した。
While the present inventors were conducting intensive research on the stabilization of ascorbic acid, they unexpectedly discovered that ascorbic acid could be stabilized even in aqueous compositions by using a small amount of dicarboxylic acid having 6 to 10 carbon atoms. I found out.

特開昭53−130433号には炭素数9のジカルボン
酸であるアゼライン酸またはそのエステルとビタミンC
を併用した色素過多皮膚病等の治療用組成物が開示され
ている。しかしなから、アゼライン酸またはそのエステ
ルの量は本発明の債と比較して多量であり、また、アゼ
ライン酸のエステルには本発明のビタミンC安定化作用
は見られない。したがって、この特開昭53−1304
33号はアルコルビン酸の安定化について何らの示唆モ
与えるものてはない。
JP-A-53-130433 discloses azelaic acid or its ester, which is a dicarboxylic acid having 9 carbon atoms, and vitamin C.
A composition for the treatment of hyperpigmented skin diseases, etc., which is used in combination with However, the amount of azelaic acid or its ester is large compared to the bond of the present invention, and the vitamin C stabilizing effect of the present invention is not observed in the ester of azelaic acid. Therefore, this Japanese Patent Application Publication No. 53-1304
No. 33 does not give any suggestion regarding the stabilization of ascorbic acid.

発明の概要 本発明はアスコルビン酸またはその誘導体と、組成物全
量に対して0.1〜10%(重量%、以下同じ)の炭素
数6〜10のジカルボン酸を配合してなるアスコルビン
酸を安定に配合した水系組成物を提供するものである。
Summary of the Invention The present invention provides a method for stabilizing ascorbic acid, which is obtained by blending ascorbic acid or a derivative thereof with a dicarboxylic acid having 6 to 10 carbon atoms in an amount of 0.1 to 10% (by weight, same hereinafter) based on the total amount of the composition. The present invention provides an aqueous composition formulated with

本発明によれば水系の組成物であっても、アスコルビン
酸が安定に保たれ、充分にその活性を発現でき、また、
用途の制限などもなく、例えば、皮膚外用剤、美白化粧
料、ドリンク剤など、医薬品、医薬部外品、化粧料、食
品のいずれの分野の水系組成物においてもアスコルビン
酸の安定化が図れる。
According to the present invention, even in an aqueous composition, ascorbic acid can be kept stable and its activity can be sufficiently expressed, and
There are no restrictions on the use, and for example, ascorbic acid can be stabilized in aqueous compositions in the fields of pharmaceuticals, quasi-drugs, cosmetics, and foods, such as external skin preparations, whitening cosmetics, and drinks.

発明の詳細 な説明の組成物に用いるアスコルビン酸は遊離の酸自体
でもよく、また、ナトリウム塩等の塩類、リン酸、硫酸
、脂肪酸等とのエステル体、糖等とのエーテル体のごと
きアスコルビン酸誘導体でもよい。これらの配合量は通
常この種の組成物に採用される範囲でよく、実際の剤形
や用途に応じて適宜選択できるが、一般に、アスコルビ
ン酸として0.1〜10%の範囲で充分である。
The ascorbic acid used in the composition described in the detailed description of the invention may be the free acid itself, or may be ascorbic acid in the form of salts such as sodium salts, esters with phosphoric acid, sulfuric acid, fatty acids, etc., or ethers with sugars, etc. It may also be a derivative. The amount of these compounds may be within the range normally adopted for this type of composition and can be selected appropriately depending on the actual dosage form and use, but in general, a range of 0.1 to 10% of ascorbic acid is sufficient. .

炭素数6〜10のジカルボン酸、すなわち、アジピン酸
、ピメリン酸、スペリン酸、アゼライン酸またはセバシ
ン酸は組成物全量に対して0.1〜10%、好ましくは
、1〜5%の範囲で配合され一般に、アスコルビン酸と
同量またはそれ以下でよい。ジカルボン酸の量は、少な
すぎるとアスコルビン酸の安定化効果が期待できず、ま
た、多すきると、ジカルボン酸による副作用が生じたり
、また、水に溶けにくいために沈澱が生ずるなどの問題
が出てくる。なお、前記のごとく、これらのジカルボン
酸のエステル誘導体やメルカプト誘導体のようなカルボ
ン酸基が変化した誘導体にはアスコルビン酸安定化効果
が見られない。
A dicarboxylic acid having 6 to 10 carbon atoms, that is, adipic acid, pimelic acid, superric acid, azelaic acid, or sebacic acid is blended in an amount of 0.1 to 10%, preferably 1 to 5%, based on the total amount of the composition. and generally in the same amount or less than ascorbic acid. If the amount of dicarboxylic acid is too small, the stabilizing effect of ascorbic acid cannot be expected, and if it is too large, problems such as side effects caused by dicarboxylic acid may occur, and precipitation may occur due to poor solubility in water. It's coming. As mentioned above, derivatives in which the carboxylic acid group has been changed, such as ester derivatives and mercapto derivatives of dicarboxylic acids, do not exhibit an ascorbic acid stabilizing effect.

か(して、本発明の組成物は常法に従って水系組成物、
すなわち、実質的な量の水を含をするローション、乳剤
、軟膏、パップ剤などの剤形の皮膚外用剤、化粧水、ク
リーム、乳液、パック、石鹸、ゲル、エアゾル等の剤形
の化粧料、ことに皮膚美白化粧料、ドリンク剤、ゲル、
ペースト等の剤形の食品とすることができる。他の成分
は特に限定するものではなく、ことに、アスコルビン酸
は水に溶解し、ジカルボン酸はアルコールや液状油に溶
解すると製造が容易である。また、特に限定するもので
はないが、アスコルビン酸の安定化効果や、組成物の使
用上の刺激等の観点から、組成物のpHを5〜7に調整
することが好ましい。
(Thus, the composition of the present invention can be prepared as an aqueous composition,
In other words, external skin preparations in the form of lotions, emulsions, ointments, poultices, etc. that contain a substantial amount of water, cosmetics in the form of lotions, creams, milky lotions, packs, soaps, gels, aerosols, etc. , especially skin whitening cosmetics, drinks, gels,
It can be a food product in the form of a paste or the like. Other components are not particularly limited, and production is particularly easy if ascorbic acid is dissolved in water and dicarboxylic acid is dissolved in alcohol or liquid oil. Further, although not particularly limited, it is preferable to adjust the pH of the composition to 5 to 7 from the viewpoint of the stabilizing effect of ascorbic acid and irritation during use of the composition.

アスコルビン酸の安定化効果 各種のジカルボン酸のアスコルビン酸の安定化に対する
効果をつぎのとおり試験した。
Stabilizing effect of ascorbic acid The effect of various dicarboxylic acids on stabilizing ascorbic acid was tested as follows.

ジカルボン酸およびアスコルビン酸を、各々、1%にな
るように20%エタ/−ル水溶液に溶解し、40℃で4
ケ月放置した。放置後、アスコルビン酸酸を定量し、当
初の添加量を100%とした場合の残存アスコルビン酸
量の相対割合(残存率、%)を算出した。また、溶液の
着色をつぎの基準に従って評価した。
Dicarboxylic acid and ascorbic acid were each dissolved in a 20% aqueous ethanol solution to a concentration of 1%, and incubated at 40°C for 4 hours.
I left it alone for a few months. After standing, ascorbic acid was quantified, and the relative proportion (residual rate, %) of the amount of residual ascorbic acid was calculated when the initial addition amount was set as 100%. In addition, the coloring of the solution was evaluated according to the following criteria.

一:はとんど着色なし、±:わずかに着色1、+:着色
、+)−:著しく着色 結果を第1表に示す。なお、第1表には溶液のpHを6
.0に調整して同様に試験した場合およびジカルボン酸
を添加せずに同様に試験した結果も示す。
1: Almost no coloring, ±: Slightly colored 1, +: Colored, +)-: Significantly colored, the results are shown in Table 1. In addition, Table 1 shows that the pH of the solution is 6.
.. The results are also shown when the test was conducted in the same manner with the dicarboxylic acid adjusted to 0, and when the test was conducted in the same manner without adding the dicarboxylic acid.

第1表 第1表に示すごとく、炭素数6〜10のジカルボン酸は
pH未調整の場合も、pH6,0に調整した場合も特異
的にアスコルビン酸を安定化させ、また着色が著しく少
ない。なお、炭素数11以上のジカルボン酸は水に対す
る溶解性が低く、使用しがたい。
Table 1 As shown in Table 1, dicarboxylic acids having 6 to 10 carbon atoms specifically stabilize ascorbic acid both when the pH is not adjusted and when the pH is adjusted to 6.0, and the coloration is extremely low. Note that dicarboxylic acids having 11 or more carbon atoms have low solubility in water and are difficult to use.

実施例 つぎに実施例を挙げて本発明をさらに詳しく説明する。Example Next, the present invention will be explained in more detail with reference to Examples.

実施例1゜ 成   分                  %A
酸成分混合、溶解し、これにB成分の混合溶解物を攪拌
下に加えてアスコルビン酸を安定に配合した皮膚美白用
クリームを得た。
Example 1゜Ingredients %A
The acid components were mixed and dissolved, and a mixed solution of component B was added thereto under stirring to obtain a skin whitening cream stably containing ascorbic acid.

実施例2 成   分                 %(グ
リセリン           25A成分を混合、溶
解し、これにB成分の混合溶解物を攪拌下に加えてアス
コルビン酸を安定に配合したローションを得た。
Example 2 Ingredients % (Glycerin) 25 Component A was mixed and dissolved, and a mixed solution of Component B was added thereto under stirring to obtain a lotion in which ascorbic acid was stably blended.

実施例3 成   分                  %A
酸成分混合、溶解し、これにB成分の混合溶解物を攪拌
下に加えて所望の乳液を得た。この乳液を40℃で4ケ
月放置したところ、着色は見られず、アスコルビン酸量
の低下も認められなかつた。
Example 3 Ingredients %A
The acid components were mixed and dissolved, and a mixed solution of component B was added thereto under stirring to obtain a desired emulsion. When this emulsion was left at 40° C. for 4 months, no coloration was observed and no decrease in the amount of ascorbic acid was observed.

実施例4 つきの処方により、常法に従い、アスコルビン酸を安定
に配合したドリンク剤を得た。
Example 4 A drink stably containing ascorbic acid was obtained according to the conventional method according to the following formulation.

成   分                    
 %レモン果汁              10砂糖
        10 ブドウ糖                 lOアス
コルビン酸             2アジピン酸 
              0,5エタノール   
            5香料        適量 精製水      100引薯 特肝出願人サンスター株式会社
Ingredients
%Lemon juice 10 Sugar 10 Glucose 10 Ascorbic acid 2 Adipic acid
0,5 ethanol
5 Fragrance Appropriate amount Purified water 100 yam special liver applicant Sunstar Co., Ltd.

Claims (4)

【特許請求の範囲】[Claims] (1)アスコルビン酸またはその誘導体と、組成物全量
に対して0.1〜10重量%の炭素数6〜10のジカル
ボン酸を配合したことを特徴とするアスコルビン酸を安
定に配合した水系組成物。
(1) An aqueous composition stably containing ascorbic acid, which is characterized by containing ascorbic acid or a derivative thereof and 0.1 to 10% by weight of a dicarboxylic acid having 6 to 10 carbon atoms based on the total amount of the composition. .
(2)皮膚外用剤である前記第(1)項の組成物。(2) The composition according to item (1) above, which is an external preparation for skin. (3)美白化粧料である前記第(1)項の組成物。(3) The composition of item (1) above, which is a whitening cosmetic. (4)ドリンク剤である前記第(1)項の組成物。(4) The composition according to item (1) above, which is a drink.
JP59254595A 1984-11-30 1984-11-30 Aqueous composition containing stabilized ascorbic acid Granted JPS61130205A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP59254595A JPS61130205A (en) 1984-11-30 1984-11-30 Aqueous composition containing stabilized ascorbic acid

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP59254595A JPS61130205A (en) 1984-11-30 1984-11-30 Aqueous composition containing stabilized ascorbic acid

Publications (2)

Publication Number Publication Date
JPS61130205A true JPS61130205A (en) 1986-06-18
JPS6245202B2 JPS6245202B2 (en) 1987-09-25

Family

ID=17267221

Family Applications (1)

Application Number Title Priority Date Filing Date
JP59254595A Granted JPS61130205A (en) 1984-11-30 1984-11-30 Aqueous composition containing stabilized ascorbic acid

Country Status (1)

Country Link
JP (1) JPS61130205A (en)

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0276868A (en) * 1987-10-19 1990-03-16 Takeda Chem Ind Ltd Production of stable sodium ascorbate composition and powder
EP0393537A2 (en) * 1989-04-18 1990-10-24 Takeda Chemical Industries, Ltd. Granulation product of calcium ascorbate
JPH0940543A (en) * 1995-07-25 1997-02-10 L'oreal Sa Stable composition containing water-oversensitive make-up and/or dermatological activator
JPH0940545A (en) * 1995-07-25 1997-02-10 L'oreal Sa Stable composition containing ascorbic acid
WO2002013778A3 (en) * 2000-08-16 2002-09-12 Cognis Deutschland Gmbh Cosmetic preparations containing dicarboxylic acids
WO2007003289A1 (en) * 2005-07-04 2007-01-11 Henkel Kommanditgesellschaft Auf Aktien Skin-lightening compositions with an improved action
US20110002900A1 (en) * 2008-03-10 2011-01-06 Geltrude Mingrone Medium chain dicarboxylic acids, their derivates and metabolic disorders
JP2012232970A (en) * 2011-04-22 2012-11-29 Rohto Pharmaceutical Co Ltd Antibacterial composition
JP2013170158A (en) * 2012-02-22 2013-09-02 Kao Corp Oral ultraviolet light resistance improver

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS53130433A (en) * 1977-04-19 1978-11-14 Nazzaro Porro Marcella Composition and method for treating hyperchromocyte skin disease

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS53130433A (en) * 1977-04-19 1978-11-14 Nazzaro Porro Marcella Composition and method for treating hyperchromocyte skin disease

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0276868A (en) * 1987-10-19 1990-03-16 Takeda Chem Ind Ltd Production of stable sodium ascorbate composition and powder
EP0393537A2 (en) * 1989-04-18 1990-10-24 Takeda Chemical Industries, Ltd. Granulation product of calcium ascorbate
JPH0940543A (en) * 1995-07-25 1997-02-10 L'oreal Sa Stable composition containing water-oversensitive make-up and/or dermatological activator
JPH0940545A (en) * 1995-07-25 1997-02-10 L'oreal Sa Stable composition containing ascorbic acid
WO2002013778A3 (en) * 2000-08-16 2002-09-12 Cognis Deutschland Gmbh Cosmetic preparations containing dicarboxylic acids
WO2007003289A1 (en) * 2005-07-04 2007-01-11 Henkel Kommanditgesellschaft Auf Aktien Skin-lightening compositions with an improved action
US20110002900A1 (en) * 2008-03-10 2011-01-06 Geltrude Mingrone Medium chain dicarboxylic acids, their derivates and metabolic disorders
AU2009224732B2 (en) * 2008-03-10 2014-08-21 Nestec S.A. Medium chain dicarboxylic acids, their derivates and metabolic disorders
US8962689B2 (en) * 2008-03-10 2015-02-24 Nestec S.A. Medium chain dicarboxylic acids, their derivates and metabolic disorders
JP2012232970A (en) * 2011-04-22 2012-11-29 Rohto Pharmaceutical Co Ltd Antibacterial composition
JP2016188258A (en) * 2011-04-22 2016-11-04 ロート製薬株式会社 Antibacterial composition
JP2013170158A (en) * 2012-02-22 2013-09-02 Kao Corp Oral ultraviolet light resistance improver

Also Published As

Publication number Publication date
JPS6245202B2 (en) 1987-09-25

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