JPS6330415A - Antioxidation agent - Google Patents

Antioxidation agent

Info

Publication number
JPS6330415A
JPS6330415A JP61171847A JP17184786A JPS6330415A JP S6330415 A JPS6330415 A JP S6330415A JP 61171847 A JP61171847 A JP 61171847A JP 17184786 A JP17184786 A JP 17184786A JP S6330415 A JPS6330415 A JP S6330415A
Authority
JP
Japan
Prior art keywords
paeoniflorin
cerebral
drug
agent
adult
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
JP61171847A
Other languages
Japanese (ja)
Other versions
JPH0772135B2 (en
Inventor
Akitane Mori
森 昭胤
Midori Hiramatsu
平松 緑
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.)
Tsumura and Co
Original Assignee
Tsumura Juntendo 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 Tsumura Juntendo Inc filed Critical Tsumura Juntendo Inc
Priority to JP61171847A priority Critical patent/JPH0772135B2/en
Publication of JPS6330415A publication Critical patent/JPS6330415A/en
Publication of JPH0772135B2 publication Critical patent/JPH0772135B2/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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  • Saccharide Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

PURPOSE:To provide an antioxidation agent containing paeoniflorin as an active component and effective in preventing the oxidation by active oxygen. CONSTITUTION:The objective agent contains paeoniflorin of formula as an active component. Paeoniflorin is a compound existing in SHAKUYAKU (root of Paeonia albiflora) known as a Chinese herb drug. The agent is effective as a remedy for arteriosclerosis, myocardial infarction, cerebral apoplexy, cerebral hemorrhage, cerebral infarction, cerebral thrombosis, cataract, inflammation, autoimmune diseases, etc., and is administered preferably at a rate of 150-300mg daily for adult as an oral drug or 3-60mg daily for adult as a parenteral drug.

Description

【発明の詳細な説明】 活性酸素(−OH1103、HvOt等)は、生体内で
作られる物質であり、禽食作用により好中球に取り込ま
れた異物を溶解する作用を有する等、生体に必要な物質
である。その半面、活性酸素は脂化 質を酸化して、動脈硬化症、脳卒中、心筋#塞等の疾病
の原因となる過酸化脂質を産生じたり、水晶体タンパク
を変性して白内障を引き起こす原因となる等、好ましく
ない作用を及ぼすことら知られている。従って、活性酸
素のラジカルを除去することによりその反応性を低下さ
ければ、脂質をはじめとする生体内物質の酸化を防ぐこ
とができるのである。
DETAILED DESCRIPTION OF THE INVENTION Active oxygen (-OH1103, HvOt, etc.) is a substance produced within the body, and is necessary for the body because it has the effect of dissolving foreign substances taken up by neutrophils through phagocytosis. It is a substance. On the other hand, active oxygen oxidizes lipids, producing lipid peroxides that cause diseases such as arteriosclerosis, stroke, and myocardial infarction, and degenerates lens proteins and causes cataracts. These substances are known to have undesirable effects. Therefore, if the reactivity of active oxygen radicals is reduced by removing them, it is possible to prevent the oxidation of substances in the body, including lipids.

そこで本発明者等は活性酸素のラジカルを除去する作用
を有する物質を見出すべく、鋭意検討を重ねた結果、和
漢薬の荀薬に含有される下記式で表されるペオニフロリ
ンに活性酸素のラジカルを除去する作用のあることを見
出し本発明を完成した。すなわちペオニフロリンは、活
性酸素による酸化を防止する効果を有するものであり、
本発明はペオニフロリンを有効成分とする抗酸化剤(以
下、本発明の薬剤と称する。)である。
Therefore, the present inventors conducted extensive research in order to find a substance that has the effect of removing active oxygen radicals, and as a result, they found that active oxygen radicals were added to paeoniflorin, which is expressed by the following formula and is contained in the Japanese and Chinese medicine Xun Yaku. The present invention was completed based on the discovery that it has the effect of removing it. In other words, paeoniflorin has the effect of preventing oxidation caused by active oxygen,
The present invention is an antioxidant containing paeoniflorin as an active ingredient (hereinafter referred to as the drug of the present invention).

建 本発明の薬剤は動脈硬化症、心筋≠基層、脳卒机 中、脳出血、脳稔塞、脳血栓、白内障、炎症および自己
免疫疾患等の治療に有効である。
The drug of the present invention is effective in the treatment of arteriosclerosis, myocardium≠substratum, stroke, cerebral hemorrhage, cerebral occlusion, cerebral thrombosis, cataract, inflammation, autoimmune diseases, and the like.

本発明の薬剤の有効成分であるペオニフロリンは、たと
えば和光純薬工業株式会社から市販されている生薬有効
成分標準品を用いることができる。
As paeoniflorin, which is the active ingredient of the drug of the present invention, a standard crude drug active ingredient commercially available from Wako Pure Chemical Industries, Ltd., for example, can be used.

次に、ペオニフロリンが抗酸化作用を有することについ
て実験例を挙げて説明する。
Next, the fact that paeoniflorin has an antioxidant effect will be explained using experimental examples.

実験例 1.1−ジフェニル−2−ピクリルヒドラジル(以下D
PPHと称する)を30μMの濃度になるようにエタノ
ールに溶解し、この溶液100Jに、ペオニフロリン2
00μgをエタノールに溶解して100JJ!Qとした
溶液を加え、10秒撹拌後、偏平セルに取り、電子スピ
ン共鳴スペクトラム(ERSスペクトロメーター)を用
いて、3350±100ガウス(Gauss)、室温の
条件下で測定した。
Experimental example 1.1-diphenyl-2-picrylhydrazyl (hereinafter referred to as D
PPH) was dissolved in ethanol to a concentration of 30 μM, and 100 J of this solution was added with 2 paeoniflorin.
Dissolve 00μg in ethanol and make 100JJ! The solution labeled Q was added, stirred for 10 seconds, taken into a flat cell, and measured using an electron spin resonance spectrum (ERS spectrometer) at 3350±100 Gauss and room temperature.

尚、ペオニフロリンを加えない場合をコントローに位置
するシグナルに注目し、この高さを測定して、内部標準
物質として加えたMnOのMn2+シグナルの高さに対
する比(相対比)を算出することによりラジカルの減少
量求めた。
In addition, we focused on the signal located in the control when paeoniflorin was not added, measured its height, and calculated the ratio (relative ratio) of MnO added as an internal standard substance to the height of the Mn2+ signal. The amount of decrease was calculated.

その結果、ペオニフロリンはDPPH由来のシグナルの
高さを15%減少させることが認められ、ペオニフロリ
ンはラジカル消去作用を有することが明らかとなった。
As a result, paeoniflorin was found to reduce the height of the signal derived from DPPH by 15%, and it was revealed that paeoniflorin has a radical scavenging effect.

次に、ペオニフロリンの急性毒性試験をddY系マウス
を用いて行ったところ(1群10匹)、2000 mg
/kgまでの経口投与で死亡例はなかった。
Next, an acute toxicity test of paeoniflorin was conducted using ddY mice (10 mice per group), and it was found that 2000 mg
There were no cases of death after oral administration of up to 1 kg/kg.

また、ペオニフロリンはそのまま、あるいは慣用の製剤
担体と共に動物および人に投与することができる。投与
形態としては、特に限定がなく、必要に応じ適宜選択し
て使用され、液剤、散剤、顆粒剤、錠剤、腸溶剤および
カプセル剤などの経口剤、注射剤、坐剤などの非経口剤
が挙げられる。
Moreover, paeoniflorin can be administered to animals and humans as it is or together with a conventional pharmaceutical carrier. The dosage form is not particularly limited and may be selected and used as appropriate, including oral preparations such as liquids, powders, granules, tablets, enteric-coated preparations and capsules, and parenteral preparations such as injections and suppositories. Can be mentioned.

経口剤として所期の効果を発揮するためには、患者の年
令、体重、疾患の程度により異なるが、通常成人でペオ
ニフロリンの重量として1日150〜300mgを3回
までに分けて服用するのが適当と思われる。
In order to achieve the desired effect as an oral agent, adults should usually take 150 to 300 mg of paeoniflorin per day in three divided doses, although this will vary depending on the age, weight, and severity of the disease of the patient. seems appropriate.

本発明において錠剤、カプセル剤、顆粒剤等の経口剤は
常法に従って製造される。錠剤は本発明の化合物をゼラ
チン、デンプン、乳糖、ステアリン酸マグネシウム、滑
石、アラビアゴム等の製剤学的賦形剤と混合し賦形する
ことにより製造され、カプセル剤は、本発明の化合物を
不活性の製剤充填剤、もしくは希釈剤と混合し、硬質ゼ
ラチンカプセル、軟質ゼラチンカプセル等に充填するこ
とにより製造される。シロップ剤、エリキシル剤は、本
発明の化合物をショ糖等の甘味剤、メチルパラベンおよ
びプロピルパラベン類等の防腐剤、着色剤、調味剤、芳
香剤、補助剤と混合して製造される。
In the present invention, oral preparations such as tablets, capsules, and granules are manufactured according to conventional methods. Tablets are prepared by mixing the compound of the present invention with pharmaceutical excipients such as gelatin, starch, lactose, magnesium stearate, talc, gum arabic, etc., and capsules are prepared by mixing the compound of the present invention with pharmaceutical excipients such as gelatin, starch, lactose, magnesium stearate, talc, gum arabic, etc. It is manufactured by mixing it with an active pharmaceutical filler or diluent and filling it into hard gelatin capsules, soft gelatin capsules, etc. Syrups and elixirs are prepared by mixing the compound of the present invention with sweetening agents such as sucrose, preservatives such as methylparabens and propylparabens, coloring agents, flavoring agents, fragrances, and adjuvants.

非経口剤として所期の効果を発揮するためには、患者の
年令、体重、疾患の程度により異なるが、通常成人でペ
オニフロリンの重量として1日3〜60mgまでの静注
、皮下注射、筋肉注射が適当と思われる。
In order to achieve the desired effect as a parenteral agent, it is usually necessary for adults to administer up to 3 to 60 mg of paeoniflorin per day by intravenous injection, subcutaneous injection, or intramuscular injection, although this will vary depending on the patient's age, weight, and severity of the disease. injection seems appropriate.

この非経口剤は常法に従って製造され、希釈剤として一
般に注射用蒸留水、生理食塩水、デキストロース水溶液
、注射用植物油、プロピレングリコール、ポリエチレン
グリコール等を用いることができる。さらに必要に応じ
て、適宜、殺菌剤、等張化剤、安定剤、防腐剤、無痛化
剤等を加えてもよい。また、この非経口剤は安定性の点
から、アンプル等に充填後冷凍し、通常の凍結乾燥技術
により水分を除去し、使用直前に凍結乾燥物から液剤を
再調製することもできる。
This parenteral preparation is manufactured according to a conventional method, and distilled water for injection, physiological saline, aqueous dextrose solution, vegetable oil for injection, propylene glycol, polyethylene glycol, etc. can generally be used as a diluent. Furthermore, if necessary, a bactericidal agent, an isotonizing agent, a stabilizer, a preservative, a soothing agent, etc. may be added as appropriate. In addition, from the viewpoint of stability, this parenteral preparation can also be filled into ampoules and the like, frozen, water removed by ordinary freeze-drying techniques, and a liquid preparation prepared from the freeze-dried product immediately before use.

その他の非経口剤としては、外用液剤、軟膏等の塗布剤
、直腸内投与のための坐剤等が挙げられ、常法に従って
製造される。
Other parenteral preparations include liquid preparations for external use, liniments such as ointments, suppositories for rectal administration, and the like, which are manufactured according to conventional methods.

次に、用例を示して本発明をさらに具体的に説明するが
、本発明はこれにより制限されるものではない。
Next, the present invention will be explained in more detail with reference to examples, but the present invention is not limited thereto.

用例! 前記具体例!で得たペオニフロリン2.5gを細末とし
、これを乳糖90.5gおよびステアリン酸マグネシウ
ム7gと混合し、この混合物を単発式スラッグ打錠機に
て打錠して直径2On++n、重量2.3gのスラッグ
錠を作りこれをオシレーターにて破砕し、整粒し、篩別
して20〜50メツシユの粒子の良好な顆粒剤を得た。
example! The above specific example! 2.5 g of paeoniflorin obtained in step 2 was made into a fine powder, mixed with 90.5 g of lactose and 7 g of magnesium stearate, and this mixture was compressed using a single-shot slug tablet machine to form tablets with a diameter of 2On++n and a weight of 2.3g. Slug tablets were prepared, crushed with an oscillator, sized, and sieved to obtain good granules of 20 to 50 mesh particles.

本顆粒剤は1g中にペオニフロリン25mgを含有して
いるが、症状に合わせて1回2〜4gを1日3回服用す
る。
Each gram of this granule contains 25 mg of paeoniflorin, and the dosage is 2 to 4 g three times a day, depending on the symptoms.

用例2 前記具体例1で得たペオニフロリン25gに微結晶セル
ロース70gおよびステアリン酸マグネシウム5gを加
えて混合し、この混合物を単発式打錠機にて打錠して径
9 mm、重量200mgの錠剤を製造した。
Example 2 70 g of microcrystalline cellulose and 5 g of magnesium stearate were added to 25 g of paeoniflorin obtained in Example 1 and mixed, and this mixture was compressed using a single-shot tablet machine to form tablets with a diameter of 9 mm and a weight of 200 mg. Manufactured.

本錠剤は、1錠中にペオニフロリン50mgを含有して
いるが、症状に合わせて1回1〜2錠を1日3回服用す
る。
This tablet contains 50 mg of paeoniflorin per tablet, and it is recommended to take 1 to 2 tablets at a time, three times a day, depending on the symptoms.

用例3 前記具体例1で得たペオニフロリンlOgを細末とし、
これを乳糖90gと混合し、 この500mgづつを硬カプセルに充填してカプセル剤
を得た。
Example 3 1Og of paeoniflorin obtained in the above specific example 1 was made into fine powder,
This was mixed with 90 g of lactose, and 500 mg of this was filled into hard capsules to obtain capsules.

本カプセル剤は、lカプセル中にペオニフロリン50m
gを含有しているが、症状に合わせて1回1〜2カプセ
ルを1日3回服用する。
This capsule contains 50m of paeoniflorin per capsule.
It contains 1 to 2 capsules three times a day, depending on the symptoms.

用例4 前記具体例【で得たペオニフロリン50gを注射剤の常
法に従って、60℃に加温した注射用蒸留水1文に加え
て懸濁し、塩化ナトリウムにより等張化した後にアンプ
ルに封入した。
Example 4 According to the conventional method for injections, 50 g of paeoniflorin obtained in Example 4 was suspended in one volume of distilled water for injection heated to 60°C, and the suspension was made isotonic with sodium chloride and then sealed in an ampoule.

本注射剤はld中にペオニフロリン50mgを含有する
。本注射剤は症状に合わせて1回2〜4 aQを静脈内
あるいは筋肉内注射する。
This injection contains 50 mg of paeoniflorin in ld. This injection is administered intravenously or intramuscularly at a dose of 2 to 4 aQ depending on the symptoms.

Claims (1)

【特許請求の範囲】[Claims] ペオニフロリンを有効成分とする抗酸化剤。An antioxidant containing paeoniflorin as an active ingredient.
JP61171847A 1986-07-23 1986-07-23 Antioxidant Expired - Lifetime JPH0772135B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP61171847A JPH0772135B2 (en) 1986-07-23 1986-07-23 Antioxidant

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP61171847A JPH0772135B2 (en) 1986-07-23 1986-07-23 Antioxidant

Publications (2)

Publication Number Publication Date
JPS6330415A true JPS6330415A (en) 1988-02-09
JPH0772135B2 JPH0772135B2 (en) 1995-08-02

Family

ID=15930873

Family Applications (1)

Application Number Title Priority Date Filing Date
JP61171847A Expired - Lifetime JPH0772135B2 (en) 1986-07-23 1986-07-23 Antioxidant

Country Status (1)

Country Link
JP (1) JPH0772135B2 (en)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005107698A1 (en) * 2004-05-10 2005-11-17 Lg Household & Health Care Ltd. Skin aging treatment comprising paeoniflorin
EP1767210A1 (en) * 2004-07-02 2007-03-28 Shanghai Institute of Materia Medica, Chinese Academy of Sciences The medical use of paeoniflorin
KR100732886B1 (en) * 2005-11-07 2007-06-27 한국화학연구원 Composition having antihypertensive effect comprising extract of moutan cortex radicis or active compounds isolated therefrom
KR100769580B1 (en) * 2005-03-07 2007-10-23 주식회사 엘지생활건강 Agnet for protection of uv inducded-dna damage in skin
CN103977387A (en) * 2014-06-02 2014-08-13 任红梅 Traditional Chinese medicinal preparation for treating cerebral thrombosis and preparation method thereof

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005107698A1 (en) * 2004-05-10 2005-11-17 Lg Household & Health Care Ltd. Skin aging treatment comprising paeoniflorin
EP1767210A1 (en) * 2004-07-02 2007-03-28 Shanghai Institute of Materia Medica, Chinese Academy of Sciences The medical use of paeoniflorin
JP2008505128A (en) * 2004-07-02 2008-02-21 中国科学院上海薬物研究所 Medical use of paeoniflorin
EP1767210A4 (en) * 2004-07-02 2010-09-08 Shanghai Inst Materia Medica The medical use of paeoniflorin
KR100769580B1 (en) * 2005-03-07 2007-10-23 주식회사 엘지생활건강 Agnet for protection of uv inducded-dna damage in skin
KR100732886B1 (en) * 2005-11-07 2007-06-27 한국화학연구원 Composition having antihypertensive effect comprising extract of moutan cortex radicis or active compounds isolated therefrom
CN103977387A (en) * 2014-06-02 2014-08-13 任红梅 Traditional Chinese medicinal preparation for treating cerebral thrombosis and preparation method thereof

Also Published As

Publication number Publication date
JPH0772135B2 (en) 1995-08-02

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