JPS61236725A - Agent for suppressing cerebral edema - Google Patents
Agent for suppressing cerebral edemaInfo
- Publication number
- JPS61236725A JPS61236725A JP7769685A JP7769685A JPS61236725A JP S61236725 A JPS61236725 A JP S61236725A JP 7769685 A JP7769685 A JP 7769685A JP 7769685 A JP7769685 A JP 7769685A JP S61236725 A JPS61236725 A JP S61236725A
- Authority
- JP
- Japan
- Prior art keywords
- agent
- quercitrin
- cerebral edema
- cerebral
- daily
- 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
Links
Landscapes
- Saccharide Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【発明の詳細な説明】
＆Ｊヱと」迫
本発明は、新規な脳浮腫抑制剤を提供することを目的と
する。DETAILED DESCRIPTION OF THE INVENTION An object of the present invention is to provide a novel cerebral edema inhibitor.
従１ｍ術
脳浮腫に対する薬剤として、現在グリセロールあるいは
マンニトールがよく使われている。しかし、これらは電
解質バランスの障害（高ナトリウム血症）や腎障害を惹
起することが知られており未だ満足しうる薬剤とは言え
ない。Currently, glycerol or mannitol is commonly used as a drug for cerebral edema following surgery. However, these drugs are known to cause disturbances in electrolyte balance (hypernatremia) and renal damage, and are not yet satisfactory drugs.
＆１五璽輩
本発明は、ケルシトリンを有効成分とする脳浮腫抑制剤
に関するものである。ケルシトリンは次の構造式を有す
るフラボノイドの一種である公知化合物である。The present invention relates to a cerebral edema inhibitor containing quercitrin as an active ingredient. Quercitrin is a known compound that is a type of flavonoid and has the following structural formula.
本発明者はケルシトリンのラットの実験的脳虚血モデル
に対する効果を検討したところ有意に優れた効果を見出
し本発明を完成した。次に実験例を挙げて説明する。The present inventor investigated the effect of quercitrin on an experimental cerebral ischemia model in rats and found a significantly superior effect, thereby completing the present invention. Next, an explanation will be given using an experimental example.
実験例：脳浮腫生成に対するケルシトリンの効果ＷｊＳ
ｔａｒラット（体重２３０〜２８０ｇ、雄）の両側椎骨
動脈の血流を遮断し、さらに両側椎骨動脈の血流を６０
分間遮断した。その後６０分間血流を再開通させてラッ
トの実験的脳虚血モデルを作成した（Ｗ、Ａ、Ｐｕ１ｓ
ｉｎｅｌｌｉ、ｅｔ ａｌ、、５ｔｒｏｋｅ、す、２６
７（１９７３）参照）。Experimental example: Effect of quercitrin on brain edema generation WjS
The blood flow in both vertebral arteries of tar rats (weight 230-280 g, male) was blocked, and the blood flow in both vertebral arteries was further reduced for 60 min.
It was shut off for a minute. Thereafter, blood flow was recanalized for 60 minutes to create an experimental cerebral ischemia model in rats (W, A, Pu1s
inelli,et al,,5stroke,su,26
7 (1973)).
本モデルに対して、血流遮断５分前にケルシトリン５
ｍ ｇ ／ ｋ ｇを生理食塩液態濁液として大腿静脈
より注入した。対照群には生理食塩液のみを注入した。In this model, 5 minutes of quercitrin was administered 5 minutes before blood flow was blocked.
mg/kg was injected into the femoral vein as a physiological saline suspension. The control group received only physiological saline.
さらに無処置動物も対照とした。In addition, untreated animals also served as controls.
−・ノリ方法（Ｊ 、 Ｎｅｕｒｏｃｈｅｍ、 。-・Nori method (J, Neurochem,.
２１．、＝、＝ｒ（１９７３））に従い液体窒素で脳を
凍結後摘出し、その前頭部的１００ｍｇを秤量後凍結乾
燥し、湿重量と乾燥重量の差から求め、これを指標とし
て効果を検討した。結果を表に示す。21. ,=,=r (1973)), the brain was frozen with liquid nitrogen, removed, and 100 mg of the frontal portion was weighed and freeze-dried. It was determined from the difference between wet weight and dry weight, and the effect was examined using this as an index. did. The results are shown in the table.
この結果から、ケルシトリン投与群における脳水分含量
は生理食塩液投与群におけるそれよりも有意に（Ｐ ＜
０．０５）低く、ケルシトリンに脳浮腫抑制作用があ
ることが明らかとなった。From this result, the brain water content in the quercitrin-administered group was significantly higher than that in the physiological saline-administered group (P <
0.05), indicating that quercitrin has a cerebral edema suppressing effect.
本発明の薬剤は、脳梗塞、脳出血などの虚血性脳血管障
害に伴なう脳浮腫の治療および予防に有効である。The drug of the present invention is effective in treating and preventing cerebral edema associated with ischemic cerebrovascular disorders such as cerebral infarction and cerebral hemorrhage.
ケルシトリンは、適当な副成分（賦形剤、結合剤、崩壊
剤、溶解剤等）と慣用の製剤技術で製剤化することがで
きる０例えば、錠剤、カプセル剤、散剤、顆粒剤、シロ
ップ剤、注射剤等の剤形を挙げることができ、経口また
は注射により投与するのが適当である。製剤の一例を次
に示す。Quercitrin can be formulated with appropriate accessory ingredients (excipients, binders, disintegrants, solubilizers, etc.) using conventional formulation techniques.For example, tablets, capsules, powders, granules, syrups, etc. Examples include dosage forms such as injections, which are suitably administered orally or by injection. An example of the formulation is shown below.
錠剤
ケルシトリン ５０ ｔｓｇカルボキ
シメチルセルロース ２５ ｔａｇでんぷん
５■ｇ結晶セルロース
４０ ｔａｇステアリン酸マグネシウム ２
ｔａｇ投与量としては、経口では成人−日当り１０ｍｇ
乃至１０ｇ、特に２００ｍｇ乃至５ｇ、静脈内注射等の
注射では１０ｍｇ乃至２ｇ、特に１００ｍｇ乃至１．５
ｇが適当であり、数回に分けて投与するのが普通であっ
て、症状や患者の状態等に応じて適宜増減する。tablet quercitrin 50 tsg carboxymethyl cellulose 25 tag starch
5g crystalline cellulose
40 tag Magnesium Stearate 2
The tag dosage is 10 mg per day for adults.
10g to 10g, especially 200mg to 5g, 10mg to 2g for injections such as intravenous injection, especially 100mg to 1.5g.
It is appropriate to administer the dose in several doses, and the dose may be increased or decreased as appropriate depending on the symptoms, patient's condition, etc.
ケルシトリンの毒性は医薬としての使用に支障のない範
囲であり、例えば、マウス腹腔内注射におけるＬＤｓｏ
は２００ｍｇ／ｋｇテある（Ｒｅｇｉｓｔｒｙ ｏｆ
ＴｏｘｉｃＥｆｆｅｃｔｓ ｏｆ Ｃｈｅｍｉｃａｌ
５ｕｂｓｔａｎｃｅｓ（１９８１−１９８２Ｅｄｉｔｉ
ｏｎ） Ｕ、Ｓ、Ｄｅｐａｒｔｍｅｎｔ ｏｆ Ｈｅａ
ｌｔｈ ａｎｄ ＨｕｍａｎＳｅｒｖｉｃｅｓ） 。The toxicity of quercitrin is within a range that does not interfere with its use as a medicine.
is 200mg/kg (Registry of
Toxic Effects of Chemical
5ubstances (1981-1982Editi
on) U, S, Department of Hea
lth and Human Services).
Claims (1)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP7769685A JPH0615473B2 (en) | 1985-04-12 | 1985-04-12 | Brain edema inhibitor |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP7769685A JPH0615473B2 (en) | 1985-04-12 | 1985-04-12 | Brain edema inhibitor |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS61236725A true JPS61236725A (en) | 1986-10-22 |
| JPH0615473B2 JPH0615473B2 (en) | 1994-03-02 |
Family
ID=13641052
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP7769685A Expired - Lifetime JPH0615473B2 (en) | 1985-04-12 | 1985-04-12 | Brain edema inhibitor |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH0615473B2 (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20030013177A (en) * | 2001-08-07 | 2003-02-14 | 황귀서 | A pharmaceutical composition containing quercitin as effective component |
| KR100989093B1 (en) | 2008-01-18 | 2010-10-25 | 한화제약주식회사 | Composition Comprising the Extracts of Branch of Lindera obtusiloba for Prevention and Treatment of Cardiovascular Diseases |
| WO2024101208A1 (en) * | 2022-11-07 | 2024-05-16 | サントリーホールディングス株式会社 | Composition for suppressing and/or improving decreased cerebral blood flow, containing quercetin and/or glycoside thereof |
-
1985
- 1985-04-12 JP JP7769685A patent/JPH0615473B2/en not_active Expired - Lifetime
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20030013177A (en) * | 2001-08-07 | 2003-02-14 | 황귀서 | A pharmaceutical composition containing quercitin as effective component |
| KR100989093B1 (en) | 2008-01-18 | 2010-10-25 | 한화제약주식회사 | Composition Comprising the Extracts of Branch of Lindera obtusiloba for Prevention and Treatment of Cardiovascular Diseases |
| WO2024101208A1 (en) * | 2022-11-07 | 2024-05-16 | サントリーホールディングス株式会社 | Composition for suppressing and/or improving decreased cerebral blood flow, containing quercetin and/or glycoside thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| JPH0615473B2 (en) | 1994-03-02 |
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