JPS63170319A - Anticataractous agent - Google Patents

Anticataractous agent

Info

Publication number
JPS63170319A
JPS63170319A JP62001365A JP136587A JPS63170319A JP S63170319 A JPS63170319 A JP S63170319A JP 62001365 A JP62001365 A JP 62001365A JP 136587 A JP136587 A JP 136587A JP S63170319 A JPS63170319 A JP S63170319A
Authority
JP
Japan
Prior art keywords
tannin
agent
anticataractous
glucopyranose
cataract
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
JP62001365A
Other languages
Japanese (ja)
Other versions
JPH0623111B2 (en
Inventor
Shuzo Iwata
岩田 修造
Takuo Okuda
奥田 拓男
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.)
Santen Pharmaceutical Co Ltd
Original Assignee
Santen Pharmaceutical 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 Santen Pharmaceutical Co Ltd filed Critical Santen Pharmaceutical Co Ltd
Priority to JP62001365A priority Critical patent/JPH0623111B2/en
Publication of JPS63170319A publication Critical patent/JPS63170319A/en
Publication of JPH0623111B2 publication Critical patent/JPH0623111B2/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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  • Saccharide Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)

Abstract

PURPOSE:To obtain an anticataractous agent, containing tannin or tannin ingredient, having excellent peroxylipid removing effects and capable of delaying opacification of crystalline lenses. CONSTITUTION:An anticataractous agent obtained by containing tannin or tannin ingredient, preferably hydrolyzable tannin, e.g. penta-O-galloyl-beta-D- glucopyranose, as an active ingredient. Internal use, instillation, etc., are cited as the administration form. The dose thereof is 10-1,000mg divided in several portions a day for internal use and eye drop or ointment in 0.01-5% concentration is administered several times a day for instillation.

Description

【発明の詳細な説明】 「産業上の利用分野」 本発明はタンニンまたはタンニン成分を主成分とする抗
白内障剤に関する。
DETAILED DESCRIPTION OF THE INVENTION "Field of Industrial Application" The present invention relates to an anti-cataract agent containing tannin or a tannin component as a main component.

「従来技術」 タンニンFi植物中に広(分布し、そのg分については
数多くの研究がなされている。またその用途としては、
ナメシ剤としての用途が古(から知らハているが、近年
その抗酸化作用が注目され種々の研究がなされている。
``Prior art'' Tannin Fi is widely distributed in plants, and many studies have been conducted on its g content.
Although it has been known since ancient times for its use as a sedative, its antioxidant effects have recently attracted attention and various studies have been conducted.

本発明者等は水晶体の酸化障害に対する各種タンニン成
分の抗酸化作用及び作用機序について研究し優′rLf
c過酸化脂質除去効果がある事を報告し、ている(あた
らし、い眼科 第2巻1293〜1296頁、同第3巻
254〜257頁、他)。
The present inventors researched the antioxidant effects and mechanisms of action of various tannin components on oxidative damage to the crystalline lens, and
It has been reported that it has a lipid peroxide removal effect (Atarashi, Ii Ophthalmology Vol. 2, pp. 1293-1296, Vol. 3, pp. 254-257, etc.).

「発明が解決しようとする問題点および問題を解決する
為の手段」 タンニン成分が抗酸化作用を有し優れた過歌化脂質除去
効果があるJ%が見い比されていふ、しかしながら、タ
ンニン成分が医薬、特に抗白内障剤とし、て利用できる
か否かについての直接的な知見はなく、その研究をする
必要があった。本発明者等はタンニン成分を動物に投与
し、白内障に対する効果tl−調べfC。
"Problems to be Solved by the Invention and Means for Solving the Problems" J%, whose tannin component has an antioxidant effect and has an excellent effect of removing hyperactive lipids, has been compared. There was no direct knowledge as to whether the ingredient could be used as a medicine, especially as an anti-cataract agent, and it was necessary to conduct research. The present inventors administered tannin components to animals and investigated the effect on cataracts.

「発明の開示」 タンニンは天然m物中に広く分布し、て層るポリフェノ
ール誘導体で、その成分につ力て様々研究がなされ、低
分子量ポリフェノール、@d合型タンニン、7IO水分
解性タンニンに大別される。タンニンのナメシ剤として
の用途は古くから知られているが、近年その各種成分に
ついての研究がなされている。本発明者等はタンニン成
分が優れた過酸化脂質除去効果があふ−Jを見す出し、
さらに医薬としての用途を鋭意研究した結果抗白内障剤
として有j目である$全見込量した。タンニンには各徨
成分があるが、その内でも原水分解性タンニンに優れた
効果がみられた。白内障は水晶体が混濁して起る病気で
、混濁した水晶体全敗り田り、眼内レンズ全挿入する方
法)がとらnている。白内障の病因については種々研究
さ几ているが、白内障に対する冷涼効果を判定するのに
、水晶体の混濁程度を測定するのが最も直接的な方法と
なる。後述の薬理試験の項で詳述すbが、刃口水分解性
タンニンの一種であるペンタ−0−ガロイル−β−D 
−グルコピラノースを遺伝性白内障マウスに投与した所
、水晶体の混濁発現が遅延し、抗白内障剤として有用で
ある事を見い出L5た。
"Disclosure of the Invention" Tannins are polyphenol derivatives that are widely distributed and layered in natural products, and various studies have been conducted on their components. Broadly classified. The use of tannin as a smearing agent has been known for a long time, but in recent years, research has been conducted on its various components. The present inventors have discovered Afu-J, which has an excellent tannin component and has an excellent lipid peroxide removal effect,
Furthermore, as a result of intensive research into its use as a medicinal agent, it was estimated that it would be used as an anti-cataract agent. Tannins have various toxic components, but among them, raw water-degradable tannins were found to have excellent effects. Cataract is a disease caused by the clouding of the crystalline lens, and the method of treatment is to remove the entire clouded lens and insert the entire intraocular lens. Although various studies have been conducted on the etiology of cataracts, the most direct method for determining the cooling effect on cataracts is to measure the degree of opacity of the crystalline lens. b, which will be explained in detail in the pharmacological test section below, is penta-0-galoyl-β-D, which is a type of water-degradable tannin at the cutting edge.
- It was discovered that when glucopyranose was administered to mice with inherited cataracts, the onset of clouding of the crystalline lens was delayed, making it useful as an anti-cataract agent.

タンニン成分としては、ペンタ−0−ガロイル−β−D
−グルコピラノース、ゲラニインで代表される加水分解
性タンニンが好ブし論が、710水分解性タンニンを特
に単離する必要はなく、他の成分と混合したままで投与
してもよい。投与形態としては内服2点眼等が挙げられ
、剤型としては錠剤、散剤、頌粒剤、刀ブセル剤9点眼
液、眼軟膏等が挙げられ、そA(’几の剤型に工6じて
医薬として計容1f′Lる賦形剤、溶解剤、軟a基剤等
を用層る事ができる。投与量につhては特に限定する必
要はなく9年令、症状等により適宜選択できるが。
As a tannin component, penta-0-galoyl-β-D
- Hydrolyzable tannins such as glucopyranose and geraniin are preferred, but it is not necessary to specifically isolate 710 hydrolyzable tannins, and they may be administered as they are mixed with other ingredients. Administrative forms include oral 2-eye drops, etc., and dosage forms include tablets, powders, granules, ophthalmic solutions, eye ointments, etc. Excipients, solubilizers, soft bases, etc. with a total volume of 1f'L can be used as medicines.The dosage does not need to be particularly limited, and can be administered as appropriate depending on the age of 9 years, symptoms, etc. You can choose.

通常内服の場合は1日JO〜1000■を数回に分は投
与り122点眼場合は0.01〜5%一度の浴剤または
軟−l:iを1日数回投与する。
In the case of oral administration, JO ~ 1000 ml is administered several times a day, and in the case of eye drops, 0.01 to 5% bath salt or soft-l:i is administered several times a day.

加水分解性タンニンの一例トして、ペンター0−カロイ
ルーβ−D−グルコピラノースヲ用いた薬坤試験例及び
製剤fllを以下の実施例に示すが。
As an example of a hydrolyzable tannin, a drug test example and a formulation using penta-0-caloyl-β-D-glucopyranose are shown in the following examples.

本発明は実施例に限定さ才するものではない。The present invention is not limited to the examples.

「実施例−1 1、薬理試験 生後14日口の遺伝性白内障マウス(25匹)ニ0.1
%(重量%)の割合でペンタ−0−ガロイル−β−D−
グルコピラノースを餌に混合して連日与えた所、水晶体
の混濁は生後21.18±2.12日才で認められなか
った。
"Example-1 1. Pharmacological test 14 days old hereditary cataract mice (25 mice) 0.1
% (wt%) of penta-0-galoyl-β-D-
When glucopyranose was mixed with the food and given daily, no clouding of the crystalline lens was observed at the age of 21.18±2.12 days.

−1対照群とり、てペンター0−ガロイル−β−D−グ
ルコピラノース無投与の遺伝性白内障マウス(1]5匹
)の混濁を観察した所、 2 (1,(1±1.86日
に水晶体の混濁が餡められた。
2 (1, (1±1.86 days The opacity of the crystalline lens has become thicker.

上記の結果はベンターO−ガロイル−β−り一グルコビ
ラノースの効果を示し、ている。このマウスでの結果を
、マウスとヒトとの寿命の差を考慮しヒトに外挿すると
、約1.5ケ月混濁を遅延させることになる。マウスで
は遺伝性白内障が非常に短期間に進行するのに対し、老
人性ヒト白内障ではその進行が緩慢である$全考慮する
と、ペンタ−O−ガロイルーβ−D−グルコピラノース
のヒト白内障に対する効果はさらに大きいものと考えら
几る。
The above results demonstrate the effect of venter O-galoyl-β-ri-glucobylanose. If this result in mice is extrapolated to humans, taking into account the difference in lifespan between mice and humans, it will delay opacification by about 1.5 months. In mice, hereditary cataracts progress in a very short period of time, whereas in senile human cataracts, the progression is slow. I thought it was something even bigger.

2、製剤例 1)ベンターO−ガロイルーβ−D−グルコピラノース
、ポリビニルピロリドン、乳糖、結晶セルロースおよび
カルボキシメチルセルロースカルシウムを混合し、常法
により顆粒とした後、ステアリン隙マグネシウムヲ加え
打錠し下記処方の錠剤を得た。
2. Formulation Example 1) Venter O-galloyrou β-D-glucopyranose, polyvinylpyrrolidone, lactose, crystalline cellulose and carboxymethyl cellulose calcium were mixed and made into granules by a conventional method, and then stearin gap magnesium was added and tableted to obtain the following formulation. tablets were obtained.

ペンタ−O−ガロイル−β−D−グルコピラノース10
0■ ポリビニルピロリドン         20■乳  
、糖                       
161Rg結晶セルロース           92
■カルポキンメチルセルロースカルシクム      
20■計                  250
■上記錠剤は通常のフィルムコーティングをしてもよく
、さらに糖衣)f4をコーティングしてもよ論。
Penta-O-galoyl-β-D-glucopyranose 10
0 ■ Polyvinylpyrrolidone 20 ■ Milk
,sugar
161Rg crystalline cellulose 92
■Carpoquin Methylcellulose Calcicum
20 ■Total 250
■The above tablets may be coated with a regular film, or even coated with sugar coating) f4.

2)ペンタ−0−40イル−β−D−グルコピラノース
、ボリンルベート80.塩化ナトリウムおよび塩化ペン
ザルコニワムを用い下記処方の点眼剤を得た。
2) Pent-0-40yl-β-D-glucopyranose, borine rubate 80. Eye drops having the following formulation were obtained using sodium chloride and penzalkoniwam chloride.

ペンタ−O−ガロイル−β−D−グルコピラノース10
00q 塩化ナトリウム          9(10”9ポリ
ソルベート8(120011P 塩化ベンザルコニウム         5m51精製
水               適量針      
             1 (10t/「発明の効
果」 タンニンまたはタンニン成分を白内障治療剤として使用
することにより、水晶体の混濁を遅延させるという効果
を有するものであり、タンニンまたはタンニン成分は抗
白内障剤として有用なものである。
Penta-O-galoyl-β-D-glucopyranose 10
00q Sodium chloride 9 (10”9 Polysorbate 8 (120011P Benzalkonium chloride 5m51 Purified water Appropriate amount Needle
1 (10t/"Effects of the Invention") Tannins or tannin components used as a cataract therapeutic agent have the effect of delaying clouding of the crystalline lens, and tannins or tannin components are useful as anti-cataract agents. be.

Claims (3)

【特許請求の範囲】[Claims] (1)タンニンまたはタンニン成分を主成分とする抗白
内障剤。
(1) Anti-cataract agents whose main ingredients are tannins or tannin components.
(2)タンニン成分が加水分解性タンニンである特許請
求の範囲第1項記載の抗白内障剤。
(2) The anti-cataract agent according to claim 1, wherein the tannin component is a hydrolyzable tannin.
(3)タンニン成分がペンタ−O−ガロイル−β−D−
グルコピラノースである特許請求の範囲第1項記載の抗
白内障剤。
(3) Tannin component is penta-O-galoyl-β-D-
The anti-cataract agent according to claim 1, which is glucopyranose.
JP62001365A 1987-01-07 1987-01-07 Anti-cataract agent Expired - Lifetime JPH0623111B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP62001365A JPH0623111B2 (en) 1987-01-07 1987-01-07 Anti-cataract agent

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP62001365A JPH0623111B2 (en) 1987-01-07 1987-01-07 Anti-cataract agent

Publications (2)

Publication Number Publication Date
JPS63170319A true JPS63170319A (en) 1988-07-14
JPH0623111B2 JPH0623111B2 (en) 1994-03-30

Family

ID=11499470

Family Applications (1)

Application Number Title Priority Date Filing Date
JP62001365A Expired - Lifetime JPH0623111B2 (en) 1987-01-07 1987-01-07 Anti-cataract agent

Country Status (1)

Country Link
JP (1) JPH0623111B2 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100588830B1 (en) 2004-09-01 2006-06-14 한불화장품주식회사 A cosmetic composition for anti-aging containing an extract of melothria heterophylla

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100588830B1 (en) 2004-09-01 2006-06-14 한불화장품주식회사 A cosmetic composition for anti-aging containing an extract of melothria heterophylla

Also Published As

Publication number Publication date
JPH0623111B2 (en) 1994-03-30

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