JPS61233622A - Eye lotion composition - Google Patents

Eye lotion composition

Info

Publication number
JPS61233622A
JPS61233622A JP7515285A JP7515285A JPS61233622A JP S61233622 A JPS61233622 A JP S61233622A JP 7515285 A JP7515285 A JP 7515285A JP 7515285 A JP7515285 A JP 7515285A JP S61233622 A JPS61233622 A JP S61233622A
Authority
JP
Japan
Prior art keywords
acid
salts
eye
mucopolysaccharide
histidine
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
JP7515285A
Other languages
Japanese (ja)
Other versions
JPS6410500B2 (en
Inventor
Masami Shinohara
篠原 正美
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.)
Riken Vitamin Co Ltd
Original Assignee
Riken Vitamin 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 Riken Vitamin Co Ltd filed Critical Riken Vitamin Co Ltd
Priority to JP7515285A priority Critical patent/JPS61233622A/en
Publication of JPS61233622A publication Critical patent/JPS61233622A/en
Publication of JPS6410500B2 publication Critical patent/JPS6410500B2/ja
Granted legal-status Critical Current

Links

Abstract

PURPOSE:To provide an eye lotion composition effective to prevent the degradation of acid mucopolysaccharide an useful for the remedy of cataract, etc., by compounding a group composed of an acid mucopolysaccharide, ascorbic acid and their salt and a group composed of tryptophan, histidine, uric acid, etc. CONSTITUTION:The objective composition contains (A) 0.01-5 wt% one or more compounds selected from acid mucopolysaccharide, ascorbic acid and their salts and (B) 0.001-1 wt% one or more compounds selected form tryptophan, histidine, uric acid and their salts. The depolymerization of acid mucopolysaccharide can be prevented even in the presence of a depolymerization acceleration factor such as ascorbic acid, metallic ion, etc., by the use of tryptophan, histidine, uric acid and their salts. Accordingly, the composition is effective for the remedy and prevention of eye diseases (e.g. catalact, glaucoma, etc.) caused by the chemical change in the acid mucopolysaccharide in the lens. It can be applied also as a preservation liquid for surgical operation of eye diseases.

Description

【発明の詳細な説明】 [産業上の利用分野] 本発明は新規な眼薬組成物、更に詳しくは酸性ムコ多糖
類、アスコルビン酸またはそれらの塩類の1種または2
種以上とトリプトファン、じスチレン、尿酸またはそれ
らの塩類の1種または2種以上を併用してなる眼薬組成
物に関する。
Detailed Description of the Invention [Industrial Application Field] The present invention provides a novel ophthalmic composition, more specifically, a novel ophthalmic composition containing one or two of acidic mucopolysaccharides, ascorbic acid, or salts thereof.
The present invention relates to an eye drug composition containing one or more of tryptophan, distyrene, uric acid, or salts thereof.

[従来の技術およびその問題点] 哺乳動物の眼水晶体にはヒアルロン酸をはじめとしコン
ドロイチン硫酸、コンドロイチンなどの酸性ムニ]多糖
類が存在し水晶体の形状保持および透明ガラス体形成等
の役割を担っているが、これ等酸性ムコ多糖類とともに
アスコルビン酸もバ存してることが知られている。また
、最近の研究では老人性眼疾患がこね等酸性ムコ多糖類
の化学的変化によると考えられ老化現象の関係が深いこ
とを示しているが、現在その予防方法はほとんどない。
[Prior art and its problems] The mammalian eye lens contains acidic polysaccharides such as hyaluronic acid, chondroitin sulfate, and chondroitin, which play a role in maintaining the shape of the lens and forming a transparent vitreous body. However, it is known that ascorbic acid is present along with these acidic mucopolysaccharides. In addition, recent research has shown that senile eye diseases are thought to be caused by chemical changes in acidic mucopolysaccharides, and are closely related to aging phenomena, but there are currently few methods for preventing them.

ざらに in VitrO研究ではあるが鉄・銅のよう
な生体組織に存在する金属イオンにより酸性ムコ多糖類
の著しい低分子化が確認され(FFBSLETTER8
96,2,238,1978)さらにアスコルビン酸の
添加により低分子化が促進される(JOIIrnal 
of l n0rjlantc  B!0CIIQII
I−istry上4,135 (1981)ことが確認
されている。しかし、正常水晶体においては酸性ムコ多
糖とアスコルビン酸が共存し当然金属イオンも含有する
と思われるが非常に安定に保たれている。
Although this is an in-VitrO study, it has been confirmed that acidic mucopolysaccharides are significantly reduced in molecular weight by metal ions such as iron and copper present in living tissues (FFBSLETTER8).
96, 2, 238, 1978) Furthermore, the addition of ascorbic acid promotes the reduction of molecular weight (JOIIrnal
of l n0rjlantc B! 0CIIQII
I-istry 4, 135 (1981). However, in a normal crystalline lens, acidic mucopolysaccharide and ascorbic acid coexist, and although it is thought that metal ions are also contained, it is kept very stable.

すなわち、第三成分の存在が推察される。In other words, the presence of a third component is inferred.

本発明り等は白内障、緑内障イTどの眼疾患が眼球内に
存在ツノている酸性ムコ多糖うI、アスコルビン酸の代
i’li巽状に」る点を考え、特に水晶体の1丁成分で
ある酸性ムコ多糖類を安定化し眼病の治療およσ予防に
、さらには眼薬どしC使用される酸I11ムコ多糖類で
あるヒアルロン酸、]コンドロイチン]ン1〜[]イデ
シン!IM、デルマタン硫酸、l\バリン、ヘパラン硫
酸、ツノラウン硫酸など、d−3よひ各)(のlルカリ
金属塩の酸化的・光的低ヅ)子化を防用1ノ、すj力持
続性の良い眼薬組成物を提供じ11−常/「眼機能キ1
1持を目的どηるものC゛ある。
The present invention has been developed based on the fact that eye diseases such as cataracts and glaucoma are caused by acidic mucopolysaccharide, which exists in the eyeball, and ascorbic acid, and in particular, it is a component of the crystalline lens. Acid I11 Mucopolysaccharide hyaluronic acid, [chondroitin]1~[]idecine! is used to stabilize certain acidic mucopolysaccharides and to treat eye diseases and prevent σ, and is also used in eye medicines. IM, dermatan sulfate, l\valine, heparan sulfate, tunoraun sulfate, etc., d-3, etc.) Prevents the oxidative and photo-degradation of alkali metal salts and maintains its strength. 11-Continue / "Eye Function Key 1"
There are some people whose purpose is to have one.

[問題点を解決する為の手段] 本ブを明省舌は眼共について検討した結果、アスコルビ
ン酸、全屈イAンなどの低分子化促進因子の(r+f−
F Cし、1〜リブ1ヘフアン、ヒスデシン、尿酸また
はでれらの塩類を」(存せしめることにより、酸I′U
: lx zr多糖類の低分子化が防山できることを見
い出し、本発明を完成した1うのである。
[Means for solving the problem] As a result of examining this topic for the eyes, we found that (r+f-
F C, 1~rib 1 hefan, hisdecine, uric acid or their salts (by containing acid I'U)
: It was discovered that reducing the molecular weight of lx zr polysaccharide can be used for mountain prevention, and the present invention was completed.

本発明の眼Aも組成物IJ耐1リム]多i1J+知、デ
ス。ニー1ルピン酸またljニーfれらの塩類の1種ま
たは2種以上と1−リブトファン、ヒスチジン、SRま
たはそれらの塩類の1種または2種以上をイ)(用J−
ることから4fる。
The eye A of the present invention also has a composition IJ resistance 1 rim] polyi1J+knowledge, death. A) One or more of these salts and one or more of 1-ributophane, histidine, SR, or their salts (a) (for J-
4f from that.

本発明でいう酸性ムコ多糖類とはヒアルロン酸、コンド
ロイチン、コンドロイチン硫酸、デルマタン硫酸、ヘパ
リン、ヘパラン硫酸、グラタン硫酸などおよびこれらの
すI〜リウム、カリウム、カルシウム、アンモニウム、
アミン、アミノMli塩などであり、アスコルビン酸お
よびそのすトリウム、カリウム、カルシウム塩などから
)巽ばれる1種または2種以上0.01〜5重量%の範
囲で配合する。
Acidic mucopolysaccharides as used in the present invention include hyaluronic acid, chondroitin, chondroitin sulfate, dermatan sulfate, heparin, heparan sulfate, gratan sulfate, etc., and these salts, potassium, calcium, ammonium,
Ascorbic acid and its thorium, potassium, calcium salts, etc.) are mixed in an amount of 0.01 to 5% by weight.

0.01重量%以下では目的どJる治療、予防効果が得
られず、5重量%以上は効果と経済性から必要ない。
If the amount is less than 0.01% by weight, the desired therapeutic or preventive effect cannot be obtained, and if it is more than 5% by weight, it is not necessary from the viewpoint of efficacy and economy.

本発明でいう]ヘリプI〜フ77ン、ヒスチジン、尿酸
またはその塩類とは、トリプトファンまたはその塩類と
してはDL−1〜リプ1〜フアン、1−−1〜リプ]へ
ファン及びこれらの塩酸塩、硝酸塩、酢酸塩、硫酸塩を
さし、じスヂジンすたはその塩類どじではL−ヒスチジ
ン及びこれの塩酸塩、硝酸塩、酢MJi、硫酸塩をさし
、尿酸またはその塩類どして1et1、尿酸、尿酸づ]
・リウム、尿酸カリウム、尿酸カルシウム、尿酸水素±
1−リウム、尿酸水素カリウノ1、尿酸水素カルシ1ク
ム、尿酸水素アンモニウム、尿酸アミノ酸塩、尿酸アミ
ン塩などをいい、添加量1110,01〜1.0重量%
であり、0.01巾帛%以十(・は目的どする効甲が得
られず、 1.0重量%以−には溶解性と効果の点で必
要ない。
In the present invention, tryptophan, histidine, uric acid, or its salts include tryptophan or its salts, including DL-1, 1--1, 1--1, and their hydrochlorides. , refers to nitrate, acetate, sulfate, and its salts include L-histidine and its hydrochloride, nitrate, vinegar MJi, and sulfate, and uric acid or its salts refers to 1et1, uric acid, uric acid]
・Rium, potassium urate, calcium urate, hydrogen urate±
1-lium, potassium hydrogen urate 1, calci hydrogen urate 1 cum, ammonium hydrogen urate, uric acid amino acid salt, uric acid amine salt, etc., added in an amount of 1110.01 to 1.0% by weight.
If the content is 0.01% by weight or more, the desired effect cannot be obtained, and if it is less than 1.0% by weight, it is unnecessary in terms of solubility and effectiveness.

まk 、眼薬は浸透1−fを調整するため食塩、リン酸
り一1〜リウムなどの無機inを添加する場合もあるが
本発明組成物には何等影響覆るものではない。
In some cases, inorganic inorganic substances such as common salt and monolithium phosphate are added to eye drops in order to adjust the penetration level 1-f, but this does not affect the composition of the present invention in any way.

なお、本発明組成物の11−1値は4.0〜8.0好ま
し)くけ6.0〜7.Oに維持することが望ましい。
The 11-1 value of the composition of the present invention is preferably 4.0 to 8.0) and 6.0 to 7. It is desirable to maintain it at 0.

p l−1値4.0以下およびpl−1値8.0以上で
は逆に眼組織の変質による刺激が強く眼薬どしでの用を
足さくr < 1.7るばかりか眼組織の炎症を誘発1
.でしまう3、 本発明眼薬組成物(,1白内障、緑内障等の水晶体内酸
11ムコ多糖化学的性質の変化により誘発される1R病
の治療rll;−は眼疾患の治療さらにはT−防子5一 段に使用されるものであるが、角膜移植手術等眼病の外
科手術時の眼組織の保存液または眼組織の形状保持用注
入液にも適用しうる。
On the other hand, when the p l-1 value is less than 4.0 and the p l-1 value is more than 8.0, the irritation caused by the deterioration of the eye tissue is strong enough to make it difficult to use eye medicine. induce inflammation 1
.. 3. The ophthalmic composition of the present invention (1) Treatment of 1R disease induced by changes in intralenticular acid 11 mucopolysaccharide chemical properties such as cataracts and glaucoma; Although the present invention is used in the first stage, it can also be applied as an eye tissue preservation solution or an injection solution for maintaining the shape of eye tissue during eye disease surgery such as corneal transplant surgery.

以下本発明服薬組成物について実施例、実験例で説明す
る。
The pharmaceutical composition of the present invention will be explained below using Examples and Experimental Examples.

実施例1.白内障防止眼薬 ヒアルロン酸ナトリウlx      0.05重量%
コンドロイチン硫酸す1ヘリウム 0 、5Onトリプ
トファン塩酸塩      0.02  〃塩化すI〜
リウム        2. Q   n滅菌精製水 
         97.43  、。
Example 1. Cataract prevention eye medicine sodium hyaluronate lx 0.05% by weight
Chondroitin sulfate 1 helium 0, 5 On tryptophan hydrochloride 0.02 Chloride I~
Rium 2. QnSterilized purified water
97.43,.

実施例2.健康美眼剤 塩酸ナファゾリン       0.1  重量%]コ
ンドロイチン硫酸1ヘリウム i、o   、。
Example 2. Healthy eye beauty agent Naphazoline hydrochloride 0.1% by weight] Chondroitin sulfate 1 helium i,o.

尿酸ナトリウム         0.1   、。Sodium urate 0.1.

サロメチール          0.2〃塩化ナトリ
ウム         2,0  .1滅菌精製水  
        96,6   、J実施例30手術用
角膜乾燥防市剤 ヒアルロン酸ナトリウム     0.3  重量%塩
化プ1〜リウム        5.OI!j話化カリ
ウム         2.0!・リン酸水水−ノトリ
ウム      0,1   nホウ酸       
      0.3   ・11p酎 ツノ リ ウ 
11                    0,0
3     ノIアス]ルピン酸ブー 1−リウム  
  0.2/I滅菌精製水          92.
1!!実施例4.=]ンタクトレンズ用点眼剤ヒフ))
し[1ン酸カリウム      0.・2  重石%1
−−ヒスチジン塩酸塩      0.111アス]ル
l:゛ン酸−ノトリ1クム    0.11Ilp化す
1〜リウム        2,0   !!滅菌精製
水          !117.6   !l実験例
1 年齢23へ・50才の事務を業とし目の疲れを毎日又は
時々感する人25人、うち女fIJ6、男性19人に実
施例2の1梨を1日3回1〜2滴使用し水剤使用前と使
用後の眼疲労感および充血性を調べ Iこ 。
Salomethyl 0.2 Sodium chloride 2.0. 1 Sterile purified water
96,6, J Example 30 Surgical corneal drying preventive agent Sodium hyaluronate 0.3% by weight Pr1-Rium chloride 5. OI! J talk potassium 2.0!・Phosphoric acid water - Notorium 0,1 n boric acid
0.3 ・11p Shochu Tsuno Riu
11 0,0
3 NoIas] 1-rium lupine acid
0.2/I sterile purified water 92.
1! ! Example 4. =] Eye drops for contact lenses Hif))
[Potassium monophosphate 0.・2 Weight%1
--Histidine hydrochloride 0.111 As]l: 1 cum of dinic acid 0.11Ilp 1~Rium 2,0! ! Sterile purified water! 117.6! l Experimental Example 1 Age 23 - 25 50-year-olds who work in office work and experience eye strain every day or occasionally, including 6 women and 19 men, were given 1 pear of Example 2 1 to 2 times a day. Eye fatigue and hyperemia were investigated using drops before and after using the solution.

本発明品は眼疲労及び充血に対して著しい効宋を示した
The product of the present invention showed remarkable effects on eye fatigue and hyperemia.

実験例2 実施例3にて調整した水溶液にラット眼球を摘出後直ち
に浸漬し眼球の鮮度および色調を調べた。
Experimental Example 2 Immediately after enucleating rat eyeballs, they were immersed in the aqueous solution prepared in Example 3, and the freshness and color tone of the eyeballs were examined.

なお湿度は5°Cにてpl−16,7に調整して行った
The humidity was adjusted to pl-16.7 at 5°C.

比較例1とは実施例3よりヒアルロン酸ナトリウム、尿
酸す1ヘリウムを除いた調整液。
Comparative Example 1 is a prepared solution obtained by removing sodium hyaluronate, uric acid, and helium from Example 3.

比較例2とは実施例3より尿酸す]〜リウムを除いた調
整液。
Comparative Example 2 is a prepared solution obtained by removing uric acid from Example 3.

たたし表中数字は摘出直後のラン1〜眼球にほぼ同じ色
調を保っていた個体数を表わす。
The numbers in the table represent the number of individuals whose eyeballs had almost the same color tone from run 1 immediately after extraction.

本発明品は48時間後でも色調が良好に保てたがヒアル
ロン酸す1〜リウムと尿酸ナトリウムを除いた比較例1
及び尿酸ナトリウムを除いた比較例2は1!い1fい8
時間稈度しか保存できなかった。
Although the product of the present invention maintained good color tone even after 48 hours, Comparative Example 1 in which mono-lium hyaluronic acid and sodium urate were excluded
And Comparative Example 2 excluding sodium urate was 1! i1f i8
Only time culm could be saved.

Claims (1)

【特許請求の範囲】[Claims] 酸性ムコ多糖類、アスコルビン酸またはそれらの塩類か
ら選ばれる1種または2種以上0.01〜5重量%およ
びトリプトファン、ヒスチジン、尿酸またはそれらの塩
類から選ばれる1種または2種以上0.001〜1重量
%を含有してなる眼薬組成物。
0.01 to 5% by weight of one or more selected from acidic mucopolysaccharides, ascorbic acid, or their salts, and 0.001 to 5% by weight of one or more selected from tryptophan, histidine, uric acid, or their salts. An eye drug composition containing 1% by weight.
JP7515285A 1985-04-09 1985-04-09 Eye lotion composition Granted JPS61233622A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP7515285A JPS61233622A (en) 1985-04-09 1985-04-09 Eye lotion composition

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP7515285A JPS61233622A (en) 1985-04-09 1985-04-09 Eye lotion composition

Publications (2)

Publication Number Publication Date
JPS61233622A true JPS61233622A (en) 1986-10-17
JPS6410500B2 JPS6410500B2 (en) 1989-02-22

Family

ID=13567943

Family Applications (1)

Application Number Title Priority Date Filing Date
JP7515285A Granted JPS61233622A (en) 1985-04-09 1985-04-09 Eye lotion composition

Country Status (1)

Country Link
JP (1) JPS61233622A (en)

Cited By (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1989000044A1 (en) * 1987-07-07 1989-01-12 Santen Pharmaceutical Co., Ltd. Artificial lacrima
JPH01294633A (en) * 1988-05-23 1989-11-28 Fujisawa Pharmaceut Co Ltd Ophthalmic solution
EP0735895A1 (en) * 1993-11-19 1996-10-09 The University Of Sydney A method for preventing or controlling cataract
US5614506A (en) * 1991-07-03 1997-03-25 Hyal Pharmaceutical Corporation Use of hyaluronic acid and forms to prevent arterial restenosis
US5811410A (en) * 1989-09-21 1998-09-22 Hyal Pharmaceutical Corporation Method of administering of a hyaluronic acid and an NSAID to decrease side effects of the NSAID
US5817644A (en) * 1991-07-03 1998-10-06 Hyal Pharmaceutical Corporation Targeting of dosages of medicine and therapeutic agents
GR970100233A (en) * 1997-06-09 1999-02-26 Use of organic, anti-oxidant substances for the protection of the lungs, the skin and the eyes from free radicals
US5942498A (en) * 1992-02-20 1999-08-24 Hyal Pharmaceutical Corporation Formulations containing hyaluronic acid
US5990095A (en) * 1991-07-03 1999-11-23 Hyal Pharmaceutical Corporation Use of hyaluronic acid and forms to prevent arterial restenosis
US6022866A (en) * 1991-07-03 2000-02-08 Hyal Pharmaceutical Corporation Use of hyaluronic acid and forms to prevent arterial restenosis
WO2001006868A1 (en) * 1999-07-28 2001-02-01 Biomar Group Feed for salmonids
WO2008050776A1 (en) 2006-10-26 2008-05-02 Senju Pharmaceutical Co., Ltd. Ophthalmic aqeous liquid preparation
JP2010180206A (en) * 2009-01-09 2010-08-19 Rohto Pharmaceut Co Ltd Method for inhibiting discoloration of composition for external use containing diphenhydramine or salt thereof and ascorbic acid or salt thereof
JP2011030455A (en) * 2009-07-30 2011-02-17 Uha Mikakuto Co Ltd Food material containing tryptophan-hyaluronic acid and food material containing peptide with high tryptophan-content and hyaluronic acid and methods for producing the same

Cited By (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1989000044A1 (en) * 1987-07-07 1989-01-12 Santen Pharmaceutical Co., Ltd. Artificial lacrima
JPH01294633A (en) * 1988-05-23 1989-11-28 Fujisawa Pharmaceut Co Ltd Ophthalmic solution
US6069135A (en) * 1989-09-21 2000-05-30 Hyal Pharmaceutical Corporation Use of hyaluronic acid or its derivatives to enhance delivery of therapeutic agents
US6194392B1 (en) 1989-09-21 2001-02-27 Hyal Pharmaceutical Corporation Treatment of conditions and disease
US5985850A (en) * 1989-09-21 1999-11-16 Hyal Pharmaceuticals Corporation Compositions comprising hyaluronic acid and drugs
US6048844A (en) * 1989-09-21 2000-04-11 Hyal Pharmaceutical Corporation Treatment of conditions and disease
US5914314A (en) * 1989-09-21 1999-06-22 Hyal Pharmaceutical Corporation Use of a form of hyaluronic acid and a medicinal agent for reducing rejection of organs transplantation in mammals
US5852002A (en) * 1989-09-21 1998-12-22 Hyal Pharmaceutical Corporation Treatment of conditions and disease
US5830882A (en) * 1989-09-21 1998-11-03 Hyal Pharmaceutical Corporation Compositions containing a form of hyaluronic acid and a medicinal agent for treating acne in mammals and methods for administration of such composition
US5811410A (en) * 1989-09-21 1998-09-22 Hyal Pharmaceutical Corporation Method of administering of a hyaluronic acid and an NSAID to decrease side effects of the NSAID
US5929048A (en) * 1989-09-21 1999-07-27 Hyal Pharmaceutical Corporation Treatment of conditions and disease
US5932560A (en) * 1989-09-21 1999-08-03 Hyal Pharmaceutical Corporation Treatment of conditions and disease
US5985851A (en) * 1989-09-21 1999-11-16 Hyal Pharmaceutical Corporation Use of hyaluronic acid or its derivatives in peritoneal dialysis and formulations thereof
US5614506A (en) * 1991-07-03 1997-03-25 Hyal Pharmaceutical Corporation Use of hyaluronic acid and forms to prevent arterial restenosis
US6022866A (en) * 1991-07-03 2000-02-08 Hyal Pharmaceutical Corporation Use of hyaluronic acid and forms to prevent arterial restenosis
US5990095A (en) * 1991-07-03 1999-11-23 Hyal Pharmaceutical Corporation Use of hyaluronic acid and forms to prevent arterial restenosis
US5817644A (en) * 1991-07-03 1998-10-06 Hyal Pharmaceutical Corporation Targeting of dosages of medicine and therapeutic agents
US6147059A (en) * 1992-02-20 2000-11-14 Hyal Pharmaceutical Corporation Formulations containing hyaluronic acid
US5942498A (en) * 1992-02-20 1999-08-24 Hyal Pharmaceutical Corporation Formulations containing hyaluronic acid
EP0735895A4 (en) * 1993-11-19 2001-03-28 Univ Sydney A method for preventing or controlling cataract
EP0735895A1 (en) * 1993-11-19 1996-10-09 The University Of Sydney A method for preventing or controlling cataract
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