JPH0245420A - Anti-cataract eye drop - Google Patents
Anti-cataract eye dropInfo
- Publication number
- JPH0245420A JPH0245420A JP63196378A JP19637888A JPH0245420A JP H0245420 A JPH0245420 A JP H0245420A JP 63196378 A JP63196378 A JP 63196378A JP 19637888 A JP19637888 A JP 19637888A JP H0245420 A JPH0245420 A JP H0245420A
- Authority
- JP
- Japan
- Prior art keywords
- glutathione
- eye drop
- crystalline lens
- type glutathione
- reduced glutathione
- 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
- 239000003889 eye drop Substances 0.000 title claims abstract description 23
- 230000001437 anti-cataract Effects 0.000 title claims abstract description 6
- 150000003839 salts Chemical class 0.000 claims abstract description 10
- 108010053070 Glutathione Disulfide Proteins 0.000 claims description 18
- YPZRWBKMTBYPTK-BJDJZHNGSA-N glutathione disulfide Chemical compound OC(=O)[C@@H](N)CCC(=O)N[C@H](C(=O)NCC(O)=O)CSSC[C@@H](C(=O)NCC(O)=O)NC(=O)CC[C@H](N)C(O)=O YPZRWBKMTBYPTK-BJDJZHNGSA-N 0.000 claims description 18
- YPZRWBKMTBYPTK-UHFFFAOYSA-N oxidized gamma-L-glutamyl-L-cysteinylglycine Natural products OC(=O)C(N)CCC(=O)NC(C(=O)NCC(O)=O)CSSCC(C(=O)NCC(O)=O)NC(=O)CCC(N)C(O)=O YPZRWBKMTBYPTK-UHFFFAOYSA-N 0.000 claims description 18
- 229940012356 eye drops Drugs 0.000 claims description 15
- 239000002075 main ingredient Substances 0.000 claims description 3
- RWSXRVCMGQZWBV-WDSKDSINSA-N glutathione Chemical compound OC(=O)[C@@H](N)CCC(=O)N[C@@H](CS)C(=O)NCC(O)=O RWSXRVCMGQZWBV-WDSKDSINSA-N 0.000 abstract description 45
- 108010024636 Glutathione Proteins 0.000 abstract description 34
- 210000000695 crystalline len Anatomy 0.000 abstract description 26
- 229960003180 glutathione Drugs 0.000 abstract description 11
- 230000003647 oxidation Effects 0.000 abstract description 4
- 238000007254 oxidation reaction Methods 0.000 abstract description 4
- 229910052708 sodium Inorganic materials 0.000 abstract description 4
- -1 amine salt Chemical class 0.000 abstract description 3
- 108010063907 Glutathione Reductase Proteins 0.000 abstract description 2
- 102100036442 Glutathione reductase, mitochondrial Human genes 0.000 abstract description 2
- 229910052791 calcium Inorganic materials 0.000 abstract description 2
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 15
- 208000002177 Cataract Diseases 0.000 description 7
- 230000007423 decrease Effects 0.000 description 7
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 6
- 238000009472 formulation Methods 0.000 description 5
- 238000000034 method Methods 0.000 description 5
- 239000000203 mixture Substances 0.000 description 5
- 239000007864 aqueous solution Substances 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 229960000686 benzalkonium chloride Drugs 0.000 description 3
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- 239000008213 purified water Substances 0.000 description 3
- 239000011734 sodium Substances 0.000 description 3
- 239000011780 sodium chloride Substances 0.000 description 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 2
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 description 2
- 229960002684 aminocaproic acid Drugs 0.000 description 2
- 229940124428 anticataract agent Drugs 0.000 description 2
- OSASVXMJTNOKOY-UHFFFAOYSA-N chlorobutanol Chemical compound CC(C)(O)C(Cl)(Cl)Cl OSASVXMJTNOKOY-UHFFFAOYSA-N 0.000 description 2
- 239000003885 eye ointment Substances 0.000 description 2
- 239000008103 glucose Substances 0.000 description 2
- 239000008187 granular material Substances 0.000 description 2
- 229940057995 liquid paraffin Drugs 0.000 description 2
- 230000004792 oxidative damage Effects 0.000 description 2
- 230000000144 pharmacologic effect Effects 0.000 description 2
- 239000001632 sodium acetate Substances 0.000 description 2
- 235000017281 sodium acetate Nutrition 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 238000013112 stability test Methods 0.000 description 2
- 239000003381 stabilizer Substances 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- 229940124597 therapeutic agent Drugs 0.000 description 2
- SLXKOJJOQWFEFD-UHFFFAOYSA-N 6-aminohexanoic acid Chemical compound NCCCCCC(O)=O SLXKOJJOQWFEFD-UHFFFAOYSA-N 0.000 description 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 description 1
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 description 1
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerol Natural products OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 1
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 0.000 description 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
- 241000700159 Rattus Species 0.000 description 1
- 241000700157 Rattus norvegicus Species 0.000 description 1
- VMHLLURERBWHNL-UHFFFAOYSA-M Sodium acetate Chemical compound [Na+].CC([O-])=O VMHLLURERBWHNL-UHFFFAOYSA-M 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 229960004926 chlorobutanol Drugs 0.000 description 1
- 238000007872 degassing Methods 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 229940009662 edetate Drugs 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 208000030533 eye disease Diseases 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 238000011534 incubation Methods 0.000 description 1
- 239000011777 magnesium Substances 0.000 description 1
- 229910052749 magnesium Inorganic materials 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 229910052751 metal Inorganic materials 0.000 description 1
- 239000002184 metal Substances 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 230000011164 ossification Effects 0.000 description 1
- 239000007800 oxidant agent Substances 0.000 description 1
- 230000001590 oxidative effect Effects 0.000 description 1
- 239000003002 pH adjusting agent Substances 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
- 235000019271 petrolatum Nutrition 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 239000001103 potassium chloride Substances 0.000 description 1
- 235000011164 potassium chloride Nutrition 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 229960002668 sodium chloride Drugs 0.000 description 1
- 229940037001 sodium edetate Drugs 0.000 description 1
- 239000001488 sodium phosphate Substances 0.000 description 1
- 229910000162 sodium phosphate Inorganic materials 0.000 description 1
- FAPWRFPIFSIZLT-HCMAANCNSA-M sodium-22(1+);chloride Chemical compound [22Na+].[Cl-] FAPWRFPIFSIZLT-HCMAANCNSA-M 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- 239000003871 white petrolatum Substances 0.000 description 1
Landscapes
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
【発明の詳細な説明】
「産業上の利用分野」
本発明は酸化型グルタチオンまたはその塩類を主成分と
する抗白内障点眼剤に関する。DETAILED DESCRIPTION OF THE INVENTION "Industrial Application Field" The present invention relates to an anti-cataract eye drop containing oxidized glutathione or its salts as a main ingredient.
「従来技術、発明が解決しようとする課題および課題を
解決するための手段」
白内障は眼の水晶体が混濁する難治性の眼疾患の一つで
ある。白内障の患者では水晶体中の還元型グルタチオン
量の減少が報告されているが（代ｍ１７，２１７３（１
９８０））、これは還元型グルタチオンの減少に伴ない
、酸化障害に対する防護能力が低下するため、水晶体が
混濁するものと考えられている（水晶体その生化学的機
構 岩田修造編著 メディカル葵出版）。"Prior Art, Problems to be Solved by the Invention, and Means for Solving the Problems" Cataract is one of the intractable eye diseases in which the crystalline lens of the eye becomes cloudy. It has been reported that the amount of reduced glutathione in the crystalline lens decreases in patients with cataracts (1997, 2173,
980)), and this is thought to be due to a decrease in the protective ability against oxidative damage due to a decrease in reduced glutathione, resulting in clouding of the crystalline lens (Biochemical Mechanism of the Lens, edited by Shuzo Iwata, Medical Aoi Publishing).
このため還元型グルタチオンの点眼剤が抗白内障剤とし
て用いられている。For this reason, reduced glutathione eye drops are used as an anti-cataract agent.
ところが、還元型グルタチオンは製剤中での安定性が悪
く、点眼剤では使用時に還元型グルタチオンの錠剤や顆
粒を溶解して用いなければならなかった。However, reduced glutathione has poor stability in formulations, and reduced glutathione tablets or granules must be dissolved before use in eye drops.
そこで本発明者らは安定性に優れ、かつ水晶体中の還元
型グルタチオンｔを増加させる方法を鋭意検討した。Therefore, the present inventors have intensively investigated a method that has excellent stability and increases reduced glutathione t in the crystalline lens.
「発明の開示」
本発明は酸化型グルタチオンまたはその塩類を主成分と
する抗白内障点眼剤に関する。上記の塩としては医薬と
して許容されるものであればよく、例えばナトリウム、
カリウム、カルシウム、マグネシウムなどの金属塩や有
機アミン塩などが含まれる。"Disclosure of the Invention" The present invention relates to an anti-cataract eye drop containing oxidized glutathione or its salts as a main ingredient. The above salts may be any pharmaceutically acceptable salts, such as sodium,
Contains metal salts such as potassium, calcium, and magnesium, and organic amine salts.
還元量グルタチオンは水晶体において透明性の維持に重
要な役割をしており、例えば水晶体中の還元型グルタチ
オンが減少すると酸化障害に対する防護能力が低下し、
その結果水晶体が混濁化し白内障が生じると考えられて
いる。このことから還元型グルタチオンの点眼剤が白内
障の治療剤として用いられている。ところが還元型グル
タチオンは製剤中での安定性が悪いことから、点眼剤で
はその使用時に還元型グルタチオンの錠剤や顆粒を溶解
しなければならなかった。Reduced amount Glutathione plays an important role in maintaining transparency in the crystalline lens. For example, when reduced glutathione in the lens decreases, the ability to protect against oxidative damage decreases.
It is thought that as a result, the lens becomes cloudy and cataracts occur. For this reason, reduced glutathione eye drops are used as a therapeutic agent for cataracts. However, since reduced glutathione has poor stability in formulations, reduced glutathione tablets or granules must be dissolved before use in eye drops.
そこで本発明者らは安定性に優れ、かつ水晶体の還元型
グルタチオン量を増加させる方法について鋭意検討した
。その結果、酸化型グルタチオンまたはその塩類（以下
特記なき限り酸化型グルタチオンと総称する）を用いる
ことにより、上記の条件を満たした優れた抗白内障治療
剤となることを見い出した。Therefore, the present inventors have intensively investigated a method that has excellent stability and increases the amount of reduced glutathione in the crystalline lens. As a result, it has been found that by using oxidized glutathione or its salts (hereinafter collectively referred to as oxidized glutathione unless otherwise specified), an excellent anti-cataract therapeutic agent that satisfies the above conditions can be obtained.
本発明の点眼剤は安定性試験の項で述べるように非常に
安定であり、還元型グルタチオンの水溶液が室温１ケ月
で残存率が約９０％であるのに対して、同じ条件ではほ
とんど残存率の低下は認められなかった。又、本発明の
点眼剤を投与すると水晶体内のグルタチオン還元酵素の
作用によ多酸化型グルタチオンが還元型グルタチオンと
変化し水晶体中の還元型グルタチオンの量が増大するこ
とを見い出し本発明の目的を完成させた。（薬理試験の
項参照）
本発明点眼剤の酸化屋グルタチオンの濃度はその効果が
発揮できるものであればよく、０．５〜５チのものが好
ましいが、症状、年令などにより適宜選択すればよい。The eye drops of the present invention are extremely stable, as described in the stability test section, and while an aqueous solution of reduced glutathione has a residual rate of about 90% at room temperature for one month, the residual rate is almost 90% under the same conditions. No decrease was observed. It was also discovered that when the eye drops of the present invention are administered, polyoxidized glutathione is converted to reduced glutathione by the action of glutathione reductase in the crystalline lens, and the amount of reduced glutathione in the crystalline lens increases. Completed. (Refer to the section on pharmacological tests) The concentration of oxidizing glutathione in the eye drops of the present invention may be as long as it can exhibit its effect, and is preferably 0.5 to 5, but it should be selected as appropriate depending on symptoms, age, etc. Bye.
ｐＨは眼科製剤に許容される範囲内にあればよいが、４
〜７の範囲が好ましい。The pH may be within the range acceptable for ophthalmic preparations, but
The range of 7 to 7 is preferable.
本製剤には点眼剤として通常に用いられる添加物、例え
ばパラオキシ安息香酸エステルや塩化ペンサルコニウム
、クロロブタノールなどの防腐剤、塩化ナトリウムや塩
化カリウムなどの等張化剤、リン酸ナトリウムなどの緩
衝化剤、エデト酸ナトリウムなどの安定化剤、水酸化ナ
トリウム等のｐＨ調節剤などを必要に応じて用いること
ができる。This preparation contains additives commonly used in eye drops, such as preservatives such as paraoxybenzoic acid ester, pensalkonium chloride, and chlorobutanol, tonicity agents such as sodium chloride and potassium chloride, and buffers such as sodium phosphate. A stabilizing agent such as a oxidizing agent, a stabilizer such as sodium edetate, a pH adjusting agent such as sodium hydroxide, etc. can be used as necessary.
尚、本発明点眼剤の剤型は点眼液、眼軟官のいずれでも
よい。以下に実施例としてその製剤例をあげる。The dosage form of the eye drops of the present invention may be either an eye drop or an eye ointment. Examples of the formulation are given below as examples.
「実施例」
実施例１（点眼液）
処方１ １００ｍ／中
酸化をグルタチオン ２．０２ε−アミノカプ
ロン酸 ０．２ ｙ塩化ナトリウム
０．６ｙ塩化ベンザルコニウム ０．００５ｙ
水酸化ナトリウム 適量
滅菌精製水
製法
滅菌精製水８０−に酸化型グルタチオン、ε−アミノカ
プロン酸、塩化ナトリウム、塩化ベンザルコニウムを加
えて溶解した後、水酸化ナトリウムを用いてｐＨを５．
０に調節する。滅菌精製水を加えて全量を１００ｍ１と
する。"Example" Example 1 (Eye Drops) Prescription 1 100ml/medium oxidation of glutathione 2.02ε-aminocaproic acid 0.2y Sodium chloride
0.6y Benzalkonium chloride 0.005y
Sodium Hydroxide Appropriate amount Sterile Purified Water Preparation Method After adding and dissolving oxidized glutathione, ε-aminocaproic acid, sodium chloride, and benzalkonium chloride in sterile purified water, adjust the pH to 5.0 using sodium hydroxide.
Adjust to 0. Add sterile purified water to bring the total volume to 100ml.
上記の同様の方法を用いて処方２〜４０点眼液を調製し
た。Formulations 2-40 eye drops were prepared using a similar method as described above.
処方２１０〇−中 （ｐＨ６，０）
酸化型グルタチオン ２．０ｙ酢酸ナトリウム
０．２２塩化ナトリウム
０．６ ｆ／塩化ペンザルコニウム
エデト酸ナトリウム
希塩酸もしくは水酸化ナトリウム
滅菌精製水
処方３ １００Ｗｄ！中 （ｐＨ５，０）酸化型グルタ
チオン
酢酸ナトリウム
グリセリン
パラオキシ安息香酸メチル
パラオキシ安息香酸プロピル
水酸化ナトリウムもしくは希塩酸
滅菌精製水
処方４１０〇−中 （ｐＨ５，２）
酸化型グルタチオン
ポリビニルアルコール
マンニトール
塩化ベンザルコニウム
水酸化ナトリウム
滅菌精製水
実施例２
０．００！ＩＭ’
０．０１ｙ
適量
２、Ｏｆｉ’
０．２ ｙ
２．０ｙ
０．００５ｙ
０．０１ｙ
適量
２．０ｙ
１．０ｙ
３．５２
０．００５７
適量
処方５（眼軟膏）
１００ｙ中
酸化型グルタチオン ２．０ｙ流動パラフイン
１０２
白色ワセリン ｓｓｙ
裂法
流動パラフィンの中に酸化型グルタチオンを加えて分散
させる。これを８０℃に熱した白色パラフィン中に加え
、脱気しながらゆっくりと撹拌し室温１で冷却する。Formula 2100-medium (pH 6.0) Oxidized glutathione 2.0y Sodium acetate 0.22 Sodium chloride
0.6 f/Sodium Penzalkonium Chloride Edetate Dilute Hydrochloric Acid or Sodium Hydroxide Sterilized Purified Water Prescription 3 100Wd! Medium (pH 5,0) Oxidized glutathione Sodium acetate Glycerin Methyl paraoxybenzoate Propyl paraoxybenzoate Sodium hydroxide or dilute hydrochloric acid Sterilized purified water formulation 4100- Medium (pH 5,2) Oxidized glutathione Polyvinyl alcohol Mannitol Benzalkonium chloride Hydroxide Sodium sterilized purified water Example 2 0.00! IM' 0.01y appropriate amount 2, Ofi' 0.2 y 2.0y 0.005y 0.01y appropriate amount 2.0y 1.0y 3.52 0.0057 appropriate amount prescription 5 (eye ointment) 100y medium oxidized glutathione 2. 0y Liquid paraffin 102 White petrolatum ssy Split method Add oxidized glutathione to liquid paraffin and disperse. This is added to white paraffin heated to 80°C, stirred slowly while degassing, and cooled to room temperature 1.
安定性試験
本発明点眼剤の安定性を調べる泥め、ｐＨを６にＭｊＩ
４整した２チの酸化型グルタチオン水溶液と還元型グル
タチオン水溶液を作り、室温で１チ月間保存した後、そ
の残存率を測定した。Stability test To check the stability of the eye drops of the present invention, the pH was adjusted to 6 using MjI.
Aqueous solutions of oxidized glutathione and reduced glutathione were prepared and stored at room temperature for one month, and then their residual rates were measured.
その結果、還元型グルタチオン水溶液の残存率が約９０
チであったのに対して、酸化型グルタチオン水溶液では
残存率の低下はほとんど認められなかった。As a result, the residual rate of the reduced glutathione aqueous solution was approximately 90%.
In contrast, almost no decrease in the residual rate was observed in the oxidized glutathione aqueous solution.
このことから本発明点眼剤が還元型グルタチオン点眼剤
に比べて安定性がはるかに優れていることがわかる。This shows that the eye drops of the present invention have much better stability than the reduced glutathione eye drops.
薬理試験
酸化型グルタチオｙを投与することにより水晶体中の還
元型グルタチオンの量がどのように変化するかをラット
の水晶体を用いて測定した。Pharmacological Test Using rat crystalline lenses, we measured how the amount of reduced glutathione in the lens changes by administering oxidized glutathione.
１）摘出直後の水晶体に対する影響
Ｗｉｓｔａｒ系雄性ラットの水晶体を摘出し、１５ｍＭ
の酸化型グルタチオンを含むブドウ糖含有リンゲル液で
５時間インキュベートした後、水晶体中の還元型グルタ
チオンの量を測定した。1) Effect on the crystalline lens immediately after removal The lens of a male Wistar rat was removed, and 15mM
After incubation for 5 hours in Ringer's solution containing oxidized glutathione containing glucose, the amount of reduced glutathione in the lens was measured.
結果 結果を表１に示した。result The results are shown in Table 1.
表１に示されているように酸化型グルタチオンを添加し
たものでは水晶体中で還元型グルタチオンが増加してい
ることは明らかである。As shown in Table 1, it is clear that reduced glutathione increases in the crystalline lens when oxidized glutathione is added.
２）糖白内障水晶体に対する影響
摘出した水晶体をあらかじめ５５．６ｍＭのグルコース
を含む溶液でインキュベートし糖白内障水晶体を作る（
Ｃａｎ、Ｊ、Ｏｐｈｔｈａｌｍｏｌ、 １６．３２（１
９８１））。これに対して１）と同様の方法を用いて実
験し、水晶体中の還元型グルタチオンの量を測定しｆＣ
８
結果
結果を表２に示した。2) Effect on sugar cataract lens The excised crystalline lens is incubated in advance in a solution containing 55.6mM glucose to create a sugar cataract lens (
Can, J. Ophthalmol, 16.32 (1
981)). To this end, we conducted an experiment using the same method as in 1) to measure the amount of reduced glutathione in the crystalline lens.
8 Results The results are shown in Table 2.
「発明の効果」
以上のように正常な水晶体でも白内障の病態モデルのど
ちらでも酸化型グルタチオンを投与すれば還元型グルタ
チオンの骨が増加することから、酸化型グルタチオンが
還元型グルタチオンのブスドラッグとして作用しており
、抗白内障剤として有用であることは明らかである。"Effects of the Invention" As described above, administration of oxidized glutathione to both normal crystalline lenses and cataract disease models increases bone formation of reduced glutathione, and oxidized glutathione acts as an ugly drug for reduced glutathione. It is clear that it is useful as an anti-cataract agent.
Claims (1)
内障点眼剤。Anti-cataract eye drops containing oxidized glutathione or its salts as the main ingredient.
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP63196378A JPH0643338B2 (en) | 1988-08-05 | 1988-08-05 | Anti-cataract eye drops |
| KR1019890011003A KR960013437B1 (en) | 1988-08-05 | 1989-08-01 | Oxidized glutathion eye-drops |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP63196378A JPH0643338B2 (en) | 1988-08-05 | 1988-08-05 | Anti-cataract eye drops |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH0245420A true JPH0245420A (en) | 1990-02-15 |
| JPH0643338B2 JPH0643338B2 (en) | 1994-06-08 |
Family
ID=16356873
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP63196378A Expired - Lifetime JPH0643338B2 (en) | 1988-08-05 | 1988-08-05 | Anti-cataract eye drops |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH0643338B2 (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000076454A3 (en) * | 1999-06-14 | 2001-06-28 | Advanced Medicine Res Inst | Therapeutic compositions for ophthalmic use and therapeutic compositions for brain central lesions |
| US7371411B2 (en) | 1998-11-23 | 2008-05-13 | Novelos Therapeutics, Inc. | Methods for production of the oxidized glutathione composite with CIS-diamminedichloroplatinum and pharmaceutical compositions based thereof regulating metabolism, proliferation, differentiation and apoptotic mechanisms for normal and transformed cells |
-
1988
- 1988-08-05 JP JP63196378A patent/JPH0643338B2/en not_active Expired - Lifetime
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7371411B2 (en) | 1998-11-23 | 2008-05-13 | Novelos Therapeutics, Inc. | Methods for production of the oxidized glutathione composite with CIS-diamminedichloroplatinum and pharmaceutical compositions based thereof regulating metabolism, proliferation, differentiation and apoptotic mechanisms for normal and transformed cells |
| WO2000076454A3 (en) * | 1999-06-14 | 2001-06-28 | Advanced Medicine Res Inst | Therapeutic compositions for ophthalmic use and therapeutic compositions for brain central lesions |
Also Published As
| Publication number | Publication date |
|---|---|
| JPH0643338B2 (en) | 1994-06-08 |
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