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JPH01246220A - Remedy for glaucoma - Google Patents

Remedy for glaucoma

Info

Publication number
JPH01246220A
JPH01246220A JP63075489A JP7548988A JPH01246220A JP H01246220 A JPH01246220 A JP H01246220A JP 63075489 A JP63075489 A JP 63075489A JP 7548988 A JP7548988 A JP 7548988A JP H01246220 A JPH01246220 A JP H01246220A
Authority
JP
Japan
Prior art keywords
compound
intraocular pressure
agent
glaucoma
remedy
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
JP63075489A
Other languages
Japanese (ja)
Other versions
JPH0778022B2 (en
Inventor
Takakazu Morita
森田 隆和
Tadashi Iso
磯 正
Terubumi Hikita
疋田 光史
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 JP7548988A priority Critical patent/JPH0778022B2/en
Publication of JPH01246220A publication Critical patent/JPH01246220A/en
Publication of JPH0778022B2 publication Critical patent/JPH0778022B2/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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  • Thiazole And Isothizaole Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

PURPOSE:To provide a remedy for glaucoma, containing a specific compound known as an excellent hypotensor as a main component and capable of depressing the intraocular pressure by topical application or general application. CONSTITUTION:The objective remedy for glaucoma contains the compound of formula or its salt (metal salt such as Na, K or Ca salt or organic amine salt) as a main component. The remedy is used in the form of an agent for topical application such as eye drop, ophthalmic ointment or injection or an agent for general application such as tablet or capsule. Preferably, the topical agent is used at a concentration of 0.01-5% and the dose of the agent for general application is 1-300mg per day.

Description

【発明の詳細な説明】 「産業上の利用分野」 本発明は局所投与もしくは全身投与することにより眼圧
を降下させる緑内障の治療剤に関するものである。
DETAILED DESCRIPTION OF THE INVENTION "Field of Industrial Application" The present invention relates to a therapeutic agent for glaucoma that lowers intraocular pressure by local or systemic administration.

「従来技術」 はその塩類(以下本化合物という)が優れた血圧降下剤
であることが知られている(特公昭61−41356号
)。しかしながら、本化合物が眼圧に対してどのような
作用を示すかについては知られておらず、この分野につ
いての応用を検討する必要があった。
``Prior Art'' It is known that its salts (hereinafter referred to as the present compound) are excellent antihypertensive agents (Japanese Patent Publication No. 41356/1983). However, it is not known what effect this compound exhibits on intraocular pressure, and it was necessary to consider its application in this field.

「味題を解決するための手段」 本発明者らは本化合物が眼圧に対してどのような作用を
有するかについて検討した結果、優れた眼圧降下作用を
示し、有用な緑内障治療剤となシ得ることを見い出した
"Means for solving the problem" The present inventors investigated the effect of this compound on intraocular pressure and found that it exhibits an excellent intraocular pressure lowering effect and is a useful glaucoma treatment agent. I found out that there are many benefits.

「発明の開示」 合物又はその塩類(本化合物)を主成分とする緑内障治
療剤に関する。本化合物における塩としてはナトリウム
、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あげられる。
"Disclosure of the Invention" The present invention relates to a therapeutic agent for glaucoma containing a compound or a salt thereof (the present compound) as a main component. Examples of the salts of this compound include metal salts such as sodium, potassium, calcium, and magnesium, and organic amine salts.

本化合物が優れた血圧降下作用を有することはすでに知
られているが、眼圧に対する作用については知られてい
なかった。
Although it is already known that this compound has an excellent antihypertensive effect, its effect on intraocular pressure was not known.

そこで、本発明者らは本化合物の眼科分野への応用を鋭
意検討した結果、薬理試股の項で述べるように、本化合
物が優れた眼圧降下作用を有しており、緑内障の治療剤
となり得ることを見い出した。
Therefore, the present inventors have intensively investigated the application of this compound to the field of ophthalmology, and as a result, as described in the pharmacological test section, this compound has an excellent ocular hypotensive effect and is a therapeutic agent for glaucoma. I discovered that it can be done.

本発明の緑内障治療剤は点眼剤、眼軟膏や注射剤などの
局所用剤でも、錠剤やカプセル剤などの全身用剤のどち
らでも良い。
The therapeutic agent for glaucoma of the present invention may be either a topical preparation such as eye drops, eye ointment, or injection, or a systemic preparation such as a tablet or capsule.

本発明における本化合物の投与量は治療効果の発揮でき
るものであれば良く、局所用剤では0.01〜5チの濃
度のもの、全身用剤では1日当りの投与量が1〜300
■のものが好ましいが、症状、年令、剤型などにより適
宜選択すればよい。
The dosage of this compound in the present invention may be as long as it can exert a therapeutic effect, and for topical preparations, the dosage is 0.01 to 5%, and for systemic preparations, the daily dosage is 1 to 300%.
(2) is preferred, but it may be selected as appropriate depending on symptoms, age, dosage form, etc.

本発明製剤は剤型に応じて本化合物に必要な添加剤を加
えて調製される。例えば、点眼剤などの局所用剤であれ
ば、塩化ナトリウム、塩化カリウム、濃グリセリンなど
の等張化剤、リン酸ナトリウム、ホウ酸、モノエタノー
ルアミンなどの緩衝化剤、エデト酸ナトリウムなどの安
定化剤、塩化ベンザルコニウム、パラオキシ安息香酸エ
ステルなどの防腐剤、ポリソルベート80などの界面活
性剤、水酸化ナトリウムなどのpH調整剤などを必要に
応じて加える。又、錠剤、カプセル剤などの全身用剤で
は、乳糖、結晶セルロースなどの賦形剤、ステアリン酸
マグネシウムなどの滑沢剤、ヒドロキシプロピルセルロ
ースなどの結合剤などを必要に応じて加える。
The preparations of the present invention are prepared by adding necessary additives to the present compound depending on the dosage form. For example, for topical preparations such as eye drops, tonicity agents such as sodium chloride, potassium chloride, and concentrated glycerin, buffering agents such as sodium phosphate, boric acid, and monoethanolamine, and stabilizers such as sodium edetate are used. A preservative such as a curing agent, benzalkonium chloride or paraoxybenzoic acid ester, a surfactant such as polysorbate 80, a pH adjuster such as sodium hydroxide, etc. are added as necessary. For systemic preparations such as tablets and capsules, excipients such as lactose and crystalline cellulose, lubricants such as magnesium stearate, and binders such as hydroxypropylcellulose may be added as necessary.

次に本発明の製剤例を実施例として示す。Next, formulation examples of the present invention will be shown as examples.

「実施例」 実施例1(点眼液) 処方 100−中 本化合物            1.Of塩化ナナト
リウム       0.92水酸化ナトリウム   
    適量 滅菌精製水 製法 滅菌精製水80m/に本化合物1.Ofi! 、塩化ナ
トリウム0.9yを加えた後、水酸化ナトリウムを用い
てpHを7に調整した。滅菌精製水を加えて全量を10
0−とした。
"Example" Example 1 (eye drops) Prescription 100-Nakamoto compound 1. Of Sodium Chloride 0.92 Sodium Hydroxide
Appropriate amount of sterilized purified water production method Add 1 of this compound to 80 m/80 ml of sterile purified water. Ofi! After adding 0.9y of sodium chloride, the pH was adjusted to 7 using sodium hydroxide. Add sterile purified water to bring the total volume to 10
It was set to 0-.

同様の方法で本化合物の0.1%、0.5%点眼液を調
製した。
0.1% and 0.5% eye drops of this compound were prepared in the same manner.

実施例2(錠剤) 処方 1錠中 本化合物              1q粉末乳糖 
           61キ結晶セルロース    
     25岬ヒドロキシプロピルセルロース   
   2ツステアリン酸マグネシウム     1キ計
  90! 製法(1000錠分) 本化合物12、粉末乳糖61yを混合した後、ヒドロキ
シプロピルセルロースを用いて造粒シタ。
Example 2 (tablets) Prescription 1 tablet contains 1 q powdered lactose of this compound
61K crystalline cellulose
25 Misaki Hydroxypropyl Cellulose
2 tubes of magnesium stearate 1 kg total 90! Manufacturing method (for 1000 tablets) After mixing the present compound 12 and powdered lactose 61y, granulate it using hydroxypropyl cellulose.

これに結晶セルロース25ノとステアリン酸マグネシウ
ム1yを加えて混合した後、6uφの8面の杆を用いて
打錠した。
After adding and mixing 25 grams of crystalline cellulose and 1 y of magnesium stearate, the mixture was compressed into tablets using a 6uφ 8-sided rod.

薬理試醗 緑内障に対する薬物の臨床への有用性を調べるため、口
内変動による眼圧上昇に対する薬物の作用を調べる方法
やウサギに水を強制投与して誘発した高眼圧への作用を
調べる方法(Thomas O。
Pharmacological testing In order to investigate the clinical usefulness of drugs for glaucoma, we conducted a method to investigate the effect of drugs on increased intraocular pressure due to intraoral fluctuations, and a method to investigate the effect on ocular hypertension induced by forced administration of water to rabbits ( Thomas O.

MeDonald他: Areh、0phthalrn
o1. 、82.381(1969))を用いた。
MeDonald et al.: Areh, 0phthalrn
o1. , 82.381 (1969)) was used.

そこで、実施例1の点眼液を用いて本化合物の眼圧降下
作用を調べた。
Therefore, using the eye drops of Example 1, the intraocular pressure lowering effect of this compound was investigated.

1)日内変動による眼圧上昇に対する作用眼圧は1日の
うちで常に一定のものではなく、日内変動があることは
良く知られている。そこで、ウサギを用い眼圧が上昇す
る時間帯を選び、本化合物によるその抑制効果を調べた
1) Effects on increased intraocular pressure due to diurnal fluctuations It is well known that intraocular pressure is not always constant throughout the day and that it fluctuates within the day. Therefore, using rabbits, we selected a time period when intraocular pressure increases and investigated the inhibitory effect of this compound.

実験方法 使用した全てのウサギ(1群5羽)の眼圧の日内変動を
あらかじめ測定し、それを対照とした。
Experimental method The diurnal fluctuations in intraocular pressure of all rabbits used (group of 5 rabbits) were measured in advance and used as a control.

実施例1に示した0、1.0.5.1.0 %の本化合
物の点眼液と生理食塩液を各々ウサギの両眼に50!1
点眼し、眼圧の変化を調べた。
The 0, 1.0, 5, 1.0% ophthalmic solution and physiological saline solution of this compound shown in Example 1 were each administered 50!1 to both eyes of a rabbit.
The eye drops were applied to examine changes in intraocular pressure.

結果 本化合物の点眼液および生理食塩液の点眼群と各々同一
のウサギの無処置群(対照)との差を求め、その眼圧降
下の最大値を図1に示した。
Results Differences between the ophthalmic solution of the present compound and the physiological saline ophthalmic solution group and the untreated group (control) of the same rabbits were determined, and the maximum value of the decrease in intraocular pressure is shown in FIG.

図1に示されているように、生理食塩液の点眼群ではそ
の効果はほとんど見られないが、本化合物の点眼群では
その濃度の増大とともに眼圧上昇抑制の効果がはっきり
と表われている。
As shown in Figure 1, this effect is hardly seen in the physiological saline eye drop group, but in the eye drop group of this compound, the effect of suppressing the rise in intraocular pressure is clearly evident as the concentration increases. .

この結果から、本化合物が眼圧降下作用を有しているこ
とは明らかである。
From this result, it is clear that this compound has an effect of lowering intraocular pressure.

2)水負荷誘発高眼圧への作用 実験方法 実施例1で示した本化合物の1チ点眼液および生理食塩
液を各々4羽のウサギの両眼に50μ1点眼した後、水
を強制投与(60■/に9)した。
2) Effect on water load-induced ocular hypertension Experimental method After instilling 50 μl of each of the ophthalmic solution and physiological saline solution of the present compound shown in Example 1 into both eyes of four rabbits, water was forcibly administered ( 60/9).

水を投与後60分まで眼圧を測定し、本化合物と生理食
塩液との比較を行なった。
Intraocular pressure was measured until 60 minutes after water was administered, and the present compound and physiological saline were compared.

結果 得られた結果(8眼の平均値)を図2に示した。result The obtained results (average value of 8 eyes) are shown in FIG. 2.

図に示したように、水投与後に眼圧上昇がみられる生理
食塩液の点眼群に対して、本化合物を点眼したものでは
有意に眼圧上昇を抑制している。
As shown in the figure, the increase in intraocular pressure was significantly suppressed in the eye drops of this compound compared to the physiological saline eye drop group where an increase in intraocular pressure was observed after water administration.

この実験からも本化合物の眼圧降下作用は明らかであり
、本発明の有用性を示すものである。
This experiment also reveals the intraocular pressure-lowering effect of the present compound, demonstrating the usefulness of the present invention.

「発明の効果」 本発明は眼圧降下作用を有する化合物を生成障 分として配合することによシ、優れた繰向治療/\ 剤を提供できるという効果を有するものである。"Effect of the invention" The present invention provides a compound that has an intraocular hypotensive effect. Excellent recurrent treatment by combining the ingredients This has the effect of providing a drug.

【図面の簡単な説明】[Brief explanation of the drawing]

図1は日内変動による眼圧上昇に対して、本化合物の点
眼液と生理食塩液の効果を示したものである。 縦軸は対照との眼圧の差の最大値(10眼の平均値、単
位wHg )を示し、横軸は点眼液の種類を示す。 図2はウサギの眼圧の時間経過を示す。 縦軸は眼圧(mHg )を示し、横軸は水投与時を0と
した経過時間扮)を示す。図中の記号を以下に示す。
Figure 1 shows the effects of the eye drops of this compound and physiological saline on the increase in intraocular pressure due to diurnal fluctuations. The vertical axis shows the maximum difference in intraocular pressure from the control (average value of 10 eyes, unit: wHg), and the horizontal axis shows the type of eye drops. Figure 2 shows the time course of intraocular pressure in rabbits. The vertical axis shows the intraocular pressure (mHg), and the horizontal axis shows the elapsed time (from 0 when water was administered). The symbols in the figure are shown below.

Claims (1)

【特許請求の範囲】 式〔▲数式、化学式、表等があります▼〕 で示される化合物又 はその塩類を主成分とする緑内障治療剤。[Claims] Formulas [▲There are mathematical formulas, chemical formulas, tables, etc.▼] The compound or is a glaucoma treatment whose main ingredient is its salts.
JP7548988A 1988-03-28 1988-03-28 Glaucoma treatment Expired - Lifetime JPH0778022B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP7548988A JPH0778022B2 (en) 1988-03-28 1988-03-28 Glaucoma treatment

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP7548988A JPH0778022B2 (en) 1988-03-28 1988-03-28 Glaucoma treatment

Publications (2)

Publication Number Publication Date
JPH01246220A true JPH01246220A (en) 1989-10-02
JPH0778022B2 JPH0778022B2 (en) 1995-08-23

Family

ID=13577750

Family Applications (1)

Application Number Title Priority Date Filing Date
JP7548988A Expired - Lifetime JPH0778022B2 (en) 1988-03-28 1988-03-28 Glaucoma treatment

Country Status (1)

Country Link
JP (1) JPH0778022B2 (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5629345A (en) * 1993-07-23 1997-05-13 Vide Pharmaceuticals Methods and compositions for ATP-sensitive K+ channel inhibition for lowering intraocular pressure
US5965620A (en) * 1993-07-23 1999-10-12 Vide Pharmaceuticals Methods and compositions for ATP-sensitive K+ channel inhibition for lowering intraocular pressure

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022167299A1 (en) 2021-02-02 2022-08-11 Inait Sa Machine annotation of photographic images

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5629345A (en) * 1993-07-23 1997-05-13 Vide Pharmaceuticals Methods and compositions for ATP-sensitive K+ channel inhibition for lowering intraocular pressure
US5965620A (en) * 1993-07-23 1999-10-12 Vide Pharmaceuticals Methods and compositions for ATP-sensitive K+ channel inhibition for lowering intraocular pressure

Also Published As

Publication number Publication date
JPH0778022B2 (en) 1995-08-23

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