[go: up one dir, main page]

JPH0778022B2 - Glaucoma treatment - Google Patents

Glaucoma treatment

Info

Publication number
JPH0778022B2
JPH0778022B2 JP7548988A JP7548988A JPH0778022B2 JP H0778022 B2 JPH0778022 B2 JP H0778022B2 JP 7548988 A JP7548988 A JP 7548988A JP 7548988 A JP7548988 A JP 7548988A JP H0778022 B2 JPH0778022 B2 JP H0778022B2
Authority
JP
Japan
Prior art keywords
intraocular pressure
compound
present
effect
glaucoma
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.)
Expired - Lifetime
Application number
JP7548988A
Other languages
Japanese (ja)
Other versions
JPH01246220A (en
Inventor
隆和 森田
正 磯
光史 疋田
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

Links

Landscapes

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

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。
TECHNICAL FIELD The present invention relates to a therapeutic agent for glaucoma which lowers intraocular pressure by local or systemic administration.

「従来技術」 式 で示される化合物又はその塩類(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つた。
"Prior art" formula Or a salt thereof (hereinafter referred to as the present compound)
Is known to be an excellent antihypertensive agent
61-41356). However, it is not known what kind of action this compound exerts on intraocular pressure,
It was necessary to consider the application in this field.

「課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り得ることを見い出し
た。
“Means for Solving the Problems” The present inventors have examined what kind of action the present compound has on intraocular pressure, and as a result, show an excellent intraocular pressure lowering action and can be a useful therapeutic agent for glaucoma. I found a thing.

「発明の開示」 本発明は式 で示される化合物又はその塩類(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 has the formula The present invention relates to a therapeutic agent for glaucoma containing a compound represented by or a salt thereof (the present compound) as a main component. Examples of the salt in 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
なかつた。
It is already known that this compound has an excellent hypotensive effect, but its effect on intraocular pressure has not been 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、薬理試験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, as a result of intensive studies on the application of the present compound to the ophthalmological field, the present inventors have found that the compound has an excellent intraocular pressure-lowering effect, and is a therapeutic agent for glaucoma, as described in the section of the pharmacological test. Found out to get.

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 a topical agent such as eye drops, eye ointment or injection, or a systemic agent such as tablets and capsules.

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%の濃度の
もの、全身用剤では1日当りの投与量が1〜300mg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 dose of the present compound in the present invention may be any as long as the therapeutic effect can be exerted, and the concentration of the topical agent is 0.01 to 5%, and the dose of the systemic agent is preferably 1 to 300 mg per day. However, it may be appropriately selected depending on the symptoms, age, dosage form and the like.

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 preparation of the present invention is prepared by adding necessary additives to the present compound depending on the dosage form. For example, for topical agents such as eye drops, isotonic agents such as sodium chloride, potassium chloride, concentrated glycerin, etc., buffering agents such as sodium phosphate, boric acid, monoethanolamine, etc., stability of sodium edetate, etc. Agents, benzalkonium chloride, preservatives such as paraoxybenzoate, surfactants such as polysorbate 80, pH adjusters such as sodium hydroxide, etc. are added as necessary. For systemic agents such as tablets and capsules,
Excipients such as lactose and crystalline cellulose, lubricants such as magnesium stearate, and binders such as hydroxypropyl cellulose are 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 100ml中 本化合物 1.0g 塩化ナトリウム 0.9g 水酸化ナトリウム 適量 滅菌精製水 〃 製法 滅菌精製水80mlに本化合物1.0g、塩化ナトリウム0.9g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100mlとした。
"Example" Example 1 (ophthalmic solution) In a 100 ml formulation, 1.0 g of the present compound, 0.9 g of sodium chloride, an appropriate amount of sodium hydroxide, sterilized purified water 〃 manufacturing method: After adding 1.0 g of this compound and 0.9 g of sodium chloride to 80 ml of sterilized purified water, The pH was adjusted to 7 with sodium hydroxide. Sterile purified water was added to bring the total volume to 100 ml.

同様の方法で本化合物の0.1%、0.5%点眼液を調製し
た。
In the same manner, 0.1% and 0.5% eye drops of the present compound were prepared.

実施例2(錠剤) 処方 1錠中 本化合物 1mg 粉末乳糖 61mg 結晶セルロース 25mg ヒドロキシプロピルセルロース 2mgステアリン酸マグネシウム 1mg 計 90mg 製法(1000錠分) 本化合物1g、粉末乳糖61g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した。これに結晶セルロ
ース25gとステアリン酸マグネシウム1gを加えて混合し
た後、6mmφのR面の杵を用いて打錠した。
Example 2 (tablets) Formulation In one tablet This compound 1 mg Powdered lactose 61 mg Crystalline cellulose 25 mg Hydroxypropyl cellulose 2 mg Magnesium stearate 1 mg Total 90 mg Manufacturing method (1000 tablets) 1 g of this compound and 61 g of powdered lactose were mixed, and then hydroxypropyl cellulose Was used for granulation. To this, 25 g of crystalline cellulose and 1 g of magnesium stearate were added and mixed, and then tableted using a 6 mmφ R-side punch.

薬理試験 緑内障に対する薬物の臨床への有用性を調べるため、日
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.McDonald他:Arch.Ophthalmol.,8
2,381(1969))を用いた。
Pharmacological test To examine the clinical usefulness of a drug for glaucoma, a method to investigate the drug's effect on intraocular pressure increase due to diurnal fluctuation or a method to investigate the effect on ocular hypertension induced by forced administration of water to rabbits (Thomas O. McDonald et al .: Arch. Ophthalmol., 8
2 , 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, the ocular hypotensive action of this compound was examined using the eye drop of Example 1.

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) Effect on intraocular pressure increase due to diurnal fluctuation It is well known that intraocular pressure is not always constant during the day and there is diurnal fluctuation. Therefore, the time period during which the intraocular pressure increased was selected using rabbits, and the inhibitory effect of this compound was investigated.

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。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50μ点眼し、眼圧の変化を調べ
た。
Experimental method The diurnal variation of intraocular pressure of all used rabbits (5 birds per group) was measured in advance and used as a control. The 0.1, 0.5 and 1.0% ophthalmic solution of the present compound and physiological saline shown in Example 1 were applied to both eyes of rabbits by 50 μm 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 The difference between the eye drop group of this compound and the eye drop group of the physiological saline solution and the untreated group (control) of the same rabbits was obtained, 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つきり
と表われている。
As shown in FIG. 1, almost no effect was observed in the eye drop group of the physiological saline solution, but in the eye drop group of the present compound, the effect of suppressing the increase in intraocular pressure was clearly shown as the concentration thereof was increased. ing.

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 intraocular pressure-lowering effect.

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%点眼液および生理食塩
液を各々4羽のウサギの両眼に50μ点眼した後、水を
強制投与(60mg/Kg)した。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つた。
2) Effect on water-load-induced ocular hypertension Experimental method 1% ophthalmic solution and physiological saline of the present compound as shown in Example 1 were instilled into both eyes of 4 rabbits at 50 μm each, followed by forced administration of water ( 60 mg / Kg). The intraocular pressure was measured up to 60 minutes after the administration of water to compare the present compound with physiological saline.

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

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, in the eye drop group of the physiological saline solution in which the intraocular pressure was observed to increase after water administration, instillation of the present compound significantly suppressed the increase in intraocular pressure.

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。
From this experiment, the ocular hypotensive action of the present compound is clear, which shows 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主成分として配
合することにより、優れな緑内障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 has an effect that an excellent therapeutic agent for glaucoma can be provided by incorporating a compound having an intraocular pressure-lowering effect as a main component.

【図面の簡単な説明】[Brief description of drawings]

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
mmHg)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(mmHg)を示し、横軸は水投与時を0とした
経過時間(分)を示す。図中の記号を以下に示す。 −△−:生理食塩液点眼群(8眼の平均値) −○−:実施例1の点眼液点眼群(8眼の平均値)
FIG. 1 shows the effect of the ophthalmic solution and physiological saline of the present compound on the increase in intraocular pressure due to diurnal fluctuation. The vertical axis is the maximum value of the difference in intraocular pressure from the control (average value of 10 eyes, unit)
mmHg) and the horizontal axis indicates the type of eye drop. FIG. 2 shows the time course of intraocular pressure in rabbits. The vertical axis represents intraocular pressure (mmHg), and the horizontal axis represents the elapsed time (minutes) when the water administration time is 0. The symbols in the figure are shown below. -△-: Saline solution eye drop group (average value of 8 eyes)-○-: Eye drop solution eye drop group of Example 1 (average value of 8 eyes)

───────────────────────────────────────────────────── フロントページの続き (56)参考文献 特開 昭55−7255(JP,A) 特開 昭54−135768(JP,A) 特開 昭54−148783(JP,A) 特開 昭56−81691(JP,A) 特開 昭55−92364(JP,A) 特開 昭55−15458(JP,A) 特開 昭56−90991(JP,A) ─────────────────────────────────────────────────── ─── Continuation of front page (56) Reference JP-A-55-7525 (JP, A) JP-A-54-135768 (JP, A) JP-A-54-148783 (JP, A) JP-A-56- 81691 (JP, A) JP-A-55-92364 (JP, A) JP-A-55-15458 (JP, A) JP-A-56-90991 (JP, A)

Claims (1)

【特許請求の範囲】[Claims] 【請求項1】 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。
1. A therapeutic agent for glaucoma comprising a compound represented by or a salt thereof as a main component.
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 JPH01246220A (en) 1989-10-02
JPH0778022B2 true 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)

Families Citing this family (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
JPH01246220A (en) 1989-10-02

Similar Documents

Publication Publication Date Title
CA1332811C (en) Treatment of ocular hypertension with class i calcium channel blocking agents
KR960005707B1 (en) Pharmaceutical composition containing benzoylphenyl acetic acid derivatives
EP0235544B1 (en) Ocular antihypertensive composition for topical use
EP1884234B1 (en) Prophylactic or therapeutic agent for corneal and conjunctival disorder
US20100041671A1 (en) Methods for treating glaucoma
JP4482726B2 (en) Glaucoma treatment agent comprising Rho kinase inhibitor and prostaglandins
JP2824863B2 (en) α ▲ Lower 1 ▼ -Blocker eye drops
EP0672417A1 (en) Reduction of elevated intraocular pressure
JP3527256B2 (en) Antiallergic eye drops
KR100192745B1 (en) 5-methyl-isoxazole-4-carboxylic acid anhydride and 2-hydroxyethylidene-cyanoacetate acetate for the treatment of eye diseases
EP0695545B1 (en) Use of diphenylethane derivatives for the manufacture of a medicament for the treatment of glaucoma
JPH11189533A (en) Eye drops
JP4300347B2 (en) Glaucoma treatment agent consisting of bunazosin and prostaglandins
JPH0778022B2 (en) Glaucoma treatment
WO2003063879A1 (en) Remedies for glaucoma comprising bunazosin and prostaglandins
WO2002040028A1 (en) Antibacterial gel eye drops
EP0608604A1 (en) Ajmaline to reduce elevated intraocular pressure
JP5087233B2 (en) Preventive or therapeutic agent for keratoconjunctival disorder
JPH08231400A (en) Intraocular pressure-lowering agent containing ifenprodil as essential ingredient
EP0277814B1 (en) Anti-glaucoma use of trifluoromethanesulfonamide
US5428030A (en) Method of reducing elevated intraocular pressure
JPH11116477A (en) Treating agent for allergic conjunctival disease
JP2007504198A (en) Composition comprising benzo [g] quinoline derivative and prostaglandin derivative
JPH0797318A (en) Intraocular pressure lowering agent containing oxyfedrine as essential component
WO2004004735A1 (en) Remedy comprising combination of levocabastine with pemirolast