Preventive and therapeutic agents for eye diseases

A therapeutic and pharmaceutical technology, applied in the field of eye disease prevention and therapeutic drugs, can solve problems that have no practical application

Inactive Publication Date: 2002-12-25
ONO PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Although in JP-A5-221872 (corresponding to EP-A519354) and JP-A6-509232 (corresponding to EP-A596118), substances derived from microorganisms having human leukocyte elastase inhibitory activity are generally described as effective on corneal scar tissue Formation or fibr...

Method used

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  • Preventive and therapeutic agents for eye diseases
  • Preventive and therapeutic agents for eye diseases
  • Preventive and therapeutic agents for eye diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0080] Aqueous eye drops were prepared using the following composition. Ingredient Quantity Compound A 0.1g sodium chloride 0.9g sodium acetate 0.1g benzalkonium chloride 0.005g hydrochloric acid appropriate amount of sodium hydroxide appropriate amount of sterilized purified water to 100ml (pH6.0)

[0081] Compound A, sodium chloride, sodium acetate and benzalkonium chloride were dissolved in about 80 ml of purified water. The pH of the solution was adjusted to 6.0 with hydrochloric acid and sodium hydroxide. Sterilized purified water was added to make the total volume 100 ml, whereby an aqueous eye drop was obtained.

Embodiment 2

[0083] Eye drops of aqueous suspension were prepared using the following composition. Ingredient Quantity Compound A 1.0g sodium chloride 0.9g sodium acetate 0.1g polysorbate 80 0.2g benzalkonium chloride 0.005g hydrochloric acid appropriate amount of sodium hydroxide appropriate amount of sterilized purified water to 100ml (pH5.0)

[0084] Sodium chloride, sodium acetate, polysorbate 80, and benzalkonium chloride were dissolved in about 80 ml of purified water. The pH of the solution was adjusted to 5.0 with hydrochloric acid and sodium hydroxide, and then compound A was added and uniformly suspended using a homogenizer. Sterilized purified water was added to make the total volume 100 ml, whereby an aqueous suspension eye drop was obtained.

Embodiment 3

[0086] Eye drops of aqueous suspension were prepared using the following composition. Ingredient amount Compound A 0.5g concentrated glycerin 2.6g Sodium acetate 0.1g Hydroxypropyl methylcellulose 0.2g Methyl p-hydroxybenzoate 0.03g Propyl p-hydroxybenzoate 0.02g Hydrochloric acid Appropriate amount Sodium hydroxide Appropriate amount Sterilization and purification Water to 100ml (pH5.0)

[0087] Dissolve methylparaben and propylparaben in warm about 80 ml of purified water. In this solution, hydroxypropylmethylcellulose was dispersed, and then cooled to room temperature to be dissolved. Concentrated glycerin and sodium acetate were added to the solution, and the pH was adjusted to 5.0 with hydrochloric acid and sodium hydroxide. Compound A was added to the solution and uniformly suspended using a homogenizer. Sterilized purified water was added to make the total volume 100 ml, thereby obtaining eye drops as an aqueous suspension. Example 4

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Abstract

The present invention provides a preventive and therapeutic drug for ophthalmic diseases, especially ocular inflammatory diseases and corneal ulcers, which contains a compound represented by formula (I) or a pharmaceutically acceptable salt or hydrate thereof as an active ingredient.

Description

technical field [0001] The present invention relates to a prophylactic and therapeutic drug for eye diseases, which has an elastase inhibitory activity derived from leukocytes (neutrophils). Background of the invention [0002] JP-B5-81586 and JP-A5-194366 (corresponding to EP-A539223) disclose compounds represented by formula (I): (hereinafter referred to as the compound of formula (I)) and a salt thereof or a hydrate thereof, which have elastase inhibitory activity derived from human neutrophils, and are useful for the prevention and treatment of diseases such as emphysema, atherosclerosis and rheumatoid Arthritis disease is effective. [0003] On the other hand, the field of ophthalmology also includes various diseases related to leukocytes and their elastase. For example, ocular infections, corneal trauma, corneal ulcers and uveitis may be mentioned. In ocular infections, cellular infiltration of leukocytes leads to abscesses in the eye [Invest. Ophthalmol. Vis. Sci....

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/222A61K45/06A61K47/04A61P27/02
CPCA61K9/0048A61K31/222A61K45/06A61P27/02A61K31/235
Inventor 中裕亮川溿和一十德重秀树
Owner ONO PHARMA CO LTD
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