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Ophthalmic composition

a technology of ophthalmic composition and composition, which is applied in the field of ophthalmic composition, can solve the problems of further aggravating the corneal lesions, unsatisfactory recovery, and the inability to achieve any of the above-mentioned treatments

Inactive Publication Date: 2002-10-31
R TECH UENO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

From the viewpoint of treatment of diabetic complications, it has been reported that aldose reductase inhibitors are effective in treatment of diabetic corneal lesions However, for example in cases where the symptoms have become aggravated so that the keratoepithelium becomes detached from the corneal parenchyma, satisfactory recovery cannot be attained at present with any of the treatments described above.
When the corneal esthesia is deteriorated, however, no subjective symptoms are noticed and this promotes to further aggravation of the corneal lesions.

Method used

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  • Ophthalmic composition
  • Ophthalmic composition
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Examples

Experimental program
Comparison scheme
Effect test

experimental example 1

Influence on the Repair Process of the Wound of Keratoepithelial Detachment in Alloxan-induced Diabetic Rabbits

[0063] 1) Test Animals and Procedures to Induce Diabetes

[0064] Alloxan monohydrate (Lot No. DLJ5619, M.W. 160.09 Wako Pure Chemical Industries, LTD.) of 80 mg / kg was dissolved in 2 mL of physiological saline, and the solution was administered once intravenously of male Japanese albino rabbits [Std: JW / CSK] (11-week-old) to induce diabetes.

[0065] Blood glucose was determined weekly after administration of alloxan monohydrate: the mean blood glucose was increased from 142.2.+-.4.7 mg / dL (mean.+-.S.E.; The same is applicable hereinafter.) before administration to 522.5.+-.13.7 mg / dL at 1 week, and this elevated level persisted thereafter. Animals with this alloxan-induced diabetes were used in the experiment.

[0066] 2) Detachment of Keratoepithelium

[0067] Under nembutal anesthesia a circular filter paper of TOYO No. 2 7.0 mm in diameter permeated with 7 .mu.L of n-heptanol was ...

experimental example 2

Influence on the Repair Process of the Wound of Keratoepithelial Detachment in Normal Rabbits

[0078] In the Experimental Example 1, the influence in rabbits with alloxan-induced diabetes was investigated, while the influence in normal (not diabetic) rabbits was investigated in this Example.

[0079] 1) Test Animals

[0080] Ten-week-old male New Zealand White rabbits (weighing 2.07.+-.0.11 kg: mean weight at the start of the experiment) were acclimation period for 7 days, while the animals were examined for the general signs including diarrhea and body weight, etc., and the anterior ocular segment was also observed. Only animals without any abnormality were used in the experiment.

[0081] 2) Detachment of Keratoepithelium

[0082] Keratoepithelial detachment wounds were prepared as described in the Experimental Example 1.

[0083] 3) Measurement of Area of the Keratoepithelial Detachment Wound

[0084] The test substance was instilled every 4 hours after the keratoepithelial detachment (the first ins...

experimental example 3

Influence on the Deteriorated Corneal esthesia and Hypolacrimation in Alloxan-induced Diabetic Rabbit

[0092] 1) Test Animals and Procedure to Induced Diabetes

[0093] Alloxan monohydrate (Lot No. DLJ5619, M.W. 160.09 Wako Pure Chemical Industries, LTD.) of 80 mg / kg was dissolved in 2 mL of physiological saline, and the solution was administered once intravenously of male Japanese albino rabbits [Std: JW / CSK] (11-week-old) to induce diabetes.

[0094] Blood glucose was determined once a week on 4 times after administration of alloxan monohydrate: animals having always blood glucose of 300 mg / dL or more were used as diabetic animals in this Experiment.

[0095] 2) Method of Administration

[0096] [3-(4-Bromo-2-fluorobenzyl)-7-chloro-2,4-dioxo-1,2,3,4-tetrahydroqu-inazolin-1-yl]acetate, an active ingredient of this invention, having aldose reductase-inhibiting effect was used for preparation of a 0.3% eye drops, and the eye drops were used as the test substance. The vehicle control was the vehicl...

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Abstract

The ophthalmic composition of this invention are used for treatment of diabetic corneal lesion and / or for treatment of deteriorated corneal esthesia, which comprises, as an active ingredient, a compound represented by the general formula (I): wherein A and B are independently lower alkylene, X, Y, and Z are independently halogen, or a pharmacologically acceptable salt thereof. In addition, the ophthalmic composition of this invention are used for treatment of non-diabetic corneal lesion, for treatment of dry eye syndrome, and / or for treatment of hypolacrimation which comprises, as an active ingredient, an aldose reductase inhibitor. The ophthalmic compositions of this invention are effective for treatment of at least one disease selected among corneal lesion, deteriorated corneal esthesia, dry eye syndrome, and hypolacrimation.

Description

[0001] This invention relates to ophthalmic compositions, in particular, those for treatment of corneal lesions, those for treatment of deteriorated corneal esthesia, those for treatment of dry eye syndrome, and those for treatment of hypolacrimation.PRIOR ART[0002] Corneal lesions are caused by defects in the corneal tissue. Defects in the epithelium generally give rise to subjective symptoms including foreign body sensation, eye pain, photophobia, tear secretion, etc. Defects in the corneal tissue are called epithalaxia or erosion when they are restricted only in the epithelium, and corneal ulcer when they extend from the Bowman's membrane to the parenchyma.[0003] There are various possible factors involved in corneal lesions, including pathological factors such as diabetes, inflammation, allergy, microorganisms (virus, bacteria, fungi, etc.) etc., chemical factors such as cytotoxicity by chemicals, caustic effect by acids or alkalis, etc., and physical factors such as dryness (dr...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/00A61K31/505A61K31/517A61P27/02
CPCA61K31/00Y10S514/912A61K31/517A61P27/02A61K31/505
Inventor UENO, RYUJIKATO, ICHIE
Owner R TECH UENO
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