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Application of 5, 6, 7-tri-hydroxy enanthic acid and analog thereof for treating dry eye disorders and uveitis

一种眼色素层炎、药物的技术，应用在治疗干眼和眼色素层炎领域，能够解决尚没有化合物干眼或眼色素层炎等问题

Inactive Publication Date: 2009-08-05
ALCON INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, to the best of our knowledge, the compounds of this invention have not been described for the treatment of dry eye or uveitis

Method used

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  • Application of 5, 6, 7-tri-hydroxy enanthic acid and analog thereof for treating dry eye disorders and uveitis
  • Application of 5, 6, 7-tri-hydroxy enanthic acid and analog thereof for treating dry eye disorders and uveitis
  • Application of 5, 6, 7-tri-hydroxy enanthic acid and analog thereof for treating dry eye disorders and uveitis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1: Protective effect of compound 1 in dry eye rabbit model.

[0040] Compound 1 was evaluated in a rabbit model of dry eye. New Zealand white rabbits (approximately 2.5kg; obtained from Myrtle's rabbit farm at Thompson Station, TN) were taken at random and used in 0.064% / BBS 50 μl of compound 1 prepared in 1, 10 or 100 μM, or with 0.064% / BBS Vehicle is administered topically twice daily. After 24 hours, the rabbits were anesthetized by subcutaneous administration of ketamine hydrochloride (30 mg / kg) and xylazine (6 mg / kg), and each rabbit was injected bilaterally with Conconavilin A (ConA) (300 μg / 30 μl) or saline (30 μl ). Drying was initiated one day after lacrimal gland injection by placing conscious animals in an environmental chamber (20-30% humidity, 75°C). After 72 hours of environmental exposure, animals were evaluated for corneal staining by exposing the corneas to the dye methylene blue; lighter staining indicated less damage to the cornea. Rabb...

Embodiment 2

[0047] Example 2: Protective effect of compound 1 in uveitis rat model

[0048] Compound 1 was evaluated for its ability to inhibit neutrophil influx into rat eyes in an endotoxin-induced uveitis model. 0.01%, 0.1%, 1.0% w / v of this compound was prepared in ophthalmic suspension vehicle, and dexamethasone (Sigma-Aldrich Company, St. Louis, MO) prepared in the same vehicle was used as a reference compound. Uveitis was induced by subplantar injection of endotoxin (200 μg in 0.1 mL saline) in the right hind paw of female Lewis rats (5 / group). Test compounds in vehicle (5 [mu]L) were topically administered to each eye of the experimental animals at the time of endotoxin injection and 4 hours later. 24 hours after endotoxin injection, animals were treated with CO 2 Death by inhalation. The total content of ocular neutrophils (PMN) was indirectly evaluated by measuring the activity of myeloperoxidase. Ocular PMN content in each group was then compared to that observed in the veh...

Embodiment 3

[0062] Element Concentration (%w / v) Compound of formula I 0.00003-0.001 ethanol 0.03-0.2 boric acid 0.1-0.3

[0063] Polyoxyethylene 40 Stearate 0.1 Edetate Disodium 0.01 Polyquaternium-1 0.001 NaOH / HCl Appropriate to pH6-8 pure water Moderate to 100%

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PUM

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Abstract

The topical use of 5,6,7-trihydroxyheptanoic acid and analogs are disclosed for the treatment of dry eye disorders and uveitis.

Description

[0001] The present invention relates to the treatment of dry eye disease. In particular, the invention relates to the use of 5,6,7-trihydroxyheptanoic acid and its analogs for the treatment of dry eye and uveitis in mammals. Background technique [0002] Dry eye disease, commonly known as keratoconjunctivitis sicca, is a common eye disease that affects millions of Americans each year. The condition is especially prevalent in postmenopausal women due to hormonal changes that occur after fertility ceases. Dry eye disease afflicts patients in varying degrees of severity. In mild cases, patients experience burning, dryness, and constant irritation, for example, often caused by small objects between the eyelids and the surface of the eye. In severe cases, vision can be severely impaired. Dry eye complications occur in other diseases such as Sjogren's syndrome and cicatricial pemphigoid. [0003] Although it appears that dry eye disease can be caused by a variety of unrelated ca...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/047A61K31/22A61P27/02A01N31/14A61K31/045A61K31/16A61K31/205A61K31/215
CPCA61K31/16A61K31/047A61K31/215A61K31/205A61K31/22A61K31/045A61P27/00A61P27/02A61P27/04A61P27/14A61P29/00
Inventor P·G·科林寇M·R·赫勒贝格D·A·盖玛彻
Owner ALCON INC