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Esters for treatment of ocular inflammatory conditions

An eye disease, ophthalmology technology, applied in the field of eye products, can solve problems such as bleeding time effects, increased cholesterol levels, disorders, etc.

Inactive Publication Date: 2014-05-21
JOHNSON & JOHNSON VISION CARE INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, oral omega-3 fatty acids do have potential side effects such as effects on bleeding time, increased cholesterol (LDL) levels, high caloric intake, fishy taste, and gastrointestinal disturbances

Method used

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  • Esters for treatment of ocular inflammatory conditions
  • Esters for treatment of ocular inflammatory conditions
  • Esters for treatment of ocular inflammatory conditions

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0128] The topical composition is formed by adding ethyl linolenate (alpha-linolenic acid ethyl ester (ALA-EE)), an esterified anti-inflammatory lipid mediator (AILM) having the following formula:

[0129] Added to a packaging solution / aqueous-based delivery system containing various surfactants / emulsifiers, wetting and chelating agents and one or more antioxidants, followed by mixing at high shear rates to provide Emulsion suitable for topical application. Table 4 summarizes the ingredients of the compositions.

[0130] Table 4:

[0131]

[0132] a=0.4% by weight boric acid, 0.2% by weight sodium borate, 0.5% by weight sodium chloride, 0.01% by weight diethylenetriaminepentaacetic acid (DTPA)

example 2

[0134] Compare

[0135] Topical compositions are formed by incorporating alpha-linolenic acid (ALA) into a packaging solution / aqueous based delivery system comprising various surfactants / emulsifiers, wetting and chelating agents and a or more antioxidants, followed by mixing at a high shear rate to provide an emulsion suitable for topical application. Table 5 summarizes the ingredients of the compositions.

[0136] table 5 :

[0137]

[0138] a=0.4% by weight boric acid, 0.2% by weight sodium borate, 0.5% by weight sodium chloride, 0.01% by weight diethylenetriaminepentaacetic acid (DTPA)

example 3

[0140] test

[0141] The compositions of Examples 1A and 1B and Comparative Example 2A were tested in vitro as follows. Fluorescein leakage (or increased transepithelial permeability) was evaluated using an in vitro model of transepithelial permeability (TEP test), in which the free acid and ester forms of α-linolenic acid were compared. The results are presented in Table 6, which shows that a high concentration (0.2%) of ALA ethyl ester performed similarly to the vehicle (packaging solution with Tween and Glucam) in effect on transepithelial permeability, while the same concentration of ALA fatty acid showed A significant increase in fluorescein leakage relative to controls was observed, consistent with clinical observations of discomfort during instillation. This suggests that, using concentrations up to 0.2%, omega-3 fatty acids in ester form will have improved instillation tolerability characteristics compared to the use of free acids.

[0142] Table 6

[0143] ...

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Abstract

The present invention relates to ophthalmic compositions and methods for the treatment of dry eye and other inflammatory ocular conditions. In particular, the present invention relates to a composition comprising an esterified anti-inflammatory lipid mediator, which is an ester of an anti-inflammatory lipid mediator that is a reaction product of the anti-inflammatory lipid mediator and a monohydric alcohol or an amide wherein the majority of the anti-inflammatory lipid mediator is present in an ester form. In this way, the compositions are substantially free of an acid form of the anti-inflammatory lipid mediators. Anti-inflammatory lipid mediators can be selected from the group consisting of polyunsaturated fatty acids (e.g., omega-three and omega-six fatty acids), resolvins or a metabolically stable analog, protectins or a metabolically stable analog, lipoxins or a metabolically stable analog, prostaglandins or a metabolically stable analog, retinoic acids, endocannabinoids, metabolites thereof, and mixtures thereof. This composition can be topically delivered to the ocular surface via a preparation, solution, gel, ointment, and / or strip and / or a contact lens.

Description

[0001] related application [0002] This application claims priority to US Patent Application Serial No. 13 / 495,052, filed June 13, 2012, and US Provisional Patent Application Serial No. 61 / 503,158, filed June 30, 2011. technical field [0003] The present invention relates to ophthalmic products comprising esterified anti-inflammatory lipid mediators for relief of dry eye or treatment of inflammatory ocular conditions. An ophthalmic composition comprising an esterified anti-inflammatory lipid mediator is provided. Also provided are sterile formulations, solutions, gels, ointments, and / or strips for administration to the eye, and / or contact lenses comprising an esterified anti-inflammatory lipid vehicle. Background technique [0004] Adequate lubrication is known to be essential for good eye health. Tears nourish the tissues of the eye and protect the surface of the eye from foreign objects. Changes to the surface of the eye caused by changes in tear quality or quantity (...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/16A61K31/201A61K31/202A61K31/203A61K31/557A61P27/02A61P27/04
CPCA61K9/0048A61K9/08A61K31/232A61K31/765A61K47/22A61K47/26A61K2300/00A61K31/557A61K31/215A61K31/5575A61K31/661A61P27/00A61P27/02A61P27/04A61P29/00A61K31/201A61K31/202A61K31/203A61K31/16A61K9/0051A61K31/683A61K9/00A61K31/21A61K31/25A61J3/00A61K47/14
Inventor A.盖洛伊斯-伯诺斯F.F.小莫洛克C.L.达维斯K.O.洛伦兹J.K.杨K.L.卡纳范F.卢
Owner JOHNSON & JOHNSON VISION CARE INC
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