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Injectable aqueous ophthalmic composition and method of use therefor

a technology of ophthalmic composition and injection aqueous, which is applied in the direction of drug composition, peptide/protein ingredient, cardiovascular disorder, etc., can solve the problems of difficulty in penetration, poor penetration, and difficulty in penetration, and achieve enhanced viscosity, enhanced viscosity, and enhanced viscosity

Inactive Publication Date: 2011-03-24
ALCON RES LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

"The present invention is about an eye drop that can be injected into the eye. It contains a therapeutic agent, a substance that increases the viscosity of the eye drop, and water. The substance that increases viscosity breaks down in the eye and releases the therapeutic agent over a period of time. The substance that increases viscosity is typically a positively charged molecule that can bind to other molecules in the eye. This can help the therapeutic agent stay in the eye for a longer time."

Problems solved by technology

While generally providing a desirable form of drug delivery, intravitreal injections also have drawbacks and can present various different complications.
Many therapeutic agents have difficulty penetrating target ocular tissue even after intravitreal injection.
In some instances, the penetration difficulty can be caused by poor solubility or hydrophilicity of the therapeutic agent.
In other instances, poor permeability due to size, molecular weight or other characteristics of the therapeutic agent can be the cause of poor penetration.
Intravitreal injections can also suffer from other drawbacks.
As one example, intravitreal injections having therapeutic agent in the form of particles (e.g., suspended submicron particles or nanoparticles) can obstruct vision if the particles disperse in an undesirable manner.
As another example, it can be difficult to consistently provide therapeutic agent close to a target location with an intravitreal injection since varying injection angles and variable eye size can cause significant variability in delivery location.
As yet another example, intravitreal injections can result in delivery of undesirably high concentrations of therapeutic agent to a target location or elsewhere particularly when the therapeutic agent is relatively soluble.
In addition to the above, therapeutic agents delivered by intravitreal injections can lack duration of action since the agents can often rapidly disperse within the eye after injection.
Such lack of duration is particularly undesirable since it can necessitate greater injection frequency.

Method used

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  • Injectable aqueous ophthalmic composition and method of use therefor

Examples

Experimental program
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Effect test

example 1

[0043]Poly-L-lysine aqueous solution (1%) was injected into a matrix material. The amine groups on the poly-lysine had a pKa value of approximately 10.5 and were positively charged and soluble in acidic to neutral solution with a charge density dependent upon pH. The matrix material was formed of vitreous fluid attained from excised pig eyes or rabbit eyes. As such, the matrix material typically included hyaluronic acid and collagen. Upon injection, the poly-L-lysine formed masses of enhanced viscosity with the hyaluronic acid and / or collagen in the form of gel complexes within the matrix material. Thereafter, each of the masses of enhanced viscosity slowly eroded over various extended time periods.

example 2

[0044]Cationic Guar C261N, 1% aqueous solution, was injected into a matrix material. The matrix material was formed of vitreous fluid attained from excised pig eyes or rabbit eyes. As such, the matrix material typically included hyaluronic acid and collagen. Upon injection, the cationic guar formed masses of enhanced viscosity with the hyaluronic acid and / or collagen in the form of gel complexes within the matrix material. Thereafter, each of the masses of enhanced viscosity slowly eroded over various extended time periods.

example 3

[0045]Chitosan and water soluble derivatives of chitosan such as lactate chitosan and carboxy methyl chitosan were injected into a matrix material. The amine groups on the chitosan had a pKa value of approximately 6.5 and were positively charged and soluble in acidic to neutral solution with a charge density dependent upon pH and % degree of acetylation-value. The matrix material was formed of vitreous fluid attained from excised pig eyes. As such, the matrix material typically included hyaluronic acid and collagen. Upon injection, the chitosan and its derivatives each formed masses of enhanced viscosity with the hyaluronic acid and / or collagen in the form of gel complexes within the matrix material. Thereafter, each of the masses of enhanced viscosity slowly eroded over various extended time periods.

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Abstract

The present invention is directed to the provision of an ophthalmic composition suitable for intravitreal injection. The composition includes an amount of complexing agent that reacts with one or more endogenous components (e.g., hyaluronic acid) in the eye to form a mass of enhanced viscosity. This mass can aid in creating a desirable release profile of therapeutic agent.

Description

CROSS REFERENCE TO RELATED APPLICATION[0001]This application claims priority under 35 U.S.C. §119 to U.S. Provisional Patent Application Ser. No. 61 / 244,916, filed Sep. 23, 2009, the entire contents of which are incorporated herein by reference.TECHNICAL FIELD OF THE INVENTION[0002]The present invention is directed to an injectable aqueous ophthalmic composition. More particularly, the present invention is directed to an injectable aqueous ophthalmic composition that includes a complexing agent (e.g., positively charged polymer or other compound) for enhancing the drug delivery capabilities of the composition when the composition is injected in an eye of human or animal.[0003]BACKGROUND OF THE INVENTION[0004]Intravitreal injections are commonly used to deliver therapeutic agents to the eye, particularly to the vitreous humor of the eye for treatment of ophthalmic maladies such as age related macular degeneration (AMD), diabetic macular edema (DME), inflammation or the like. Intravit...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K38/16A61K38/00A61P27/02A61P29/00A61P31/12
CPCA61K9/0048A61K9/0051A61K38/16A61K47/42A61K38/00A61K47/36A61P27/00A61P27/02A61P29/00A61P31/12A61K9/0019A61K47/34A61K47/38
Inventor CHOWHAN, MASOOD A.HOHMAN, THOMAS C.CASTILLO, ERNESTO J.HAN, WESLEY WEHSIN
Owner ALCON RES LTD