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Buffered ophthalmic compositions and methods of use thereof

An ophthalmic composition and composition technology, applied in the direction of drug combination, medical preparations with no active ingredients, medical preparations containing active ingredients, etc., can solve the problem of not enhancing wound closure, etc.

Inactive Publication Date: 2013-08-14
HEALOR LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are no drugs that enhance wound closure and avoid scarring
In severe cases, a corneal transplant may be required to restore vision when existing treatments have not helped

Method used

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  • Buffered ophthalmic compositions and methods of use thereof
  • Buffered ophthalmic compositions and methods of use thereof
  • Buffered ophthalmic compositions and methods of use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0152] Therapeutic Effects of Ophthalmic Buffers

[0153] Formulation 1 was formulated for eye treatment and to potentiate the action of MPDY-1. In order to determine the therapeutic effect of Ophthalmic Buffer Formulation 1 on corneal ulcers and ocular conditions, a series of experiments were performed with rabbit eyes. Corneal ulcers were induced in rabbit eyes by mechanical or chemical means and subsequently treated with formulation 1 buffer solution or control. Corneal ulcers are induced as follows:

[0154] Mechanical corneal ulceration: 6 mm corneal trephine (Grieshaber, Switzerland), preset to 50 microns deep, and a uniform central corneal epithelial erosion, 6 mm in diameter and 50 microns deep, using a mini-blade under an operating microscope.

[0155]Chemical Alkaline Ulceration: 5 mm absorbent paper disks were used to perform corneal alkaline erosions by placing 120 μl of NaOH 1 N for 10 seconds. Eyes were rinsed thoroughly with sterile irrigation water until t...

Embodiment 2

[0170] Therapeutic Effects of MPDY-1 Alone and in Combination with Additional Pharmaceutical Activities

[0171] This example discussion shows that soluble in BSS or DPBS - / - (referred to as formulation 2) of MPDY-1 and dissolved in DPBS with insulin - / - Experiment of the therapeutic effect of MPDY-1 (referred to as formulation 3) or MPDY-1 dissolved in HOB-10 (referred to as HO / 05 / 09) on mechanical and chemical corneal trauma.

[0172] Rabbits were subjected to mechanical corneal trauma as discussed in Example 1. Eyes were treated with twice-daily ocular instillation treatments for 3 consecutive days. Corneal erosion was measured at six-hour intervals using fluorescent staining. Figure 8 Display with separate vehicle (DPBS - / - , left), formulation 3 (MPDY-1 0.1 μg / eye / treatment and insulin 0.01 μg / eye / treatment, (center) and formulation 2 (MPDY-1 0.1 μg / eye / treatment, right) with completely closed Comparison of the percentage of eyes. Formulation 3 and Formulation 2 c...

Embodiment 3

[0187] Anti-inflammatory effect of MPDY-1

[0188] This example discusses experiments showing the anti-inflammatory effects of MPDY-1. The anti-inflammatory effect of MPDY-1 was confirmed using different in vitro, ex vivo and in vivo models. MPDY-1 was shown to attenuate ICAM-1 expression on epithelial cells and keratinocytes, inhibit the infiltration of macrophages, neutrophils and T cells into inflammatory sites and attenuate the activity of macrophages at inflammatory sites.

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PUM

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Abstract

The present disclosure provides a buffered ophthalmic composition for formulation of topically administrable suspensions useful for treating eye disorders by promoting wound healing, delivery of pharmaceutically active agents, and lubricating the eye. In particular the ophthalmic composition includes a buffer solution compatible with application to a mammalian eye, wherein the buffer provides increased mechanism of action of pharmaceutically active agents as well as therapeutic qualities. The ophthalmic composition exhibits dual therapeutic action to alleviate various eye disorders as it concomitantly treats corneal ulcerations and excessive inflammation which results from various eye injuries.

Description

technical field [0001] The present invention relates generally to ophthalmic compositions and more particularly to ophthalmic buffers for formulating topically acceptable suspensions useful in the delivery of pharmaceutically active agents and treatments of ocular disorders, injuries and diseases. The present invention also relates to methods of treating ocular conditions, injuries and diseases using the ophthalmic buffer formulations of the present invention, alone or in combination with pharmaceutically active agents, and methods of preparing buffers and formulations based on said buffers. The buffered solutions work particularly well with PKC activators or inhibitors, such as PKα inhibitors. Background technique [0002] Various ocular conditions resulting from disease or injury have been described and treated with varying success. For example, one condition is a corneal ulcer, which is an open sore that develops on the superficial cornea as a result of bacterial, viral ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/55A61K38/08
CPCA61K47/02A61K9/0048A61K38/28A61K47/12A61K38/55A61K38/08A61K38/10A61P27/02A61K2300/00A61K45/06C07K7/06
Inventor 塔玛·滕宁鲍姆利奥拉·布赖曼-维克斯曼尤瓦尔·萨吉夫奥芙拉·利维-哈查姆
Owner HEALOR LTD
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