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Ophthalmic topical composition comprising dobesilic acid for treating diseases of posterior segment of eye

A technology of dobesilicic acid and ophthalmic compositions, applied in sensory diseases, drug combinations, active ingredients of anhydride/acid/halide, etc.

Pending Publication Date: 2020-08-14
LAB SALVAT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0018] Furthermore, it is scientifically well-established that topical eye drop administration can only be used to treat anterior segment disease, whereas treatment of the posterior segment of the eye is an important therapeutic target with unmet medical need (del Amo et al., “Current and future ophthalmic drug delivery systems. A shift to the posterior segment”, DrugDiscovery Today-2008, 13(3 / 4), pp. 135-143)

Method used

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  • Ophthalmic topical composition comprising dobesilic acid for treating diseases of posterior segment of eye
  • Ophthalmic topical composition comprising dobesilic acid for treating diseases of posterior segment of eye
  • Ophthalmic topical composition comprising dobesilic acid for treating diseases of posterior segment of eye

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0133] Example 1. Composition

[0134] Weigh an appropriate amount of CDO or phenanthramine in a suitable container, and add the distilled water mentioned in Table 1.

[0135] Dissolve CDO or phenanthramine in water with slow stirring.

[0136] Table 1

[0137]

[0138] q.s. add to full

Embodiment 2

[0139] Example 2. Ocular Distribution of CDO in Rats and Rabbits (Topical Ophthalmic and Oral Single-Dose Administration)

[0140] method

[0141] The ocular distribution of CDO was determined in rat and rabbit animal models to compare the bioavailability after oral administration and eye instillation.

[0142] Ocular Distribution of CDO in Rats (Topical Ocular and Oral Administration)

[0143] In Sprague Dawley (SD) rats weighing about 200 g, by topical eye drops (10 μl / eye) at 10 mg / ml (composition 2 of Example 1), 100 mg / ml (composition 5 of Example 1) or by Oral feeding tube CDO was administered at 50 mg / kg, 200 mg / kg or 750 mg / kg in water (compositions 1, 3 and 4 of Example 1, respectively). At 15, 60, 180, and 360 minutes post-administration, animals were euthanized and plasma and ocular tissue (including sclera, cornea, retina, vitreous humor / lens, and optic nerve) were collected.

[0144] Based on Human Equivalent Dose (HED) calculations, a 50 mg / kg (10 mg) oral d...

Embodiment 3

[0176] Example 3. Ocular distribution of phenantham after topical ocular single dose administration in rats

[0177] method

[0178] The ocular distribution of phenantham was determined to determine the absorption of the drug in the posterior segment of the eye.

[0179] Ethylamine (compositions 6 and 7 of Example 1) was administered by topical eye drops (10 μl / eye) in Sprague Dawley (SD) rats weighing approximately 200 g. At 15, 60 and 180 minutes after administration, animals were euthanized and ocular tissue (including retina and optic nerve) were collected.

[0180] Analysis conditions

[0181] As described in Example 2.

[0182] result

[0183] Table 4 below shows the experimental results:

[0184] Table 4

[0185]

[0186] Absorption of another dobesilate (phenanthramine) was confirmed. When the active ingredients are applied topically to the surface of the eye (eye drops onto the cornea and conjunctiva), they reach the back segment of the eye, specifically the...

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PUM

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Abstract

The invention relates to a new therapeutic approach for the treatment and / or prevention of a disease of the posterior segment of the eye, in particular for retinal and optic nerve pathologies. Dobesilic acid and / or a pharmaceutically acceptable salt, or an ester of any of the acid or the salt, are proposed for use topically administered onto eye surface. There are also disclosed new compositions comprising dobesilic acid and / or a pharmaceutically acceptable salt, or an ester of any of the acid or the salt, adapted for performing the treatment and / or prevention of diseases of the posterior segment of the eye.

Description

[0001] This application claims the benefit of European Patent Application 17382832.8 filed on December 4, 2017. technical field [0002] The present invention relates to the field of medical methods for the treatment of diseases of the posterior chamber of the eye, including retinopathy and disorders of the optic nerve. The present invention also relates to ophthalmic compositions. Background technique [0003] The eye is a complex organ with different specialized cells and tissues that are regulated to maintain optimal visual function. This function is achieved by the presence of tight barriers in the anterior and posterior segments of the eye, which play a key role by selectively controlling the inward and / or outward movement of fluids and solutes. Local and systemic diseases may affect different regions of the eye, but the anatomy of the eye and the complex physiology of the retina and optic nerve present challenges to the development of effective drugs. [0004] The ey...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/185A61P27/02
CPCA61K31/185A61P27/02A61K9/0048A61K9/08
Inventor X·卡普德维拉·诺尔特斯J·萨纳古斯廷·阿奎鲁M·I·德尔加多·加南
Owner LAB SALVAT
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