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Compositions for the improvement of distance vision and the treatment of refractive errors of the eye

A composition and vision technology, which can be applied in the directions of drug combination, drug delivery, medical preparations of inactive ingredients, etc., and can solve problems such as rebound congestion and increase

Active Publication Date: 2018-03-27
伦茨治疗股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, use of brimonidine at concentrations of 0.05% w / v or above resulted in increased rebound congestion

Method used

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  • Compositions for the improvement of distance vision and the treatment of refractive errors of the eye
  • Compositions for the improvement of distance vision and the treatment of refractive errors of the eye
  • Compositions for the improvement of distance vision and the treatment of refractive errors of the eye

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0128] In another embodiment, the ophthalmic composition comprises:

[0129] Aceclidinium in a concentration of about 1.42% w / v;

[0130] Tropicamide in a concentration of about 0.042% w / v;

[0131] polyethylene glycol 40 stearate in a concentration of about 5.5% w / v;

[0132] Mannitol in a concentration of about 4.0% w / v;

[0133] citrate in a concentration of about 0.2% w / v;

[0134] Acetate buffer at a concentration of about 3.0 mM;

[0135] wherein said composition has a pH of about 5.0.

[0136] In another embodiment, the ophthalmic composition comprises:

[0137] Aceclidinium in a concentration of about 1.50% w / v;

[0138] Tropicamide in a concentration of about 0.042% w / v;

[0139] polyethylene glycol 40 stearate in a concentration of about 4.0% w / v;

[0140] Mannitol in a concentration of about 4.0% w / v;

[0141] (Carbomer 934), effectively reaching 30-33cps after local instillation;

[0142] citrate in a concentration of about 0.2% w / v;

[0143] Acetate b...

Embodiment 1

[0225] Example 1 - Effect of Acecidine on Visual Acuity of Subjects Aged 47 to 67

[0226] Table 1 shows the effect on the near focusing ability of presbyopic subjects before and after ophthalmic administration of acecidine-containing compositions. Each composition contained aceclidine at the indicated concentrations together with 5.5% w / v of HPβCD, 0.75% w / v of CMC, 0.25% w / v of NaCl and 0.01% w / v of BAK. Additionally, the composition administered to subjects 4 and 5 contained 0.125% w / v tropicamide. Because aceclidinine is an enantiomer, clinical effectiveness can vary with different ratios. For the current study, an almost exact 50:50 ratio of stereoisomers was best determined by polarimetry.

[0227] Table 1 The influence of acecidine on the vision of presbyopia patients

[0228]

[0229] As can be seen from Table 1, all subjects had worse than perfect near vision (20.20) for both left and right eyes (objects at 15 inches from the eye) and most subjects had worse tha...

Embodiment 2

[0230]The influence of the concentration of the concentration of embodiment 2 aceclidine and tropicamide

[0231] Table 2 Effect of concentration of aceclidinium and tropicamide concentration

[0232]

#1

#2

#3

#4

#5(OD)

#5(0S)

#6

#7

Brimonidine

0.03％

0.03％

0.03％

0.03％

0.03％

0.03％

0.03％

Poloxamer 407

5.5％

HPBCD

5.5％

5.5％

5.5％

5.5％

5.5％

5.5％

5.5％

Clinidine

1.5％

1.5％

0.75％

1.1％

1.1％

1.1％

1.1％

1.1％

Tropicamide

0.014％

0.021％

0.028％

0.042％

0.062％

NaCl

0.25％

0.25％

0.25％

0.25％

0.25％

0.25％

0.25％

0.25％

CMC

0.75％

0.75％

0.75％

0.75％

0.75％

0.75％

0.75％

0.75％

BAK

0.1％

0.1％

0.1％

0.1％

0.1％

0.1％

0.1％

0.1％

Redness (15m)

3+

1

0.5

...

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Abstract

The invention provides compositions and methods for the improvement of distance vision. The invention further provides compositions and methods for the treatment of refractive errors of the eye. The invention further provides compositions that preferably comprise aceclidine lyophilized with a cryoprecipitate separate or together with a diluent comprising a cycloplegic agent, a surfactant, and optionally a viscosity enhancer.

Description

Background technique [0001] As a person ages, the minimum distance from the eye to an object in focus increases, except for corrected distance vision or excellent unaided vision. For example, a 10-year-old can focus on an object "focal point" that is only three inches (0.072 m) from his eye while still maintaining excellent distance vision; a 40-year-old at six inches (0.15 m); a 60-year-old person, at an uncomfortable 39 inches (1.0 m). The condition of progressive minimum focus in individuals with excellent unaided distance vision is known as presbyopia, roughly translated as "old man's eye". [0002] Excellent uncorrected distance vision is also known as emmetropia. The inability to focus on a far focus point is called nearsightedness, and the inability to focus on a near focus point is called hyperopia. Specifically, "far" vision is considered to be any focal point that is 1 meter or more from the eye, while near vision is any focal point that is less than 1 meter from ...

Claims

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Application Information

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IPC IPC(8): A61K31/439A61K31/165A61P27/02
CPCA61K31/439A61K9/0048A61K47/10A61K9/08A61P27/10A61K31/4409A61K47/26A61K31/137A61K31/216A61K31/4025A61K31/5365A61K31/5513A61P27/02A61P43/00A61K2300/00A61K47/14
Inventor 杰拉尔德·霍恩李·诺丹
Owner 伦茨治疗股份有限公司
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