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Storage stable compositions and methods for the treatment of refractive errors of the eye

A composition and ophthalmic technology, applied in the fields of aceclidinium composition, muscarinic agonist, and composition for treating presbyopia, which can solve problems such as improper recombination and improper treatment of presbyopia

Inactive Publication Date: 2018-04-17
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

The two-container system risks improper reconstitution and thus improper treatment of presbyopia

Method used

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  • Storage stable compositions and methods for the treatment of refractive errors of the eye
  • Storage stable compositions and methods for the treatment of refractive errors of the eye
  • Storage stable compositions and methods for the treatment of refractive errors of the eye

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0164] In another embodiment, the ophthalmic composition comprises:

[0165] Aceclidinium at a concentration of about 1.75% w / v;

[0166] Tropicamide at a concentration of about 0.042% w / v;

[0167] Macrogol 40 stearate at a concentration of about 4.5% w / v;

[0168] Mannitol at a concentration of about 2.5% w / v;

[0169] Acetate buffer at a concentration of about 3.0 mM; and

[0170] BAK at a concentration of about 0.02% w / v,

[0171] wherein said composition has a pH of about 4.75.

[0172] In another embodiment, the ophthalmic composition comprises:

[0173] Aceclidinium at a concentration of about 1.55% w / v;

[0174] Tropicamide at a concentration of about 0.042% w / v;

[0175] Macrogol 40 stearate at a concentration of about 5.5% w / v;

[0176] Citric acid monohydrate at a concentration of about 0.1% w / v;

[0177] Mannitol at a concentration of about 4.0% w / v;

[0178] Concentration of 0.09% w / v (Carbomer) 940; and acetate buffer at a concentration of about 3.0 mM;...

Embodiment 1

[0227] The influence of embodiment 1-acecidine on the visual acuity of 47 to 67 years old subjects

[0228] Table 1 shows the effect on the near-point focusing ability of presbyopic subjects before and after ocular administration of an ophthalmic composition comprising acecidine. Each composition included aceclidine at the concentrations indicated and 5.5% w / v HPβCD, 0.75% w / v CMC, 0.25% w / v NaCl and 0.01% w / v BAK. Additional compositions administered to Subjects 4 and 5 included 0.125% w / v tropicamide. Since aceclidinine is an enantiomer, its clinical effect may vary with different ratios. For the present study, the best stereoisomer ratio obtained by polarimetric measurements was approximately 50:50.

[0229] Table 1. Effect of acecidine on vision in patients with presbyopia

[0230]

[0231] As can be seen from Table 1, all subjects' left and right eyes (target distance 15 feet from the eye) were below ideal nearsightedness (20.20), and most subjects' farsightedness w...

Embodiment 2

[0232] Example 2 - Concentration Effects of Aceclidine and Tropicamide Concentrations

[0233] Table 2: Concentration Effect of Acecidine and Tropicamide Concentrations

[0234]

#1

#2

#3

#4

#5(OD)

#5(OS)

#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 (15 minutes)

3+

1

0.5

0.5

0

0

0

0

Redness (30 minutes)

1.5

0.5

0.25

0...

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PUM

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Abstract

The invention provides compositions and methods for achieving storage stable aceclidine. The compositions preferably comprise aceclidine, a cycloplegic agent, a surfactant, a tonicity adjuster and optionally a viscosity enhancer and an antioxidant. The invention further provides methods for treating refractive errors of the eye with a storage stable aceclidine composition.

Description

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

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/498A61K31/4164A61K31/165A61K31/439A61K31/4409A61K47/14A61K47/10A61K47/32A61K47/12A61K47/18A61K47/24A61K47/40A61K47/38A61K47/02
CPCA61K31/439A61K9/0048A61K47/10A61K9/08A61P27/10A61K31/4409A61K47/26A61K31/137A61K31/216A61K31/4025A61K31/5365A61K31/5513A61P27/02A61P43/00A61K45/06A61P27/06A61K2300/00A61K47/14
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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