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Compositions and methods for the treatment of presbyopia

A kind of composition, technology of hyperopia, applied in some more preferred implementation areas, capable of solving problems such as adjustment-induced distance blur

Inactive Publication Date: 2018-11-23
PRESBYOPIA THERAPIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, to date, no aceclidinium composition with a cycloplegic dose lower than that defined in US 9089562 has been effective in the treatment of hyperopia because, as noted above, aceclidinine alone, especially in young People and middle-aged and elderly people (ages 45 to 58), severe ciliary muscle spasm and possibly accommodation-induced distance blurring in some cases

Method used

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  • Compositions and methods for the treatment of presbyopia
  • Compositions and methods for the treatment of presbyopia
  • Compositions and methods for the treatment of presbyopia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0212] In one embodiment, the ophthalmic composition comprises:

[0213] Aceclidinium in a concentration of about 1.75% w / v; and

[0214] Mannitol at a concentration of about 2.5% w / v.

[0215] In another embodiment, the ophthalmic composition comprises:

[0216] Aceclidinium in a concentration of about 1.75% w / v;

[0217] Mannitol in a concentration of about 2.5% w / v; and

[0218] Tropicamide at a concentration of about 0.02% w / v.

[0219] In another embodiment, the ophthalmic composition comprises:

[0220] Aceclidinium in a concentration of about 1.75% w / v;

[0221] Mannitol in a concentration of about 2.5% w / v;

[0222] polysorbate 80 at a concentration of about 5.0% w / v;

[0223] Carboxymethylcellulose at a concentration of about 1.4% w / v;

[0224] BAK at a concentration of about 0.015% w / v; and

[0225] Phosphate buffer at a concentration of about 3 mM,

[0226] Wherein, the pH is about 5.

[0227] In another embodiment, the ophthalmic composition comprises: ...

Embodiment 1

[0489] The effect of embodiment 1 acecidine on the visual acuity of 47 to 67 years old subjects

[0490] Table 1 shows the effect on the near focusing ability of hyperopic subjects before and after ophthalmic administration of acecidine-containing compositions. Each composition included aceclidinium at the concentrations indicated and 5.5% w / v HP[beta]CD, 0.75% w / v CMC, 0.25% w / v NaCl and 0.01% w / v BAK. Additionally, the composition administered to subjects 4 and 5 included 0.125% w / v tropicamide. Because aceclidinium is an enantiomer, clinical effectiveness varies with the ratio. For the current study, a nearly exact 50:50 ratio of stereoisomers was measured, as best determined by polarimetry.

[0491] Table 1. The effect of acecidine on the visual acuity of patients with hyperopia

[0492]

[0493] As can be seen from Table 1, all subjects had poorer than perfect near vision (20.20) for both left and right eyes (objects 15 inches from eye) and most subjects did not hav...

Embodiment 2

[0494] The concentration influence of the concentration of embodiment 2 aceclidine and tropicamide

[0495] Table 2: Concentration Effect of Acecidine and Tropicamide Concentrations

[0496]

[0497] Abbreviations: (C) corrected visual acuity, (m) minutes, (hr) hours, mm millimeters, BD baseline distance vision; BN baseline near vision, BP baseline pupil size, OD right eye; OS indicates the left eye, and OU indicates both eyes.

[0498] All percentages are w / v. "pt" reflects the size of the printed material, 4 equals 20 / 20 vision, and 3 equals 20 / 15 vision.

[0499] "Time" refers to the duration of action.

[0500] As can be seen from Table 2, acecidine at a concentration of at least 1.1% w / v was able to reduce the pupil size to 1.63 mm after 1 hour of topical instillation, which resulted in corrected near and distance vision for at least 10 hours. Reducing the concentration of aceclidinium to 0.75% w / v (Formulation #3) reduced the miotic effect to 2.0-2.5 mm after 1 ho...

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Abstract

The invention provides compositions and methods for the treatment of presbyopia and other vision defects. The compositions preferably comprise aceclidine and a polyol and / or a cycloplegic agent. The compositions optionally contain a surfactant, a viscosity enhancer, an osmolarity modifier and a preservative.

Description

Background technique [0001] As a person ages, the minimum distance from the eye to which an object is focused increases, in addition to corrected distance vision or excellent unaided distance vision. For example, a 10-year-old can focus on an object, or "focal point," only 3 inches (0.072 m) from his eye while still maintaining excellent distance vision; a 40-year-old at 6 inches (0.15 m); and a 60-year-old at An inconvenient 39 inches (1.0m). The condition of increasing minimum focal distance in individuals with excellent unaided distance vision is called hypermetropia, roughly translated as "presbyopia". [0002] Excellent uncorrected distance vision is also known as emmetropia. The inability to focus at a far focal point is known as myopia, and the inability to focus at a near focal point is known as hyperopia. Specifically, "distance" vision is considered to be any focus that is 1 meter or more from the eye, and near vision is any focus that is less than 1 meter from th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/439A61K31/4409A61K47/38
Inventor 杰拉尔德·霍恩李·诺丹
Owner PRESBYOPIA THERAPIES
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