KR-102963524-B1 - Composition and method for treating presbyopia, hyperopia, astigmatism, reduced stereoscopic vision, and reduced contrast sensitivity

Abstract

Methods and compositions for treating impaired vision caused by presbyopia, hyperopia, or astigmatism, and methods and compositions for improving contrast sensitivity and stereoscopic vision are disclosed. Generally, a topical composition comprising about 0.05 to 10 weight% of methylated xanthine and about 1 to 10 weight% of ophthalmic miotic agent is applied to the outer surface of at least one eyelid of a subject.

Inventors

• 난두리 파드마
• 다이어 아론

Assignees

• 인트라투스-네바다, 인크.

Dates

Publication Date

20260511

Application Date

20210903

Priority Date

20200911

Claims (20)

1. A pharmaceutical composition for use in treating presbyopia, hyperopia, astigmatism, reduced contrast sensitivity, or reduced stereoscopic vision in a subject, comprising 0.05 to 10 weight% of caffeine, at least one methylated xanthine selected from theophylline, diphylline, theobromine, aminophylline, and pentoxifylline, or a pharmaceutically acceptable salt thereof, and 1 to 10 weight% of a miotic agent selected from pilocarpine, 1 to 3 weight% of carvacol, 4 to 15 weight% of sevimelin, and 0.25 to 3 weight% of physostigmine, formulated for topical application to the outer surface of at least one eyelid of a subject, wherein application of the pharmaceutical composition to the outer surface of at least one eyelid of a subject reduces the incidence of at least one adverse effect associated with the application of the miotic agent to the eye, and the adverse effect is selected from miosis and myopia.
2. A pharmaceutical composition according to claim 1, wherein the miotic agent is pilocarpine.
3. In paragraph 1, the miotic agent is a pharmaceutical composition of carvacol.
4. In paragraph 1, the miotic agent is a pharmaceutical composition in which physostigmine.
5. In paragraph 1, the miotic agent is a pharmaceutical composition of sevimelin.
6. A pharmaceutical composition according to claim 1, wherein the methylated xanthine is caffeine.
7. A pharmaceutical composition according to claim 1, wherein the methylated xanthine is pentoxifyllin.
8. A pharmaceutical composition according to claim 1, wherein the methylated xanthine is theophylline.
9. A pharmaceutical composition in which the methylated xanthine in paragraph 2 is caffeine.
10. In claim 1, the subject is a pharmaceutical composition having presbyopia.
11. A pharmaceutical composition according to any one of claims 1 to 10, wherein the application of the composition to the outer surface of at least one eyelid results in an improvement in accommodation, distant vision, near vision, contrast sensitivity, stereoscopic vision, or a combination thereof.
12. A pharmaceutical composition according to claim 11, wherein at least one of accommodation, distant vision, near vision, contrast sensitivity, stereopsis, or a combination thereof is improved for at least 4 hours.
13. In paragraph 1, (i) Methylated xanthines contain caffeine, and miotics contain carvacol; (ii) Methylated xanthines contain caffeine, and miotics contain pilocarpine; (iii) The methylated xanthine is pentoxifyllin, and the miotic agent is carvacol or; (iv) the methylated xanthine is pentoxifyllin and the miotic is pilocarpine; or (v) A pharmaceutical composition in which the methylated xanthine is pentoxifyllin and the miotic agent is physostigmine.
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Description

Composition and method for treating presbyopia, hyperopia, astigmatism, reduced stereoscopic vision, and reduced contrast sensitivity The present disclosure relates to methods and compositions for treating impaired vision generally caused by presbyopia, hyperopia, or astigmatism, and to methods and compositions for improving contrast sensitivity and stereoscopic vision. Presbyopia is a major cause of visual impairment in healthy eyes. It is an aging-related process in which the eye's natural lens gradually thickens and loses its flexibility. These age-related changes occur within the lens's proteins, making the lens harder and less elastic over time. Age-related changes also occur in the muscle fibers surrounding the lens. As elasticity decreases, it becomes difficult for the eye to focus on close objects. A young, properly functioning eye can see at close distances, a ability that deteriorates with aging. Presbyopia generally occurs as a person ages and is associated with the natural loss of accommodation. Presbyopia results in the loss of the ability to quickly and easily focus on objects at close distances. The most common treatment for presbyopia is using over-the-counter reading glasses. Reading glasses allow the eyes to focus on close objects and maintain a clear image. This approach is similar to treating hyperopia. Contact lenses and intraocular lenses (IOLs) have also been used to treat presbyopia by relying on, for example, monovision (where one eye is corrected for distance vision while the other is corrected for near vision) or bifocal or multifocal lenses. Laser ablation has also been used to treat presbyopia. These procedures involve drastic steps (surgery, laser ablation, etc.) to resolve the problem for long-term purposes or require the wearing of corrective lenses. Hyperopia is a common visual condition in which distant objects appear clear, but close objects may appear blurry. The degree of hyperopia affects the eye's ability to focus. People with severe hyperopia have blurry vision for both near and far objects, whereas those with mild hyperopia generally have blurry vision at a distance and severely blurry vision for close objects. Hyperopia (or farsightedness) is generally present at birth and tends to run in families. Hyperopia is easily corrected with glasses or contact lenses. Another treatment option is surgery. Astigmatism is a type of refractive error in which the eye fails to focus light evenly onto the retina, causing distorted or blurry vision at any distance. Other symptoms may include eye strain, headaches, and difficulty driving at night. If astigmatism develops during childhood, it can lead to amblyopia later in life. The exact cause of astigmatism is unclear, but it is believed to be partially related to genetic factors. The underlying mechanism involves irregular curvature of the cornea or abnormalities in the lens of the eye. Astigmatism can be corrected with glasses, contact lenses, or refractive surgery. Glasses are the simplest and safest option, but contact lenses can provide a wider field of vision. Refractive surgery can completely eliminate the need for corrective lenses by permanently changing the shape of the eye, but like all elective surgeries, it carries greater risks and costs than non-invasive options. Contrast sensitivity is the visual ability to distinguish between an object and its background, and it is not the same as visual acuity. Poor contrast sensitivity is common in many visual impairments, including cataracts, diabetic retinopathy, and many retinal disorders. In these patients, contrast sensitivity is generally treated by using high-contrast filters, better lighting, and sharper high-contrast materials. In patients with cataracts, surgical removal of the cataract can significantly reduce contrast sensitivity. Stereopsis refers to the perception of depth and three-dimensional structures based on visual information derived from both eyes by individuals with normally developed binocular vision. The most common cause of stereopsis loss is reduced near or far vision due to refractive errors. Other less common causes of stereopsis include deviating eye (where one eye fails to form adequate input to the visual cortex), reduced binocular vision due to amblyopia, and anisometropia. Photopic vision is the visual acuity of the eye under bright lighting conditions (luminance levels of 10 to 10⁸ cd/ m² ). In humans and many other animals, photopic vision allows for color perception mediated by cone cells, as well as visual acuity and temporal resolution much higher than is available with scotopic vision. Most older adults lose photopic spatial contrast sensitivity. Adults in their 70s require about three times more contrast to detect higher spatial frequencies than adults in their 20s. Scotopic vision is the visual acuity of the eye under low illumination levels (luminance levels of 10⁻⁶ to 10⁻³⁵ cd/ m² ). In the human eye, cone cells do not function at low vi