Dietary supplement particularly indicated for combatting macular degeneration, capsule comprising said supplement and its use

Abstract

The present invention relates to a dietary supplement indicated for combating macular degeneration, more specifically a dietary supplement formulated to aid in the prevention of macular degeneration. It is developed based on fish oil (a source of omega-3 TG) combined with cysteine, taurine, lutein, zeaxanthin, and vitamins, contributing to visual health through a synergistic action of its components in addition to the benefits of omega-3. The present invention further relates to a capsule comprising said dietary supplement and the use of said supplement for combating macular degeneration.

Description

“FOOD SUPPLEMENT PARTICULARLY INDICATED FOR COMBATING MACULAR DEGENERATION, CAPSULE COMPRISING SAID SUPPLEMENT AND ITS USE” FIELD OF APPLICATION

[0001] . The present invention belongs to the food technology sector and refers to a food supplement indicated for combating macular degeneration, more specifically a food supplement to help combat macular degeneration, developed based on fish oil (source of omega 3-TG) with a combination of cysteine, taurine, lutein, zeaxanthin and vitamins, helping with vision health, which act synergistically in its composition added to the benefits of omega-3.

[0002] . Furthermore, the present invention relates to a capsule comprising said food supplement and the use of said supplement to combat macular degeneration. BACKGROUND OF THE INVENTION

[0003] Human aging is associated with a series of metabolic changes that predispose to the development of chronic degenerative diseases. Among the diseases that affect the elderly, those that compromise vision stand out. The most severe of these is Age-Related Macular Degeneration (AMD), which leads to severe vision loss and has no effective treatment available on the market. AMD, like other chronic morbidities, is associated with changes in cellular metabolism, particularly oxidative stress and inflammation. In addition, purinergic signaling, still little studied in this disease, is directly associated with the oxidative and inflammatory processes. Therefore, it is important to understand the relationship between the purinergic system and the main processes. associated with the development of AMD.

[0004] Age-related Macular Degeneration (AMD) is a degenerative change in the main region of the retina, the macula, responsible for refined, refined central visual acuity (VA) that allows for the vision of details. It typically affects individuals over 60 years of age and includes changes in the retinal pigment epithelium (RPE), such as hypo or hyperpigmentation, associated with drusen, in the initial phases, and may progress to complete atrophy of the RPE and choriocapillaris (geographic atrophy) or also to the development of choroidal neovascularization and consequent subretinal fibrous scarring, called disciform scarring, in its initial phases.

[0005] . Due to the involvement of the macula, the patient presents distorted and blurred central vision with significant impairment of visual function, significantly impacting their daily activities and quality of life.

[0006] The pathophysiology of AMD is multifactorial, complex, and still not completely understood. Age-related changes, a complex metabolic and functional interaction, genetic, and environmental factors can contribute to the development of chronic changes in ocular structures in the macular region (choriocapillaris, Bruch's membrane, retinal pigment epithelium (RPE), and photoreceptors), which evolve into varying degrees of AMD. Oxidative stress, decreased choroidal circulation, changes in lipid metabolism, Bruch's membrane degeneration, and chronic inflammation are involved in the pathophysiology of AMD. Based on clinical and pathological characteristics, AMD is classified as dry (atrophic) and wet (exudative, neovascular).

[0007] The dry form is characterized by the presence of drusen, progressive degeneration of photoreceptors, and RPE alterations in the macular region. Drusen consist of deposits of abnormal material. derived from the RPE in Bruch's membrane, due to the likely inability to clear waste in this region. The dry form can progress to geographic atrophy or the neovascular form.

[0008] The neovascular form occurs due to the growth of blood vessels in the subretinal space, originating from the choriocapillaris and growing through defects in Bruch's membrane, called subretinal neovascular membrane or choroidal neovascularization (CNV). CNV may be confined to the sub-RPE space or subsequently expand into the subretinal space. Leakage from these neovessels leads to the accumulation of serous or serosanguineous contents between the RPE and the neurosensory retina.

[0009] . A molecule called vascular endothelial growth factor (VEGF) has been recognized as a key mediator in neovascular angiogenesis. This molecule promotes blood vessel proliferation and is considered the primary agent responsible for disease progression.

[0010] AMD is one of the leading causes of legal blindness in developed countries among individuals over 50 years of age, accounting for 5.93% of blindness cases worldwide. International data estimate that 18% of the population aged 65 to 74 and 30% of the population aged 75 or older have some stage of AMD. Statistical data in Brazil are scarce. With increasing life expectancy and an aging population, the prevalence of this condition is expected to increase.

[0011] The prevalence, incidence, and progression of all forms of AMD vary, with age being the main risk factor. Smoking is the second main non-genetic risk factor.

[0012] AMD is more prevalent in Caucasians. Other associated risk factors include family history, cardiovascular disease, high blood pressure, increased lipid intake, and a diet low in omega-3s. lutein-containing vegetables, obesity, and lack of physical activity. Multiple genes have been implicated in predisposition to the disease. The literature is inconclusive regarding risk factors such as light-colored irises and excessive sunlight exposure.

[0013] The neovascular form accounts for 10% of all cases of the disease. Meanwhile, it is responsible for approximately 80% of all cases of legal blindness attributed to AMD. This form is characterized by the formation of CNV, leading to rapid loss of central vision. CNV extends anteriorly through the RPE, leading to the accumulation of fluid and blood, or lipids, in the subretinal space.

[0014] . These side effects of the disease, combined with the presence of scar or fibrous tissue, cause severe loss of central vision.

[0015] . Patients with exudative AMD present with complaints of sudden worsening of visual acuity, associated with metamorphopsia and central or paracentral scotomas.

[0016] Clinically, CNV presents as a rounded, grayish lesion, with or without hemorrhage, hard exudates, and detachment of the neurosensory retina and / or RPE. In the final stage of the disease, the fibroblasts that accompany the growth of CNV organize into fibrovascular tissue in the subretinal space, called a disciform scar.

[0017] . Tests used in the diagnosis and monitoring of AMD are fundoscopy, autofluorescence, fluorescein angiography and optical coherence tomography (OCT).

[0018] . Several literary references address various existing studies regarding nutrition in visual acuity and, therefore, several nutrients and their role have gained prominence in this new scenario, such as: antioxidants (vitamins B, C and E), carotenes (lutein, zeaxanthin and carotene), zinc and polyunsaturated omega-3 fatty acids - acid docosahexaenoic acid (DHA) and its precursor eicosapentaenoic acid (EPA).

[0019] . Many experts believe that the use of supplements has seen significant growth as a way to promote health and prevent and treat chronic degenerative diseases. In recent years, an eye care aid has been studied: omega supplementation.

[0020] . Risk factors for macular degeneration include: age, family history, smoking, cardiovascular disease, hypertension, some genetic abnormalities, and sun exposure.

[0021] There are two types of macular degeneration: dry and wet. - Dry macular degeneration: causes the macular tissues to become thinner as the cells disappear, and is the most common (85% of cases). - Wet macular degeneration: develops when abnormal blood vessels develop in front of the choroid, and is also the main cause of central vision loss.

[0022] . We highlight below some teachings from the state of the art that refer to this matter:

[0023] . Document BR 11 2022 012676-0 deals with chemical compounds C that are derived from norbixin and have tropism for the eye, and are intended for use in the treatment of ocular diseases in mammals, in particular in the context of alteration of the retinal pigment epithelium and more particularly in the context of age-related macular degeneration (AMD) and Stargardt disease.

[0024] . Document BR 0410651-2 describes new thiotungstate derivatives, methods of manufacturing thiotungstate derivatives, pharmaceutical compositions containing thiotungstate derivatives to treat diseases associated with aberrant vascularization, copper metabolism disorder and obesity, neurodegenerative disorders or NF-kB dysregulation.

[0025] . Therefore, as can be seen below, there is no solution in the state of the art equivalent to that presented here in the present invention that combines technical differences, economic advantages, safety and reliability. OBJECTIVES OF THE INVENTION

[0026] . The objective of the present invention is to provide a food supplement based on fish oil (source of omega 3-TG), with a combination of: cysteine, taurine, lutein, zeaxanthin and vitamins, helping with vision health, which act synergistically in its composition, added to the benefits of omega-3.

[0027] . It is a further objective of the present invention to provide a dietary supplement composition whose supportive therapy with lutein and zeaxanthin can have a beneficial effect in delaying the progression of eye diseases such as age-related macular degeneration (AMD) and cataracts.

[0028] . It is also an objective of the present invention to provide a dietary supplement composition with lutein that is beneficial for preventing the progression of AMD by increasing the optical density of the macular pigment, partially reversing visual loss in its early stages.

[0029] . The object of the present invention is to provide a food supplement particularly suitable for combating macular degeneration that can be administered in a 1.5g capsule. SUMMARY OF THE INVENTION

[0030] . The present invention achieves these and other objectives by means of a dietary supplement particularly indicated for combating macular degeneration that comprises fish oil, silicon dioxide, cysteine, lutein, zeaxanthin, vitamin B12, vitamin A, vitamin E, taurine and an acceptable vehicle.

[0031] . Furthermore, the present invention achieves these and other objectives by means of a capsule comprising the above supplement.

[0032] . Furthermore, the present invention achieves these and other objectives through the use of said supplement to prepare the capsule to combat macular degeneration. DETAILED DESCRIPTION OF THE INVENTION

[0033] The present invention is a dietary supplement based on fish oil (a source of omega-3-TG), with a combination of cysteine, taurine, lutein, zeaxanthin, and vitamins A, E, and B12, supporting vision health by acting synergistically in its composition, combined with the benefits of omega-3. The present invention, therefore, relates to a dietary supplement particularly indicated for combating macular degeneration that comprises fish oil, silicon dioxide, cysteine, lutein, zeaxanthin, vitamin B12, vitamin A, vitamin E, taurine, and an acceptable carrier.

[0034] . In a preferred embodiment of the present invention, the dietary supplement particularly indicated for combating macular degeneration comprises: - fish oil comprising omega-3, with 1812 net TG present in an amount of 0.744g, - silicon dioxide powder in an amount of 0.06g, - cysteine being N-acetyl cysteine present in an amount of 0.03g, - lutein in an amount of 0.10g, - zeaxanthin being 10% zeaxanthin present in an amount of 0.01 g, - vitamin B12 being methylcobalamin 5% present in an amount of 0.000024g, - vitamin A being retinol acetate 500000 present in an amount of 0.00045g, - vitamin E being tocopherol acetate in an amount of 0.0075g, - taurine powder in an amount of 0.048g,

[0035] . Preferably, the acceptable vehicle is water.

[0036] . Further, the present invention may comprise glycerin being double distilled vegetable glycerin USP in an amount of 0.09g and gelatin being bovine edible gelatin (210) in an amount of 0.022g.

[0037] . The present invention may be comprised in a 1.5g capsule.

[0038] . As can be seen later, the present invention brings technical advantages over the state of the art because:

[0039] Omega-3: Omega-3 fatty acids are a type of fat we need for health that our bodies cannot produce. The two main omega-3s with health benefits are eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA). They are found in animal sources, such as fatty fish.

[0040] Lutein: Lutein is a substance linked to eye health, as it can offer protection against damage caused by visible light, helping to filter high-energy wavelengths found in blue light and protecting the eyes against the formation of reactive oxygen species and free radicals. Lutein, or lipochrome, is a lemon-yellow carotenoid found in some vegetables such as spinach, zucchini, cauliflower, peas, broccoli, and some fruits such as oranges, papayas, peaches, and kiwis, as well as egg yolks.

[0041] Zeaxanthin: Zeaxanthin is a substance responsible for the color of fish, poultry, flowers, and food. It is found predominantly in yellow, orange, red, and green vegetables such as nectarines, oranges, papayas, peaches, broccoli, Brussels sprouts, cabbage, cauliflower, peas, corn, arugula, eggs, and others. This substance offers numerous health benefits, such as preventing premature aging and protecting vision, as it protects the eyes against UV rays emitted by the sun.

[0042] Cysteine: Cysteine is a non-essential amino acid produced by the body and is important for the formation of collagen and keratin. Cysteine also has antioxidant properties and is important for the production of muscles, hormones, and enzymes, strengthening the immune system.

[0043] . For AMD, carotenoids and omega-3 fatty acids have also proven sufficient in preventing neurodegeneration.

[0044] N-acetyl L-cysteine: This is a derivative of the natural amino acid cysteine, which serves as a substrate for the synthesis of glutathione (GSH) in the body, which has an antioxidant effect. This reduces the formation of pro-inflammatory cytokines such as IL-9 and TNF-a. GSH levels decrease with age and with certain health conditions, such as chronic non-communicable diseases.

[0045] Taurine: Taurine, or 2-aminoethanesulfonic acid, is a sulfur-containing organic acid found in bile. It is one of the most abundant non-essential amino acids in our bodies, especially in the central nervous system, skeletal muscles, heart, brain, intestines, and skeletal bones. It has antioxidant and anti-inflammatory properties, helping to improve immunity, maintain eye health, and prevent premature aging.

[0046] . Vitamin E: Vitamin E is a fat-soluble vitamin essential for the body's functioning due to its antioxidant action and anti-inflammatory properties, which help improve the immune system, skin and hair, as well as prevent degenerative diseases.

[0047] . Vitamin A: Vitamin A helps fight free radicals, agents that accelerate cellular aging. This means it has antioxidant properties, ensuring the preservation of various tissues, especially skin, mucous membrane, eye, and bone cells.

[0048] . Vitamin B12: Vitamin B12, also known as cyanocobalamin, is a very important vitamin for our body, as it is involved in the formation of our blood cells and acts directly on the nervous system, helping in the formation of neurons.

[0049] . In view of all the data, based on the results of studies evaluating the beneficial effects of compounds to aid in the treatment

[0050] . Supportive therapy with lutein and zeaxanthin may have a beneficial effect in slowing the progression of eye diseases such as age-related macular degeneration (AMD) and cataracts.

[0051] . High intake of specific nutrients, use of antioxidant supplements, and adherence to a Mediterranean diet decrease the risk of progression from early to late AMD.

[0052] Lutein supplementation is beneficial in preventing the progression of AMD by increasing macular pigment optical density, partially reversing early-stage vision loss. It has proven to be an effective treatment strategy for this disease, as a decrease in macular pigment optical density (MPOD) has been shown to be a determining factor in the onset of AMD in its more advanced stages.

[0053] Lutein and zeaxanthin supplementation confers clinical benefit. However, it may be an appropriate preventive measure for patients at high risk of developing AMD. Compared to beta-carotene, lutein / zeaxanthin has a potentially beneficial association with late AMD progression.

[0054] . Having described an example of a preferred embodiment of the present invention, it should be understood that the scope of the present invention encompasses other possible variations of the inventive concept described, being limited only by the content of the appended claims, including possible equivalents.

Claims

CLAIMS 1. Food supplement particularly indicated for combating macular degeneration characterized by comprising fish oil, silicon dioxide, cysteine, lutein, zeaxanthin, vitamin B12, vitamin A, vitamin E, taurine and an acceptable vehicle.

2. Supplement according to claim 1, characterized in that the fish oil comprises omega-3, being 1812 net TG and being present in an amount of 0.744g.

3. Supplement according to claim 1 or 2, characterized in that silicon dioxide is present in powder form in an amount of 0.06g.

4. Supplement according to any one of claims 1 to 3, characterized in that cysteine is N-acetyl cysteine present in an amount of 0.03g.

5. Supplement according to any one of claims 1 to 4, characterized in that lutein is present in powder form in an amount of 0.10g.

6. Supplement according to any one of claims 1 to 5, characterized in that 10% zeaxanthin is present in an amount of 0.01 g.

7. Supplement according to any one of claims 1 to 6, characterized in that vitamin B12 is 5% methylcobalamin and is present in an amount of 0.000024g.

8. Supplement according to any one of claims 1 to 7, characterized in that vitamin A is retinol acetate 500000 and is present in an amount of 0.00045g.

9. Supplement according to any one of claims 1 to 8, characterized in that vitamin E is present in an amount of 0.0075g.

10. Supplement according to any one of claims 1 to 9, characterized in that taurine is present in powder form in an amount of 0.048g.

11. Supplement according to any one of claims 1 to 10, characterized in that it comprises glycerin being double-distilled vegetable glycerin USP in an amount of 0.09g.

12. Supplement according to any one of claims 1 to 11, characterized in that it comprises gelatin being bovine edible gelatin (210) in an amount of 0.022g.

13. Capsule characterized by comprising a food supplement as defined in any one of claims 1 to 12.

14. Use of the food supplement as defined in any one of claims 1 to 12, characterized in that it is for preparing a capsule to combat macular degeneration.