Mesozeaxanthin formulations for treatment of retinal disorders

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – C-o-group doai

Reexamination Certificate

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C514S912000

Reexamination Certificate

active

06329432

ABSTRACT:

BACKGROUND OF THE INVENTION
1. Field of the Invention
The invention relates to the use of meso-zeaxanthin to increase the deposition of macular pigment in the human eye, and for the therapeutic treatment or prophylaxis of diseases and disorders of the macula, and in particular age-related macular degeneration (AMD).
2. Background Information
The macula is the anatomical region of the retina which in man is responsible for central vision. Centered on the fovea, where the visual axis meets the retina, it extends radially outwards to a distance of about 2.75 mm (Davson, 1990). The macula is divided into the inner macula and the outer macula. The inner macula extends radially out to a distance of 1.5 mm while the outer macula is defined by the surrounding annular ring. The central portion of the macula is easily recognizable because of its yellow coloration which results from the presence of macular pigment.
Despite its small size, the macula is endowed with the highest degree of visual acuity. It is therefore not surprising that considerable effort is devoted to understanding and, when possible, treating diseases which disrupt the nominal functioning of the macula. One such disease is age-related macular degeneration (AMD) which occurs in about 20% of the population above the age of 65 and is the leading cause of visual impairment in the USA and UK. AMD has up to the present time been an irreversible condition.
Pooled extracts of the macular pigment were found by Wald (1945) to have a carotenoid-like absorption spectrum which appeared to match that of lutein. Further work in the 1980's demonstrated that it consisted of lutein and zeaxanthin (Bone et al., 1985).
More recent work (Bone et al., 1993) has shown that the zeaxanthin component found in the human retina is itself composed of all three of the possible stereoisomers.
FIG. 1
shows the stereochemical structures of the macular pigment components. The 3′ hydroxy groups on lutein and meso-zeaxanthin have the same absolute configuration making interconversion possible by a movement of the 4′, 5′ double bond (lutein) to the 5′, 6′ position (meso-zeaxanthin). Of the three stereoisomers, SSZ is present only as a relatively small component. RRZ is of dietary origin whereas RSZ (meso-zeaxanthin) is not common in the diet and is not detected in human serum. It has been suggested that the presence of RSZ may be the result of isomerization of lutein to RSZ by an enzyme.
The function of the macular pigment has not been unequivocally determined. It has been proposed that one function may be to reduce the adverse effect of chromatic aberration in the ocular media thereby increasing acuity (Walls, 1967, Reading and Weale, 1974). A more generally held current view is that the pigment probably acts in a protective capacity against the damaging effects of blue light (Dicthburn, 1973; Kirshfeld, 1982; Bone et al., 1984) which can induce the formation of reactive free radicals within the retina and the formation of such species may be greatly reduced in individuals having a high level of macular pigmentation. The macular pigment may also serve passively as a filter and shield sensitive tissues from harmful excessive blue light.
AMD is a disease that develops gradually over a period of many years with loss of sight being the ultimate result. The damaged tissue has an unusually high lipid content that it has been suggested oxidizes to form lipofuscin, a fluorescent product of lipid oxidation. It has been postulated that exposure of the retina to excessive blue light may increase the rate of lipofuscin formation (Feeney-Burns et al., 1990; Gottsch et al., 1990).
To date, little is known about the factors that influence the uptake of carotenoids into the macula and there is no effective cure or prevention of AMD.
The studies of plasma carotenoids in case control studies of AMD have been equivocal. In the Beaver Dam eye study (Mares-Perlman et al., 1995), no differences were observed between 167 cases and 167 controls in serum including lutein or zeaxanthin. In the Eye Disease Case Control Study Group (1993) results of 421 cases and 615 controls were reported. People with serum carotenoid levels in the medium to high group had one half to one third risk of AMD compared with the low group. All of the carotenoids measured, including lutein, zeaxanthin, beta carotene, alpha carotene and cryptoxanthin were implicated. In a further publication (Seddon et al., 1994), these authors found that the consumption of lutein and zeaxanthin (which are primarily obtained from dark green leafy vegetables) were most strongly associated with a reduced risk of AMD. However, some people with a high consumption of green vegetables still suffered from AMD.
In an abstract published in the March 1995 issue of Investigative Ophthalmology and Visual Science (36, suppl, 892), the carotenoid analysis of 8 normal eyes and 8 eyes from patients with AMD was reported. The results suggested a positive correlation existed between lowered macular pigment and the prevalence of AMD, but recommended that caution should be exercised in this interpretation because the reduced macular pigment could be a result, rather than a cause of the disease. When the subject matter of the above mentioned abstract was submitted for publication to a peer-reviewed journal, the referees recommended rejection because the number of samples analyzed was too small. Further results were therefore necessary before any conclusion could be made on the possible preventative role of lutein/zeaxanthin in AMD.
SUMMARY OF THE INVENTION
It is the object of the present invention to increase macular pigment and to prevent or cure AMD by the administration of in meso-zeaxanthin.
It is a further object of the invention to provide novel compositions comprising meso-zeaxanthin either alone or in combination with other pharmaceutically effective compounds for the treatment and/or prevention of AMD.
Within the above context, we anticipate that supplements containing meso-zeaxanthin or an ester thereof will increase the macular pigment in the human macula which is expected to lead to the prevention and/or treatment of AMD in those people at risk of or having the disease.
It has been found in a sufficiently large sample to warrant conclusions, that the lutein/zeaxanthin content of the retinas of eyes from people with AMD was 30% less than in normal eyes. While it could be expected that since the macula contains lutein/zeaxanthin, the administration of lutein/zeaxanthin in quantities similar to that occurring in green vegetables would raise the cocentration of macular pigment, it has been found rather surprisingly that when certain carotenoids, such as lutein, are given orally in concentrated form the amount required to be effective in the short term is considerably greater than expected.
Meso-zeaxanthin not being found in normally consumed foodstuffs, the concentration to be administered for effective treatment is greater than that which is found in the normal human diet. Accordingly, the present invention in one aspect provides meso-zeaxanthin for the use as pharmaceutical or food supplements, particularly in the elevation of macular pigment and the prevention or management of age related macular degeneration. For this purpose, meso-zeaxanthin may be administered alone, or with pharmaceutically acceptable excipients or carriers, or in combination with other active compounds such as lutein and other carotenoids.
Generally speaking, the meso-zeaxanthin may be used in the total dosage regime of up to 100 mg per day, typically 0.5-50 mg/day with an optimum dosage of 5-10 mg/day. The dosage depends upon the time of administration. When the macula is depleted of macular pigment, a relatively high dose of lutein (circa 30 mg/day) is normally used.
During the initial period of administration, it is preferred to use a large dose of meso-zeaxanthin, circa 30 mg/day. However, when a plateau is achieved in the concentration of macular pigment, a maintenance dose of, for example, 5-10 mg/day, or lower, ma

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Mesozeaxanthin formulations for treatment of retinal disorders does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Mesozeaxanthin formulations for treatment of retinal disorders, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Mesozeaxanthin formulations for treatment of retinal disorders will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-2594911

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.