Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Food or edible as carrier for pharmaceutical
Reexamination Certificate
1999-09-17
2003-06-24
Dodson, Shelley A. (Department: 1616)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Food or edible as carrier for pharmaceutical
Reexamination Certificate
active
06582721
ABSTRACT:
BACKGROUND OF THE INVENTION
Dietary supplements are taken for a variety of reasons including the improvement of vision or prophylaxis of vision loss. An example of a set of dietary supplements useful in promoting healthy eyes are the ICAPS® Dietary Supplements (Alcon Laboratories, Inc., Fort Worth, Tex.). Dietary supplements are generally in the form of powders, tablets, capsules or gel-caps and comprise a variety of vitamins, minerals, and herbal or other organic constituents. Some dietary supplements are formulated with beadlets.
Beadlets contain dietary substances and are generally small spheroids of less than about a millimeter in diameter. There are a variety of functions and purposes of beadlets. For example, beadlets may provide for the separate containment of ingredients within the dietary supplement to improve the stability of the entrapped ingredients.
Various beadlet compositions are known and can be obtained from a number of food ingredient or pharmaceutical manufacturers including H. Reisman Corp. (Orange, N.J.), BASF (Mount Olive, N.J.) and Hoffmann-LaRoche (Nutley, N.J.). Particular beadlet compositions have been the subject of several patents including U.S. Pat. No. 4,254,100 (Keller et al.) and U.S. Pat. No. 3,998,753 (Antoshkiw et al.). Methods of beadlet manufacture have been disclosed in U.S. Pat. No. 4,670,247 (Scialpi) and U.S. Pat. No. 3,998,753.
Current beadlet compositions used in dietary supplements generally are restricted to the use of inert ingredients and excipients complementary to a single nutritional compound. In other instances, when molecules of the same class are refined from a particular source, for example a major component with a minor related constituent, and both compounds produce parallel effects, such molecules may not necessarily be isolated but mixed together in a beadlet. These may be considered pseudo-single-component beadlets, and there are examples in the market place, e.g., Lutrinol® and FloraGLO® beadlets, which are a combination of lutein and zeaxanthin as formulated in Retoxil® Dietary Supplements. Examples of ingredients benefiting from beadlet confinement have included natural vitamins such as Vitamins A, D, E, and K; xanthophylls such as lutein, zeaxanthin, canthaxanthin, and astaxanthin; and carotenes, such as beta-carotene, lycopene, and retinol.
Recent data has suggested that the inclusion of xanthophylls and other carotenoids in dietary supplements may provide superior dietary supplements useful in enhancing the health of the eye. Studies have shown the selective uptake of the carotenoids, zeaxanthin and lutein, by the macula of the eye (Bernstein et al.,
Retinal Tubulin Binds Macular Carotenoids, Inv Ophthal & Vis Sci
, volume 38, No. 1, pages 167-175 (1997); Hammond et al.,
Dietary Modification of Human Macular Pigment Density, Inv Ophthal
&
Vis Sci
, volume 38, No. 9, pages 1795-1801 (1997); and Handelman et al.,
Biological Control of Primate Macular Pigment: Biochemical and Densitometric Studies, Inv Ophthal
&
Vis Sci
, volume 32, No. 2, pages 257-267 (1991)).
Xanthophylls are effective phytochemical antioxidants and are known to localize in the macula of the retina. It has been suggested that the particular xanthophylls, zeaxanthin and its isomer lutein, may be beneficial in improving the health of the macula and the clarity of the lens. These molecules may function in a number of ways to protect the eye from high intensity radiation or other insults. It has been suggested that foveal proteins bind the xanthophylls and localize xanthophylls within the fovea. Since xanthophylls are capable of absorbing photoexcitative radiation of short visible wavelength, they also may shield the light-sensitive, underlying cells of the fovea. Such cells are responsible for high-definition vision and have been shown by epidemiological studies to be adversely affected by exposure to high intensity radiation or even chronic exposure to visible wavelength radiation. The carotenoids are believed to complement the activity of these cells, and also to protect them against photochemical insult. See, eg., Snodderly,
Evidence for protection against age
-
related macular degeneration by carotenoids and antioxidant vitamins, Am J Clin Nutr
, volume 62(suppl), pages 1448S-1461S (1995) and Seddon et al.,
Dietary Carotenoids, Vitamins A, C and E, and Advanced Age
-
Related Macular Degeneration, JAMA
, volume 272, No. 8, pages 1413-1420 (1994).
Studies have also shown that the portion of the retina associated with xanthophyll deposition undergoes one of the highest metabolic rates in the body (Berman,
Biochemistry of the Eye
, (Plenum, 1991). The energy to sustain this metabolism is derived from oxidation. While xanthophylls do not appear to undergo rapid turnover characteristic of water-soluble antioxidants (Hammond, et al.,
Dietary modification of human macular pigment density, IOVS
, volume 38, pages 1795-1801 (1997)), continuous exchange of xanthophylls occurs in response to both environmental challenge and tissue environment, and their depletion without nutritional replacement may portend tissue damage (Hammond, et al.,
Sex differences in macular pigment optical density: relation to plasma carotenoid concentrations and dietary patterns, Vision Research
, volume 36, pages 2001-2012 (1996); Hammond, et al.,
Cigarette smoking and retinal carotenoids: implications for age
-
related macular degeneration, Vision Research
, volume 36, pages 3003-3009 (1996); and Seddon, et al.,
Dietary carotenoids, vitamins A, C, and E, and advanced age
-
related macular degeneration, JAMA
, volume 272, pages 1413-1420 (1994)).
The carotenes are conjugated C
40
compounds that include beta carotene (a provitamin A precursor). The carotenes are deeply colored compounds and are found throughout the plant kingdom, e.g., in leafy vegetables such as spinach and kale, and brilliantly colored fruits such as melons and pineapple. While the carotenes are ubiquitous in the plant kingdom, they generally are not available biosynthetically in mammals. Since the carotenes are essential for normal mammalian health, mammals need to ingest various sources of the carotenes, e.g., fruits and vegetables. In particular, the absence of carotenoids from the diet, especially the carotene derivative, vitamin A, is known to be associated with degenerative eye diseases.
SUMMARY OF THE INVENTION
The present invention is directed to improved beadlet formulations useful for inclusion in dietary supplements. In particular, the improved beadlets comprise one or more xanthophylls; one or more carotenes, retinoids or combinations thereof; one or more antioxidants; and excipients. Preferred beadlets may also contain one or more bioflavonoids. The beadlets are particularly useful for incorporation in dietary supplements customized for improving ocular nutrition.
The present invention is also directed to improved dietary supplements comprising the improved beadlets. Preferred dietary supplements have been formulated as an aid to ocular health. The present invention is also directed to methods of using the beadlets and dietary supplements for improving nutritional health. The methods of the present invention are particularly directed to the enhancement of ocular health and the prophylaxis of retinal disorders, including age-related macular degeneration.
One advantage of the beadlets of the present invention is that they provide one or more xanthophylls and one or more carotenes in a single beadlet formulation. Because these molecules contain multiple, conjugated double bonds, they are highly susceptible to degradation. Consequently, antioxidants have been required in dietary supplements to prevent premature oxidation of xanthophylls and carotenes during processing, manufacture, and storage. By coupling these mutually vulnerable components and the necessary antioxidants in one beadlet, the amount of stabilizing (antioxidant) component in the overall dietary supplement can be reduced, since the stabilizing components are distributed more proximately to the xanthophylls and carotenes, the
Alcon Inc.
Dodson Shelley A.
Schultz Teresa J.
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