Pure 3r-3'r stereoisomer of zeaxanthin for treating macular...

A - Human Necessities – 61 – K

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A61K 31/045 (2006.01) A23L 1/30 (2006.01) A61K 9/107 (2006.01) A61K 9/48 (2006.01) A61K 31/047 (2006.01) C12P 7/02 (2006.01)

Patent

CA 2188983

Methods and formulations are disclosed for making and purifying the 3R-3'R stereoisomer of zeaxanthin as a sole detectable isomer, in any desired quantity, for use as a drug or vitamin by humans. Zeaxanthin, a yellowish pigment which is naturally present in macular cells in the center of the human retina, absorbs blue and near- ultraviolet light radiation, thereby protecting retinal cells against phototoxic damage. Zeaxanthin preparations which contain only the desired 3R-3'R stereoisomer can be produced by a strain of Flavobacterium mul tivorum cells (ATCC accession number 55238). These cells (and other cells transformed with their zeaxanthin-producing genes) do not create any detectable quantities of the undesired S-S or S-R isomers of zeaxanthin, and they do not synthesize significant quantities of other carotenoids which might compete against zeaxanthin for alimentary uptake after oral ingestion. After synthesis using microbial fermentation, the zeaxanthin can be concentrated to about 5 to 20% by simple and inexpensive steps such as solvent extraction. It can also be purified to much higher levels by other methods, if desired. The pure R-R isomer can be taken orally, either as a therapeutic drug by patients suffering from macular degeneration, or as a vitamin or nutritional supplement by anyone who wants to reduce his or her risk of suffering from age-related macular degeneration, which is widespread among people over the age of about 50 or 60. Extraction solvents, stabilizing agents, and convenient formulations for oral ingestion (such as mixed with vegetable oil and encapsulated, or used as a margarine or food additive) are also disclosed.

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