Lipidic calcium compounds and use for treatment of osteoporosis

Organic compounds -- part of the class 532-570 series – Organic compounds – Fatty compounds having an acid moiety which contains the...

Reexamination Certificate

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C514S425000

Reexamination Certificate

active

06586608

ABSTRACT:

FIELD OF THE INVENTION
The present invention relates to a method to treat various conditions resulting from calcium deficiency and preparation of the same. Specifically, the invention relates to the administration of novel calcium-in-oil reaction products for the treatment of osteoporosis.
BACKGROUND OF THE INVENTION
Calcium is an essential nutrient that is involved in many physiological processes, including nerve and muscle functions. The phosphate salts of calcium provide mechanical rigidity to the bones and teeth, where 99% of the body's calcium resides. Calcium in the skeleton has the additional role of acting as a reserve supply of calcium to meet the body's metabolic needs in states of calcium deficiency. Calcium deficiency is easily induced because of the obligatory losses of calcium via bowel, kidneys, and skin. Nutritional and metabolic deficiencies of calcium can have broad-ranging adverse effects. Many of these effects are manifested through deficiencies in the structure, function and integrity of the skeletal system.
The most common metabolic bone disorder is osteoporosis. Osteoporosis is a crippling disease that emerges as an important public health problem in developed as well as developing countries. The clinical condition of osteoporosis is characterized mainly by loss of bone mineral mass, rendering bones more fragile and susceptible to fracture. In humans, osteoporosis is a common feature of aging.
Nutritional therapies for osteoporosis have been proposed. Studies demonstrate that, in general, adequate calcium intake during lifetime contributes to a decreased risk of osteoporosis. Many commercial preparations, typically containing calcium carbonate, are also available. Calcium chloride, calcium gluceptate, calcium gluconate, calcium phosphate, calcium citrate, and other calcium salts have also been described for use in calcium supplement. The use of calcium citrate, for example, is described by Pak in U.S. Pat. No. 4,772,467. Also, U.S. Pat. No. 5,128,374 by Kochanowski teaches the use of calcium citrate malate as a calcium supplement.
Currently, available calcium products have proven of very limited help in treating osteoporosis and other pathological conditions including arthritis, heart disease, Paget's disease, multiple sclerosis, and periodontal conditions. Pathological lesions typically contain free lipids. Currently available non-lipidic calcium formulations have minimal effect on these lesions because the calcium formulations are not taken up effectively by the cells.
The present invention now addresses this problem by providing new formulations and treatment methods for administering calcium to a subject.
SUMMARY OF THE INVENTION
It has now been discovered that calcium can be administered by way of a simple formulation where calcium is incorporated into a lipid by bonding calcium to the non-polar part of the lipid. It has also been found that the lipid-incorporated calcium is much more active biologically then non-lipidic formulations that contain calcium.
The present invention thus relates to novel compositions of lipids which include calcium incorporated therein. There compositions are lipid calcium or calcium-in-oil reaction products that are made by adding a calcium compound to a lipid component and heating the lipid component to a temperature of at least about 230° C. for a sufficient time to incorporate a predetermined amount of calcium into the lipid. At least about 0.1% by weight of calcium should incorporated, but preferably between 1 and 10% by weight are incorporated.
The compositions of the invention may be administered to a patient who has cells or tissues that are deficient in calcium to address the problem. One particular treatment is for subjects experiencing symptoms of osteoporosis to control pain, as well as to treat symptoms of diseases caused by cells and tissue deficient in calcium. The incorporated lipidic calcium is taken up preferentially by free lipids in abnormal cells or tissue, thus providing an increased level of calcium which is useful for effectively treating osteoporosis or other pathological conditions involving calcium deficiency.


REFERENCES:
patent: 4649152 (1987-03-01), Revici
patent: 4772467 (1988-09-01), Pak
patent: 5128374 (1992-07-01), Kochanowski
Donangelo, C.M., “Calcium and Osteoporosis,” Arch Latinoam Nutr Jun. 1997;47(2 Suppl 1):13-6.
Dowd, R., “Role of Calcium, Vitamin D, and Other Essential Nutrients in the Prevention and Treatment of Osteoporosis,” Nurs Clin North Am Sep. 2001;36(3):417-31, viii.
Heaney, R.P., “Calcium, Dairy Products and Osteoporosis,” J Am Coll Nutr Apr. 2000;19(2 Suppl):83S-99S.
Kanis, J.A., “The Use Of Calcium in the Management of Osteoporosis”, Bone Apr. 1999;24(4):279-290.
Nordin, B.E., “Calcium and Osteoporosis,” Nutrition Jul.-Aug. 1997;13(7-8):664-86.
Revici, Emanuel, Research in Physiopathology as Basis of Guided ChemotherapyWith Special Application to Cancer, 401-402 (D. Van Nostrand Company, Inc.) (1961).

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