Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Reexamination Certificate
2001-12-31
2004-03-30
Fay, Zohreh (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
C514S663000, C514S671000, C514S557000, C514S502000, C514S561000
Reexamination Certificate
active
06713513
ABSTRACT:
BACKGROUND OF THE INVENTION
The invention relates to a method for preventing or treating cartilage related diseases, and particularly a method for preventing or treating cartilage related diseases by administering an effective amount of calcium L-threonate to a subject suffering from such diseases.
There are many kinds of cartilage related diseases, the common examples of which are osteoarthritis, rheumatoid arthritis, multiple chondritis, articular cartilage damage, and osteochondrosis, etc. These diseases are often accompanied by the loss of cartilage.
Osteoarthritis is also called retrograde arthropathy, hyperplastic osteoarthritis. Its main characteristic is the formation of new bone accompanied with cartilage retrograde affection. Based on preliminary epidemiological investigations, the morbidity rate of osteoarthritis of knee joints in China is 9.56%. The rate reaches 78.5% among the people more than 60 years old, which is similar to that of western countries. Regretfully, there are no effective drugs available to treat osteoarthritis. The non-steroidal drugs are mainly used, such as Ibuprofen, Naproxen, etc. They have certain effects of alleviating pain, however, they have severe side effects and can not cure the disease in essence.
The occurrence of osteoarthritis is related to obesity, bone density, trauma and force burden, and heredity (see, Internal Medicine, 4th ed., Chen Haozhu, Li Zongming, etc.). Articular cartilage is formed by the aggregation of collagen fibers with a thickness of 1-2 mm, glucoprotein and hyaluronate. It functions by hydration as a cushion to absorb and disperse the endured burden and mechanical force. Under physiological conditions, articular cartilage depends on the contraction of muscles around the joint and the subchondral bone to fulfil the above-mentioned task. When there is something wrong with the muscles around the joint and the subchondral bone, for example, the subchondral bone has an abnormality such as senile retrograde change, osteoporosis, or the muscles endure excessive pressure such as obesity, trauma, etc., this can lead to the damage of cartilage, and possibly lead to osteoarthritis. What is worth mentioning herein is bone density. When the subchondral bone trabeculae become thin and stiff, their tolerance to endure pressure will decrease, and therefore the probability of the occurrence of osteoarthritis in the patient suffered from osteoporosis increases.
The pathologic changes of osteoarthritis show that articular cartilage degenerates firstly, then the loss of glucoprotein in the cartilage matrix softens the cartilage in the superficial layer of the joint. Fracture occurs in the part which endures pressure, causing the surface of the cartilage to have the appearance of velvet. Then the cartilage exfoliates gradually and the cartilage layer becomes thin or even disappears. Microfracture and sclerosis occur in the subchondral bone. Hyperosteogeny in the articular surface and its surrounding bone form the osteopetrosis, osteophyte and bone cystic degeneration in the X-line (epiphyseal line).
Rheumatoid arthritis and multiple chondritis are related to autoimmunity. Their common characteristics are the damage and loss of cartilage.
Damage of articular cartilage is acute or chronic damage of articular cartilage, which often appears in sport injuries. An example of acute damage is simple cartilage fracture. Chronic damage appears as retrograde affection and degeneration of cartilage, which will develop to osteoarthritis in the long term.
Osteochondrosis is an idiopathic disease of epiphysis in children, the characteristics of which are ischemic necrosis of epiphysis and disturbance of endochondral ossification in epiphysis, which finally can lead to malformed joints. It can be seen from the above that cartilage related diseases are often related to the damage, loss and functional degradation of cartilage.
The inventors conducted research on this, and found that calcium L-threonate could significantly improve the positive expression percentage of mRNA of collagen I in chondrocytes and osteoblasts, could significantly increase the positive expression percentage of chondrocytes in articular cartilage and epiphyseal cartilage, promote the growth of chondrocytes, increase the quantity of bone collagen, and promote the growth of bone, formation of cartilage matrix and the synthesis of protein mucopolysaccharide. It can also promote the formation of nourishing blood vessels in the bone and improve the microcirculation of the bone.
Therefore, it is an object of the present invention to provide a method for preventing or treating of cartilage related diseases, in particular a method for preventing or treating of cartilage related diseases, such as osteoarthritis, rheumatoid arthritis, multiple chondritis, articular cartilage damage and osteochondrosis, etc.
It is another object of the present invention to provide a pharmaceutical composition for preventing or treating cartilage related diseases, comprising an effective amount of the calcium L-threonate of the present invention and a pharmaceutically acceptable carrier.
It is a further object of the present invention to provide a calcium L-threonate compound for preventing or treating cartilage related diseases.
It is also an object of the present invention to provide a new use of calcium L-threonate in the preparation of a pharmaceutical composition for preventing or treating cartilage related diseases.
It is also an object of the present invention to provide a new use of calcium L-threonate to prevent or treat cartilage related diseases.
BRIEF SUMMARY OF THE INVENTION
The present invention provides a method for preventing or treating cartilage related diseases, in particular a method for preventing or treating cartilage related diseases, such as osteoarthritis, rheumatoid arthritis, multiple chondritis, articular cartilage damage, osteochondrosis, diseases related to cervical vertebra or diseases related to lumbar vertebra, etc., which comprises administering an effective amount of calcium L-threonate to a subject suffering from said diseases.
The present invention also provides a pharmaceutical composition for preventing or treating cartilage related diseases, comprising an effective amount of the calcium L-threonate of the present invention and pharmaceutically acceptable carrier.
The present invention also provides a calcium L-threonate compound for preventing or treating cartilage related diseases.
The present invention further provides a new use of calcium L-threonate in the manufacture of a pharmaceutical composition for preventing or treating cartilage related diseases.
The present invention further provides a new use of calcium L-threonate to prevent or treat cartilage related diseases.
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Review Article by Neil Gonter, Department of Rheumatology, University of Pennsylvania Healthsystem, 2002.*
“Lean about Arthritis”, WholeHealthMD.com, 2000.
Dai Xiangguo
Wang Zhiwen
Yu Kai
Alston & Bird LLP
Fay Zohreh
Juneng Industry Co., Ltd.
Kwon Brian S.
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