Drug – bio-affecting and body treating compositions – Plant material or plant extract of undetermined constitution... – Containing or obtained from a fruit – including berry
Reexamination Certificate
2000-09-21
2001-09-18
Krass, Frederick (Department: 1614)
Drug, bio-affecting and body treating compositions
Plant material or plant extract of undetermined constitution...
Containing or obtained from a fruit , including berry
C424S401000, C424S439000, C424S440000, C424S769000, C514S025000, C514S027000
Reexamination Certificate
active
06290996
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
This invention relates to inhibiting blood platelet aggregation in humans, and, more particularly, to the use of an extract blend of the fruit of the Emblica officinalis plant for effectively controlling said aggregation.
2. Description of the Prior Art
Cerebral, cardiovascular, inflammatory disorders and geriatric progression represent atheromatous syndromes or vascular aging in humans resulting in progressive hypoxia caused in part by the action free radicals, such as the hemoglobin-oxo-ferryl (IV) radical. This radical induces lipid peroxidation which is implied in the pathophysiology of atherosclerosis. Through a similar mechanism, an alteration of the blood platelet function, promoted by free radicals, causes the formation of thrombi which constitutes the basis of infarction. Antioxidants, such as ascorbic acid (AA), alpha-tocopherol (Vitamin E), and pycnogenols (procyanidins) (U.S. Pat. No. 5,720,956), have been indicated for preventing or inhibiting the harmful effects of hypoxia following atherosclerosis and for surveillance against cardiac and cerebral infarction.
Reactive oxygen species (ROS) in the body also can cause lipid peroxidation of membranes which generate fragments that bind to platelet activating factor (PAF)-receptors on target cells and exert a PAF-like effect, namely, aggregation of blood platelets. ROS also can inactivate PAF-acetyl hydrolase, an enzyme present within plasma lipoproteins, that rapidly destroys PAF.
Certain biochemical agents, e.g. ADP, adrenaline and collagen, that promote PAF-like activity, also can cause lipid peroxidation which results in platelet aggregation. ADP can act via a metallo-complex-ROS system through its potent iron binding capacity, as shown in the equation below:
The oxoferryl radical, which is a complex ROS, can cause platelet aggregation in platelet rich plasma (PRP).
Accordingly, it is an object of this invention to provide an improved method of inhibiting induced-blood platelet aggregation in humans which can result in atherosclerosis.
Another object of the present invention is to provide a method of controlling free radical induced pathogenesis which can result in progressive hypoxia.
Still another object herein is to provide a method of inhibiting blood platelet aggregation which may be induced by a reactive oxygen species, such as ADP, adrenaline or collagen, or by human behavior patterns, such as smoking.
A feature of the invention is the provision of a method of inhibiting blood platelet aggregation in humans by administering a dose amount of 50-500 mg/day of an extract blend of the fruit of the Emblica officinalis plant.
Another feature of the invention is the inhibition of blood platelet aggregation by an extract of the Emblica officinalis plant without causing adverse side effects.
Still another feature of the invention is the provision of a pharmaceutical composition which includes about 50-500 mg of the extract blend.
These and other objects and features of the invention will be made apparent from the following more detailed description of the invention.
DETAILED DESCRIPTION OF THE INVENTION
The antagonist for inhibition of blood platelet aggregation in humans according to the invention is an extract blend, hereinafter referred to as “CAPROS™”, which is isolated in stable form from the fruit of the Emblica officinalis plant, as described in detail in the aforementioned co-pending patent application. The extraction process includes treating the finely-pulped fruit with a dilute aqueous or alcoholic-water salt solution, e.g. a 0.1 to 5% (w/w) sodium chloride solution, or the like, preferably at about 70° C.±5° C., or with a buffer solution, e.g. 0.1 to 5% (w/w) of sodium citrate/citric acid, or the like, filtering and drying, to provide the extract in powder form.
The CAPROS™ extract includes the active constituents Emblicanin-A and -B, which are gallic/ellagic acid derivatives of 2-keto-glucono-&dgr;-lactone, in an amount, by weight, of about 35-55%; as well as Punigluconic acid, or 2,3-di-O-galloyl-4,6(S)-hexahydroxydiphenoyl gluconic acid (about 4-15%); Pedunculagin, or 2,3,4,6-bis-(S)-hexahydroxydiphenoyl-D-glucose (about 10-20%); Rutin, or flavanol-3-glycoside or 3′,4′,5,7-tetrahydroxyflavone-3-)-rhamnoglucoside (about 5-15%); and low-to-medium molecular weight tannoids of gallic/ellagic acid (about 10-30%); gallic acid (about 0-5%) and ellagic acid (about 0-5%).
REFERENCES:
Chemical Abstract 103:27136, “Emblica officinalis reduces serum, aortic and hepatic cholesterol in rabbits” (1985).
Katz Walter
Krass Frederick
Natreon Inc.
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