Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Particulate form
Reexamination Certificate
1994-12-13
2004-08-31
Spear, James M. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Particulate form
C424S451000, C424S455000, C514S834000
Reexamination Certificate
active
06783774
ABSTRACT:
BACKGROUND OF THE INVENTION
The present invention pertains to the field of blood coagulation, which is further related to evaluation of coagulation tests; e.g. prothrombin time, partial thromboplastin time and activated partial thromboplastin time etc., and coagulation factor disorders. However, the blood coagulation mechanism of action of powdered D,L-threo-hex-2-enono-1,4-lactone which was administered topically does not fall into either intrinsic or extrinsic pathway cascade of blood coagulation scheme, since it works the same for blood coagulation in normal situation as in chronic hepatitis, colon cancer, and hemophilia patients in whom the coagulation factors 1, 2, 5, 7, 9, 10 and platelets in the liver disease and factor 8 or 9 in the hemophilia A or B are abnormal, or suppressed the syntheses, and destroyed and deficient (Harrison's Principles of Internal Medicine, 12
th
Edition, 1991, Pages 1314-1315). In other words, powdered D,L-threo-hex-2-enono-1,4-lactone stops any bleeding and forms black blood coagulation on contact, with the same amount of powdered D,L-threo-hex-2-enono-1,4-lactone per unit volume of blood for any normal or diseased blood.
The present methods available to stop bleeding in surgery are cautery, epinephrine injection, pressure and some fiber foam. The cautery can cause tissue necrosis in some cases. The epinephrine, pressure and fiber foam can not work for bleeding tendency patients, and fiber foam can cause tissue hematoma, nor can they work for diffuse capillary bleeding and oozing, while powdered D,L-threo-hex-2-enono-1,4-lactone does not cause any tissue necrosis and work particularly well for diffuse capillary bleeding and oozing and any traditionally uncontrollable bleeding tendency patients such as for patients with liver diseases, hemophilia and rectal anal cancer and for postoperative bleeding tendency of the kinds of aforementioned patients. The D,L-threo-hex-2-enono-1,4-lactone can facilitate wound healing also by increasing type 1 procollagen mRNA in the regulation of collagen synthesis.
SUMMARY OF THE INVENTION
The present invention is directed to a method for stopping bleeding, comprising administering powdered D,L-threo-hex-2-enono-1,4-lactone tablets thereof to the wound site in an amount of 0.1568 grams for every milliliter of blood. This powder has a very potent coagulation action to stop bleeding when spraying topically on the bleeding area for any normal or diseased patients. When the powder comes in contact with the blood, the black tar like material is formed, and later becomes solid. The amount of the powder that is needed to react completely with the blood is proportional to the amount of the blood that comes out of the blood vessels. In rats, one capillary, one venous and one femoral artery bleeding were stanched within one second, if sufficient amount of the powder of D,L-threo-hex-2-enono-1,4-lactone was applied. The artery bleeding needs much more this powder of interest. In the test tube conditions, it requires 0.1568 grams of powdered D,L-threo-hex-2-enono-1,4-lactone added to 1 ml of normal or diseased human blood to turn the mixture black and, after 6 minutes, mixture does not move by shaking or pouring. This is the same for normal, colon cancer and hemophilia patients; 1 ml of normal blood needs 0.1568 grams of D,L-threo-hex-2-enono-1,4-lactone powder, 1 ml of colon cancer needs 0.1568 grams of D,L-threo-hex-2-enono-1,4-lactone, 1 ml of hemophilia blood needs 0.1568 grams of D,L-threo-hex-2-enono-1,4-lactone. Sufficient powdered D,L-threo-hex-2-enono-1,4-lactone is particularly useful to stop bleeding in the case of diffuse capillary oozing and mistakenly cut off artery or arteries that can not be found during massive bleeding so as to save the patients's lives therefor. When D,L-threo-hex-2-enono-1,4-lactone is absorbed into the system, it is good for health by making the leucocytes stronger and slowing the aging process etc. However, at the end of operation before closure, the excessive black tar gel like material can be wiped away with Ringer's solution.
DETAILED DESCRIPTION OF THE INVENTION
The present invention is grounded on applicant's discovery that any bleeding, either normal or diseased blood, is stopped on contact, and is formed black blood coagulation, by administration topically of a composition comprising powdered D,L-threo-hex-2-enono-1,4-lactone or its derivative, D,L-threo-hex-2-enono-1,4-lactone-2-R1-5-R2-6-R3, even when contaminated with impurities, and excipients, in an amount of 0.1568 grams for every milliliter of blood.
A composition comprising powdered D,L-threo-hex-2-enono-1,4-lactone or its derivative, D,L-threo-hex-2-enono-1,4-lactone-2-R1-5-R2-6-R3 contains impurities and excipients. D,L-threo-hex-2-enono-1,4-lactone-2-R1-5-R2-6-R3, wherein R1 is organic residue having molecular weight of from 15-700, R2 is hydrogen or hydroxyl, R3 is hydrogen, acyl, optionally substituted phosphono or sulfo, and R3 and hydroxyl or R2 may form acetal residue or ketal residue, and a salt thereof are provided, D,L-threo-hex-2-enono-1,4-lactone derivative, D,L-threo-hex-2-enono-1,4-lactone-2-R1-5-R2-6-R3, wherein R1 is of the formula-CH2-R, wherein R is a C5-22 straight-chain or branched alkyl;
a C1-10 straight-chain or branched-chain alkyl group having one to three substituents selected from the group comprising the step of: (1) C1-6 alkoxyxarbonyl, (2) phenyl or naphthyl optionally substituted with one to three substituents selected from the group comprising the step of C1-5 alkyl, C1-3 alkoxy, halogen, nitro, amino, oxo, hydroxyl and benzyloxy, (3) benzyl or phenethyl optionally substitutd with one to three substituents selected from the group comprising the step of C1-5 alkyl, C1-3 alkoxy, halogen, nitro, amino, oxo, hydroxyl and benzyloxy, (4) phenylcarbonyloxy or naphthylcarbonyloxy optionally substituted with one to three substituents selected from the group comprising the step of C1-5 alkyl, C1-3 alkoxy, halogen, nitro, amino, oxo, hydroxyl and benzyloxy, (5) benzylcarbonyloxy or phenethylcarbonyloxy optionally substituted with one to three substituents selected from the group comprising the step of: C1-5 alkyl, C1-3 alkoxy, halogen, nitro, amino, oxo, hydroxy and benzyloxy, (6) 2,3,5-trimethyl-1,4-benzoquinonyl, (7) 2,3-dimethoxy-5-methyl-1,4-benzoquinonyl and (8) 2-methyl-1,4-napthoquinonyl;
a C2-20 alkenyl group having one to three substituents selected from phenyl, naththyl, benzyl or phenethyl, 3-pyridyl, thienyl and furyl;
a phenyl, naphthyl, benzyl or phenethyl optionally substituted with one to three substituents selected from the group comprising the step of C1-5 alkyl, methoxy, methylenedioxy and hydroxyl;
a C1-9 acyl group selected from the group comprising the step of formyl, acetyl, propionyl, n-butyryl, isobutyryl, benzoyl, morpholino-carbonyl, C1-3 alkoxycarbonyl prrolidinocarbonyl, C1-3 alkoxycarbonyl, phenylcarbonyl or naphthylcarbonyl optionally substituted with one to three substitutents selected from the group comprising the step of: hydroxyl, C1-5 alkyl and C1-3 alkoxy, benzylcarbonyl or phenethylcarbonyl optionally substituted with one to three substituents selected from the group comprising the step of: hydroxyl, C1-5 alkyl and C1-3 alkoxy;
a phenyloxy, naphthyloxy, benzyloxy or phenethyloxy optionally substituted with one to three substitutents selected from the group comprising the step of: hydroxyl, C1-5 alkyl and C1-3 alkoxy;
R2 is hydrogen or hydroxy; and
R3 is hydrogen, or acyl; or R2 and R3 may together form an O,O-isopropylidene residue; or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carier, vehicle or diluent therefor.
The derivative, D,L-threo-hex-2-enono-1,4-lactone-2-R1-5-R2-6-R3, wherein R3 is acyl, R1 is a C1-10 straight chain or branched chain alkyl group which has one to three substituents, the substituent being the class comprising the step of: (1) C1-6 alkoxycarbonyl, (2) phenyl or naphthyl which may hve one or three substituents(s) of the class comprising the step of: C1-5 alkyl, C1-3 alkoxy, halogen, n
Song Leslie B.
Spear James M.
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