Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1987-05-19
1991-12-31
Waddell, Frederick E.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
5142225, 514457, 514822, A61K 31725, A61K 3154, A61K 3135
Patent
active
050772813
DESCRIPTION:
BRIEF SUMMARY
DESCRIPTION
It is known to counter a blood embolus formation (thrombosis) to a certain extent by administration of coagulation-inhibiting medicaments. Coagulation-inhibiting medicaments (anticoagulants) in the narrower sense delay or prevent the blood coagulation; to these medicaments belong heparin and the coumarins, such as e.g. Marcumar.RTM. (3-(1-phenylpropyl)-4-hydroxycoumarin). In addition, there are also known so-called coagulation-inhibiting medicaments in the wider sense which are certain fibrinolytic and thrombolytic (i.e. fibrin- and blood embolus-dissolving) materials, such as e.g. streptokinase and urokinase, and inhibiting materials of the thrombocyte aggregation or of the prostaglandin synthesis, such as e.g. acetylsalicylic acid.
Taurolin is used in medicine as a good bactericidally-active substance. Taurolin has a low solubility in water (about 1%). Because of its very good bactericidal and other properties (no resistance against this substance known; apart from individually occurring slight local tissue irritation, other undesired side effects are not known), solutions of taurolin are used for bone lavage for the combating and treatment of bacterial osteolitis and bacterial suppurative peritonitis. Besides the very good bactericidal effectiveness, for taurolin is also known an inhibiting action on the formation of adhesions of the peritoneum after operative intervention into the abdominal cavity, as well as the suitability of taurolin for the neutralization of the endotoxin in the case of the so-called endotoxin shock; further medicinal fields of use have hitherto not been known for taurolin (cf. e.g. C. Steinbach-Lebbin et.al., Arzneimittelforschung/Drug Research 32 (II), No. 12 (1982), 1542-1546; W. Siegenthaler, Klinische Pathophysiologie, Georg Thieme Verlag, Stuttgart 1976).
It has now been found that, besides its known good bactericidal action, taurolin surprisingly also displays a coagulation-inhibiting action. Therefore, the subject of the present invention is the use of taurolin as blood coagulation-inhibiting agent, especially for the extracorporeal circulation, for example for plasmaphoresis, dialysis, blood lavage, oxygenators and for protheses in the vascular system.
The action according to the invention is surprising and also in "Taurolin", published by W. L. Bruckner and R. W. Pfirrmann, Verlag Urban und Schwarzenberg, Munchen 1985, it is expressly stated that taurolin does not influence the blood coagulation and displays no anti-phlogistic action.
Since the coagulation-inhibiting action of taurolin occurs not only in vivo but also in vitro, taurolin can, as mentioned, also be used for the coagulation inhibition in the extracorporeal circulation (e.g. in the case of heart operations or in the case of haemodialysis in the artificial kidney). The use of taurolin is thereby above all indicated in those cases in which the formation or entrainment of blood emboli in the vascular system (e.g. thrombosis, embolism) is to be prevented, thus in the first place in the case of heart infarct and in the case of vein thrombosis with the danger of a lung embolism, but also in the case of threatening blockage of blood vessels, in the case of blood vessel diseases and after injuries or operations for the prevention of the post-traumatic thromboses.
An undesired side effect of the known anti-coagulants, such as heparin or the coumarin derivatives, results, above all, from their desired coagulation-inhibiting and therefore, inter alia, blood flow-promoting actions. It can thereby, above all, result in hemorrhages in the gastro-intestinal tract (e.g. in the case of the so-called "quiet" gastric ulcer, in brain hemorrhages and in hemorrhages in the draining off urinary tract or in would hemorrhages during and after operations and after injuries. For the avoidance of such undesired phenomena, it is, therefore, important to monitor the remaining coagulatability of the blood during the administration by means of various coagulation tests, e.g. by the so-called "Quick test". In the case of an over
REFERENCES:
patent: 4337251 (1982-06-01), Pfiermann
patent: 4587268 (1986-05-01), Pfirrmann
Stedman's Medical Dictionary 24th ed p. 25.
The Molecular and Cellular Biology of Wound Repair Clark et al, 1988 pp. 3-33.
R. W. Pfirrmann "A New Concept for Antimicrobial Chemotherapy of Surgical Infections, Introduction and Overview" pp. 3-23 in Taurolin published by W. L. Bruckner & R. W. Pfirrmann Verlag Urban and Schwazenberg, Munchen 1985.
Von C. Steinbach-Lebbin et al, "On the Pharmacokinectics of Taurolin" pp. 1542-1546, Arzneim.-Forsch./Drug Res. (II), Nr. 12 (1982).
Henley III Raymond J.
Waddell Frederick E.
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