Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1992-11-04
1994-06-28
Killos, Paul J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
A01N 3712
Patent
active
053247493
DESCRIPTION:
BRIEF SUMMARY
The subject of the present invention is a stable pharmaceutical aqueous solution of 4-[2-(benzenesulphonylamino)-ethyl]-phenoxyacetic acid. This solution is used as injection or infusion solution or, in concentrated form, as additive to infusion solutions.
The active material 4-[2-(benzenesulphonylamino)-ethyl]-phenoxyacetic acid and its preparation is described in EP-A-004,011 as Example 1. This compound is especially suitable for the preparation of medicaments for the treatment of diseases which are involved with an increased thrombocyte aggregation. The active material displays a significant lipid-sinking action and possesses an outstanding inhibiting action on the thrombocyte aggregation.
Diseases which can be treated with this active material are, for example, atherosclerotic diseases of the blood vessel system, diseases of the kidney, as well as the treatment of shock lung. Furthermore, in this connection, the following indications come into question: prevention of the damaging of the microcirculation due to radiation therapy (e.g. in the kidney); treatment of hearing precipitation; prevention of reocclusion in the case of by-pass operations, in the case of coronary and peripheral thrombolysis, as well as lysis in the venous circulation, in combination with fibrinolytics (e.g. urokinase, streptokinase, tPA and its derivatives); prevention or reduction of the thrombocyte decrease in the case of dialysis or extracorporeal circulation, as well as keeping open of arterial and venous cannulae and catheters, also together with prostacyclin and prostacyclin mimetics; prevention of the side effects arising in the case of the neutralisation of heparin with protamine sulphate; prevention of attacks in the case of unstable angina and TIA (transient ischaemic attacks) and in combinations with prostaglandins (e.g. PGE.sub.1); improvement of the kidney function in the case of various types of glomerulonephrites, in the case of systemic lupus erythrematosus, in the case of nephrotoxicities induced by cyclosporin-A or other medicaments and as consequence of a hydronephrosis; prevention of ischaemic organ damages in the case of shock; prevention of rejection crises in the case of organ transplants, as well as maintenance of organ function in vitro and improvement of the organ blood supply after transplants, improvement of the kidney function or reduction of the side effects in the case of combinations with diuretics of various types of action (e.g. loop diuretics); improvement of peripheral circulatory disturbances, also in combination with prostacyclin (mimetics) and other prostaglandins (e.g. PEG.sub.1); treatment and prophylaxis of gastrointestinal inflammations; prevention or weakening of asthma attacks and of bronchial hyperreactivity, also in combination with other anti-asthmatics (e.g. .beta.-mimetics, theophylline and glucocorticosteroids); for the treatment of eclampsia and inhibition of premature labour pains; treatment of brain infarcts and of subarachnoid haemorrhage; treatment of arythmias. In principle, the active material can be administered in the form of solid medicinal forms, such as e.g. tablets, pellets or dragees, or also of liquid medicinal formulations as injection or infusion solution.
In the course of the development of an injection solution produced according to usual processes from the sodium salt of the active material, it has been shown that these solutions are not vein compatible. The active material was administered in a relatively high concentration of 25 to 50 mg/ml, whereby the solutions used for injection purposes display a pH value of 9.6 to 9.8. In the case of use of such injection solutions, in many cases parietal thromboses occurred at the point of injection which have indicated the interarterial incompatibility of these solutions. In one case, incompatibilities arose in the case of a dosage of 250 mg/10 ml of sodium 4-[2-benzenesulphonylamino)-ethyl]-phenoxyacetate in the case of the treatment of shock lung in humans.
Furthermore, the problem existed that the active material sh
REFERENCES:
Kopia, G. A. et al., The J. of Pharmacology and Experimental Therapeut. 250 (3) Sep. 1989.
Demmer Fritz
Gruber Werner
Heller Werner
Woog Heinrich
Boehringer Mannheim GmbH
Killos Paul J.
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