Preparation for the prophylaxis of restenosis

Abstract

The invention relates to a preparation for restenosis prevention. The preparations for restenosis prevention known as yet do not reach sufficient active agent concentrations in the affected sections of the vascular walls as higher doses cause undesirable side effects. The present invention is a preparation to which at least one antihyperplastic agent is added that has a distribution ratio between butanol and water .gtoreq.0.5. The lipophilic active agent is absorbed by the vascular wall fast and in sufficient quantity. The preparation may be a liquid that can pass through capillaries and may contain a contrast agent so that the active agent is transferred into the vascular wall without any additional effort while the usually required contrast radiograms are taken. The preparation may also be applied to a catheter.

1 . A preparation containing at least one antihyperplastic agent with a distribution ratio between butanol and water of ≧0.5 in liquid form suitable for passing through capillaries together with an agent for enhancing artery/vein imaging. 
     
     
         2 . A preparation containing at least one antihyper plastic agent with a distribution ratio between butanol and water of ≧0.5 that is applied to a catheter. 
     
     
         3 . A preparation in aqueous solution that may optionally contain additives as well as at least one antihyperplastic agent with a distribution ratio between butanol and water of ≧0.5 at a concentration that exceeds the saturation concentration in the purely aqueous medium wherein the active agent is not enclosed in micelles. 
     
     
         4 . The preparation according to  claim 1  wherein the antihyperplastic agent is a cytostatic, a corticoid, a prostacyclin, an antioxidant, an antibiotic, an agent inhibiting cell proliferation or an immunosuppressant. 
     
     
         5 . The preparation according to  claim 1  wherein the antihyperplastic agent is a taxoid. 
     
     
         6 . The preparation according to  claim 1  wherein the antihyperplastic agent is paclitaxel, docetaxel, probucol, a porphyrin derivative, colchicine or epithilone. 
     
     
         7 . The preparation according to  claim 1  wherein the agent for enhancing artery/vein imaging consists of solutions, suspensions or emulsions that the vessels can tolerate and that are used in Xraying, sonography, optical imaging, or magnetic resonance imaging for improved representation of the blood vessels or the bloodstream. 
     
     
         8 . The preparation according to  claim 1  wherein the agent for enhancing artery/vein imaging is an X-ray contrast medium. 
     
     
         9 . The preparation according to  claim 1  wherein the agent for enhancing artery/vein imaging is iodixanol (Visipaque), gadolinium-DTPA (Magnevist), Gd-DO3A-butrol (Gadovist), iopromide (Ultravist), iohexol (Omnipaque), or iopamidol (Solutrast) 
     
     
         10 . The preparation according to  claim 1 , characterized in that the preparation additionally contains coagulation inhibitors and/or platelet aggregation inhibitors and/or enzyme inhibitors and/or calcium chelators. 
     
     
         11 . The preparation according to  claim 1  wherein the active agent irreversibly or reversibly binds to tissue at a minimum percentage of 10%. 
     
     
         12 . The preparation according to  claim 1  wherein the active agent or the component carrying the active agent comprises a specific affinity to vascular walls. 
     
     
         13 . The preparation according to  claim 1  wherein the preparation contains a solubility promoter that does not form micelles. 
     
     
         14 . Use of the preparation according to  claim 1  for restenosis prevention. 
     
     
         15 . Use of the preparation according to  claim 1  for treating tumor diseases.