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 prep
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.
대표청구항▼
1. A catheter balloon having a surface and composition applied thereto; wherein the composition comprises: at least one lipophilic anti-hyperplastic agent selected from paclitaxel, 7-(2′,3′-dihydroxypropyl oxycarbonyl)-paclitaxel, docetaxel, probucol, azithromycin, roxithromycin, heparin, prostacycl
1. A catheter balloon having a surface and composition applied thereto; wherein the composition comprises: at least one lipophilic anti-hyperplastic agent selected from paclitaxel, 7-(2′,3′-dihydroxypropyl oxycarbonyl)-paclitaxel, docetaxel, probucol, azithromycin, roxithromycin, heparin, prostacyclins, colchicine, epithilone, and rapamycin;wherein said balloon surface does not contain a pharmacological polymer, andwherein said composition is of a form suitable for administration into a blood vessel section;wherein the composition contains a solubility promoter that does not form micelles. 2. The catheter balloon according to claim 1, wherein said at least one lipophilic anti hyperplastic agent is rapamycin. 3. The catheter balloon according to claim 1, wherein said at least one lipophilic anti hyperplastic agent is paclitaxel. 4. The catheter balloon according to claim 1, wherein said composition further comprises an X-ray contrast agent selected from iodixanol, gadolinium-DTPA, GD-DO3A-butrol, iopromide, iohexol, and iopamidol. 5. The catheter balloon according to claim 4, wherein said X-ray contrast agent is iohexol. 6. The catheter balloon according to claim 1, wherein said composition further comprises a coagulation inhibitor, a platelet aggregation inhibitor, an enzyme inhibitor, and/or a calcium chelator. 7. The catheter balloon according to claim 1, wherein said at least one lipophilic anti hyperplastic agent irreversibly or reversibly binds to tissue at a minimum percentage of 10%. 8. The catheter balloon according to claim 1, wherein said at least one lipophilic anti hyperplastic agent is paclitaxel, docetaxel, or 7-(2″,3″-dihydroxypropyl oxycarbonyl)-paclitaxel. 9. A method for restenosis prevention in a patient, comprising administering to said patient a composition from the catheter balloon according to claim 1. 10. A catheter balloon having a surface and a coating applied thereto wherein said coating is a dried layer obtained from a solution consisting essentially of: at least one lipophilic anti-hyperplastic agent selected from paclitaxel, 7-(2″,3″-dihydroxypropyl oxycarbonyl)-paclitaxel, docetaxel, probucol, azithromycin, roxithromycin, heparin, prostacyclins, colchicine, epithilone, and rapamycin;at least one solvent;optionally at least one X-ray contrast agent selected from iodixanol, gadolinium-DTPA, GD-DO3A-butrol, iopromide, iohexol, and iopamidol; andoptionally a coagulation inhibitor, a platelet aggregation inhibitor, an enzyme inhibitor, and/or a calcium chelator;wherein said balloon surface does not contain a pharmacological polymer; andwherein the composition contains a solubility promoter that does not form micelles. 11. The catheter balloon according to claim 10, wherein said at least one lipophilic anti hyperplastic agent is rapamycin. 12. The catheter balloon according to claim 10, wherein said at least one lipophilic anti hyperplastic agent is paclitaxel.
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