| 摘要 |
<p>#CMT# #/CMT# A new preparation (I), comprises: (A) at least one antihyperplastic active agent (A) with a partition coefficient between butanol and water of at least 0.5, in capillary-accessible liquid form; and (B) an agent (B) for improving venous and arterial imaging. #CMT# : #/CMT# An independent claim is also included for a preparation (II) containing at least one agent (A) (with partition coefficient as above), which is applied from a catheter. #CMT#ACTIVITY : #/CMT# Vasotropic; Cytostatic. 7-(2'',3''-Dihydroxypropoxycarbonyl)-paclitaxel) (A') (7 mg) was dissolved in ethanol then added to Ultravist (RTM; iopromide-based X-ray contrast agent; 370 mg/iodine per ml) (100 ml), to give an X-ray contrast agent (I') for restenosis prevention. In tests in anesthetized pigs with stent-induced arterial wall thickening, the degree of arterial thickening after 4 weeks in pigs treated with (I') was 50% of that in pigs treated with Ultravist (RTM) without addition of (A'). No side-effects were observed, despite the relatively high toxicity of (A'). #CMT#MECHANISM OF ACTION : #/CMT# None given in the source material. #CMT#USE : #/CMT# The use of (I) or (II) is claimed in the prevention of restenosis or the treatment of tumor diseases. #CMT#ADVANTAGE : #/CMT# (I) and (II) provide an effective local therapy of potentially hyperproliferative tissue, and are easy to handle and harmless to patients. The lipophilic active agents (A) are rapidly taken up in significant amounts by the vascular walls after local administration of (I) or (II), so that high systemic doses (with the risk of side-effects) are unnecessary. Typically paclitaxel (as (A)) is effective on local administration at 10% or less of the maximum acceptable systemic dose. If (B) is present, the need for additional administration of contrast agents is unnecessary. #CMT#PHARMACEUTICALS : #/CMT# Preferred Components: (A) is a cytostatic agent, corticoid, prostacyclin, antioxidant, antibiotic, cellular proliferation inhibitor or immunosuppressant, specifically a taxoid (especially pacitaxel or docetaxel), probucol, a porphyrin derivative, colchicine or epothilone. (B) is a blood vessel-compatible solution, suspension or emulsion, which improves the X-ray, ultrasonic, optical or magnetic resonance imaging of blood vessels or blood flow, preferably an X-ray contrast agent, especially Visipaque (RTM; iodixanol), Magnevist (RTM; gadolinium DPTA), Gadovist (RTM; Gd-DO3A-butrol), Ultravist (RTM; iopromide), Omnipaque (RTM; iohexol) or Solutrast (RTM; iopamidol). (I) or (II) optionally additionally contains a coagulation inhibitor, platelet aggregation inhibitor, enzyme inhibitor and/or calcium chelator. At least 10% of the active agent binds reversibly or irreversibly to tissue. The active agent or active agent-carrying component shows specific affinity for vascular walls. (I) or (II) optionally contains a non-micelle forming solubilizer.</p> |
