Locally administered preparation for prevention of restenosis or treatment of tumors, comprises lipophilic antihyperplastic active agent and vascular imaging agent in liquid formulation

摘要

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. 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. ACTIVITY : 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'). MECHANISM OF ACTION : None given in the source material.