Speck Ulrich, Scheller Bruno, Abramjuk Claudia, Grossmann Stephan, Mahnkopf Dirk, Simon Oliver
Department of Radiology, Charité, Humboldt University, Berlin, Germany.
Invest Radiol. 2004 Mar;39(3):182-6. doi: 10.1097/01.rli.0000116125.96544.64.
Paclitaxel added to angiographic contrast medium (CM) has been shown to inhibit restenosis in the porcine coronary overstretch model. This study determined early local tissue concentrations after the administration of different paclitaxel doses and preparations.
Fifteen pigs received 2 stents each in the left coronary artery. During and/or after the intervention, paclitaxel-containing CM or diluted Taxol was injected. Fifteen minutes after the last intracoronary injection, paclitaxel concentrations in the arterial wall and myocardium were measured by high-performance liquid chromatography.
Mean paclitaxel concentrations in the left coronary arteries reached 3-10 microM. Higher volumes and higher paclitaxel concentrations resulted in higher tissue concentrations. Paclitaxel in CM was better tolerated and led to higher local concentrations than diluted Taxol. Low paclitaxel concentrations in the uninjected right coronary artery and in plasma indicate selectivity.
When admixed to CM, paclitaxel results in local tissue concentrations proportional to the amount of the drug injected.
已证明在血管造影剂（CM）中添加紫杉醇可抑制猪冠状动脉过度伸展模型中的再狭窄。本研究测定了给予不同剂量和制剂的紫杉醇后的早期局部组织浓度。
15只猪在左冠状动脉各植入2个支架。在干预期间和/或之后，注射含紫杉醇的CM或稀释的紫杉醇。最后一次冠状动脉内注射后15分钟，通过高效液相色谱法测量动脉壁和心肌中的紫杉醇浓度。
左冠状动脉中的平均紫杉醇浓度达到3 - 10微摩尔。更大的体积和更高的紫杉醇浓度导致更高的组织浓度。与稀释的紫杉醇相比，CM中的紫杉醇耐受性更好且导致更高的局部浓度。未注射的右冠状动脉和血浆中的低紫杉醇浓度表明具有选择性。
当与CM混合时，紫杉醇导致局部组织浓度与注射的药物量成比例。
