Carlsson K, Patwardhan A, Poullain J C, Gerentes I
Royal Institute of Technology, Stockholm.
J Mal Vasc. 1996;21 Suppl C:270-4.
The vein wall is nourished by diffusion of blood nutrients from the lumen and from the vasa vasorum. It is likely that drugs take the same ways to reach and diffuse through the vessel wall. Thus the uptake of a drug with affinity for the vein wall should give information on its transport to the tissue. This study aimed to explore troxerutin uptake by the long saphenous vein. Troxerutin is a naturally fluorescent flavonoid which has been known to improve subjective signs of patients with chronic venous insufficiency. Nine patients undergoing surgical treatment of varicosis were enrolled in the study. They received for the last 4 days before surgery either 3,500 mg of troxerutin (n = 4) or 1,000 mg twice daily (n = 2). Three patients as controls did not receive any drug. Two samples from thigh and calf long saphenous vein were harvested in each patients and investigated with a confocal laser scanning microscope developed by our institute measuring the fluorescence emitted by troxerutin after excitation by a 458 nm wavelength laser-beam. The intensity of the overall fluorescence was significantly higher in the treated groups (p < 0,001) and slightly higher in the patient who received 3,500 mg of troxerutin than with the lower dosage. The outer wall region provided the highest fluorescence in the treated group while a significant difference was observed in the fluorescence of the medial region between treated and control group. These results showed a marked affinity of troxerutin for the venous wall. The highest uptake in the outer wall region is likely to result from transport through vasa vasorum, owing to the rheologic properties of the drug. The significant medial fluorescence may account for the venous tone improvement with the drug.
静脉壁通过从管腔和血管滋养管扩散血液营养物质来获得营养。药物很可能通过相同的途径到达并扩散穿过血管壁。因此,对静脉壁具有亲和力的药物的摄取应该能提供其向组织转运的信息。本研究旨在探讨曲克芦丁被大隐静脉摄取的情况。曲克芦丁是一种天然荧光黄酮类化合物,已知可改善慢性静脉功能不全患者的主观症状。九名接受静脉曲张手术治疗的患者被纳入该研究。他们在手术前的最后4天,要么服用3500毫克曲克芦丁(n = 4),要么每天两次服用1000毫克(n = 2)。三名作为对照的患者未服用任何药物。在每位患者身上采集大腿和小腿大隐静脉的两个样本,并用我们研究所开发的共聚焦激光扫描显微镜进行研究,测量458纳米波长激光束激发后曲克芦丁发出的荧光。治疗组的整体荧光强度显著更高(p < 0.001),服用3500毫克曲克芦丁的患者的荧光强度略高于较低剂量组。治疗组中外壁区域的荧光最高,而治疗组和对照组之间在内侧区域的荧光观察到显著差异。这些结果表明曲克芦丁对静脉壁具有明显的亲和力。外壁区域的最高摄取量可能是由于药物的流变学性质通过血管滋养管转运所致。内侧显著的荧光可能解释了该药物对静脉张力的改善作用。