Prolongation of Spinal Anesthesia with Bupivacaine-Loaded (DL-Lactide) Microspheres
Prolongation of Spinal Anesthesia with Bupivacaine-Loaded (DL-Lactide) Microspheres
复制标题
使用布比卡因（DL-丙交酯）微球延长脊髓麻醉时间
作者：
J. Estebe;P. Corre;Y. Mallédant;F. Chevanne;R. Leverge
开发一种持续释放的局部麻醉剂制剂以提供持久的麻醉并降低全身毒性具有相当大的兴趣。在脊髓注射后评价了两种不同类型的聚乳酸微球（PLA 1和PLA 2）中负载的10 mg布比卡因（B），并与2 mg普通布比卡因（p B）进行比较。实验在六只新西兰兔身上进行。与pB相比，PLA 1的运动阻滞持续时间显著延长（177.5 +/- 79.5 min vs 44.6 +/- 18.0 min; P < 0.05），恢复时间也显著延长（545.0 +/- 299.6 min vs 44.2 +/- 21.5 min; P < 0.05）。PLA 2的持续时间和恢复时间未延长。通过使用高效液相色谱法从血液样品测量鞘内注射后B的全身释放。pB和PLA 1之间的最大B血浆浓度无显著差异（326 +/- 81 mg/mL vs 321 +/- 57 ng/mL）。达到最大血浆浓度所需的时间（6.6 +/- 2.6 min vs 41.7 +/- 20.4 min; P < 0.05）有显著差异。本研究表明，使用布比卡因（DL-丙交酯）微球可以延长脊髓运动阻滞。（Anesth Analg 1995;81：99-103）
There is considerable interest in developing a sustained-release local anesthetic formulation to provide long-lasting anesthesia and to decrease systemic toxicity. Bupivacaine (B), 10 mg, loaded in two different types of polylactide microspheres (PLA1 and PLA2) was evaluated after spinal injection and compared with plain bupivacaine (pB), 2 mg. Experiments were performed in six New Zealand rabbits. Duration of motor block was significantly prolonged for PLA1 compared to pB (177.5 +/- 79.5 min vs 44.6 +/- 18.0 min; P < 0.05), as well as for the recovery time (545.0 +/- 299.6 min vs 44.2 +/- 21.5 min; P < 0.05). The duration and recovery were not prolonged for PLA2. Systemic release of B after intrathecal injection was measured from blood samples by using high-performance liquid chromatography. There was no significant difference in maximum B plasma concentration between pB and PLA1 (326 +/- 81 mg/mL vs 321 +/- 57 ng/mL). The time taken to reach the maximum plasma concentration (6.6 +/- 2.6 min vs 41.7 +/- 20.4 min; P < 0.05) was significantly different. This study demonstrated that the use of bupivacaine-loaded (DL-lactide) microspheres can prolong spinal motor block. (Anesth Analg 1995;81:99-103)