Motor and Blood Pressure Effects of Epidural Sustained-Release Bupivacaine from Polymer Microspheres: A Dose-Response Study in Rabbits
Motor and Blood Pressure Effects of Epidural Sustained-Release Bupivacaine from Polymer Microspheres: A Dose-Response Study in Rabbits
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聚合物微球硬膜外缓释布比卡因对运动和血压的影响：兔子剂量反应研究
DOI：
10.1097/00000539-199509000-00016
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发表时间：
1995
影响因子：
5.7
通讯作者：
R. Souron
中科院分区：
文献类型：
--
作者：
J. Malinovsky;J. Bernard;P. Le Corre;Jean;J. Lepage;R. Le Verge;R. Souron
将局部麻醉剂掺入可注射聚合物微球中可用于提供延长的区域效应。本随机研究旨在比较布比卡因和布比卡因载药微球对经皮注射家兔运动阻滞时程的影响。采用溶剂挥发/萃取法，以聚d，l-乳酸为原料，制备了1-10 μ m的布比卡因载药微球和无药微球。在26只家兔中研究了布比卡因和相似量的布比卡因载药微球的作用，如下：0.9%氯化钠，然后是无药物微球，然后是1.25 mg布比卡因和1.25 mg布比卡因载药微球5 mg布比卡因，然后2.5mg布比卡因负载的微球（组II; n = 8）;以及5 mg布比卡因和5 mg布比卡因负载的微球（组III; n = 10）。通过观察行走障碍，使用0（自由运动）至3（完全肢体瘫痪）的量表，盲法评价运动阻滞。每次注射之间间隔3天。注射0.9%氯化钠和无药物微球后，未观察到运动受限。在5 mg时，两种布比卡因溶液均提供完全运动阻滞，其中布比卡因载药微球的运动阻滞时间显著长于布比卡因（+244% +/-129%，平均值+/- SD）。与布比卡因相比，2.5和1.25 mg布比卡因微球的阻滞强度较低，阻滞持续时间较短。我们的结论是，从布比卡因加载微球产生的块是高度影响的聚合物最初释放的药物的量。（Anesth Analg 1995;81：519-24）
The incorporation of local anesthetics into injectable polymer microspheres can be useful in providing prolonged regional effects.This randomized study was designed to compare the effects of bupivacaine and bupivacaine-loaded microspheres on the time course of motor block in rabbits injected epidurally. Bupivacaine-loaded microspheres and drug-free microspheres 1-10 micro meter in size were devised from poly-d,l-lactic acid by using a solvent evaporation/extraction method. The effects of bupivacaine and of similar amounts of bupivacaine-loaded microspheres were studied in 26 rabbits as follows: 0.9% sodium chloride, followed by drug-free microspheres, then 1.25 mg of bupivacaine and 1.25 mg of bupivacaine-loaded microspheres (Group I; n = 8); 2.5 mg of bupivacaine, then 2.5 mg of bupivacaine-loaded microspheres (Group II; n = 8); and 5 mg of bupivacaine and 5 mg of bupivacaine-loaded microspheres (Group III; n = 10). Motor block was evaluated blindly by observation of walking disturbances, using a scale from 0 (free movements) to 3 (total limb paralysis). A period of 3 days elapsed between each injection. No limitation on movements was observed after 0.9% sodium chloride and drug-free microsphere injection. With 5 mg, both bupivacaine solutions provided complete motor block which was significantly more prolonged (+244% +/- 129%, mean +/- SD) with bupivacaine-loaded microspheres than bupivacaine. With 2.5 and 1.25 mg, block intensity was less marked, and block duration was shorter after administration of bupivacaine-loaded microspheres than after bupivacaine. We concluded that blocks resulting from bupivacaine-loaded microspheres are highly influenced by the amount of drug initially released by the polymer. (Anesth Analg 1995;81:519-24)