公开(公告)号：US06326020B1

公开(公告)日：2001-12-04

申请号：US09079622

申请日：1998-05-15

申请人： Daniel S. Kohane ,  Charles B. Berde ,  Gary Strichartz ,  Robert S. Langer

发明人： Daniel S. Kohane ,  Charles B. Berde ,  Gary Strichartz ,  Robert S. Langer

IPC分类号： A61F200

摘要： Combinations of naturally occurring site 1 sodium channel blockers, such as tetrodotoxin (TTX), saxitoxin (STX), decarbamoyl saxitoxin, and neosaxitoxin (referred to jointly herein as “toxins”), with other agents, have been developed to give long duration block with improved features, including safety and specificity. In one embodiment, duration of block is greatly prolonged by combining a toxin with a local anesthetic, vasoconstrictor, glucocorticoid, and/or adrenergic drugs, both alpha agonists (epinephrine, phenylephrine), beta-blockers (propranalol), and mixed central-peripheral alpha-2 agonists (clonidine), or other agents. In another embodiment, the duration of nerve block from toxin can be greatly enhanced by the inclusion of amphiphilic or lipophilic solvents. In still another embodiment, the effectiveness of these compositions is enhanced by microencapsulation within polymeric carriers, preferably biodegradable synthetic polymeric carriers. Modality specific nerve block can be obtained using combinations of toxin with vanilloids.

摘要翻译： 已经开发出天然存在的1位钠通道阻断剂如河豚毒素（TTX），沙毒素（STX），脱氨甲酰沙司苏辛和新西沙毒素（本文共同称为“毒素”）与其他药物的组合，以产生长期阻滞 具有改进的特征，包括安全性和特异性。 在一个实施方案中，通过将毒素与局部麻醉剂，血管收缩剂，糖皮质激素和/或肾上腺素能药物α激动剂（肾上腺素，去氧肾上腺素），β-阻滞剂（propranalol）和混合的中枢外周 α-2激动剂（可乐定）或其它药剂。 在另一个实施方案中，通过包含两亲或亲脂性溶剂可以大大增强来自毒素的神经阻滞的持续时间。 在另一个实施方案中，这些组合物的有效性通过聚合物载体（优选可生物降解的合成聚合物载体）内的微囊化来增强。 可以使用毒素与香草素的组合获得形态特异性神经阻滞。