KOHANE DANIEL S.;SAGIE ITAY;SIMONS EMMANUEL J.;MASSACHUSETTS INSTITUTE OF TECHNOLOGY;CHILDREN'S MEDICAL CENTER CORPORATION
发明人:
KOHANE DANIEL S.,SAGIE ITAY,SIMONS EMMANUEL J.
申请号：
US20090993759
公开号：
US8658699(B2)
申请日:
2009.05.19
申请国别(地区):
美国
年份:
2014
代理人:
摘要：
Chemical permeation enhancers (CPEs) improve access of local anesthetics to the nerve, thereby improving their performance. Surfactants, representing three CPE sub-groups: anionic, cationic, and nonionic surfactants, were co-injected with tetrodotoxin (TTX) or bupivacaine at the sciatic nerve of Sprague-Dawley rats. All enhancers produced marked concentration-dependent improvements in the frequency and duration of block with TTX but not bupivacaine. An in vitro toxicity assay showed a wide range of CPE myotoxicity, but in vivo histological assessment showed no signs of muscle or nerve damage at concentrations of CPEs that produced a half-maximal increase in the duration of block of TTX. There was no systematic relationship between the enhancers' charge or hydrophobicity and their enhancement of block duration or potency. Thus, CPEs can provide marked prolongation of nerve blockade from TTX, without apparent local tissue toxicity, and therefore enhance the clinical applicability of TTX for prolonged-duration local anesthesia.
