兔蛛网膜下腔注射布比卡因PLGA缓释微球量效学研究  

Motor Effects of Spinal Administration of Sustained-Release Bupivacaine from PLGA Microspheres:A Dose-Response Study in Rabbits

作　　者：傅强[1] 王新华[2] 钟延强[3] 王鹏 高申[3] 张宏 

机构地区：[1]解放军总医院麻醉科,北京100853 [2]同济大学附属东方医院麻醉科,上海200120 [3]第二军医大学药学院药剂教研室,上海200433

出　　处：《解放军药学学报》2007年第2期97-99,共3页Pharmaceutical Journal of Chinese People's Liberation Army

摘　　要：目的 比较布比卡因注射液和布比卡因聚乳酸-聚羟乙酸嵌段共聚物（PLGA）缓释微球在兔蛛网膜下腔注射的运动阻滞时间、强度。方法 布比卡因PLGA微球采用乳化溶媒蒸发法制备，直径大小在50～135txm左右。24只新西兰兔随机分为3组（n=8）。组Ⅰ注射生理氯化钠溶液和无药微球后注射2．5mg布比卡因注射液，3d后注射2．5mg布比卡因（PLGA）缓释微球，组Ⅱ注射5mg布比卡因注射液，3d后注射5mg布比卡因PLGA缓释微球。组Ⅲ注射10mg布比卡因，3d后注射10mgPL—GA布比卡因缓释微球。运动神经阻滞效果采用行走运动障碍作为观察指标并进行评级。结果注射生理氯化钠溶液和无药微球后，新西兰家兔无运动功能障碍。注射10mg布比卡因微球与10mg布比卡因注射液，均可提供完全运动神经阻滞，布比卡因微球阻滞时间较布比卡因注射液明显延长。注射5、2．5mg布比卡因微球与注射液运动阻滞不完全，布比卡因微球组运动神经阻滞时间短于布比卡因注射液。结论 布比卡因微球运动阻滞效果很大程度上取决从微球中突释出来的布比卡因药量。Aim To study the dose-motor response effect of spinal administration of sustained-release PLGA bupivacaine in rabbits. Methods Bupivacaine-loaded microspheres and drug-free microspheres 50 - 150μm in size were devised from poly-（ lactic-co-glycolic ） acid （PLGA） by using an emulsifying-solvent evaporation method. The effects of bupivacaine and of similar amounts of bupivacaine-loaded microspheres were studied in 24 rabbits as follows： 0.9% sodium chloride, followed by drug-free microspheres, then 2.5 mg of bupivacaine and 2.5mg of bupivacaine -loaded microspheres （ Group Ⅰ ; n = 8 ）, 5mg of bupivacaine, then 5 mg of bupivacaine -loaded microspheres （ Group Ⅱ ; n = 8 ） , and 10 mg of bupivacaine and 10mg of bupivacaine-loaded microspheres （ Group Ⅲ ; n = 8 ）. Motor block was evaluated blindly by observing walking disturbances, using a scale from 0 （ free movements） to 3 （ total limb paralysis）. A period of 3 days elapsed between each injection. Results No limitation on movements was observed after 0.9% sodium chloride and drug-free microspheres injection. With 10mg, both bupivacaine solutions provided complete motor block, which was significantly more prolonged with bupivacaine-loaded microspheres than bupivacaine. With 5 and 2.5 mg, block intensity was less marked, and block duration was shorter after administration of bupivacaine-loaded microspheres than after bupivacaine. Conclusion Motor blocks resulting from bupivacaine-loaded microspheres depend largely on the amount of drug initially released by the polymer.

关 键 词：布比卡因 微球 蛛网膜下腔注射 量效反应 

分 类 号：R965[医药卫生—药理学]