兔蛛网膜下腔注射布比卡因PLGA微球药代动力学研究  

Pharmacokinetics of intrathecally injected bupivacaine PLGA microspheres in rabbits

作　　者：傅强[1] 钟延强[2] 王新华[3] 张宏[1] 米卫东[1] 

机构地区：[1]解放军总医院麻醉手术中心,北京100853 [2]第二军医大学药剂学教研室,上海200433 [3]同济大学附属东方医院麻醉科,上海200120

出　　处：《军医进修学院学报》2009年第2期123-125,共3页Academic Journal of Pla Postgraduate Medical School

基　　金：国家自然科学基金资助项目(39870757)~~

摘　　要：目的:研究新西兰兔蛛网膜下腔注射布比卡因PLGA微球的药代动力学。方法:新西兰兔12只,随机分成2组,每组6只。对照组蛛网膜下腔注射盐酸布比卡因注射液,实验组蛛网膜下腔注射布比卡因PLGA微球混悬型注射剂,两组有效布比卡因剂量均为5mg/kg。高效液相色谱法(HPLC)测定血浆中布比卡因浓度。结果:对照组血药浓度在给药后0.5h达到峰值,Cmax为0.576μg/mL,随后浓度快速下降,至8h已检测不到药物浓度。微球组血药浓度在0.5h和2h产生两个峰值,峰浓度分别为0.332和0.290μg/mL,随后血药浓度下降缓慢并一直维持较低水平至48h,微球组两峰浓度(0.5h,2h)值显著低于对照组(P<0.05),微球组MRT明显长于对照组(P<0.05)。结论:蛛网膜下腔注射布比卡因PLGA微球在新西兰兔体内具有缓释作用。Objective： To study the pharmacokinetics of bupivacaine PLGA microspheres in rabbits. Methods： Twelve rabbits were randomly divided into groups A and B （n = 6）. Rabbits in group A were intrathecally injected with bupivacaine solution （5mg/kg）, rabbits in group B were intrathecally injected with bupivacaine PLGA microspheres （5mg/kg）. High performance liquid chromatography was used to determine the plasma concentration of bupivacaine. Results： In group A, the plasma concentration of bupivacaine reached its peak quickly about 0. 5h after subarachnoid space injection, the Cmax was 0. 567μg/mL. Then, the plasma concentration of bupivacaine quickly declined and became indetectable within 8h. In group B, the plasma concentration of bupivacaine PLGA microspheres reached its peak O. 5h and 2h, respectively, after injection bupivacaine PLGA microspheres, the Cmax was 0. 332 and 0. 290μg/mL, respectively. Then, the plasma concentration of bupivacaine PLGA microspheres slowly declined and became stable within 48h （ P 〈 0. 05 ）. The mean retention time （MRT） was significantly longer in group B than in group A （P 〈 0.05 ）. Conclusion： Incorporation of local anesthetics into injectable PLGA microspheres has a prolonged spinal anesthesia effect in rabbits.

关 键 词：布比卡因 蛛网膜下腔 给药系统 药代动力学 

分 类 号：R614[医药卫生—麻醉学] R916.42[医药卫生—外科学]