罗哌卡因PLGA微球在小鼠坐骨神经旁的缓释作用  

THE SUSTAINED-RELEASE OF ROPIVACAINE PLGA MICROSPHERES IN THE MOUSE SCIATIC NERVE

作　　者：田洪居[1] 陈仲清[2] 刘永前[1] 刘玲玲[1] 

机构地区：[1]厦门市第二医院麻醉科,厦门361026 [2]南方医科大学附属南方医院SICU,广州510515

出　　处：《中国疼痛医学杂志》2010年第5期296-299,共4页Chinese Journal of Pain Medicine

摘　　要：目的:研究罗哌卡因PLGA微球(ROP-PLGA-MS)在小鼠坐骨神经旁的缓释作用。方法:昆明小鼠110只,随机均分为A、B两组,给药侧坐骨神经旁分别植入ROP-PLGA-MS和罗哌卡因PL-GA空白微球混合物(ROP/PLGA-MS);对照侧均植入PLGA空白微球(PLGA-MS),建立动物模型(每侧植药量800mg/Kg)。各组小鼠均随机分11组(n=5),分布于给药后5min、15min、30min、1h、2h、3h、4h、10h、18h、30h、48h时间点,采用热踏板法及4-point scale评分测定坐骨神经阻滞时效,高效液相色谱法(HPLC)测定血药浓度。结果:两组小鼠坐骨神经阻滞结果发现A组的局麻药阻滞时间较B组延长约10倍。血药浓度变化显示:A组3h后测罗哌卡因,血药浓度相对平稳,达到峰值时间晚,峰值(Cmax)=129.80±259.70ng/ml,且血药浓度一直维持较低水平。B组在5min时血浆即可测及较高浓度罗哌卡因,并迅速达到Cmax=1559.00±123.39ng/ml,其后快速下降。结论:ROP-PLGA-MS在小鼠体内具有缓释作用,有效延长罗哌卡因时效,且血药浓度低,毒性小。Objective： To study the sustained-release effect of ropivacaine PLGA microspheres（ROP-PLGA-MS） nearby the mouse sciatic nerve.Methods： 110 Kunming mice were randomly divided into A,B group（n=55）.The drug sides of group A were implanted with ROP-PLGA-MS nearby the sciatic nerves,the group B were implanted with the mixtures of Ropivacaine and blank PLGA microspheres（ROP/PLGA-MS）,and the control sides were all implanted with the placebo microspheres（PLGA-MS）,the implanted volume of each side was 800mg/kg.Each group was randomly divided into eleven sub-group according to（n=5） the time point（5min,15min,30min,1h,2h,3h,4h,10h,18h,30h and 48h） after administration.The efficacy of the drug was determined by measure the sensory and motor nerve blockade by the hot plate test and 4-point scale.The blood concentration of drug was measured by the high-performance liquid chromatography（HPLC） in corresponding time point.Results： The blockade effect of sciatic nerve was found that ROP-PLGA-MS caused sensory and motor never block more than 30 hours,and that ROP/PLGA-MS caused sensory and motor never block less than 3 hours.Plasma concentration changes suggest that the micro-ropivacaine were detected in plasma of group A mice,and reach the peak（Cmax） slowly in 10h,Cmax = 129.80±259.70ng/ml,plasma concentration of ropivacaine maintained a relatively low level,drug stay about 30 hours.In Group B the higher plasma concentrations of ropivacaine can be detected in 5min,and reach Cmax（1559.00±123.39ng/ml） quickly,then decreased rapidly.Conclusion： ROP-PLGA-MS has sustained release effect in mice and can prolonged analgesia of ropivacaine with little toxicity.

关 键 词：小鼠 罗哌卡因PLGA微球 植入 坐骨神经 神经阻滞 

分 类 号：R614[医药卫生—麻醉学]