罗哌卡因-醋酸地塞米松聚乳酸羟基乙酸共聚物微球药效学和

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1、·502·%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%南方医科大学学报(J%South%Med%Univ)%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%%2010;30(3)罗哌卡因-醋酸地塞米松聚乳酸羟基乙酸共聚物微球药效学和药动学的观察余让辉1，陈仲清1，陈辉1，傅卫军1，徐岩2（1南方医科大学南方医院麻醉科，广东广州510515；2中国人民解放军第四二一医院173临床部，广东广州516001）摘要：目的罗哌卡因和地塞米松聚乳酸-羟基乙酸微球小鼠坐骨神经旁包埋的药效学和药

2、动学的研究。方法165只雌性昆明小鼠随机均分为A、B、C三组，各组分别于坐骨神经旁包埋罗哌卡因-醋酸地塞米松聚乳酸-羟基乙酸微球(ROP-DXM-PLGA-MS)、罗哌卡因聚乳酸-羟基乙酸微球(RoP-PLGA-MS)、空白乳酸-羟基乙酸微球（PLGA-MS）400%mg-1。每组植入微球后按0.5、1、2、4、8、12、24、36、48、72、96%h时间点，以小鼠热踏板法检测小鼠埋药侧小鼠舔后足·kg的潜伏期为痛阈指标值的变化评价微球镇痛效果，每个时间点测定5只小鼠；小鼠热踏板测定结束后摘眼球取血，采用HPLC测定给药后各时间点血浆罗哌卡因浓度。结果药效学实验表明ROP-DXM-PLGA

3、-MS组麻醉镇痛时间达72%h以上较RoP-PLGA-MS组36%h明显延长（P<0.01)，空白微球未显示麻醉镇痛作用；药动学实验显示A、B两组罗哌卡因药动学参数Cmax、Tmax、AUC、MRT、t分别为117.8和119.8%ng·ml-1，24和12%h，8793.2和6861.15%ng·h·ml-1，43.74911/2和38.7743%h，65.799和46.166%h，A、B、C三组均未测到地塞米松血药浓度数据，C组罗哌卡因和地塞米松血药浓度均未测到。结论罗哌卡因聚乳酸-羟基乙酸微球中包入地塞米松可明显延长罗哌卡因的麻醉镇痛作用。关键词：罗哌卡因；醋酸地塞米松；微球；乳酸-羟

4、基乙酸共聚物；高效液相色谱法；药效学；药动学中图分类号：R969.1%%%%%%%%文献标识码：A%%%%%%%%文章编号：1673-4254（2010）03-0502-04Pharmacokineticsandpharmacodynamicsofpoly(lactide-co-glycolide)microspherescontainingropivacaineanddexamethasoneforsciaticnerveblockinmiceYU%Rang-hui1,%CHEN%Zhong-qing1,%CHEN%Hui1,%FU%Wei-jun1,%XU%Yan21Department

5、%of%Anesthesiology,%Nanfang%Hospital,%Southern%Medical%University,%Guangzhou%510515,%China;%2173%Clinical%Department,%421%Hospital%of%PLA,%Guangzhou%516001,%ChinaAbstract:ObjectiveTo%investigate%the%pharmacokinetics%and%pharmacodynamics%of%poly(lactide-co-glycolide)%microspheres%containing%ropivaca

6、ine%and%dexamethasone%for%sciatic%nerve%block%in%mice.%MethodsA%total%of%165%female%mice%were%randomly%assigned%into%3%groups,%namely%dexamethasone-loaded%ropivacaine%microsphere%group%(group%A,%n=55),%ropivacaine%microsphere%group%(group%B,%n=55)%and%PLGA%microsphere%group%(group%C,%n=55).%The%mic

7、e%received%surgical%implantation%of%the%corresponding%preparations%near%the%sciatic%nerve%at%the%dose%of%400%mg/kg.%Hot%plate%test%was%used%to%evaluate%the%anesthetic%effect%of%these%microspheres%at%differe