摘要
目的研究布比卡因聚乳酸微球在家兔体内的药代学和药效学。方法新西兰兔16只,随机分为2组:皮下注射布比卡因注射液5 mg/kg(A组,n=8),皮下植入布比卡因聚乳酸微球5mg/kg(B组,n=8)。高效液相色谱法(HPLC)测定血浆中布比卡因浓度。采用仿豚鼠皮丘法建立动物模型进行局麻药效学测定。结果 血药浓度变化显示,A组血药浓度迅速达到峰值,且浓度较高,Cmax=2.4664μg/ml,随后浓度快速下降。B组血药浓度相对较平稳,达峰较晚,Cmax=0.7781 μg/ml,且血药浓度一直维持较低水平,平均滞留时间(MRT)明显延长(P<0.05)。药效学发现布比卡因微球组的局麻作用时间较布比卡因注射液组明显延长(P<0.05)。结论 药代学和药效学结果说明布比卡因微球在家兔体内具有缓释作用。
Objective To evaluate the pharmacokinetics and pharmacodynamics of bupivacaine polylactic acid microspheres in rabbits. Methods Sixteen New Zealand rabbits weighing (2.58±0.17) kg were randomly divided into two groups:in group A a bolus of bupivacaine solution 5 mg·kg-1 was injected subcutaneously, in group B a bolus of bupivacaine polylactic acid microspheres 5 mg · kg-1 was implanted in subcutaneous tissue. Blood samples were obtained for determination of plasma bupivacaine concentration at 5,10,20,30,45 min and 1,2,3,4, 6,8,12,24h after subcutaneous injection in group A and at 0.5,1,2,3,4,5,6,8,12,24,36,48 and 60 h after subcutaneous implantation in group B. Pharmacodynamics study was conducted using a model evaluating the efficacy of regional anesthesia by skin incision and needle pricking. Results In group A plasma bupivacaine concentration peaked quickly at about 0. 34h after subcutaneous injection, then quickly declined and became indetectable in plasma within 12 h. In group B plasma bupivacaine concentration reached a peak much slowly at about 13h after subcutaneous implantation. Cmax was 0.7781 ± 0.3573 μg·ml-1 significantly lower than that in group A [Cmax = (2.4664 ± 0.7822) μg·ml-1 ] . The mean retention time (MRT) was 25.2667 ± 2.4857 h, significantly longer than that in group A [MRT= (5.5580 ± 1.3843)h] . Pharmacodynamic study showed that the duration of regional sensory block was significantly longer in group B than that in group A( P < 0.05) . Conclusion Bupivacaine polylactic acid microspheres have sustained release effect in rabbits and can be used as super- long-acing local anesthetic.
出处
《中华麻醉学杂志》
CAS
CSCD
北大核心
2004年第3期206-208,共3页
Chinese Journal of Anesthesiology
