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背景:布比卡因广泛应用于治疗及缓解因手术、炎症、肿瘤等引起的急、慢性疼痛,其镇痛作用时间不能满足临床对药物缓慢释放延长镇痛时间的要求。目的:采用高效液相色谱法和仿豚鼠皮丘法,检测以高分子聚合物——聚乳酸为载体制成的布比卡因聚乳酸微球在家兔体内所具有的缓释效应。设计:完全随机对照动物实验。单位:解放军第二军医大学药学院。材料:新西兰兔16只,体质量(2.58±0.17)kg。干预:实验于2002-09/11在解放军第二军医大学药学院药剂教研室完成。①采用仿豚鼠皮丘法建立动物模型。①新西兰兔16只,随机分为两组,每组8只。注射组皮下注射布比卡因注射液5mg/kg;微球组皮下植入布比卡因微球5mg/kg。注射组兔于射液后5,10,20,30,45min,1,2,3,4,6,8,12,24h及微球组兔于给药后0.5,1,2,3,4,5,6,8,12,24,36,48和60h耳缘静脉采血1.5mL进行指标测定。③高效液相色谱法测定血浆中布比卡因浓度及进行药物缓释作用测定。主要观察指标:血浆中布比卡因浓度的变化和局麻药作用直径。结果:16只兔进入结果分析。①血药浓度变化结果:注射组血药浓度迅速达到峰值,且浓度较高,为2.4664mg/L,随后浓度快速下降。微球组血药浓度相对较平稳,达峰较晚,峰浓度=0.7781mg/L,且血药浓度一直维持较低水平,平均滞留时间明显延长(P<0.05)。②药效缓释作用结果:发现布比卡因微球组的镇痛作用时间较布比卡因注射液组明显延长(P<0.05)。结论:布比卡因微球制剂在家兔体内具有缓慢释放镇痛效应的作用。
BACKGROUND: Bupivacaine is widely used in the treatment and relief of acute and chronic pain caused by surgery, inflammation and tumor. Its analgesic effect can not meet the clinical requirement of slow release and prolonged analgesia. OBJECTIVE: To investigate the sustained-release effect of bupivacaine-loaded polylactic acid (PLA) microspheres made from macromolecule polymer-polylactic acid (PLLA) in rabbits by high performance liquid chromatography (HPLC) Design: Complete randomized controlled animal experiments. Unit: PLA Second Military Medical University School of Pharmacy. Material: New Zealand rabbits 16, body weight (2.58 ± 0.17) kg. Intervention: The experiment was carried out in pharmacy department of School of Pharmacy, Second Military Medical University, People’s Liberation Army from September to November 2002. ① using guinea pig skin method to establish animal model. ① New Zealand rabbits 16 were randomly divided into two groups of 8. Injection group, subcutaneous injection of bupivacaine 5mg / kg; microspheres subcutaneous implantation of bupivacaine microspheres 5mg / kg. Injection group rabbits after injection 5,10,20,30,45min, 1,2,3,4,6,8,12,24 h and microsphere group rabbits after administration 0.5,1,2,3,4 , 5,6,8,12,24,36,48 and 60h ear vein blood 1.5mL indicators were measured. ③ HPLC determination of plasma concentration of bupivacaine and drug release measured. MAIN OUTCOME MEASURES: Changes in the concentration of bupivacaine in plasma and the role of local anesthetic diameter. Results: Sixteen rabbits entered the result analysis. ① changes in plasma concentration results: the injection group plasma concentration peaked rapidly, and a higher concentration of 2.4664mg / L, followed by rapid decline in concentration. The concentration of plasma in the microspheres group was relatively stable with a peak at late peak concentration of 0.7781 mg / L. The plasma concentration remained at a low level for a long time and the average residence time was significantly prolonged (P <0.05). ② effect of sustained-release effect: found bupivacaine microsphere group analgesic effect than the bupivacaine injection group was significantly longer (P <0.05). Conclusion: Bupivacaine microspheres have a slow release analgesic effect in rabbits.