聚丙交酯-乙交酯微球包裹罗哌卡因和地塞米松用于小鼠坐骨神经阻滞的药代动力学和药效学研究

[Pharmacokinetics and pharmacodynamics of poly (lactide-co-glycolide) microspheres containing ropivacaine and dexamethasone for sciatic nerve block in mice].

作者信息

Yu Rang-hui, Chen Zhong-qing, Chen Hui, Fu Wei-jun, Xu Yan

机构信息

Department of Anesthesiology, Nanfang Hospital, Southern Medical University, Guangzhou, China.

出版信息

Nan Fang Yi Ke Da Xue Xue Bao. 2010 Mar;30(3):502-5.

PMID:20335120

Abstract

OBJECTIVE

To investigate the pharmacokinetics and pharmacodynamics of poly (lactide-co-glycolide) microspheres containing ropivacaine and dexamethasone for sciatic nerve block in mice.

METHODS

A 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 mice 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 different time points after the implantation, and high-performance liquid chromatography (HPLC) was employed to determine plasma ropivacaine concentration.

RESULTS

Pharmacodynamic study showed that the duration of sciatic nerve sensory block was significantly longer in group A than in group B (P<0.05). The analysis of pharmacokinetics variables demonstrated that T(1/2) in group A was prolonged as compared with that of group B. No anesthetic effect was observed in group C.

CONCLUSION

Dexamethasone-loaded ropivacaine microspheres can significantly prolong the analgesic effect of ropivacaine in mice.

摘要

目的

研究含罗哌卡因和地塞米松的聚乳酸-羟基乙酸共聚物微球用于小鼠坐骨神经阻滞的药代动力学和药效学。

方法

将165只雌性小鼠随机分为3组，即载地塞米松罗哌卡因微球组（A组，n = 55）、罗哌卡因微球组（B组，n = 55）和聚乳酸-羟基乙酸共聚物微球组（C组，n = 55）。小鼠以400 mg/kg的剂量在坐骨神经附近接受相应制剂的手术植入。采用热板试验评估植入后不同时间点这些微球的麻醉效果，并用高效液相色谱法（HPLC）测定血浆罗哌卡因浓度。