鞘内给予脂质体布比卡因制剂在大鼠体内的抗伤害作用。

Antinociceptive Effect of Liposomal Bupivacaine Formulations After Intrathecal Administration in Rats.

出版信息

Turk J Med Sci. 2019 Feb 11;49(1):429-434. doi: 10.3906/sag-1806-200.

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7350835/

Abstract

BACKGROUND/AIM: Based on our previous in vitro study with multilamellar liposomal bupivacaine (MLB) versus bupivacaine alone in artificial cerebrospinal fluid, we aimed to investigate in vivo antinociceptive effect of intrathecal MLB by determining tail flick latency (TFL) time after thermal stimulation in rats.

MATERIALS AND METHODS

After preparing MLB and high-yield drug entrapment in liposome (HYDEL) bupivacaine, 18 female Wistar rats were assigned to 3 groups as control (bupivacaine) and study groups (MLB and HYDEL bupivacaine) including 6 rats in each group to administer these drugs intrathecally. Antinociceptive activity was determined in terms of TFL time after thermal stimulation. Maximum possible effect (MPE) calculated from TFL times and rats with motor block were documented.

RESULTS

TFL times after intrathecal injection of HYDEL bupivacaine were significantly longer than that of the control and MLB groups (P < 0.05) and returned to baseline 180 min after intrathecal injection. MPE (100%) with intrathecal HYDEL bupivacaine occurred between 10 to 45 min. Afterwards, MPEs were 70% and 50% for the control and MLB groups, respectively. Motor block disappeared after 20 min in the study groups while it lasted 75 min in the control.

CONCLUSION

Intrathecal administration of MLB and HYDEL bupivacaine in rats resulted in longer duration of antinociceptive activity with shorter motor block duration.

摘要

背景/目的：基于我们之前在人工脑脊液中用多层脂质体布比卡因（MLB）与布比卡因进行的体外研究，我们旨在通过测定热刺激后大鼠的尾巴拍打潜伏期（TFL）时间来研究鞘内 MLB 的体内镇痛效果。

材料和方法

在制备 MLB 和高载药量包封脂质体布比卡因（HYDEL）布比卡因后，将 18 只雌性 Wistar 大鼠分为 3 组，即对照组（布比卡因）和研究组（MLB 和 HYDEL 布比卡因），每组 6 只大鼠，鞘内给予这些药物。通过 TFL 时间测定来评估镇痛活性。从 TFL 时间计算最大可能效应（MPE）并记录有运动阻滞的大鼠。

结果

HYDEL 布比卡因鞘内注射后的 TFL 时间明显长于对照组和 MLB 组（P < 0.05），并且在鞘内注射后 180 分钟恢复到基线。HYDEL 布比卡因鞘内注射的 MPE（100%）发生在 10 至 45 分钟之间。之后，对照组和 MLB 组的 MPE 分别为 70%和 50%。研究组的运动阻滞在 20 分钟后消失，而对照组持续了 75 分钟。