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一种可注射的基于oleogel的bupivacaine配方,用于长期的非阿片类药物术后止痛
Susan Wojtalewicz1, Jack Shuckra2, Keelah Barger2
1Rebel Medicine Inc, 48 S Rio Grande St., Salt Lake City, UT, 84101, USA. susanwojt@gmail.com.
这项研究开发了一种新的注射布皮瓦卡因 (bupivacaine) 凝,用于延长术后疼痛缓解. 该配方在临床前模型中证明了安全有效的多天止痛,为阿片类药物提供了有希望的替代品.
科学领域:
- 麻醉学 麻醉学
- 制药科学 制药科学
- 生物材料是一种生物材料.
背景情况:
- 阿片类止痛药是术后疼痛的标准,但具有严重的风险,如成和过量服用.
- 局部麻醉剂提供有效的疼痛控制,但受到短期持续时间的限制.
- 需要长期起作用的,安全的替代物来治疗术后疼痛.
研究的目的:
- 为多天的术后疼痛管理特征一个优化的注射性oleogel-basedbupivacaine配方.
- 在临床相关的猪模型中评估这种配方的体内疗效和安全性.
- 评估其作为一次性使用的长效局部麻醉剂的潜力.
主要方法:
- 关于稳定性,可注射性,药物加载和释放动力学的oleogel配方的基板表征.
- 在使用局部灌注和超声波引导的外围神经块的猪模型中对配方的体内评估.
- 对局部麻醉剂系统毒性的药理动力学分析和安全性评估.
主要成果:
- 油凝配方表现出理想的特性:稳定,可注射,高药载荷,持续释放超过5天.
- 通过局部灌注和神经阻塞的管理,通过局部灌注和神经阻塞的管理,实现了统计学上显著的多天止痛.
- 与对照组相比,药理动力学显示Cmax没有显著差异,即使在较高剂量下也没有观察到全身毒性.
结论:
- 可注射的基于oleogel的bupivacaine配方在临床前是安全和有效的,用于多天的术后疼痛管理.
- 这种配方显示出作为一次性使用,长效局部麻醉剂的潜力,适用于本地和区域应用.
- 它代表了阿片类药物的可行替代品,用于治疗术后疼痛,降低相关风险.
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