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在猫头 (Aotus spp.) 中对持续释放布普伦诺芬配方的药理动力学分析
Taylor A Sheridan1,2,3,4, Celia L Saney2,3,4, Amadis Vivas2,3,4
11University Research Animal Resources, Office of Research, University of Georgia, Athens, Georgia.
持续释放布伦诺芬 (BSR) 和Ethiqa XR (EXR) 在猫头中维持了72小时的治疗水平. 需要更高的EXR剂量才能达到人类的疗效值,并观察到一些副作用.
科学领域:
- 兽医药理学 兽医药理学
- 非人类灵长类动物 (NHP) 医学
- 药理动力学 药理动力学
背景情况:
- 布普伦诺芬是兽医中有效的阿片类止痛药.
- 常规布普伦诺芬的频繁剂量对于持续的治疗水平是必要的.
- 持续释放 (SR) 布普伦诺芬配方提供了更好的剂量方便性,但在NHP中的数据有限.
研究的目的:
- 在SR buprenorphine (BSR) 或Ethiqa XR (EXR) 皮下注射72小时后,在猫头中确定血布伦诺芬度.
- 评估这些配方是否保持了NHP中的治疗性布普伦诺芬水平.
主要方法:
- 猫头接受了0.2 mg/kg的单次皮下剂量BSR或EXR.
- 血布伦诺芬度在多个时间点测量,长达72小时.
- 评估了随后的剂量升级到0.3 mg/kg EXR.
主要成果:
- 无论是0.2 mg/kg BSR还是EXR,都保持了血布伦诺芬在72小时内超过NHP治疗值 (0.1 ng/mL).
- 0.2 mg/kg的剂量在72小时内没有维持度超过人类疗效值 (0.5 ng/mL).
- 在大多数子中,0.3 mg/kg的EXR剂量在72小时内达到并维持了>0.5 ng/mL的度,并增加了镇静和ptyalism.
结论:
- 单次皮下剂量为0.2 mg/kg的BSR或EXR有效地维持布普伦诺芬在72小时内超过NHP治疗值.
- 需要更高的EXR剂量 (0.3mg/kg) 来达到和维持在72小时内在猫头中超过人类疗效值的度.
- 剂量优化对于在NHP中实现延长释放布诺芬所需的治疗结果至关重要.
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