外用长效丁丙诺啡在新西兰大白兔体内的药动学评价。

Stephanie Thi, Gerry Hish, Tara L Martin, Xiangbo Kong, Patrick A Lester
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引用次数: 0

摘要

兔子通常被用作手术模型,因此需要止痛剂来缓解疼痛和优化动物福利。丁丙诺啡是一种部分微阿片类药物,市面上有各种浓度和缓释制剂,历史上一直被用作家兔镇痛药。一种外用长效丁丙诺啡制剂(Zorbium, Bup-TP)已被批准用于猫的镇痛,但尚未在家兔中进行评估。本研究对新西兰白兔(Oryctolagus cuuniculus) Bup-TP的血药浓度和药动学参数进行了评价。采用随机交叉设计,选取健康成年雄性新西兰白兔(n = 4)和雌性新西兰白兔(n = 4),分别给予高剂量(7 mg/kg)和低剂量(3 mg/kg) Bup-TP。在本研究中,Bup-TP在给药后0.5小时开始在成年新西兰大白兔中达到血浆血药浓度>0.25 ng/mL,并在给药后72小时保持不变。与基线相比,给药后粪便和尿量平均减少3.5天;在给药后平均10天,食物消耗减少。经过时间和支持性护理,一切都解决了。应用部位的任何家兔均未见明显病变。Bup-TP可能是一种有效、持久、无创的家兔镇痛方法。建议进一步研究以优化剂量和程序止痛效果。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Pharmacokinetic Evaluation of Topical Long-Acting Buprenorphine in New Zealand White Rabbits (Oryctolagus cuniculus).

Rabbits are commonly used as surgical models, thus requiring analgesics for painful procedures and optimal animal welfare. Buprenorphine, a partial µ opioid, is commercially available in various concentrations and sustained-release formulations and has historically been used as an analgesic in rabbits. A topical long-acting buprenorphine formulation (Zorbium, Bup-TP) has been approved for analgesic use in cats but has not yet been evaluated in rabbits. The present study evaluated the plasma concentrations and pharmacokinetic parameters of Bup-TP in New Zealand white rabbits (Oryctolagus cuniculus). Healthy adult male (n = 4) and female (n = 4) New Zealand white rabbits were used in a randomized crossover design and received a single high (7 mg/kg) and low (3 mg/kg) dose of Bup-TP. In this study, Bup-TP achieved a plasma blood concentration >0.25 ng/mL starting at 0.5 hours after dosing that was maintained up to 72 hours after dosing in adult New Zealand white rabbits. Compared with baseline, fecal and urinary output were reduced for an average of 3.5 days after dosing; food consumption was reduced for an average of 10 days after dosing. All resolved with time and supportive care. No lesions were grossly visible on any rabbit at site of application. Bup-TP may be an effective, long-lasting, and noninvasive method of providing analgesia in rabbits. Future study is recommended to optimize dosing and procedural analgesic efficacy.

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