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在使用UPLC-MS/MS对大鼠口服和静脉注射后对普尼卡拉的药理学研究

Zhanying Chang¹, Guihua Liu², Zixin Chen³

¹Pharmacy College of Xinjiang Medical University, Urumqi, Xinjiang 830017, China; The State Key Laboratory for the Cause and Prevention of High Morbidity was jointly established in Central Asia, Urumqi, Xinjiang 830011, China.

Journal of chromatography. B, Analytical technologies in the biomedical and life sciences

|October 31, 2025

概括

榴中的关键化合物尼卡拉 (PUN) 在老鼠中显示缓慢的排泄和低的口服生物利用性. 这项研究描述了它的药理动力学,揭示了剂量依赖的吸收和广泛的组织分布,以获得临床前见解.

科学领域:

药理学和药理动力学药理学和药理动力学
自然产品化学自然产品化学
药物的新陈代谢和处置

背景情况:

普尼卡拉金 (PUN) 是石榴中主要的生物活性基素,以其潜在的健康益处而闻名.
在口服后对PUN的吸收,生物可用性和药理动力学存在有限的数据.
了解PUN的体内行为对于其治疗发展至关重要.

研究的目的:

开发和验证一种UPLC-MS/MS方法,用于量化大鼠血中的PUN.
在Sprague-Dawley大鼠的静脉和胃内给药后,描述PUN的药理学特征.
为了评估PUN的剂量比例性和生物可用性.

主要方法:

开发一种敏感的UPLC-MS/MS试验,用于PUN量化 (LLOQ:0.125μg/mL).
在一次性静脉注射 (10毫克/公斤) 和胃内 (100-400毫克/公斤) 后,在斯普拉格-道利大鼠中进行了药理动力学研究.
对血样本进行分析,以确定t1/2,Vd,Tmax,Cmax,AUC和绝对生物可用性等关键的药理学参数.

主要成果:

在静脉注射后,PUN表现出缓慢的排泄 (t1/2 = 6.45 ± 2.11 h) 和受限制的分布 (Vd = 0.94 ± 0.23 L/kg).
口服显示剂量依赖的吸收 (Tmax ≈2小时),绝对生物利用率极低 (3.22-5.38%).
在口服后观察到广泛的组织分布 (Vd = 14.0-44.5 L/kg) 和Cmax和AUC的剂量成比例增加.

结论:

开发的UPLC-MS/MS方法可靠地描述了PUN的药理动力学.
在老鼠中,PUN显示口服生物可用性较差,组织分布广泛.
这些发现为未来PUN的临床前和临床研究提供了重要的药理动力学数据.

关键词:

生物可用性生物可用性药物动力学药物动力学石榴果石榴果是一种在Punicalagin中使用.在 UPLC-MS/MS 中使用.

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