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在Pedunculoside及其Beta-CD聚合物包容复合物的体外稳定性和药理动力学研究

Liang Wu^1,2, Danfeng Li¹, Peijing Wang¹

¹School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China.

|May 25, 2024

概括

一种新型β-环氧烯聚合物复合物 (pedunculoside-βCDP) 通过改善血暴露和减少排泄,增强了潜在的心血管药物pedunculoside的生物可用性和药物动力学特征.

科学领域:

药理学药理学是指药理学的学科.
药物运输药物运输药物运输
自然产品自然产品

背景情况:

来自伊莱克斯物种的三二烯沙波宁Pedunculoside在心血管疾病方面显示出有前途.
临床使用受到生物可用性差,快速排泄和肠道广泛代谢到轮酸的限制.

研究的目的:

准备一个水溶性纳入复杂的pedunculoside与β-cyclodextrin聚合物 (pedunculoside-βCDP).
为了比较pedunculoside和pedunculoside-βCDP的体外稳定性和体内药理动力学行为.

主要方法:

准备和表征丁化物-βCDP.
在模拟的胃和肠液以及特定的肠道细菌中进行体外稳定性研究.
开发和验证一种LC-MS/MS方法,用于在老鼠血中量化pedunculoside和rotundic酸.
向大鼠静脉注射佩登古赛德和佩登古赛德-βCDP,以评估药物动力学参数.

主要成果:

这两种化合物在模拟的胃和肠液中都表现出良好的稳定性.
观察到Bifidobacterium adolescentis和Bifidobacterium breve具有显著的新陈代谢.
佩登古化物-βCDP显著改善了佩登古化物的药物动力学特征,增加了血暴露,降低了排泄率.
在肠道中,pedunculoside的代谢被βCDP复合物降低.

结论:

Pedunculoside-βCDP有效地增强了pedunculoside的药物动力学特性.
这种配方策略有可能推动pedunculoside在心血管治疗中的临床应用.
需要进一步研究pedunculoside-βCDP的代谢命运和药理动力学.

关键词:

这是LC-MS/MS.肠道代谢肠道代谢方法验证方法的验证方法.这种药物是 pedunculoside.pedunculosideβCDP的使用情况药物动力学行为

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