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溶剂和载体对圣草酚在大鼠体内药代动力学的影响。

Influences of Solubility and Vehicle Carriers on Eriodictyol Pharmacokinetics in Rats.

机构信息

U.S. Horticultural Research Laboratory, U.S. Department of Agriculture, Agricultural Research Service, 2001 S. Rock Road, Fort Pierce, Florida 34945, United States.

Laboratory of Nutrition, School of Pharmaceutical Sciences, São Paulo State University - UNESP, Araraquara 14800-903, SP, Brazil.

出版信息

J Agric Food Chem. 2022 Apr 20;70(15):4667-4676. doi: 10.1021/acs.jafc.2c00319. Epub 2022 Apr 8.

Abstract

In this study, the pharmacokinetics of oral doses of eriodictyol in 1% sodium carboxymethylcellulose and in saline/PEG400/Tween80 (75/20/5, v/v/v) in rats were compared. The pharmacokinetics of eriocitrin administered as a dissolved solution in water were also characterized. Metabolites of eriodictyol and eriocitrin in whole blood consisted mainly of eriodictyol, homoeriodictyol, and hesperetin glucuronides and ring-fission metabolites. In whole blood, no free nonconjugated flavanone aglycones were detected. Significant differences were observed in the pharmacokinetics of eriodictyol administered as a suspension in 1% sodium carboxymethylcellulose versus administration as a dissolved solution in saline/PEG400/Tween80 (75/20/5, v/v/v). At a dose of 25 mg kg eriodictyol administered with 1% sodium carboxymethylcellulose, a biphasic pharmacokinetic curve was observed, while only a single concentration peak was observed following an administration of 25 mg kg eriodictyol dissolved in saline/PEG400/Tween80 (75/20/5, v/v/v). For all trials, the pharmacokinetics of eriodictyol differed from those of eriocitrin dissolved in water.

摘要

在这项研究中,比较了大鼠口服 1% 羧甲基纤维素钠和生理盐水/PEG400/Tween80(75/20/5,v/v/v)中桃叶珊瑚苷的药代动力学。还描述了水溶解的橙皮苷给药后的药代动力学特征。橙皮苷和桃叶珊瑚苷在全血中的代谢物主要由橙皮苷、同型橙皮苷和橙皮素葡萄糖醛酸苷和环裂代谢物组成。在全血中,未检测到游离的非结合黄烷酮苷元。以悬浮液形式在 1% 羧甲基纤维素钠中给药的桃叶珊瑚苷与以溶解形式在生理盐水/PEG400/Tween80(75/20/5,v/v/v)中给药的桃叶珊瑚苷的药代动力学存在显著差异。在 25mg/kg 桃叶珊瑚苷以 1% 羧甲基纤维素钠给药时,观察到双相药代动力学曲线,而在以生理盐水/PEG400/Tween80(75/20/5,v/v/v)溶解的 25mg/kg 桃叶珊瑚苷给药后仅观察到单个浓度峰值。对于所有试验,桃叶珊瑚苷的药代动力学与水溶解的橙皮苷不同。

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