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大鼠口服山柰提取物后潘多拉丁A的药代动力学

Pharmacokinetics of panduratin A following oral administration of a Boesenbergia pandurata extract to rats.

作者信息

Won Jihyun, Noh Keumhan, Hwang Jae-Kwan, Shin Beom Soo, Kang Wonku

机构信息

College of Pharmacy, Chung-Ang University, Seoul 06974, South Korea.

Deapartment of Pharmaceutical Sciences, Leslie Dan Faculty of Pharmacy, University of Toronto, Toronto, ON M55 3M2, Canada.

出版信息

J Food Drug Anal. 2021 Dec 15;29(4):676-683. doi: 10.38212/2224-6614.3382.

Abstract

Boesenbergia pandurata and its major active ingredient, panduratin A (PAN), exhibit antibacterial, anti-oxidant, anti-inflammatory, and anti-obesity effects. We explored the time course of the plasma and tissue (in the major organs, gums and skin) concentrations of PAN after oral administration of a B. pandurata extract to rats. Model-dependent analysis was used to quantify the skin distribution of PAN after systemic exposure. The PAN level peaked at 1.12 ± 0.22 μg/mL after 3 h, and then biexponentially decayed with a terminal half-life of 9 h. The mean clearance (Cl/F) was 2.33 ± 0.68 L/h/kg. The PAN levels in organs were in the following order (highest first): skin, lung, heart, gum, liver, spleen, kidney, and brain. For the first time, the time course of PAN levels in plasma and organs was investigated after oral administration of a BPE. This study helps to explain the pharmacological activities of PAN in the skin and gums. The pharmacokinetic model provided data in the plasma and skin concentrations of PAN, which are of fundamental importance to evaluate its efficacy.

摘要

竹芋叶舞花姜及其主要活性成分竹芋素A(PAN)具有抗菌、抗氧化、抗炎和抗肥胖作用。我们研究了给大鼠口服竹芋叶舞花姜提取物后,血浆和组织(主要器官、牙龈和皮肤)中PAN浓度的时间进程。采用模型依赖分析来量化全身暴露后PAN在皮肤中的分布。给药3小时后,PAN水平达到峰值,为1.12±0.22μg/mL,然后呈双指数衰减,终末半衰期为9小时。平均清除率(Cl/F)为2.33±0.68L/h/kg。各器官中PAN水平的顺序如下(从高到低):皮肤、肺、心脏、牙龈、肝脏、脾脏、肾脏和大脑。首次研究了口服竹芋叶舞花姜提取物后血浆和器官中PAN水平的时间进程。本研究有助于解释PAN在皮肤和牙龈中的药理活性。药代动力学模型提供了血浆和皮肤中PAN浓度的数据,这对于评估其疗效至关重要。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/167e/9931020/6f99c264c7ca/jfda-29-676f1.jpg

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