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小鼠单次口服鲁布拉黄烷酮的药代动力学特征

Single dose oral pharmacokinetic profile rubraxanthone in mice.

作者信息

Susanti Meri, Darmianti Riski, Harahap Yahdiana, Itam Afrizal, Hamidi Dachriyanus

机构信息

Faculty of Pharmacy, Universitas Andalas, Padang, West Sumatra, 25163, Indonesia.

Faculty of Pharmacy, Universitas Indonesia, Depok, West Java, Indonesia.

出版信息

Heliyon. 2022 Mar 14;8(3):e09104. doi: 10.1016/j.heliyon.2022.e09104. eCollection 2022 Mar.

Abstract

Rubraxanthone is a main active constituent of kandis ( Roxb), has showed many biological activity including antimicrobial, anti hypercholesterolemic, antiplatelet, antioxidant, cytotoxic, and anti-inflammatory properties. To the best of our knowledge, no reports on the pharmacokinetics (PK) of this rubraxanthone have been published. The PK of rubraxanthone in mice was examined after a single oral dose of 700 mg/kg rubraxanthone suspension in virgin coconut oil. Plasma samples were collected at different time points and further analyzed using validated chromatographic method. Pharmacokinetic parameters were calculated from observed plasma concentration-time profile. The maximum concentration of rubraxanthone in plasma was discovered in 1.5 h. The peak plasma concentration (C) was 4.267 μg/mL, and the area under the curve (AUCt0-t ) was 560.99 μg h/L, with a 6.72-hour terminal half-life (T). The volume of distribution (Vd/F) was 1200.19 mL/kg and 1123.88 mL/h/kg clearance (Cl/F).

摘要

红没药醇是毛叶巴豆(Roxb)的主要活性成分,已显示出多种生物活性,包括抗菌、抗高胆固醇血症、抗血小板、抗氧化、细胞毒性和抗炎特性。据我们所知,尚未有关于这种红没药醇药代动力学(PK)的报道。在单次口服700 mg/kg红没药醇悬浮于初榨椰子油中的剂量后,对小鼠体内的红没药醇药代动力学进行了研究。在不同时间点采集血浆样本,并使用经过验证的色谱方法进行进一步分析。根据观察到的血浆浓度-时间曲线计算药代动力学参数。红没药醇在血浆中的最大浓度在1.5小时时被发现。血浆峰浓度(C)为4.267μg/mL,曲线下面积(AUCt0-t )为560.99μg h/L,终末半衰期(T)为6.72小时。分布容积(Vd/F)为1200.19 mL/kg,清除率(Cl/F)为1123.88 mL/h/kg。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/20af/8941156/b38b799b4ecb/gr1.jpg

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