Investigation on pharmacokinetics, tissue distribution and excretion of 1-triacontanol in rats by gas chromatography-tandem mass spectrometry (GC-MS/MS). (January 2015)

• Record Type: Journal Article
• Authors: Wang, Chunfeng; Fan, Ali; Deng, Shuhua; Gao, Wenchao; Zhang, Wei; Yang, Wei; Zhu, Xiaojie; Lu, Yang; Chen, Xijing
• Is Part Of: Xenobiotica. Volume 45:Number 1(2015:Jan.)
• Page Start: 71
• Page End: 78
• Publication Date: 2015-01
• Subjects: Metabolism -- Periodicals; Drugs -- Physiological effect -- Periodicals; Food additives -- Periodicals; Chemicals -- Physiological effect -- Periodicals; Biochemistry -- Periodicals; Pharmaceutical Preparations -- metabolism -- Periodicals; Metabolism -- Periodicals; 574.133
• DOI: 10.3109/00498254.2014.943334
• Languages: English
• ISSNs: 0049-8254

Abstract

<abstract> <title>Abstract</title> <p>1. 1-Triacontanol (TA) recently shows promising anti-tumor activity. The present study was aimed to develop a sensitive gas chromatography-tandem mass spectrometry method to explore the pharmacokinetic profiles, distribution and excretion of TA in Sprague-Dawley rats after oral administration of TA. Chromatography separation was performed on a HP-5MS column. 1-Octacosanal was used as the internal standard (IS). Quantification of TA and IS was carried out at <italic>m</italic>/<italic>z</italic> 495.6 → 97.0 and <italic>m</italic>/<italic>z</italic> 467.5 → 97.0, respectively, in positive electron ionization and multiple reaction monitoring mode. The pharmacokinetic parameters were calculated by non-compartmental analysis.</p> <p>2. The area under concentration-time curve AUC<sub>0–6 h</sub> and AUC<sub>0–∞</sub> for TA at 60 mg/kg were 87.737±13.574 and 93.617±17.62, respectively. The mean residence time was 3.25 ± 0.17 h. In addition, the elimination half-lives (<italic>t</italic><sub>1/2</sub>) were (2.37±1.23, 1.27±0.49, 2.07±0.93) h after single oral administration of 30, 60 and 120 mg/kg of TA. After oral administration, TA was extensively distributed in stomach and intestine. The majority of TA excreted via feces, and its accumulative excretion ratio during the period of 72 h was 26.68 ± 7.14%, but only 0.0023 ± 0.0015% and 0.0027 ± 0.0006% for urines and bile, respectively. The absolute bioavailability (<italic>F</italic>, %) of TA was about 2.0%.</p> </abstract>