title: Investigation on pharmacokinetics, tissue distribution and excretion of 1-triacontanol in rats by gas chromatography-tandem mass spectrometry (GC-MS/MS).
abstract: 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 m/z 495.6 → 97.0 and m/z 467.5 → 97.0, respectively, in positive electron ionization and multiple reaction monitoring mode. The pharmacokinetic parameters were calculated by non-compartmental analysis. 2. The area under concentration-time curve AUC0-6 h and AUC0-∞ 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 (t1/2) 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 (F, %) of TA was about 2.0%.
authors: Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University , Nanjing , People's Republic of China and.
authors: Chunfeng
authors: C
authors: Wang
authors: Ali
authors: A
authors: Fan
authors: Shuhua
authors: S
authors: Deng
authors: Wenchao
authors: W
authors: Gao
authors: Wei
authors: W
authors: Zhang
authors: Wei
authors: W
authors: Yang
authors: Xiaojie
authors: X
authors: Zhu
authors: Yang
authors: Y
authors: Lu
authors: Xijing
authors: X
authors: Chen
mesh_terms: D000818:Animals; D004365:Drugs, Chinese Herbal / Q000032:analysis / Q000493:pharmacokinetics*; D005233:Fatty Alcohols / Q000032:analysis / Q000493:pharmacokinetics*; D005243:Feces / Q000737:chemistry; D005260:Female; D008401:Gas Chromatography-Mass Spectrometry; D008297:Male; D017207:Rats, Sprague-Dawley; D053719:Tandem Mass Spectrometry; D014018:Tissue Distribution
chemical_list: D004365:Drugs, Chinese Herbal; D005233:Fatty Alcohols; C047578:1-triacontanol
keywords: 1-triacontanol; GC-MS/MS; pharmacokinetics