Pharmacokinetics of [6]-shogaol,a pungent ingredient of <Emphasis Type="Italic">Zingiber officinale</Emphasis> Roscoe (Part I) |
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Authors: | Akitoshi Asami Tsutomu Shimada Yasuharu Mizuhara Takayuki Asano Shuichi Takeda Takashi Aburada Ken-ichi Miyamoto Masaki Aburada |
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Institution: | (1) Department of Clinical Pharmacy, Graduate School of Natural Science and Technology, Kanazawa University, Kakuma-machi, Kanazawa Ishikawa, 920-1192, Japan;(2) Research Institute of Pharmaceutical Sciences, Musashino University, 1-1-20 Shinmachi, Nishitokyo Tokyo, 202-8585, Japan;(3) Tsumura & Co., Tokyo, Japan; |
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Abstract: | To investigate the pharmacokinetics of 6]-shogaol, a pungent ingredient of Zingiber officinale Roscoe, the pharmacokinetic parameters were determined by using 14C-6]-shogaol (labeled compound) and 6]-shogaol (non-labeled compound). When the labeled compound was orally administered
to rats, the maximum plasma concentration (C
max) and the area under the curve (AUC) of plasma radioactivity concentration increased in a dose-dependent manner. When the
labeled compound was orally administered at a dose of 10 mg/kg, 20.0 ± 1.8% of the radioactivity administered was excreted
into urine, 64.0 ± 12.9% into feces, and 0.2 ± 0.1% into breath. Thus, more of the radioactivity was excreted into feces than
into urine, and almost no radioactivity was excreted into breath. Furthermore, when the labeled compound was orally administered
at a dose of 10 mg/kg, cumulative biliary radioactivity excretion over 48 h was 78.5 ± 4.5% of the radioactivity administered,
and cumulative urinary radioactivity excretion over 48 h was 11.8 ± 2.7%, showing that about 90% of the dose administered
orally was absorbed from the digestive tract and most of the fecal excretion was via biliary excretion. On the other hand,
when the non-labeled compound 6]-shogaol was orally administered, the plasma concentration and biliary excretion of the unchanged
form were extremely low. When these results are combined with those obtained with the labeled compound, it would suggest that
6]-shogaol is mostly metabolized in the body and excreted as metabolites. |
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