British Journal of Nutrition

Metabolism and Metabolic Studies

Pharmacokinetics and first-pass metabolism of astaxanthin in rats

Hye Duck Choia1, Hee Eun Kanga1, Si Hyung Yanga1, Myung Gull Leea1 and Wan Gyoon Shina1 c1

a1 College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, San 56-1, Sillim-Dong, Gwanak-Gu, Seoul 151-742, South Korea

Abstract

Astaxanthin is a carotenoid with antioxidant, anti-cancer and anti-inflammatory properties. The pharmacokinetics of astaxanthin after its intravenous (5, 10, and 20 mg/kg) and oral (100 and 200 mg/kg) administration and its first-pass extraction ratios after its intravenous, intraportal or intragastric (20 mg/kg) administration were evaluated in rats. The pharmacokinetic parameters of astaxanthin were dose dependent after its intravenous administration, due to the saturable hepatic metabolism of astaxanthin, but dose independent after oral administration. The gastrointestinal absorption of astaxanthin followed the flip-flop model. The hepatic and gastrointestinal first-pass extraction ratios of astaxanthin were approximately 0·490 and 0·901, respectively. Astaxanthin was metabolised primarily by hepatic cytochrome P-450 1A1/2 in rats. Astaxanthin was unstable up to 4 h incubation in four rat gastric juices and up to 24 h incubation in various buffer solutions having a pH of 1–13. The tissue/plasma ratios of astaxanthin at 8 and 24 h after its oral administration (100 mg/kg) were greater than unity for all tissues studied, except in the heart, at 8 h, indicating that the rat tissues studied had high affinity for astaxanthin.

(Received June 02 2010)

(Revised August 04 2010)

(Accepted August 06 2010)

(Online publication September 07 2010)

Correspondence:

c1 Corresponding author: Professor W. G. Shin, fax +82 2 766 8556, email wgshin@snu.ac.kr

Footnotes

Abbreviations: AUC, the total area under the concentration–time curve; CL, time-averaged total body clearance; CLR, renal clearance; CLNR, non-renal clearance; Cmax, peak plasma concentration

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