Skip to main content
×
Home
    • Aa
    • Aa

Pharmacokinetics and first-pass metabolism of astaxanthin in rats

  • Hye Duck Choi (a1), Hee Eun Kang (a1), Si Hyung Yang (a1), Myung Gull Lee (a1) and Wan Gyoon Shin (a1)...
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.

  • View HTML
    • Send article to Kindle

      To send this article to your Kindle, first ensure no-reply@cambridge.org is added to your Approved Personal Document E-mail List under your Personal Document Settings on the Manage Your Content and Devices page of your Amazon account. Then enter the ‘name’ part of your Kindle email address below. Find out more about sending to your Kindle.

      Note you can select to send to either the @free.kindle.com or @kindle.com variations. ‘@free.kindle.com’ emails are free but can only be sent to your device when it is connected to wi-fi. ‘@kindle.com’ emails can be delivered even when you are not connected to wi-fi, but note that service fees apply.

      Find out more about the Kindle Personal Document Service.

      Pharmacokinetics and first-pass metabolism of astaxanthin in rats
      Available formats
      ×
      Send article to Dropbox

      To send this article to your Dropbox account, please select one or more formats and confirm that you agree to abide by our usage policies. If this is the first time you use this feature, you will be asked to authorise Cambridge Core to connect with your Dropbox account. Find out more about sending content to Dropbox.

      Pharmacokinetics and first-pass metabolism of astaxanthin in rats
      Available formats
      ×
      Send article to Google Drive

      To send this article to your Google Drive account, please select one or more formats and confirm that you agree to abide by our usage policies. If this is the first time you use this feature, you will be asked to authorise Cambridge Core to connect with your Google Drive account. Find out more about sending content to Google Drive.

      Pharmacokinetics and first-pass metabolism of astaxanthin in rats
      Available formats
      ×
Copyright
Corresponding author
*Corresponding author: Professor W. G. Shin, fax +82 2 766 8556, email wgshin@snu.ac.kr
References
Hide All
1Higuera-Ciapara I, Félix-Valenzuela L & Goyocoolea FM (2006) Astaxanthin: a review of its chemistry and applications. Crit Rev Food Sci Nutr 46, 186196.
2Miki W (1991) Biological functions and activities of animal carotenoids. Pure Appl Chem 63, 141146.
3Pashkow FJ, Watumull DG & Campbell CL (2008) Astaxanthin: a novel potential treatment for oxidative stress and inflammation in cardiovascular disease. Am J Cardiol 101, 58D68D.
4Comhaire FH, El Garem Y, Mahmoud A, et al. (2008) Combined conventional/antioxidant ‘astaxanthin’ treatment for male infertility: a double blind, randomized trial. Asian J Androl 7, 257262.
5Kupcinskas L, Lafolie P, Lignell A, et al. (2008) Efficacy of the natural antioxidant astaxanthin in the treatment of functional dyspepsia in patients with or without Helicobacter pylori infection: a prospective, randomized, double blind, and placebo-controlled study. Phytomedicine 15, 391399.
6Parisi V, Tedeschi M, Gallinaro G, et al. (2008) Carotenoids and antioxidants in age-related maculopathy Italian study: multifocal electroretinogram modifications after 1 year. Ophthalmology 115, 324344.
7Nagao A (2009) Absorption and function of dietary carotenoids. Forum Nutr 61, 5563.
8Odeberg JM, Lignell A, Pettersson A, et al. (2003) Oral bioavailability of the antioxidant astaxanthin in humans is enhanced by incorporation of lipid based formulations. Eur J Pharm Sci 19, 299304.
9Okada Y, Ishikura M & Maoka T (2009) Bioavailability of astaxanthin in Haematococcus algal extract: the effects of timing of diet and smoking habits. Biosci Biotechnol Biochem 73, 19281932.
10Showalter LA, Weinman SA, Østerlie M, et al. (2004) Plasma appearance and tissue accumulation of non-esterified, free astaxanthin in C57BL/6 mice after oral dosing of a disodium disuccinate diester of astaxanthin (Heptax). Comp Biochem Physiol C Toxicol Pharmacol 137, 227236.
11Petri D & Lundebye AK (2007) Tissue distribution of astaxanthin in rats following exposure to graded levels in the feed. Comp Biochem Physiol C Toxicol Pharmacol 145, 202209.
12Kistler A, Liechti H, Pichard L, et al. (2002) Metabolism and CYP-inducer properties of astaxanthin in man and primary human hepatocytes. Arch Toxicol 75, 665675.
13Erich W, Hans L, Brightte N, et al. (1999) Characterization of metabolites of astaxanthin in primary cultures of rat hepatocytes. Drug Metab Dispos 27, 456462.
14Correia MA (1995) Appendices B. Rat and human liver cytochromes 450: substrate and inhibitor specificities and functional markers. In Cytochrome 450. Structure, Mechanism, and Biochemistry, 2nd ed., pp. 607630. New York: Plenum Press.
15Kim SH, Choi YM & Lee MG (1993) Pharmacokinetics and pharmacodynamics of furosemide in protein–calorie malnutrition. J Pharmacokinet Biopharm 21, 17.
16Murakami T, Nakanishi M, Yoshimori T, et al. (2003) Separate assessment of intestinal and hepatic first-pass effects using a rat model with double cannulation of the portal and jugular veins. Drug Metab Pharmacokinet 18, 242260.
17Choi YH, Kim SG & Lee MG (2006) Dose-independent pharmacokinetics of metformin in rats: hepatic and gastrointestinal first-pass effects. J Pharm Sci 95, 25432552.
18Williams JF, Lowitt S & Szentivanyi A (1979) Effect of phenobarbital and 3-methylcholanthrene pretreatment on the plasma half-life and urinary excretion profile of theophylline and its metabolites in rats. Biochem Pharmacol 28, 29352940.
19Choi YM, Kim SH & Lee MG (1991) Effect of phenobarbital and 3-methylcholanthrene pretreatment on the pharmacokinetics and pharmacodynamics of furosemide in rats. J Pharm Sci 80, 638642.
20Lee DY, Kim JY, Kim YC, et al. (2005) Dose-independent pharmacokinetics of torasemide after intravenous and oral administration to rats. Biopharm Drug Dispos 26, 173182.
21Yu SY, Bae SK & Kim EJ (2003) Dose-independent pharmacokinetics of a new reversible proton pump inhibitor, KR-60436, after intravenous and oral administration to rats: gastrointestinal first-pass effect. J Pharm Sci 92, 15921603.
22Gibaldi M & Perrier D (1980) Pharmacokinetics, 2nd ed.New York: Marcel Dekker.
23Chiou WL (1978) Critical evaluation of potential error in pharmacokinetic studies using the linear trapezoidal rule method for the calculation of the area under the plasma level-time curve. J Pharmacokinet Biopharm 6, 539546.
24Boxenbaum H (1998) Pharmacokinetics tricks and traps: flip-flop models. J Pharm Pharm Sci 1, 9091.
25Goto S, Kogure K, Abe K, et al. (2001) Efficient radical trapping at the surface and inside the phospholipid membrane is responsible for highly potent antiperoxidative activity of the carotenoid astaxanthin. Biochim Biophys Acta 1512, 251258.
26Zhi J, Melia AT, Koss-Twardy SG, et al. (1996) The effect of orlistat, an inhibitor of dietary fat absorption, on the pharmacokinetics of beta-carotene in healthy volunteers. J Clin Pharmacol 36, 152159.
27Xu MJ, Plezia PM, Alberts DS, et al. (1992) Reduction in plasma or skin alpha-tocopherol concentration with long-term oral administration of beta-carotene in humans and mice. J Natl Cancer Inst 84, 15591565.
28White WS, Stacewicz-Sapuntzakis M, Erdman JW Jr, et al. (1994) Pharmacokinetics of beta-carotene and canthaxanthin after ingestion of individual and combined doses by human subjects. J Am Coll Nutr 13, 665671.
Recommend this journal

Email your librarian or administrator to recommend adding this journal to your organisation's collection.

British Journal of Nutrition
  • ISSN: 0007-1145
  • EISSN: 1475-2662
  • URL: /core/journals/british-journal-of-nutrition
Please enter your name
Please enter a valid email address
Who would you like to send this to? *
×

Keywords:

Metrics

Altmetric attention score

Full text views

Total number of HTML views: 33
Total number of PDF views: 179 *
Loading metrics...

Abstract views

Total abstract views: 291 *
Loading metrics...

* Views captured on Cambridge Core between September 2016 - 20th October 2017. This data will be updated every 24 hours.