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Int. J. Mol. Sci. 2015, 16(9), 22781-22794; doi:10.3390/ijms160922781

Enantioselective Pharmacokinetics of α-Lipoic Acid in Rats

1
Department of Biopharmaceutics, Faculty of Pharmaceutical Science, Tokyo University of Science, 2641 Yamazaki, Noda-shi, Chiba 278-8510, Japan
2
CycloChem Bio Co., Ltd., KIBC654R 5-5-2 Minatojima-minamimachi, Chuo-ku, Kobe 650-0047, Japan
3
Graduate School of Medicine, Kobe University, 7-5-2 Kusunoki-cho, Chuo-ku, Kobe 650-0017, Japan
*
Author to whom correspondence should be addressed.
Academic Editor: Mateus Webba da Silva
Received: 20 August 2015 / Revised: 9 September 2015 / Accepted: 11 September 2015 / Published: 21 September 2015
(This article belongs to the Section Biochemistry, Molecular and Cellular Biology)
View Full-Text   |   Download PDF [1021 KB, uploaded 21 September 2015]   |  

Abstract

α-Lipoic acid (LA) is widely used for nutritional supplements as a racemic mixture, even though the R enantiomer is biologically active. After oral administration of the racemic mixture (R-α-lipoic acid (RLA) and S-α-lipoic acid (SLA) mixed at the ratio of 50:50) to rats, RLA showed higher plasma concentration than SLA, and its area under the plasma concentration-time curve from time zero to the last (AUC) was significantly about 1.26 times higher than that of SLA. However, after intravenous administration of the racemic mixture, the pharmacokinetic profiles, initial concentration (C0), AUC, and half-life (T1/2) of the enantiomers were not significantly different. After oral and intraduodenal administration of the racemic mixture to pyrolus-ligated rats, the AUCs of RLA were significantly about 1.24 and 1.32 times higher than that of SLA, respectively. In addition, after intraportal administration the AUC of RLA was significantly 1.16 times higher than that of SLA. In conclusion, the enantioselective pharmacokinetics of LA in rats arose from the fraction absorbed multiplied by gastrointestinal availability (FaFg) and hepatic availability (Fh), and not from the total clearance. View Full-Text
Keywords: α-lipoic acid; pharmacokinetics; enantioselective; gastrointestinal availability; hepatic availability; clearance; rat α-lipoic acid; pharmacokinetics; enantioselective; gastrointestinal availability; hepatic availability; clearance; rat
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Uchida, R.; Okamoto, H.; Ikuta, N.; Terao, K.; Hirota, T. Enantioselective Pharmacokinetics of α-Lipoic Acid in Rats. Int. J. Mol. Sci. 2015, 16, 22781-22794.

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