Enantioselective Pharmacokinetics of α-Lipoic Acid in Rats
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 co...
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| Format: | Online |
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MDPI
2015
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| Online Access: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4613335/ |
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pubmed-46133352015-10-26 Enantioselective Pharmacokinetics of α-Lipoic Acid in Rats Uchida, Ryota Okamoto, Hinako Ikuta, Naoko Terao, Keiji Hirota, Takashi Article 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. MDPI 2015-09-21 /pmc/articles/PMC4613335/ /pubmed/26402669 http://dx.doi.org/10.3390/ijms160922781 Text en © 2015 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/). |
| repository_type |
Open Access Journal |
| institution_category |
Foreign Institution |
| institution |
US National Center for Biotechnology Information |
| building |
NCBI PubMed |
| collection |
Online Access |
| language |
English |
| format |
Online |
| author |
Uchida, Ryota Okamoto, Hinako Ikuta, Naoko Terao, Keiji Hirota, Takashi |
| spellingShingle |
Uchida, Ryota Okamoto, Hinako Ikuta, Naoko Terao, Keiji Hirota, Takashi Enantioselective Pharmacokinetics of α-Lipoic Acid in Rats |
| author_facet |
Uchida, Ryota Okamoto, Hinako Ikuta, Naoko Terao, Keiji Hirota, Takashi |
| author_sort |
Uchida, Ryota |
| title |
Enantioselective Pharmacokinetics of α-Lipoic Acid in Rats |
| title_short |
Enantioselective Pharmacokinetics of α-Lipoic Acid in Rats |
| title_full |
Enantioselective Pharmacokinetics of α-Lipoic Acid in Rats |
| title_fullStr |
Enantioselective Pharmacokinetics of α-Lipoic Acid in Rats |
| title_full_unstemmed |
Enantioselective Pharmacokinetics of α-Lipoic Acid in Rats |
| title_sort |
enantioselective pharmacokinetics of α-lipoic acid in rats |
| description |
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. |
| publisher |
MDPI |
| publishDate |
2015 |
| url |
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4613335/ |
| _version_ |
1613490581634285568 |