1. Effect of piperine on the bioavailability and pharmacokinetics of emodin in rats.
- Author
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Di X, Wang X, Di X, and Liu Y
- Subjects
- Administration, Oral, Alkaloids administration & dosage, Animals, Area Under Curve, Benzodioxoles administration & dosage, Biological Availability, Drug Interactions, Emodin administration & dosage, Emodin blood, Female, Glucuronides metabolism, Limit of Detection, Linear Models, Piperidines administration & dosage, Polyunsaturated Alkamides administration & dosage, Rats, Sprague-Dawley, Reproducibility of Results, Alkaloids pharmacology, Benzodioxoles pharmacology, Chromatography, High Pressure Liquid methods, Emodin pharmacokinetics, Piperidines pharmacology, Polyunsaturated Alkamides pharmacology, Tandem Mass Spectrometry methods
- Abstract
Emodin (1,3,8-trihydroxy-6-methylanthraquinone) has been widely used as a traditional medicine and was shown to possess a multitude of health-promoting properties in pre-clinical studies, but its bioavailability was low due to the extensive glucuronidation in liver and intestine, hindering the development of emodin as a feasible chemopreventive agent. In this study, piperine, as a bioenhancer, was used to enhance the bioavailability of emodin by inhibiting its glucuronidation. The pharmacokinetic profiles of emodin after oral administration of emodin (20mg/kg) alone and in combination with piperine (20mg/kg) to rats were investigated via a validated LC/MS/MS method. As the in vivo pharmacokinetic studies had indicated, the AUC and Cmax of emodin were increased significantly after piperine treatment, and the glucuronidation of emodin was markedly inhibited. Our study demonstrated that piperine significantly improved the in vivo bioavailability of emodin and the influence of piperine on the pharmacokinetics of emodin may be attributed to the inhibition of glucuronidation of emodin. Further research is needed to investigate the detailed mechanism of improved bioavailability of emodin via its combination with piperine., (Copyright © 2015 Elsevier B.V. All rights reserved.)
- Published
- 2015
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