Effect of piperine on the bioavailability and pharmacokinetics of emodin in rats
[Display omitted] •Pharmacokinetics of emodin and its glucuronidation were investigated by LC–MS/MS method.•The comparison of bioavailability and pharmacokinetics between emodin alone and in combination with piperine were carried out.•Piperine significantly improved the in vivo bioavailability of em...
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| Veröffentlicht in: | Journal of pharmaceutical and biomedical analysis 2015-11, Vol.115, p.144-149 |
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| creator | Di, Xin Wang, Xin Liu, Youping |
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•Pharmacokinetics of emodin and its glucuronidation were investigated by LC–MS/MS method.•The comparison of bioavailability and pharmacokinetics between emodin alone and in combination with piperine were carried out.•Piperine significantly improved the in vivo bioavailability of emodin via the inhibition of its glucuronidation.
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. |
| doi_str_mv | 10.1016/j.jpba.2015.06.027 |
| format | Article |
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•Pharmacokinetics of emodin and its glucuronidation were investigated by LC–MS/MS method.•The comparison of bioavailability and pharmacokinetics between emodin alone and in combination with piperine were carried out.•Piperine significantly improved the in vivo bioavailability of emodin via the inhibition of its glucuronidation.
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.</description><identifier>ISSN: 0731-7085</identifier><identifier>EISSN: 1873-264X</identifier><identifier>DOI: 10.1016/j.jpba.2015.06.027</identifier><identifier>PMID: 26201645</identifier><language>eng</language><publisher>England: Elsevier B.V</publisher><subject>Administration, Oral ; Alkaloids - administration & dosage ; Alkaloids - pharmacology ; Animals ; Area Under Curve ; Benzodioxoles - administration & dosage ; Benzodioxoles - pharmacology ; Biological Availability ; Chromatography, High Pressure Liquid - methods ; Drug Interactions ; Emodin - administration & dosage ; Emodin - blood ; Emodin - pharmacokinetics ; Emodin Piperine UDP-glucuronosyltransferases (UGTs) Inhibition ; Female ; Glucuronides - metabolism ; Limit of Detection ; Linear Models ; Pharmacokinetics bioavailability ; Piperidines - administration & dosage ; Piperidines - pharmacology ; Polyunsaturated Alkamides - administration & dosage ; Polyunsaturated Alkamides - pharmacology ; Rats, Sprague-Dawley ; Reproducibility of Results ; Tandem Mass Spectrometry - methods</subject><ispartof>Journal of pharmaceutical and biomedical analysis, 2015-11, Vol.115, p.144-149</ispartof><rights>2015 Elsevier B.V.</rights><rights>Copyright © 2015 Elsevier B.V. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c422t-7cae601241d0cd2fcb37c9bc602da2522084a9ebe49b42b7851b95c118b7f5263</citedby><cites>FETCH-LOGICAL-c422t-7cae601241d0cd2fcb37c9bc602da2522084a9ebe49b42b7851b95c118b7f5263</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0731708515300467$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/26201645$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Di, Xin</creatorcontrib><creatorcontrib>Wang, Xin</creatorcontrib><creatorcontrib>Liu, Youping</creatorcontrib><title>Effect of piperine on the bioavailability and pharmacokinetics of emodin in rats</title><title>Journal of pharmaceutical and biomedical analysis</title><addtitle>J Pharm Biomed Anal</addtitle><description>[Display omitted]
•Pharmacokinetics of emodin and its glucuronidation were investigated by LC–MS/MS method.•The comparison of bioavailability and pharmacokinetics between emodin alone and in combination with piperine were carried out.•Piperine significantly improved the in vivo bioavailability of emodin via the inhibition of its glucuronidation.
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.</description><subject>Administration, Oral</subject><subject>Alkaloids - administration & dosage</subject><subject>Alkaloids - pharmacology</subject><subject>Animals</subject><subject>Area Under Curve</subject><subject>Benzodioxoles - administration & dosage</subject><subject>Benzodioxoles - pharmacology</subject><subject>Biological Availability</subject><subject>Chromatography, High Pressure Liquid - methods</subject><subject>Drug Interactions</subject><subject>Emodin - administration & dosage</subject><subject>Emodin - blood</subject><subject>Emodin - pharmacokinetics</subject><subject>Emodin Piperine UDP-glucuronosyltransferases (UGTs) Inhibition</subject><subject>Female</subject><subject>Glucuronides - metabolism</subject><subject>Limit of Detection</subject><subject>Linear Models</subject><subject>Pharmacokinetics bioavailability</subject><subject>Piperidines - administration & dosage</subject><subject>Piperidines - pharmacology</subject><subject>Polyunsaturated Alkamides - administration & dosage</subject><subject>Polyunsaturated Alkamides - pharmacology</subject><subject>Rats, Sprague-Dawley</subject><subject>Reproducibility of Results</subject><subject>Tandem Mass Spectrometry - methods</subject><issn>0731-7085</issn><issn>1873-264X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2015</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE1LxDAQhoMo7rr6BzxIj15ak2w-WvAiy_oBgh4UvIUknWLWtqlJd8F_b8qqR2FgLs_7DvMgdE5wQTARV5tiMxhdUEx4gUWBqTxAc1LKZU4FeztEcyyXJJe45DN0EuMGY8xJxY7RjIoUEozP0fO6acCOmW-ywQ0QXA-Z77PxHTLjvN5p12rjWjd-Zbqvs-Fdh05b_5G40dk45aDzteuzNEGP8RQdNbqNcPazF-j1dv2yus8fn-4eVjePuWWUjrm0GgQmlJEa25o21iylrYwVmNaackpxyXQFBlhlGDWy5MRU3BJSGtlwKpYLdLnvHYL_3EIcVeeihbbVPfhtVEQSLtIFJhNK96gNPsYAjRqC63T4UgSryaTaqMmkmkwqLFQymUIXP_1b00H9F_lVl4DrPQDpy52DoKJ10FuoXUhGVe3df_3ffK-EfA</recordid><startdate>20151110</startdate><enddate>20151110</enddate><creator>Di, Xin</creator><creator>Wang, Xin</creator><creator>Liu, Youping</creator><general>Elsevier B.V</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20151110</creationdate><title>Effect of piperine on the bioavailability and pharmacokinetics of emodin in rats</title><author>Di, Xin ; Wang, Xin ; Liu, Youping</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c422t-7cae601241d0cd2fcb37c9bc602da2522084a9ebe49b42b7851b95c118b7f5263</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2015</creationdate><topic>Administration, Oral</topic><topic>Alkaloids - administration & dosage</topic><topic>Alkaloids - pharmacology</topic><topic>Animals</topic><topic>Area Under Curve</topic><topic>Benzodioxoles - administration & dosage</topic><topic>Benzodioxoles - pharmacology</topic><topic>Biological Availability</topic><topic>Chromatography, High Pressure Liquid - methods</topic><topic>Drug Interactions</topic><topic>Emodin - administration & dosage</topic><topic>Emodin - blood</topic><topic>Emodin - pharmacokinetics</topic><topic>Emodin Piperine UDP-glucuronosyltransferases (UGTs) Inhibition</topic><topic>Female</topic><topic>Glucuronides - metabolism</topic><topic>Limit of Detection</topic><topic>Linear Models</topic><topic>Pharmacokinetics bioavailability</topic><topic>Piperidines - administration & dosage</topic><topic>Piperidines - pharmacology</topic><topic>Polyunsaturated Alkamides - administration & dosage</topic><topic>Polyunsaturated Alkamides - pharmacology</topic><topic>Rats, Sprague-Dawley</topic><topic>Reproducibility of Results</topic><topic>Tandem Mass Spectrometry - methods</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Di, Xin</creatorcontrib><creatorcontrib>Wang, Xin</creatorcontrib><creatorcontrib>Liu, Youping</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Journal of pharmaceutical and biomedical analysis</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Di, Xin</au><au>Wang, Xin</au><au>Liu, Youping</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Effect of piperine on the bioavailability and pharmacokinetics of emodin in rats</atitle><jtitle>Journal of pharmaceutical and biomedical analysis</jtitle><addtitle>J Pharm Biomed Anal</addtitle><date>2015-11-10</date><risdate>2015</risdate><volume>115</volume><spage>144</spage><epage>149</epage><pages>144-149</pages><issn>0731-7085</issn><eissn>1873-264X</eissn><abstract>[Display omitted]
•Pharmacokinetics of emodin and its glucuronidation were investigated by LC–MS/MS method.•The comparison of bioavailability and pharmacokinetics between emodin alone and in combination with piperine were carried out.•Piperine significantly improved the in vivo bioavailability of emodin via the inhibition of its glucuronidation.
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.</abstract><cop>England</cop><pub>Elsevier B.V</pub><pmid>26201645</pmid><doi>10.1016/j.jpba.2015.06.027</doi><tpages>6</tpages></addata></record> |
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| subjects | Administration, Oral Alkaloids - administration & dosage Alkaloids - pharmacology Animals Area Under Curve Benzodioxoles - administration & dosage Benzodioxoles - pharmacology Biological Availability Chromatography, High Pressure Liquid - methods Drug Interactions Emodin - administration & dosage Emodin - blood Emodin - pharmacokinetics Emodin Piperine UDP-glucuronosyltransferases (UGTs) Inhibition Female Glucuronides - metabolism Limit of Detection Linear Models Pharmacokinetics bioavailability Piperidines - administration & dosage Piperidines - pharmacology Polyunsaturated Alkamides - administration & dosage Polyunsaturated Alkamides - pharmacology Rats, Sprague-Dawley Reproducibility of Results Tandem Mass Spectrometry - methods |
| title | Effect of piperine on the bioavailability and pharmacokinetics of emodin in rats |
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