Differential Effect of Grapefruit Juice on Intestinal Absorption of Statins Due to Inhibition of Organic Anion Transporting Polypeptide and/or P-glycoprotein
The purpose of this study is to examine the contributions of organic anion transporting polypeptide (Oatp) and/or P-glycoprotein (P-gp) to grapefruit juice (GFJ) interaction with two statins, pravastatin and pitavastatin, which undergo negligible metabolism in rats. The two statins were found to be...
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| Veröffentlicht in: | Journal of pharmaceutical sciences 2011-09, Vol.100 (9), p.3843-3853 |
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| creator | Shirasaka, Yoshiyuki Suzuki, Kensuke Nakanishi, Takeo Tamai, Ikumi |
| description | The purpose of this study is to examine the contributions of organic anion transporting polypeptide (Oatp) and/or P-glycoprotein (P-gp) to grapefruit juice (GFJ) interaction with two statins, pravastatin and pitavastatin, which undergo negligible metabolism in rats. The two statins were found to be substrates of both Oatp1a5 and Oatp2b1, whereas pitavastatin, but not pravastatin, was a substrate of P-gp. The plasma concentration of pravastatin after oral administration was significantly decreased by GFJ and naringin, whereas that of pitavastatin was significantly increased. Naringin inhibited Oatp1a5- and Oatp2b1-mediated uptake of pravastatin and Oatp1a5-mediated, but not Oatp2b1-mediated, uptake of pitavastatin. Naringin also inhibited P-gp-mediated transport of pitavastatin. These results suggested that the decrease of pravastatin absorption in the presence of GFJ is due to the inhibitory effect of naringin on Oatp, whereas the increase of pitavastatin is due to the inhibition of P-gp. These observations are consistent with the results of in situ absorption studies. In conclusion, Oatp and/or P-gp contribute to the intestinal absorption of statins, and the differential effect of GFJ on pravastatin and pitavastatin absorption is at least partly accounted for by the different inhibitory effects of naringin on these transporters. © 2011 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 100:3843–3853, 2011 |
| doi_str_mv | 10.1002/jps.22586 |
| format | Article |
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The two statins were found to be substrates of both Oatp1a5 and Oatp2b1, whereas pitavastatin, but not pravastatin, was a substrate of P-gp. The plasma concentration of pravastatin after oral administration was significantly decreased by GFJ and naringin, whereas that of pitavastatin was significantly increased. Naringin inhibited Oatp1a5- and Oatp2b1-mediated uptake of pravastatin and Oatp1a5-mediated, but not Oatp2b1-mediated, uptake of pitavastatin. Naringin also inhibited P-gp-mediated transport of pitavastatin. These results suggested that the decrease of pravastatin absorption in the presence of GFJ is due to the inhibitory effect of naringin on Oatp, whereas the increase of pitavastatin is due to the inhibition of P-gp. These observations are consistent with the results of in situ absorption studies. In conclusion, Oatp and/or P-gp contribute to the intestinal absorption of statins, and the differential effect of GFJ on pravastatin and pitavastatin absorption is at least partly accounted for by the different inhibitory effects of naringin on these transporters. © 2011 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 100:3843–3853, 2011</description><identifier>ISSN: 0022-3549</identifier><identifier>EISSN: 1520-6017</identifier><identifier>DOI: 10.1002/jps.22586</identifier><identifier>PMID: 21520088</identifier><identifier>CODEN: JPMSAE</identifier><language>eng</language><publisher>Hoboken: Elsevier Inc</publisher><subject>Animals ; ATP-Binding Cassette, Sub-Family B, Member 1 - antagonists & inhibitors ; Beverages ; Biological and medical sciences ; Chromatography, Liquid ; Citrus paradisi ; Flavanones - pharmacology ; General pharmacology ; grapefruit juice ; Hydroxymethylglutaryl-CoA Reductase Inhibitors - pharmacokinetics ; interaction ; Intestinal Absorption ; LLC-PK1 Cells ; Male ; Medical sciences ; naringin ; OATP ; Organic Anion Transporters - antagonists & inhibitors ; P-glycoprotein ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; pitavastatin ; pravastatin ; Rats ; Rats, Wistar ; Swine ; Tandem Mass Spectrometry ; Xenopus laevis</subject><ispartof>Journal of pharmaceutical sciences, 2011-09, Vol.100 (9), p.3843-3853</ispartof><rights>2011 Wiley-Liss, Inc.</rights><rights>Copyright © 2011 Wiley‐Liss, Inc.</rights><rights>2015 INIST-CNRS</rights><rights>Copyright © 2011 Wiley-Liss, Inc.</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c5656-4854fe60afa96a6558ff99f8e91be4baea0e2bd913a8784f59cf990d8ae413f43</citedby><cites>FETCH-LOGICAL-c5656-4854fe60afa96a6558ff99f8e91be4baea0e2bd913a8784f59cf990d8ae413f43</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1002%2Fjps.22586$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1002%2Fjps.22586$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>315,781,785,1418,27926,27927,45576,45577</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=24487549$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/21520088$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Shirasaka, Yoshiyuki</creatorcontrib><creatorcontrib>Suzuki, Kensuke</creatorcontrib><creatorcontrib>Nakanishi, Takeo</creatorcontrib><creatorcontrib>Tamai, Ikumi</creatorcontrib><title>Differential Effect of Grapefruit Juice on Intestinal Absorption of Statins Due to Inhibition of Organic Anion Transporting Polypeptide and/or P-glycoprotein</title><title>Journal of pharmaceutical sciences</title><addtitle>J. Pharm. Sci</addtitle><description>The purpose of this study is to examine the contributions of organic anion transporting polypeptide (Oatp) and/or P-glycoprotein (P-gp) to grapefruit juice (GFJ) interaction with two statins, pravastatin and pitavastatin, which undergo negligible metabolism in rats. The two statins were found to be substrates of both Oatp1a5 and Oatp2b1, whereas pitavastatin, but not pravastatin, was a substrate of P-gp. The plasma concentration of pravastatin after oral administration was significantly decreased by GFJ and naringin, whereas that of pitavastatin was significantly increased. Naringin inhibited Oatp1a5- and Oatp2b1-mediated uptake of pravastatin and Oatp1a5-mediated, but not Oatp2b1-mediated, uptake of pitavastatin. Naringin also inhibited P-gp-mediated transport of pitavastatin. These results suggested that the decrease of pravastatin absorption in the presence of GFJ is due to the inhibitory effect of naringin on Oatp, whereas the increase of pitavastatin is due to the inhibition of P-gp. These observations are consistent with the results of in situ absorption studies. In conclusion, Oatp and/or P-gp contribute to the intestinal absorption of statins, and the differential effect of GFJ on pravastatin and pitavastatin absorption is at least partly accounted for by the different inhibitory effects of naringin on these transporters. © 2011 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 100:3843–3853, 2011</description><subject>Animals</subject><subject>ATP-Binding Cassette, Sub-Family B, Member 1 - antagonists & inhibitors</subject><subject>Beverages</subject><subject>Biological and medical sciences</subject><subject>Chromatography, Liquid</subject><subject>Citrus paradisi</subject><subject>Flavanones - pharmacology</subject><subject>General pharmacology</subject><subject>grapefruit juice</subject><subject>Hydroxymethylglutaryl-CoA Reductase Inhibitors - pharmacokinetics</subject><subject>interaction</subject><subject>Intestinal Absorption</subject><subject>LLC-PK1 Cells</subject><subject>Male</subject><subject>Medical sciences</subject><subject>naringin</subject><subject>OATP</subject><subject>Organic Anion Transporters - antagonists & inhibitors</subject><subject>P-glycoprotein</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>pitavastatin</subject><subject>pravastatin</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Swine</subject><subject>Tandem Mass Spectrometry</subject><subject>Xenopus laevis</subject><issn>0022-3549</issn><issn>1520-6017</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2011</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp10s2O0zAQAGALgdhSOPACyBJCiEO2zo8T51i1S9mlYittEUfLccbFJY2DnQB9GN6VKW0XCcHJ0cznmdhjQp7H7DJmLJlsu3CZJFzkD8go5gmLchYXD8kIc0mU8qy8IE9C2DLGcsb5Y3KRHBQTYkR-zq0x4KHtrWroFX7rnjpDF151YPxge3ozWA3UtfS67SH0tkU4rYLzXW8xiviuVxgOdD4A7R26z7ay5-St36jWajptD4G1V23onEe_oSvX7DvAMjVQ1dYT5-kq2jR77TrverDtU_LIqCbAs9M6Jh_fXq1n76Ll7eJ6Nl1Gmuc8jzLBMwM5U0aVuco5F8aUpRFQxhVklQLFIKnqMk6VKERmeKkxz2qhIItTk6Vj8vpYF_t-HfCQcmeDhqZRLbghSFHwIkkF4jF5-ZfcusHjlQQZ87hIRVHmAtWbo9LeheDByM7bnfJ7GTN5GJnEkcnfI0P74lRxqHZQ38vzjBC8OgEVtGoM3qC24Y_LMvy9rEQ3ObrvtoH9_zvKm9XduXV03GFDDz_udyj_ReZFWnD56cNCrvlsvp6_z-QSfXr0gLP4ZsHLoC20Gmrr8d3I2tl_HPAXr-zQYw</recordid><startdate>201109</startdate><enddate>201109</enddate><creator>Shirasaka, Yoshiyuki</creator><creator>Suzuki, Kensuke</creator><creator>Nakanishi, Takeo</creator><creator>Tamai, Ikumi</creator><general>Elsevier Inc</general><general>Wiley Subscription Services, Inc., A Wiley Company</general><general>Wiley</general><general>American Pharmaceutical Association</general><general>Elsevier Limited</general><scope>BSCLL</scope><scope>IQODW</scope><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>7QO</scope><scope>7QP</scope><scope>7QR</scope><scope>7TK</scope><scope>7U7</scope><scope>8FD</scope><scope>C1K</scope><scope>FR3</scope><scope>P64</scope><scope>RC3</scope><scope>7X8</scope></search><sort><creationdate>201109</creationdate><title>Differential Effect of Grapefruit Juice on Intestinal Absorption of Statins Due to Inhibition of Organic Anion Transporting Polypeptide and/or P-glycoprotein</title><author>Shirasaka, Yoshiyuki ; Suzuki, Kensuke ; Nakanishi, Takeo ; Tamai, Ikumi</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c5656-4854fe60afa96a6558ff99f8e91be4baea0e2bd913a8784f59cf990d8ae413f43</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2011</creationdate><topic>Animals</topic><topic>ATP-Binding Cassette, Sub-Family B, Member 1 - antagonists & inhibitors</topic><topic>Beverages</topic><topic>Biological and medical sciences</topic><topic>Chromatography, Liquid</topic><topic>Citrus paradisi</topic><topic>Flavanones - pharmacology</topic><topic>General pharmacology</topic><topic>grapefruit juice</topic><topic>Hydroxymethylglutaryl-CoA Reductase Inhibitors - pharmacokinetics</topic><topic>interaction</topic><topic>Intestinal Absorption</topic><topic>LLC-PK1 Cells</topic><topic>Male</topic><topic>Medical sciences</topic><topic>naringin</topic><topic>OATP</topic><topic>Organic Anion Transporters - antagonists & inhibitors</topic><topic>P-glycoprotein</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>pitavastatin</topic><topic>pravastatin</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Swine</topic><topic>Tandem Mass Spectrometry</topic><topic>Xenopus laevis</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Shirasaka, Yoshiyuki</creatorcontrib><creatorcontrib>Suzuki, Kensuke</creatorcontrib><creatorcontrib>Nakanishi, Takeo</creatorcontrib><creatorcontrib>Tamai, Ikumi</creatorcontrib><collection>Istex</collection><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Biotechnology Research Abstracts</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>Chemoreception Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Toxicology Abstracts</collection><collection>Technology Research Database</collection><collection>Environmental Sciences and Pollution Management</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>Genetics Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Journal of pharmaceutical sciences</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Shirasaka, Yoshiyuki</au><au>Suzuki, Kensuke</au><au>Nakanishi, Takeo</au><au>Tamai, Ikumi</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Differential Effect of Grapefruit Juice on Intestinal Absorption of Statins Due to Inhibition of Organic Anion Transporting Polypeptide and/or P-glycoprotein</atitle><jtitle>Journal of pharmaceutical sciences</jtitle><addtitle>J. Pharm. Sci</addtitle><date>2011-09</date><risdate>2011</risdate><volume>100</volume><issue>9</issue><spage>3843</spage><epage>3853</epage><pages>3843-3853</pages><issn>0022-3549</issn><eissn>1520-6017</eissn><coden>JPMSAE</coden><abstract>The purpose of this study is to examine the contributions of organic anion transporting polypeptide (Oatp) and/or P-glycoprotein (P-gp) to grapefruit juice (GFJ) interaction with two statins, pravastatin and pitavastatin, which undergo negligible metabolism in rats. The two statins were found to be substrates of both Oatp1a5 and Oatp2b1, whereas pitavastatin, but not pravastatin, was a substrate of P-gp. The plasma concentration of pravastatin after oral administration was significantly decreased by GFJ and naringin, whereas that of pitavastatin was significantly increased. Naringin inhibited Oatp1a5- and Oatp2b1-mediated uptake of pravastatin and Oatp1a5-mediated, but not Oatp2b1-mediated, uptake of pitavastatin. Naringin also inhibited P-gp-mediated transport of pitavastatin. These results suggested that the decrease of pravastatin absorption in the presence of GFJ is due to the inhibitory effect of naringin on Oatp, whereas the increase of pitavastatin is due to the inhibition of P-gp. These observations are consistent with the results of in situ absorption studies. In conclusion, Oatp and/or P-gp contribute to the intestinal absorption of statins, and the differential effect of GFJ on pravastatin and pitavastatin absorption is at least partly accounted for by the different inhibitory effects of naringin on these transporters. © 2011 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 100:3843–3853, 2011</abstract><cop>Hoboken</cop><pub>Elsevier Inc</pub><pmid>21520088</pmid><doi>10.1002/jps.22586</doi><tpages>11</tpages><oa>free_for_read</oa></addata></record> |
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| subjects | Animals ATP-Binding Cassette, Sub-Family B, Member 1 - antagonists & inhibitors Beverages Biological and medical sciences Chromatography, Liquid Citrus paradisi Flavanones - pharmacology General pharmacology grapefruit juice Hydroxymethylglutaryl-CoA Reductase Inhibitors - pharmacokinetics interaction Intestinal Absorption LLC-PK1 Cells Male Medical sciences naringin OATP Organic Anion Transporters - antagonists & inhibitors P-glycoprotein Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments pitavastatin pravastatin Rats Rats, Wistar Swine Tandem Mass Spectrometry Xenopus laevis |
| title | Differential Effect of Grapefruit Juice on Intestinal Absorption of Statins Due to Inhibition of Organic Anion Transporting Polypeptide and/or P-glycoprotein |
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