Effect of probucol on the oral bioavailability of cyclosporine A
We have previously reported the reduction in oral bioavailability of cyclosporine A (CsA) by probucol, a lipid-lowering drug. To evaluate the mechanism, we examined the effect of probucol on the transport of CsA across Caco-2 cell monolayers, on the influence of CsA pharmacokinetics in rats, and on...
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| Veröffentlicht in: | European journal of pharmaceutical sciences 2004-05, Vol.22 (1), p.71-77 |
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| creator | Sugimoto, Koh-ichi Sudoh, Toshiaki Tsuruoka, Shuichi Yamamoto, Yoshihisa Maezono, Sachiko Watanabe, Yoshiteru Fujimura, Akio |
| description | We have previously reported the reduction in oral bioavailability of cyclosporine A (CsA) by probucol, a lipid-lowering drug. To evaluate the mechanism, we examined the effect of probucol on the transport of CsA across Caco-2 cell monolayers, on the influence of CsA pharmacokinetics in rats, and on the change of ultraviolet-absorption spectrum of the drug. Pretreatment with probucol (50
μM) inhibited (
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| doi_str_mv | 10.1016/j.ejps.2004.02.009 |
| format | Article |
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μM) inhibited (
P<0.001) both the apical-to-basal (−73.1%) and basal-to-apical (−77.8%) fluxes of [
3
H
]-CsA. In rats, probucol orally given 6
h after, but not simultaneous with CsA did not decrease peak CsA concentration or area under the blood CsA concentration–time curve following a single oral dosing of CsA after the pretreatment with probucol for 7 days. These data indicate that P-glycoprotein-mediated active transport from intracellular to apical is not involved in the mechanism of probucol–CsA interaction, and absorption of CsA decreases in the presence of probucol in the gastrointestinal tract. In difference spectral analysis, probucol reduced the absorption peak of CsA in a concentration-dependent manner, indicating that probucol could form a complex with CsA. These results suggest that probucol interferes with CsA absorption probably by physicochemical mechanism such as complex formation, but not the enhancement of P-glycoprotein function.</description><identifier>ISSN: 0928-0987</identifier><identifier>EISSN: 1879-0720</identifier><identifier>DOI: 10.1016/j.ejps.2004.02.009</identifier><identifier>PMID: 15113585</identifier><language>eng</language><publisher>Shannon: Elsevier B.V</publisher><subject>Administration, Oral ; Animals ; Anticholesteremic Agents - administration & dosage ; Anticholesteremic Agents - pharmacology ; ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism ; Bioavailability ; Biological and medical sciences ; Biological Availability ; Biological Transport, Active ; Caco-2 ; Caco-2 Cells ; Cyclosporine - antagonists & inhibitors ; Cyclosporine - pharmacokinetics ; Cyclosporine A ; General pharmacology ; Humans ; Intestinal Absorption - drug effects ; Male ; Medical sciences ; P-glycoprotein ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Probucol ; Probucol - administration & dosage ; Probucol - pharmacology ; Rats ; Rats, Wistar ; Spectrophotometry, Ultraviolet ; Time Factors</subject><ispartof>European journal of pharmaceutical sciences, 2004-05, Vol.22 (1), p.71-77</ispartof><rights>2004 Elsevier B.V.</rights><rights>2005 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c382t-1d30058804f1833eaebce16ae6faba4e7c8d84503a82c86a2983d7e11b40f5593</citedby><cites>FETCH-LOGICAL-c382t-1d30058804f1833eaebce16ae6faba4e7c8d84503a82c86a2983d7e11b40f5593</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.ejps.2004.02.009$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=15723895$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/15113585$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Sugimoto, Koh-ichi</creatorcontrib><creatorcontrib>Sudoh, Toshiaki</creatorcontrib><creatorcontrib>Tsuruoka, Shuichi</creatorcontrib><creatorcontrib>Yamamoto, Yoshihisa</creatorcontrib><creatorcontrib>Maezono, Sachiko</creatorcontrib><creatorcontrib>Watanabe, Yoshiteru</creatorcontrib><creatorcontrib>Fujimura, Akio</creatorcontrib><title>Effect of probucol on the oral bioavailability of cyclosporine A</title><title>European journal of pharmaceutical sciences</title><addtitle>Eur J Pharm Sci</addtitle><description>We have previously reported the reduction in oral bioavailability of cyclosporine A (CsA) by probucol, a lipid-lowering drug. To evaluate the mechanism, we examined the effect of probucol on the transport of CsA across Caco-2 cell monolayers, on the influence of CsA pharmacokinetics in rats, and on the change of ultraviolet-absorption spectrum of the drug. Pretreatment with probucol (50
μM) inhibited (
P<0.001) both the apical-to-basal (−73.1%) and basal-to-apical (−77.8%) fluxes of [
3
H
]-CsA. In rats, probucol orally given 6
h after, but not simultaneous with CsA did not decrease peak CsA concentration or area under the blood CsA concentration–time curve following a single oral dosing of CsA after the pretreatment with probucol for 7 days. These data indicate that P-glycoprotein-mediated active transport from intracellular to apical is not involved in the mechanism of probucol–CsA interaction, and absorption of CsA decreases in the presence of probucol in the gastrointestinal tract. In difference spectral analysis, probucol reduced the absorption peak of CsA in a concentration-dependent manner, indicating that probucol could form a complex with CsA. These results suggest that probucol interferes with CsA absorption probably by physicochemical mechanism such as complex formation, but not the enhancement of P-glycoprotein function.</description><subject>Administration, Oral</subject><subject>Animals</subject><subject>Anticholesteremic Agents - administration & dosage</subject><subject>Anticholesteremic Agents - pharmacology</subject><subject>ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism</subject><subject>Bioavailability</subject><subject>Biological and medical sciences</subject><subject>Biological Availability</subject><subject>Biological Transport, Active</subject><subject>Caco-2</subject><subject>Caco-2 Cells</subject><subject>Cyclosporine - antagonists & inhibitors</subject><subject>Cyclosporine - pharmacokinetics</subject><subject>Cyclosporine A</subject><subject>General pharmacology</subject><subject>Humans</subject><subject>Intestinal Absorption - drug effects</subject><subject>Male</subject><subject>Medical sciences</subject><subject>P-glycoprotein</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Probucol</subject><subject>Probucol - administration & dosage</subject><subject>Probucol - pharmacology</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Spectrophotometry, Ultraviolet</subject><subject>Time Factors</subject><issn>0928-0987</issn><issn>1879-0720</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2004</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kEtLAzEUhYMotlb_gAuZje5mvEnmkQEXllIfUHCj65DJ3GBKOqnJVOi_d4YWdOXqbr5zOPcj5JpCRoGW9-sM19uYMYA8A5YB1CdkSkVVp1AxOCVTqJlIoRbVhFzEuAaAUlRwTia0oJQXopiSx6UxqPvEm2QbfLPT3iW-S_pPTHxQLmmsV9_KOtVYZ_v9yOm9dj5ufbAdJvNLcmaUi3h1vDPy8bR8X7ykq7fn18V8lWouWJ_SlgMUQkBuqOAcFTYaaamwNKpROVZatCIvgCvBtCgVqwVvK6S0ycEURc1n5O7QO8z82mHs5cZGjc6pDv0uymp4nOZ5PoDsAOrgYwxo5DbYjQp7SUGO3uRajt7k6E0Ck4O3IXRzbN81G2x_I0dRA3B7BFTUypmgOm3jH65iXNQj93DgcHDxbTHIqC12GlsbBs-y9fa_HT-dQIrk</recordid><startdate>20040501</startdate><enddate>20040501</enddate><creator>Sugimoto, Koh-ichi</creator><creator>Sudoh, Toshiaki</creator><creator>Tsuruoka, Shuichi</creator><creator>Yamamoto, Yoshihisa</creator><creator>Maezono, Sachiko</creator><creator>Watanabe, Yoshiteru</creator><creator>Fujimura, Akio</creator><general>Elsevier B.V</general><general>Elsevier</general><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>7X8</scope></search><sort><creationdate>20040501</creationdate><title>Effect of probucol on the oral bioavailability of cyclosporine A</title><author>Sugimoto, Koh-ichi ; Sudoh, Toshiaki ; Tsuruoka, Shuichi ; Yamamoto, Yoshihisa ; Maezono, Sachiko ; Watanabe, Yoshiteru ; Fujimura, Akio</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c382t-1d30058804f1833eaebce16ae6faba4e7c8d84503a82c86a2983d7e11b40f5593</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2004</creationdate><topic>Administration, Oral</topic><topic>Animals</topic><topic>Anticholesteremic Agents - administration & dosage</topic><topic>Anticholesteremic Agents - pharmacology</topic><topic>ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism</topic><topic>Bioavailability</topic><topic>Biological and medical sciences</topic><topic>Biological Availability</topic><topic>Biological Transport, Active</topic><topic>Caco-2</topic><topic>Caco-2 Cells</topic><topic>Cyclosporine - antagonists & inhibitors</topic><topic>Cyclosporine - pharmacokinetics</topic><topic>Cyclosporine A</topic><topic>General pharmacology</topic><topic>Humans</topic><topic>Intestinal Absorption - drug effects</topic><topic>Male</topic><topic>Medical sciences</topic><topic>P-glycoprotein</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Probucol</topic><topic>Probucol - administration & dosage</topic><topic>Probucol - pharmacology</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Spectrophotometry, Ultraviolet</topic><topic>Time Factors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Sugimoto, Koh-ichi</creatorcontrib><creatorcontrib>Sudoh, Toshiaki</creatorcontrib><creatorcontrib>Tsuruoka, Shuichi</creatorcontrib><creatorcontrib>Yamamoto, Yoshihisa</creatorcontrib><creatorcontrib>Maezono, Sachiko</creatorcontrib><creatorcontrib>Watanabe, Yoshiteru</creatorcontrib><creatorcontrib>Fujimura, Akio</creatorcontrib><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>MEDLINE - Academic</collection><jtitle>European journal of pharmaceutical sciences</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Sugimoto, Koh-ichi</au><au>Sudoh, Toshiaki</au><au>Tsuruoka, Shuichi</au><au>Yamamoto, Yoshihisa</au><au>Maezono, Sachiko</au><au>Watanabe, Yoshiteru</au><au>Fujimura, Akio</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Effect of probucol on the oral bioavailability of cyclosporine A</atitle><jtitle>European journal of pharmaceutical sciences</jtitle><addtitle>Eur J Pharm Sci</addtitle><date>2004-05-01</date><risdate>2004</risdate><volume>22</volume><issue>1</issue><spage>71</spage><epage>77</epage><pages>71-77</pages><issn>0928-0987</issn><eissn>1879-0720</eissn><abstract>We have previously reported the reduction in oral bioavailability of cyclosporine A (CsA) by probucol, a lipid-lowering drug. To evaluate the mechanism, we examined the effect of probucol on the transport of CsA across Caco-2 cell monolayers, on the influence of CsA pharmacokinetics in rats, and on the change of ultraviolet-absorption spectrum of the drug. Pretreatment with probucol (50
μM) inhibited (
P<0.001) both the apical-to-basal (−73.1%) and basal-to-apical (−77.8%) fluxes of [
3
H
]-CsA. In rats, probucol orally given 6
h after, but not simultaneous with CsA did not decrease peak CsA concentration or area under the blood CsA concentration–time curve following a single oral dosing of CsA after the pretreatment with probucol for 7 days. These data indicate that P-glycoprotein-mediated active transport from intracellular to apical is not involved in the mechanism of probucol–CsA interaction, and absorption of CsA decreases in the presence of probucol in the gastrointestinal tract. In difference spectral analysis, probucol reduced the absorption peak of CsA in a concentration-dependent manner, indicating that probucol could form a complex with CsA. These results suggest that probucol interferes with CsA absorption probably by physicochemical mechanism such as complex formation, but not the enhancement of P-glycoprotein function.</abstract><cop>Shannon</cop><pub>Elsevier B.V</pub><pmid>15113585</pmid><doi>10.1016/j.ejps.2004.02.009</doi><tpages>7</tpages></addata></record> |
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| ispartof | European journal of pharmaceutical sciences, 2004-05, Vol.22 (1), p.71-77 |
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| subjects | Administration, Oral Animals Anticholesteremic Agents - administration & dosage Anticholesteremic Agents - pharmacology ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism Bioavailability Biological and medical sciences Biological Availability Biological Transport, Active Caco-2 Caco-2 Cells Cyclosporine - antagonists & inhibitors Cyclosporine - pharmacokinetics Cyclosporine A General pharmacology Humans Intestinal Absorption - drug effects Male Medical sciences P-glycoprotein Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Probucol Probucol - administration & dosage Probucol - pharmacology Rats Rats, Wistar Spectrophotometry, Ultraviolet Time Factors |
| title | Effect of probucol on the oral bioavailability of cyclosporine A |
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