Importance of bile acids for novel oral absorption system containing polyamines to improve intestinal absorption
The synergetic improving effect of bile acids with spermine (SPM), a major polyamine, on the absorption of rebamipide, a poorly soluble and poorly absorbable drug (BCS Class IV), was evaluated in rats and beagle dogs. Although the absorption of rebamipide was improved by the addition of polyamines a...
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Veröffentlicht in: | Journal of controlled release 2006-10, Vol.115 (2), p.130-133 |
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creator | Miyake, Masateru Minami, Takanori Toguchi, Hajime Odomi, Masaaki Ogawara, Ken-ichi Higaki, Kazutaka Kimura, Toshikiro |
description | The synergetic improving effect of bile acids with spermine (SPM), a major polyamine, on the absorption of rebamipide, a poorly soluble and poorly absorbable drug (BCS Class IV), was evaluated in rats and beagle dogs. Although the absorption of rebamipide was improved by the addition of polyamines alone in normal rats, it was not improved in bile duct ligated (BDL) rats. The combinatorial use of sodium taurocholate (STC), a bile acid, with SPM improved the absorption of rebamipide even in BDL rats. In the beagle dogs, the oral administration of SPM alone did not enhance the absorption of rebamipide, but the combinatorial use of STC with SPM improved the absorption as well as in the BDL rats. These results indicate that bile acids are indispensable for the novel formulation containing SPM to improve the absorption of rebamipide after oral administration. |
doi_str_mv | 10.1016/j.jconrel.2006.07.015 |
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Although the absorption of rebamipide was improved by the addition of polyamines alone in normal rats, it was not improved in bile duct ligated (BDL) rats. The combinatorial use of sodium taurocholate (STC), a bile acid, with SPM improved the absorption of rebamipide even in BDL rats. In the beagle dogs, the oral administration of SPM alone did not enhance the absorption of rebamipide, but the combinatorial use of STC with SPM improved the absorption as well as in the BDL rats. These results indicate that bile acids are indispensable for the novel formulation containing SPM to improve the absorption of rebamipide after oral administration.</description><identifier>ISSN: 0168-3659</identifier><identifier>EISSN: 1873-4995</identifier><identifier>DOI: 10.1016/j.jconrel.2006.07.015</identifier><identifier>PMID: 16973235</identifier><identifier>CODEN: JCREEC</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Alanine - administration & dosage ; Alanine - analogs & derivatives ; Alanine - pharmacokinetics ; Animals ; Area Under Curve ; Beagle dog ; Bile acid ; Bile Acids and Salts - pharmacology ; Bile duct ligated rat ; Bile Ducts - physiology ; Biogenic Polyamines - pharmacology ; Biological and medical sciences ; Dogs ; General pharmacology ; Intestinal absorption ; Intestinal Absorption - drug effects ; Ligation ; Male ; Medical sciences ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Polyamine ; Quinolones - administration & dosage ; Quinolones - pharmacokinetics ; Rats ; Rats, Sprague-Dawley ; Spermine - pharmacology ; Taurocholic Acid - pharmacology</subject><ispartof>Journal of controlled release, 2006-10, Vol.115 (2), p.130-133</ispartof><rights>2006 Elsevier B.V.</rights><rights>2006 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c490t-f36091eabbf52a4ba5655cad31312a0c3646d3659fc7a4291c195e17e31e25a43</citedby><cites>FETCH-LOGICAL-c490t-f36091eabbf52a4ba5655cad31312a0c3646d3659fc7a4291c195e17e31e25a43</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.jconrel.2006.07.015$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3536,27903,27904,45974</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=18218378$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/16973235$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Miyake, Masateru</creatorcontrib><creatorcontrib>Minami, Takanori</creatorcontrib><creatorcontrib>Toguchi, Hajime</creatorcontrib><creatorcontrib>Odomi, Masaaki</creatorcontrib><creatorcontrib>Ogawara, Ken-ichi</creatorcontrib><creatorcontrib>Higaki, Kazutaka</creatorcontrib><creatorcontrib>Kimura, Toshikiro</creatorcontrib><title>Importance of bile acids for novel oral absorption system containing polyamines to improve intestinal absorption</title><title>Journal of controlled release</title><addtitle>J Control Release</addtitle><description>The synergetic improving effect of bile acids with spermine (SPM), a major polyamine, on the absorption of rebamipide, a poorly soluble and poorly absorbable drug (BCS Class IV), was evaluated in rats and beagle dogs. Although the absorption of rebamipide was improved by the addition of polyamines alone in normal rats, it was not improved in bile duct ligated (BDL) rats. The combinatorial use of sodium taurocholate (STC), a bile acid, with SPM improved the absorption of rebamipide even in BDL rats. In the beagle dogs, the oral administration of SPM alone did not enhance the absorption of rebamipide, but the combinatorial use of STC with SPM improved the absorption as well as in the BDL rats. These results indicate that bile acids are indispensable for the novel formulation containing SPM to improve the absorption of rebamipide after oral administration.</description><subject>Alanine - administration & dosage</subject><subject>Alanine - analogs & derivatives</subject><subject>Alanine - pharmacokinetics</subject><subject>Animals</subject><subject>Area Under Curve</subject><subject>Beagle dog</subject><subject>Bile acid</subject><subject>Bile Acids and Salts - pharmacology</subject><subject>Bile duct ligated rat</subject><subject>Bile Ducts - physiology</subject><subject>Biogenic Polyamines - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Dogs</subject><subject>General pharmacology</subject><subject>Intestinal absorption</subject><subject>Intestinal Absorption - drug effects</subject><subject>Ligation</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Polyamine</subject><subject>Quinolones - administration & dosage</subject><subject>Quinolones - pharmacokinetics</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Spermine - pharmacology</subject><subject>Taurocholic Acid - pharmacology</subject><issn>0168-3659</issn><issn>1873-4995</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2006</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkc1q3DAURkVpaabTPkKLNs3OrmT92FqVEtI2EOgmWQtZvi4aZMmVNIF5-2gYQ-gqK23Od--nexD6TElLCZXfDu3BxpDAtx0hsiV9S6h4g3Z06FnDlRJv0a5yQ8OkUFfoQ84HQohgvH-PrqhUPeuY2KH1blljKiZYwHHGo_OAjXVTxnNMOMQn8Dgm47EZc0xrcTHgfMoFFlzXF-OCC3_xGv3JLC5AxiVit6ypBrELBXJx4b_0R_RuNj7Dp-3do8eftw83v5v7P7_ubn7cN5YrUpqZSaIomHGcRWf4aIQUwpqJUUY7QyyTXE7nr822N7xT1FIlgPbAKHTCcLZH15e5tcu_Y-2hF5cteG8CxGPWclBSSiVeBanikvB6rz0SF9CmmHOCWa_JLSadNCX67EQf9OZEn51o0uvqpOa-bAuO4wLTS2qTUIGvG2CyNX5O1YbLL9zQ0YH1Q-W-Xziod3tykHS2Dqq5ySWwRU_RvVLlGd82r0s</recordid><startdate>20061010</startdate><enddate>20061010</enddate><creator>Miyake, Masateru</creator><creator>Minami, Takanori</creator><creator>Toguchi, Hajime</creator><creator>Odomi, Masaaki</creator><creator>Ogawara, Ken-ichi</creator><creator>Higaki, Kazutaka</creator><creator>Kimura, Toshikiro</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>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>20061010</creationdate><title>Importance of bile acids for novel oral absorption system containing polyamines to improve intestinal absorption</title><author>Miyake, Masateru ; Minami, Takanori ; Toguchi, Hajime ; Odomi, Masaaki ; Ogawara, Ken-ichi ; Higaki, Kazutaka ; Kimura, Toshikiro</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c490t-f36091eabbf52a4ba5655cad31312a0c3646d3659fc7a4291c195e17e31e25a43</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2006</creationdate><topic>Alanine - administration & dosage</topic><topic>Alanine - analogs & derivatives</topic><topic>Alanine - pharmacokinetics</topic><topic>Animals</topic><topic>Area Under Curve</topic><topic>Beagle dog</topic><topic>Bile acid</topic><topic>Bile Acids and Salts - pharmacology</topic><topic>Bile duct ligated rat</topic><topic>Bile Ducts - physiology</topic><topic>Biogenic Polyamines - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Dogs</topic><topic>General pharmacology</topic><topic>Intestinal absorption</topic><topic>Intestinal Absorption - drug effects</topic><topic>Ligation</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Polyamine</topic><topic>Quinolones - administration & dosage</topic><topic>Quinolones - pharmacokinetics</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Spermine - pharmacology</topic><topic>Taurocholic Acid - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Miyake, Masateru</creatorcontrib><creatorcontrib>Minami, Takanori</creatorcontrib><creatorcontrib>Toguchi, Hajime</creatorcontrib><creatorcontrib>Odomi, Masaaki</creatorcontrib><creatorcontrib>Ogawara, Ken-ichi</creatorcontrib><creatorcontrib>Higaki, Kazutaka</creatorcontrib><creatorcontrib>Kimura, Toshikiro</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>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Journal of controlled release</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Miyake, Masateru</au><au>Minami, Takanori</au><au>Toguchi, Hajime</au><au>Odomi, Masaaki</au><au>Ogawara, Ken-ichi</au><au>Higaki, Kazutaka</au><au>Kimura, Toshikiro</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Importance of bile acids for novel oral absorption system containing polyamines to improve intestinal absorption</atitle><jtitle>Journal of controlled release</jtitle><addtitle>J Control Release</addtitle><date>2006-10-10</date><risdate>2006</risdate><volume>115</volume><issue>2</issue><spage>130</spage><epage>133</epage><pages>130-133</pages><issn>0168-3659</issn><eissn>1873-4995</eissn><coden>JCREEC</coden><abstract>The synergetic improving effect of bile acids with spermine (SPM), a major polyamine, on the absorption of rebamipide, a poorly soluble and poorly absorbable drug (BCS Class IV), was evaluated in rats and beagle dogs. Although the absorption of rebamipide was improved by the addition of polyamines alone in normal rats, it was not improved in bile duct ligated (BDL) rats. The combinatorial use of sodium taurocholate (STC), a bile acid, with SPM improved the absorption of rebamipide even in BDL rats. In the beagle dogs, the oral administration of SPM alone did not enhance the absorption of rebamipide, but the combinatorial use of STC with SPM improved the absorption as well as in the BDL rats. These results indicate that bile acids are indispensable for the novel formulation containing SPM to improve the absorption of rebamipide after oral administration.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>16973235</pmid><doi>10.1016/j.jconrel.2006.07.015</doi><tpages>4</tpages></addata></record> |
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subjects | Alanine - administration & dosage Alanine - analogs & derivatives Alanine - pharmacokinetics Animals Area Under Curve Beagle dog Bile acid Bile Acids and Salts - pharmacology Bile duct ligated rat Bile Ducts - physiology Biogenic Polyamines - pharmacology Biological and medical sciences Dogs General pharmacology Intestinal absorption Intestinal Absorption - drug effects Ligation Male Medical sciences Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Polyamine Quinolones - administration & dosage Quinolones - pharmacokinetics Rats Rats, Sprague-Dawley Spermine - pharmacology Taurocholic Acid - pharmacology |
title | Importance of bile acids for novel oral absorption system containing polyamines to improve intestinal absorption |
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