Enhancement of Oral Bioavailability of Spironolactone by β- and γ-Cyclodextrin Complexations
Inclusion complex formations of spironolactone (SP) with three cyclodextrins (α-, β-, γ-CyDs) in aqueous solution and in the solid state were studied by the solubility method, by spectroscopic methods (UV, CD, IR) and by X-ray diffractometry, and their modes of interaction were assessed. The solid c...
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| Veröffentlicht in: | Chemical & pharmaceutical bulletin 1983/01/25, Vol.31(1), pp.286-291 |
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| container_title | Chemical & pharmaceutical bulletin |
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| creator | SEO, HAKARU TSURUOKA, MICHIO HASHIMOTO, TSUYOSHI FUJINAGA, TOSHIO OTAGIRI, MASAKI UEKAMA, KANETO |
| description | Inclusion complex formations of spironolactone (SP) with three cyclodextrins (α-, β-, γ-CyDs) in aqueous solution and in the solid state were studied by the solubility method, by spectroscopic methods (UV, CD, IR) and by X-ray diffractometry, and their modes of interaction were assessed. The solid complexes of SP with β- and γ-CyDs were obtained in molar ratios of 1 : 2 and 2 : 3, respectively, and their dissolution, membrane permeation and oral absorption properties were examined. The rates of dissolution and permeation through a cellophane membrane in water were significantly increased by inclusion complexation (γ-CyD complex>β-CyD complex>SP alone), depending upon the solubility of the test samples. The serum levels of SP following oral administration of CyD complexes were found to be greater than those after administration of SP alone. The results indicated that the γ-CyD complex rather than β-CyD complex may have great utility as a faster dissolving form of SP able to produce higher serum levels. |
| doi_str_mv | 10.1248/cpb.31.286 |
| format | Article |
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The solid complexes of SP with β- and γ-CyDs were obtained in molar ratios of 1 : 2 and 2 : 3, respectively, and their dissolution, membrane permeation and oral absorption properties were examined. The rates of dissolution and permeation through a cellophane membrane in water were significantly increased by inclusion complexation (γ-CyD complex>β-CyD complex>SP alone), depending upon the solubility of the test samples. The serum levels of SP following oral administration of CyD complexes were found to be greater than those after administration of SP alone. The results indicated that the γ-CyD complex rather than β-CyD complex may have great utility as a faster dissolving form of SP able to produce higher serum levels.</description><identifier>ISSN: 0009-2363</identifier><identifier>EISSN: 1347-5223</identifier><identifier>DOI: 10.1248/cpb.31.286</identifier><identifier>PMID: 6850944</identifier><language>eng</language><publisher>Japan: The Pharmaceutical Society of Japan</publisher><subject>Animals ; beta-Cyclodextrins ; Biological Availability ; Cyclodextrins - pharmacology ; Dextrins - pharmacology ; Dogs ; gamma-Cyclodextrins ; Male ; serum level of canrenone in dog ; Spironolactone - metabolism ; Starch - pharmacology</subject><ispartof>Chemical and Pharmaceutical Bulletin, 1983/01/25, Vol.31(1), pp.286-291</ispartof><rights>The Pharmaceutical Society of Japan</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4216-9afb8bfeb49c6ea7023af708d6cc190c6e0595fbde303961e28675728dfb68fc3</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,1883,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/6850944$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>SEO, HAKARU</creatorcontrib><creatorcontrib>TSURUOKA, MICHIO</creatorcontrib><creatorcontrib>HASHIMOTO, TSUYOSHI</creatorcontrib><creatorcontrib>FUJINAGA, TOSHIO</creatorcontrib><creatorcontrib>OTAGIRI, MASAKI</creatorcontrib><creatorcontrib>UEKAMA, KANETO</creatorcontrib><title>Enhancement of Oral Bioavailability of Spironolactone by β- and γ-Cyclodextrin Complexations</title><title>Chemical & pharmaceutical bulletin</title><addtitle>Chem. Pharm. Bull.</addtitle><description>Inclusion complex formations of spironolactone (SP) with three cyclodextrins (α-, β-, γ-CyDs) in aqueous solution and in the solid state were studied by the solubility method, by spectroscopic methods (UV, CD, IR) and by X-ray diffractometry, and their modes of interaction were assessed. The solid complexes of SP with β- and γ-CyDs were obtained in molar ratios of 1 : 2 and 2 : 3, respectively, and their dissolution, membrane permeation and oral absorption properties were examined. The rates of dissolution and permeation through a cellophane membrane in water were significantly increased by inclusion complexation (γ-CyD complex>β-CyD complex>SP alone), depending upon the solubility of the test samples. The serum levels of SP following oral administration of CyD complexes were found to be greater than those after administration of SP alone. The results indicated that the γ-CyD complex rather than β-CyD complex may have great utility as a faster dissolving form of SP able to produce higher serum levels.</description><subject>Animals</subject><subject>beta-Cyclodextrins</subject><subject>Biological Availability</subject><subject>Cyclodextrins - pharmacology</subject><subject>Dextrins - pharmacology</subject><subject>Dogs</subject><subject>gamma-Cyclodextrins</subject><subject>Male</subject><subject>serum level of canrenone in dog</subject><subject>Spironolactone - metabolism</subject><subject>Starch - pharmacology</subject><issn>0009-2363</issn><issn>1347-5223</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1983</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFkF9LwzAUxYMoc05ffBfyLHTmT5umj1rmHxjsQX21JGniMtqkpFXWr6XfY5_Jjo75ci-c37kH7gHgGqM5JjG_U42cUzwnnJ2AKaZxGiWE0FMwRQhlEaGMnoOLtt0gRBKU0gmYMJ6gLI6n4GPh1sIpXWvXQW_gKogKPlgvvoWthLSV7fq9_trY4J2vhOq801D2cPcTQeFKuPuN8l5VvtTbLlgHc183ld6KznrXXoIzI6pWXx32DLw_Lt7y52i5enrJ75eRiglmUSaM5NJoGWeKaZEiQoVJES-ZUjhDg4aSLDGy1BTRjGE9vJomKeGlkYwbRWfgdsxVwbdt0KZogq1F6AuMin1HxdBRQXExHA7mm9HcfMlal0froZSB5yPftJ341EcuQmdVpfdROEv4Pg6PY0j9p2sRCu3oHzdTfJU</recordid><startdate>198301</startdate><enddate>198301</enddate><creator>SEO, HAKARU</creator><creator>TSURUOKA, MICHIO</creator><creator>HASHIMOTO, TSUYOSHI</creator><creator>FUJINAGA, TOSHIO</creator><creator>OTAGIRI, MASAKI</creator><creator>UEKAMA, KANETO</creator><general>The Pharmaceutical Society of Japan</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></search><sort><creationdate>198301</creationdate><title>Enhancement of Oral Bioavailability of Spironolactone by β- and γ-Cyclodextrin Complexations</title><author>SEO, HAKARU ; TSURUOKA, MICHIO ; HASHIMOTO, TSUYOSHI ; FUJINAGA, TOSHIO ; OTAGIRI, MASAKI ; UEKAMA, KANETO</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4216-9afb8bfeb49c6ea7023af708d6cc190c6e0595fbde303961e28675728dfb68fc3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1983</creationdate><topic>Animals</topic><topic>beta-Cyclodextrins</topic><topic>Biological Availability</topic><topic>Cyclodextrins - pharmacology</topic><topic>Dextrins - pharmacology</topic><topic>Dogs</topic><topic>gamma-Cyclodextrins</topic><topic>Male</topic><topic>serum level of canrenone in dog</topic><topic>Spironolactone - metabolism</topic><topic>Starch - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>SEO, HAKARU</creatorcontrib><creatorcontrib>TSURUOKA, MICHIO</creatorcontrib><creatorcontrib>HASHIMOTO, TSUYOSHI</creatorcontrib><creatorcontrib>FUJINAGA, TOSHIO</creatorcontrib><creatorcontrib>OTAGIRI, MASAKI</creatorcontrib><creatorcontrib>UEKAMA, KANETO</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><jtitle>Chemical & pharmaceutical bulletin</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>SEO, HAKARU</au><au>TSURUOKA, MICHIO</au><au>HASHIMOTO, TSUYOSHI</au><au>FUJINAGA, TOSHIO</au><au>OTAGIRI, MASAKI</au><au>UEKAMA, KANETO</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Enhancement of Oral Bioavailability of Spironolactone by β- and γ-Cyclodextrin Complexations</atitle><jtitle>Chemical & pharmaceutical bulletin</jtitle><addtitle>Chem. Pharm. Bull.</addtitle><date>1983-01</date><risdate>1983</risdate><volume>31</volume><issue>1</issue><spage>286</spage><epage>291</epage><pages>286-291</pages><issn>0009-2363</issn><eissn>1347-5223</eissn><abstract>Inclusion complex formations of spironolactone (SP) with three cyclodextrins (α-, β-, γ-CyDs) in aqueous solution and in the solid state were studied by the solubility method, by spectroscopic methods (UV, CD, IR) and by X-ray diffractometry, and their modes of interaction were assessed. The solid complexes of SP with β- and γ-CyDs were obtained in molar ratios of 1 : 2 and 2 : 3, respectively, and their dissolution, membrane permeation and oral absorption properties were examined. The rates of dissolution and permeation through a cellophane membrane in water were significantly increased by inclusion complexation (γ-CyD complex>β-CyD complex>SP alone), depending upon the solubility of the test samples. The serum levels of SP following oral administration of CyD complexes were found to be greater than those after administration of SP alone. The results indicated that the γ-CyD complex rather than β-CyD complex may have great utility as a faster dissolving form of SP able to produce higher serum levels.</abstract><cop>Japan</cop><pub>The Pharmaceutical Society of Japan</pub><pmid>6850944</pmid><doi>10.1248/cpb.31.286</doi><tpages>6</tpages><oa>free_for_read</oa></addata></record> |
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| ispartof | Chemical and Pharmaceutical Bulletin, 1983/01/25, Vol.31(1), pp.286-291 |
| issn | 0009-2363 1347-5223 |
| language | eng |
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| source | MEDLINE; J-STAGE (Japan Science & Technology Information Aggregator, Electronic) Freely Available Titles - Japanese; EZB-FREE-00999 freely available EZB journals; Free Full-Text Journals in Chemistry |
| subjects | Animals beta-Cyclodextrins Biological Availability Cyclodextrins - pharmacology Dextrins - pharmacology Dogs gamma-Cyclodextrins Male serum level of canrenone in dog Spironolactone - metabolism Starch - pharmacology |
| title | Enhancement of Oral Bioavailability of Spironolactone by β- and γ-Cyclodextrin Complexations |
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