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Pharmacokinetics of albendazole sulfoxide enantiomers administered in racemic form and separately in rats
The pharmacokinetic behaviour of albendazole sulfoxide (ABZSO) enantiomers was studied in rats after the oral administration of 10 mg/kg of rac-ABZSO, 5 mg/kg of (−)-ABZSO or 5 mg/kg of (+)-ABZSO. The disposition profiles of ABZSO enantiomers were similar in all treatments, but the calculated area u...
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Published in: | The veterinary journal (1997) 2008-08, Vol.177 (2), p.297-299 |
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container_title | The veterinary journal (1997) |
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creator | Capece, Bettencourt P.S. Castells, Gloria Godoy, Carlo Arboix, Margarita Cristòfol, Carles |
description | The pharmacokinetic behaviour of albendazole sulfoxide (ABZSO) enantiomers was studied in rats after the oral administration of 10
mg/kg of
rac-ABZSO, 5
mg/kg of (−)-ABZSO or 5
mg/kg of (+)-ABZSO. The disposition profiles of ABZSO enantiomers were similar in all treatments, but the calculated area under the curve for the (−)-ABZSO was higher in all cases compared with (+)-ABZSO. The results suggest that there is no chiral inversion of ABZSO enantiomers. After the administration of
rac-ABZSO, 17.2% of the total dose was recovered in urine as albendazole ABZ (0.1%), albendazole sulfone ABZSO
2 (0.3%), albendazole 2-aminosulfone (ABZ-SO
2NH
2) (3.1%) and ABZSO (13.7%). The ratio (+) to (−) was similar in urine (1.6) and blood (1.7). |
doi_str_mv | 10.1016/j.tvjl.2007.04.011 |
format | article |
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mg/kg of
rac-ABZSO, 5
mg/kg of (−)-ABZSO or 5
mg/kg of (+)-ABZSO. The disposition profiles of ABZSO enantiomers were similar in all treatments, but the calculated area under the curve for the (−)-ABZSO was higher in all cases compared with (+)-ABZSO. The results suggest that there is no chiral inversion of ABZSO enantiomers. After the administration of
rac-ABZSO, 17.2% of the total dose was recovered in urine as albendazole ABZ (0.1%), albendazole sulfone ABZSO
2 (0.3%), albendazole 2-aminosulfone (ABZ-SO
2NH
2) (3.1%) and ABZSO (13.7%). The ratio (+) to (−) was similar in urine (1.6) and blood (1.7).</description><identifier>ISSN: 1090-0233</identifier><identifier>EISSN: 1532-2971</identifier><identifier>DOI: 10.1016/j.tvjl.2007.04.011</identifier><identifier>PMID: 17566773</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Administration, Oral ; albendazole ; Albendazole - administration & dosage ; Albendazole - analogs & derivatives ; Albendazole - blood ; Albendazole - chemistry ; Albendazole - pharmacokinetics ; Albendazole sulfoxide ; animal diseases ; animal models ; Animals ; Anthelmintics - administration & dosage ; Anthelmintics - blood ; Anthelmintics - chemistry ; Anthelmintics - pharmacokinetics ; dosage ; Dose-Response Relationship, Drug ; drug evaluation ; drug formulations ; drug therapy ; Enantiomers ; Enantioselectivity ; helminthiasis ; Isomerism ; metabolites ; oral administration ; Pharmacokinetics ; Rats ; veterinary drugs ; veterinary medicine</subject><ispartof>The veterinary journal (1997), 2008-08, Vol.177 (2), p.297-299</ispartof><rights>2007 Elsevier Ltd</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c378t-9cbe3c3b0b125924ee1d8896d4a6c3a5d66e5402284801621042c6f7b6d4a3523</citedby><cites>FETCH-LOGICAL-c378t-9cbe3c3b0b125924ee1d8896d4a6c3a5d66e5402284801621042c6f7b6d4a3523</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27901,27902</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/17566773$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Capece, Bettencourt P.S.</creatorcontrib><creatorcontrib>Castells, Gloria</creatorcontrib><creatorcontrib>Godoy, Carlo</creatorcontrib><creatorcontrib>Arboix, Margarita</creatorcontrib><creatorcontrib>Cristòfol, Carles</creatorcontrib><title>Pharmacokinetics of albendazole sulfoxide enantiomers administered in racemic form and separately in rats</title><title>The veterinary journal (1997)</title><addtitle>Vet J</addtitle><description>The pharmacokinetic behaviour of albendazole sulfoxide (ABZSO) enantiomers was studied in rats after the oral administration of 10
mg/kg of
rac-ABZSO, 5
mg/kg of (−)-ABZSO or 5
mg/kg of (+)-ABZSO. The disposition profiles of ABZSO enantiomers were similar in all treatments, but the calculated area under the curve for the (−)-ABZSO was higher in all cases compared with (+)-ABZSO. The results suggest that there is no chiral inversion of ABZSO enantiomers. After the administration of
rac-ABZSO, 17.2% of the total dose was recovered in urine as albendazole ABZ (0.1%), albendazole sulfone ABZSO
2 (0.3%), albendazole 2-aminosulfone (ABZ-SO
2NH
2) (3.1%) and ABZSO (13.7%). The ratio (+) to (−) was similar in urine (1.6) and blood (1.7).</description><subject>Administration, Oral</subject><subject>albendazole</subject><subject>Albendazole - administration & dosage</subject><subject>Albendazole - analogs & derivatives</subject><subject>Albendazole - blood</subject><subject>Albendazole - chemistry</subject><subject>Albendazole - pharmacokinetics</subject><subject>Albendazole sulfoxide</subject><subject>animal diseases</subject><subject>animal models</subject><subject>Animals</subject><subject>Anthelmintics - administration & dosage</subject><subject>Anthelmintics - blood</subject><subject>Anthelmintics - chemistry</subject><subject>Anthelmintics - pharmacokinetics</subject><subject>dosage</subject><subject>Dose-Response Relationship, Drug</subject><subject>drug evaluation</subject><subject>drug formulations</subject><subject>drug therapy</subject><subject>Enantiomers</subject><subject>Enantioselectivity</subject><subject>helminthiasis</subject><subject>Isomerism</subject><subject>metabolites</subject><subject>oral administration</subject><subject>Pharmacokinetics</subject><subject>Rats</subject><subject>veterinary drugs</subject><subject>veterinary medicine</subject><issn>1090-0233</issn><issn>1532-2971</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2008</creationdate><recordtype>article</recordtype><recordid>eNp9kM1u1TAQRq0K1JbCC7AAr9glHf_ESSQ2qKIUqVKRoGvLsSfgS2JfbN-K8vRNlCt1x2pGmvN9Gh1C3jKoGTB1uavLw26qOUBbg6yBsRNyzhrBK9637MWyQw8VcCHOyKucdwDQS8lPyRlrG6XaVpwT_-2XSbOx8bcPWLzNNI7UTAMGZ_7FCWk-TGP86x1SDCYUH2dMmRo3--BzwYSO-kCTsTh7S8eYZmqCoxn3JpmC0-N2Lvk1eTmaKeOb47wg99eff1zdVLd3X75efbqtrGi7UvV2QGHFAAPjTc8lInNd1ysnjbLCNE4pbCRw3slukcAZSG7V2A4rIRouLsiHrXef4p8D5qJnny1OkwkYD1mrnnPZ8WYB-QbaFHNOOOp98rNJj5qBXgXrnV4F61WwBqkXwUvo3bH9MMzoniNHowvwfgNGE7X5mXzW9985MLHIh5b164MfNwIXCw8ek87WY7DofEJbtIv-fx88ARVklwU</recordid><startdate>20080801</startdate><enddate>20080801</enddate><creator>Capece, Bettencourt P.S.</creator><creator>Castells, Gloria</creator><creator>Godoy, Carlo</creator><creator>Arboix, Margarita</creator><creator>Cristòfol, Carles</creator><general>Elsevier Ltd</general><scope>FBQ</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>20080801</creationdate><title>Pharmacokinetics of albendazole sulfoxide enantiomers administered in racemic form and separately in rats</title><author>Capece, Bettencourt P.S. ; Castells, Gloria ; Godoy, Carlo ; Arboix, Margarita ; Cristòfol, Carles</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c378t-9cbe3c3b0b125924ee1d8896d4a6c3a5d66e5402284801621042c6f7b6d4a3523</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2008</creationdate><topic>Administration, Oral</topic><topic>albendazole</topic><topic>Albendazole - administration & dosage</topic><topic>Albendazole - analogs & derivatives</topic><topic>Albendazole - blood</topic><topic>Albendazole - chemistry</topic><topic>Albendazole - pharmacokinetics</topic><topic>Albendazole sulfoxide</topic><topic>animal diseases</topic><topic>animal models</topic><topic>Animals</topic><topic>Anthelmintics - administration & dosage</topic><topic>Anthelmintics - blood</topic><topic>Anthelmintics - chemistry</topic><topic>Anthelmintics - pharmacokinetics</topic><topic>dosage</topic><topic>Dose-Response Relationship, Drug</topic><topic>drug evaluation</topic><topic>drug formulations</topic><topic>drug therapy</topic><topic>Enantiomers</topic><topic>Enantioselectivity</topic><topic>helminthiasis</topic><topic>Isomerism</topic><topic>metabolites</topic><topic>oral administration</topic><topic>Pharmacokinetics</topic><topic>Rats</topic><topic>veterinary drugs</topic><topic>veterinary medicine</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Capece, Bettencourt P.S.</creatorcontrib><creatorcontrib>Castells, Gloria</creatorcontrib><creatorcontrib>Godoy, Carlo</creatorcontrib><creatorcontrib>Arboix, Margarita</creatorcontrib><creatorcontrib>Cristòfol, Carles</creatorcontrib><collection>AGRIS</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>The veterinary journal (1997)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Capece, Bettencourt P.S.</au><au>Castells, Gloria</au><au>Godoy, Carlo</au><au>Arboix, Margarita</au><au>Cristòfol, Carles</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Pharmacokinetics of albendazole sulfoxide enantiomers administered in racemic form and separately in rats</atitle><jtitle>The veterinary journal (1997)</jtitle><addtitle>Vet J</addtitle><date>2008-08-01</date><risdate>2008</risdate><volume>177</volume><issue>2</issue><spage>297</spage><epage>299</epage><pages>297-299</pages><issn>1090-0233</issn><eissn>1532-2971</eissn><abstract>The pharmacokinetic behaviour of albendazole sulfoxide (ABZSO) enantiomers was studied in rats after the oral administration of 10
mg/kg of
rac-ABZSO, 5
mg/kg of (−)-ABZSO or 5
mg/kg of (+)-ABZSO. The disposition profiles of ABZSO enantiomers were similar in all treatments, but the calculated area under the curve for the (−)-ABZSO was higher in all cases compared with (+)-ABZSO. The results suggest that there is no chiral inversion of ABZSO enantiomers. After the administration of
rac-ABZSO, 17.2% of the total dose was recovered in urine as albendazole ABZ (0.1%), albendazole sulfone ABZSO
2 (0.3%), albendazole 2-aminosulfone (ABZ-SO
2NH
2) (3.1%) and ABZSO (13.7%). The ratio (+) to (−) was similar in urine (1.6) and blood (1.7).</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>17566773</pmid><doi>10.1016/j.tvjl.2007.04.011</doi><tpages>3</tpages></addata></record> |
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subjects | Administration, Oral albendazole Albendazole - administration & dosage Albendazole - analogs & derivatives Albendazole - blood Albendazole - chemistry Albendazole - pharmacokinetics Albendazole sulfoxide animal diseases animal models Animals Anthelmintics - administration & dosage Anthelmintics - blood Anthelmintics - chemistry Anthelmintics - pharmacokinetics dosage Dose-Response Relationship, Drug drug evaluation drug formulations drug therapy Enantiomers Enantioselectivity helminthiasis Isomerism metabolites oral administration Pharmacokinetics Rats veterinary drugs veterinary medicine |
title | Pharmacokinetics of albendazole sulfoxide enantiomers administered in racemic form and separately in rats |
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