Sumatriptan absorption from different regions of the human gastrointestinal tract
Sumatriptan exhibits low oral bioavailability partly due to presystemic metabolism, which may vary with regional differences in metabolic activity throughout the gastrointestinal tract. This study evaluated sumatriptan absorption in humans after administration orally and by oroenteric tube into the...
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| Veröffentlicht in: | Pharmaceutical research 1995, Vol.12 (1), p.138-143 |
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| container_title | Pharmaceutical research |
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| creator | WARNER, P. E BROUWER, K. L. R HUSSEY, E. K DUKES, G. E HEIZER, W. D DONN, K. H DAVIS, I. M POWELL, J. R |
| description | Sumatriptan exhibits low oral bioavailability partly due to presystemic metabolism, which may vary with regional differences in metabolic activity throughout the gastrointestinal tract. This study evaluated sumatriptan absorption in humans after administration orally and by oroenteric tube into the jejunum and cecum. Because the site of cecal administration varied, pharmacokinetic parameters for sumatriptan and its major metabolite were compared statistically only after oral and jejunal administration. One-half of the oral dose was recovered in the urine as parent (3%) and metabolite (46%). Sumatriptan was absorbed throughout the gastrointestinal tract; absorption was similar after oral and jejunal administration, and less after cecal administration. The metabolite AUC and the AUC ratio (metabolite/parent) were significantly lower after jejunal compared to oral administration; the AUC ratio was two-fold lower after cecal administration. Results suggest that presystemic metabolism of sumatriptan varies throughout the gastrointestinal tract and/or regional differences exist in the absorption of metabolite formed within the gastrointestinal tract. |
| doi_str_mv | 10.1023/A:1016211409315 |
| format | Article |
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E ; BROUWER, K. L. R ; HUSSEY, E. K ; DUKES, G. E ; HEIZER, W. D ; DONN, K. H ; DAVIS, I. M ; POWELL, J. R</creator><creatorcontrib>WARNER, P. E ; BROUWER, K. L. R ; HUSSEY, E. K ; DUKES, G. E ; HEIZER, W. D ; DONN, K. H ; DAVIS, I. M ; POWELL, J. R</creatorcontrib><description>Sumatriptan exhibits low oral bioavailability partly due to presystemic metabolism, which may vary with regional differences in metabolic activity throughout the gastrointestinal tract. This study evaluated sumatriptan absorption in humans after administration orally and by oroenteric tube into the jejunum and cecum. Because the site of cecal administration varied, pharmacokinetic parameters for sumatriptan and its major metabolite were compared statistically only after oral and jejunal administration. One-half of the oral dose was recovered in the urine as parent (3%) and metabolite (46%). Sumatriptan was absorbed throughout the gastrointestinal tract; absorption was similar after oral and jejunal administration, and less after cecal administration. The metabolite AUC and the AUC ratio (metabolite/parent) were significantly lower after jejunal compared to oral administration; the AUC ratio was two-fold lower after cecal administration. Results suggest that presystemic metabolism of sumatriptan varies throughout the gastrointestinal tract and/or regional differences exist in the absorption of metabolite formed within the gastrointestinal tract.</description><identifier>ISSN: 0724-8741</identifier><identifier>EISSN: 1573-904X</identifier><identifier>DOI: 10.1023/A:1016211409315</identifier><identifier>PMID: 7724476</identifier><identifier>CODEN: PHREEB</identifier><language>eng</language><publisher>New York, NY: Springer</publisher><subject>Administration, Oral ; Adult ; Biological and medical sciences ; Cardiovascular system ; Cecum - metabolism ; Digestive System - metabolism ; Humans ; Intestinal Absorption ; Intubation, Gastrointestinal ; Jejunum - metabolism ; Male ; Medical sciences ; Pharmacology. Drug treatments ; Sumatriptan - administration & dosage ; Sumatriptan - blood ; Sumatriptan - pharmacokinetics ; Vasodilator agents. 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K</creatorcontrib><creatorcontrib>DUKES, G. E</creatorcontrib><creatorcontrib>HEIZER, W. D</creatorcontrib><creatorcontrib>DONN, K. H</creatorcontrib><creatorcontrib>DAVIS, I. M</creatorcontrib><creatorcontrib>POWELL, J. R</creatorcontrib><title>Sumatriptan absorption from different regions of the human gastrointestinal tract</title><title>Pharmaceutical research</title><addtitle>Pharm Res</addtitle><description>Sumatriptan exhibits low oral bioavailability partly due to presystemic metabolism, which may vary with regional differences in metabolic activity throughout the gastrointestinal tract. This study evaluated sumatriptan absorption in humans after administration orally and by oroenteric tube into the jejunum and cecum. Because the site of cecal administration varied, pharmacokinetic parameters for sumatriptan and its major metabolite were compared statistically only after oral and jejunal administration. One-half of the oral dose was recovered in the urine as parent (3%) and metabolite (46%). Sumatriptan was absorbed throughout the gastrointestinal tract; absorption was similar after oral and jejunal administration, and less after cecal administration. The metabolite AUC and the AUC ratio (metabolite/parent) were significantly lower after jejunal compared to oral administration; the AUC ratio was two-fold lower after cecal administration. Results suggest that presystemic metabolism of sumatriptan varies throughout the gastrointestinal tract and/or regional differences exist in the absorption of metabolite formed within the gastrointestinal tract.</description><subject>Administration, Oral</subject><subject>Adult</subject><subject>Biological and medical sciences</subject><subject>Cardiovascular system</subject><subject>Cecum - metabolism</subject><subject>Digestive System - metabolism</subject><subject>Humans</subject><subject>Intestinal Absorption</subject><subject>Intubation, Gastrointestinal</subject><subject>Jejunum - metabolism</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Pharmacology. Drug treatments</subject><subject>Sumatriptan - administration & dosage</subject><subject>Sumatriptan - blood</subject><subject>Sumatriptan - pharmacokinetics</subject><subject>Vasodilator agents. 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Cerebral vasodilators</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>WARNER, P. E</creatorcontrib><creatorcontrib>BROUWER, K. L. R</creatorcontrib><creatorcontrib>HUSSEY, E. K</creatorcontrib><creatorcontrib>DUKES, G. E</creatorcontrib><creatorcontrib>HEIZER, W. D</creatorcontrib><creatorcontrib>DONN, K. H</creatorcontrib><creatorcontrib>DAVIS, I. M</creatorcontrib><creatorcontrib>POWELL, J. R</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>MEDLINE - Academic</collection><jtitle>Pharmaceutical research</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>WARNER, P. E</au><au>BROUWER, K. L. R</au><au>HUSSEY, E. K</au><au>DUKES, G. E</au><au>HEIZER, W. 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Because the site of cecal administration varied, pharmacokinetic parameters for sumatriptan and its major metabolite were compared statistically only after oral and jejunal administration. One-half of the oral dose was recovered in the urine as parent (3%) and metabolite (46%). Sumatriptan was absorbed throughout the gastrointestinal tract; absorption was similar after oral and jejunal administration, and less after cecal administration. The metabolite AUC and the AUC ratio (metabolite/parent) were significantly lower after jejunal compared to oral administration; the AUC ratio was two-fold lower after cecal administration. Results suggest that presystemic metabolism of sumatriptan varies throughout the gastrointestinal tract and/or regional differences exist in the absorption of metabolite formed within the gastrointestinal tract.</abstract><cop>New York, NY</cop><pub>Springer</pub><pmid>7724476</pmid><doi>10.1023/A:1016211409315</doi><tpages>6</tpages></addata></record> |
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| ispartof | Pharmaceutical research, 1995, Vol.12 (1), p.138-143 |
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| language | eng |
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| source | MEDLINE; SpringerNature Journals |
| subjects | Administration, Oral Adult Biological and medical sciences Cardiovascular system Cecum - metabolism Digestive System - metabolism Humans Intestinal Absorption Intubation, Gastrointestinal Jejunum - metabolism Male Medical sciences Pharmacology. Drug treatments Sumatriptan - administration & dosage Sumatriptan - blood Sumatriptan - pharmacokinetics Vasodilator agents. Cerebral vasodilators |
| title | Sumatriptan absorption from different regions of the human gastrointestinal tract |
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