Document Detail


Sevelamer, a phosphate-binding polymer, is a non-absorbed compound.
MedLine Citation:
PMID:  12083979     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
OBJECTIVE: To examine the absorption, distribution and excretion of sevelamer hydrochloride in rats and humans. PARTICIPANTS: Twelve male Sprague-Dawley rats were used in the animal study, and twenty human volunteers participated in the clinical trial. METHODS: In the animal study, six rats received a single oral dose of [(3)H]sevelamer and six rats were pretreated with unlabelled sevelamer in the diet for 28 days followed by a single dose of [(3)H]sevelamer on day 29. Total urine and faeces were collected at intervals up to 72 hours post dose, and tissues were obtained at the time of sacrifice. In the clinical trial, subjects received a single oral dose of [(14)C]sevelamer following 28 days of pretreatment with unlabelled sevelamer. Blood, urine and faeces samples were collected at intervals up to 96 hours. RESULTS: In the rat study, no significant urinary excretion of radioactivity was observed. The average recovery of radioactivity in the faeces was 98% in the single-dose group and greater than 100% in the group pretreated with unlabelled sevelamer for 28 days. A total of less than 0.1% of the dose was found in the tissues. In the human study, no detectable amount of (14)C was found in the blood of any subject at any time. The majority of subjects had no detectable amounts of (14)C recovered in the urine. In subjects where (14)C was recovered in the urine, less than 0.02% was detected, a level equivalent to the free (14)C detected in the [(14)C]sevelamer preparation. On average, greater than 99% of the administered dose was recovered in the faeces of the subjects. CONCLUSION: These studies demonstrate that sevelamer is a non-absorbed compound.
Authors:
Melissa A Plone; John S Petersen; David P Rosenbaum; Steven K Burke
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Publication Detail:
Type:  Clinical Trial; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Clinical pharmacokinetics     Volume:  41     ISSN:  0312-5963     ISO Abbreviation:  Clin Pharmacokinet     Publication Date:  2002  
Date Detail:
Created Date:  2002-06-26     Completed Date:  2002-08-23     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  7606849     Medline TA:  Clin Pharmacokinet     Country:  New Zealand    
Other Details:
Languages:  eng     Pagination:  517-23     Citation Subset:  IM    
Affiliation:
GelTex Pharmaceuticals, Inc., 153 Second Avenue, Waltham, MA 02451, USA. mplone@geltex.com
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MeSH Terms
Descriptor/Qualifier:
Absorption
Administration, Oral
Animals
Carbon Radioisotopes / diagnostic use
Epoxy Compounds / blood,  pharmacokinetics*,  urine
Feces / chemistry
Humans
Male
Phosphates / metabolism*
Polyamines
Polyethylenes / pharmacokinetics*
Polymers / pharmacokinetics*
Rats
Rats, Sprague-Dawley
Species Specificity
Time Factors
Tissue Distribution
Tritium / diagnostic use
Chemical
Reg. No./Substance:
0/Carbon Radioisotopes; 0/Epoxy Compounds; 0/Phosphates; 0/Polyamines; 0/Polyethylenes; 0/Polymers; 10028-17-8/Tritium; 182683-00-7/sevelamer

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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