Abstract:
PURPOSE:To assess the uridine diphosphate (UDP)-glucuronosyltransferase (UGT) isozymes involved in the glucuronidation of niflumic acid in human liver. METHODS:The glucuronidation activity of niflumic acid was determined in liver microsomes and recombinant UGT isozymes by incubation of niflumic acid with UDP-glucuronic acid (UDPGA). RESULTS:Incubation of niflumic acid with liver microsomes and UDPGA produced one peak, which was identified as a glucuronide from mass spectrometric analysis. A study involving a panel of recombinant human UGT isozymes showed that glucuronidation activity was highest in UGT1A1 among the isozymes investigated. The glucuronidation in human liver microsomes (HLMs) followed Michaelis-Menten kinetics with a Km value of 16 microM, which is similar to that found with recombinant UGT1A1. The glucuronidation activity of niflumic acid in microsomes from eight human livers significantly correlated with UGT1A1-catalyzed estradiol 3beta-glucuronidation activity (r=0.78, p<0.05). Beta-estradiol inhibited niflumic acid glucuronidation with an IC50 of 25 microM in HLMs, comparable to that for UGT1A1. CONCLUSIONS:These findings indicate that UGT1A1 is the main isozyme involved in the glucuronidation of niflumic acid in the human liver.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Mano Y,Usui T,Kamimura Hdoi
10.1007/s11095-006-0250-5subject
Has Abstractpub_date
2006-07-01 00:00:00pages
1502-8issue
7eissn
0724-8741issn
1573-904Xjournal_volume
23pub_type
杂志文章abstract:PURPOSE:In this work a novel pH-responsive nanoscale polymer network was investigated for potential applications in nanomedicine. These consisted of a polybasic core surface stabilized with poly(ethylene glycol) grafts. The ability to control swelling properties via changes in core hydrophobicity and crosslinking feed ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-008-9704-2
更新日期:2009-01-01 00:00:00
abstract:PURPOSE:Study the radiolysis of solid-state metoclopramide hydrochloride at various absorbed doses. Elucidate the structure of the degradation products to gain information on the radiolysis mechanisms. METHODS:Solid-state metoclopramide samples were irradiated at several doses with gamma rays and high-energy electrons...
journal_title:Pharmaceutical research
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更新日期:2006-06-01 00:00:00
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journal_title:Pharmaceutical research
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更新日期:2018-08-30 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:2008-02-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:1997-06-01 00:00:00
abstract:PURPOSE:Delivery of apoptosis-inducing compounds to hepatic stellate cells (HSC) may be an effective strategy to reverse liver fibrosis. The aim of this study was therefore to examine the selective targeting of the apoptosis-inducing drug 15-deoxy-delta12,14-prostaglandin J2 (15dPGJ2) with two different HSC-carriers: h...
journal_title:Pharmaceutical research
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abstract::Nasal sprays containing different concentrations of the somatostatin analogue octreotide and sodium tauro-24,25-dihydrofusidate (STDHF) as an absorption promoter were evaluated in two consecutive pharmacokinetic studies in healthy volunteers to characterize their bioavailability and local tolerability. The concentrati...
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更新日期:2011-08-01 00:00:00
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更新日期:1999-06-01 00:00:00
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更新日期:2001-08-01 00:00:00
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更新日期:2004-08-01 00:00:00
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更新日期:1998-05-01 00:00:00
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更新日期:2015-03-01 00:00:00
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pub_type: 杂志文章
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更新日期:2012-05-01 00:00:00
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更新日期:2013-04-01 00:00:00
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更新日期:2014-11-01 00:00:00
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更新日期:2007-02-01 00:00:00
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更新日期:2009-02-01 00:00:00
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更新日期:2020-03-25 00:00:00