Abstract:
:The authors evaluated the effect of high-dose aspirin at a therapeutic dose, using chlorzoxazone as a probe for CYP2E1 enzyme activity. In a randomized, open-label, 2-way crossover study, 10 healthy men were treated 3 times daily for 6 days with 1 g aspirin or placebo. On day 7, 1 dose of 400 mg chlorzoxazone was administered orally. Plasma concentrations of chlorzoxazone and its metabolite, 6-hydroxychlorzoxazone, were measured. During the aspirin phase, the area under the time-concentration curve (AUC) and peak plasma concentration of chlorzoxazone were 95% (90% confidence interval [CI], 87%-103%) and 90% (90% CI, 80%-101%) of the values during the placebo phase, respectively. High-dose aspirin did not affect the oral clearance of chlorzoxazone significantly (90% CI, 98%-120%; P = .24). The AUC ratio and plasma concentration ratios of 6-hydroxychlorzoxazone/chlorzoxazone were not changed significantly by high-dose aspirin. High-dose aspirin at a therapeutic dose does not affect CYP2E1 activity in humans.
journal_name
J Clin Pharmacoljournal_title
Journal of clinical pharmacologyauthors
Park JY,Kim KA,Park PW,Ha JMdoi
10.1177/0091270005282635subject
Has Abstractpub_date
2006-01-01 00:00:00pages
109-14issue
1eissn
0091-2700issn
1552-4604pii
46/1/109journal_volume
46pub_type
临床试验,杂志文章,随机对照试验abstract::Sinbaglustat (ACT-519276), a brain-penetrating inhibitor of glucosylceramide synthase and nonlysosomal glucosylceramidase, is developed as a new therapy for lysosomal storage disorders. In the first-in-human study, sinbaglustat was primarily excreted unchanged in urine. This study was conducted to evaluate the effect ...
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journal_title:Journal of clinical pharmacology
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journal_title:Journal of clinical pharmacology
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