Source:http://linkedlifedata.com/resource/pubmed/id/11499619
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
1
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| pubmed:dateCreated |
2001-8-13
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| pubmed:abstractText |
Bucolome (BCP) is a non-steroidal anti-inflammatory drug, which is used in the treatment of chronic articular rheumatism. Bucolome N-glucuronide (BCP-NG), a metabolite of BCP, is the first unique N-glucuronide of barbituric acid derivatives. First, the stability of BCP-NG in various pH aqueous solutions was studied. BCP-NG was quite unstable under neutral and acidic conditions, and is easily hydrolyzed to BCP. Based on these characteristics of BCP-NG, a simple, rapid and highly sensitive method for the simultaneous determination of BCP and BCP-NG with phenylbutazone (I.S.) in biological fluids was developed using high-performance liquid chromatography (HPLC). A reversed-phase ODS column was used for the separation of BCP, BCP-NG and I.S. A pharmacokinetic study for BCP and BCP-NG was carried out in male Wistar/ST rats following i.v. administration of BCP at a dose of 10 mg/kg body weight. The slow plasma elimination of BCP with time was shown. A major metabolite of BCP in bile was N-glucuronide. The cumulative amounts of BCP and BCP-NG in the bile over 8 h were approximately 2.4 +/- 1.4% and 12.6 +/- 2.3% of the dose, respectively. BCP and BCP-NG in the urine were 2.7 +/- 0.7% and 3.2 +/- 0.3% of the dose. Although BCP had a long half-life (over 8.5 h), the preliminary pharmacokinetic parameters (0-8 h) were determined: t 1/2, 8.52 +/- 1.96 h; AUC, 419.9 +/- 45.2 microg x h/ml; MRT, 3.29 +/- 0.11 h; CLtot, 5.93 +/- 0.54 ml/h; and Vdss, 19.5 +/- 1.3 l. These observations are the first pharmacokinetic findings for the N-glucuronide of the barbituric acid derivatives.
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| pubmed:language |
eng
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| pubmed:journal | |
| pubmed:citationSubset |
IM
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| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Aug
|
| pubmed:issn |
1387-2273
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| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:day |
5
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| pubmed:volume |
759
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| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
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| pubmed:pagination |
153-9
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| pubmed:dateRevised |
2003-11-14
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| pubmed:meshHeading |
pubmed-meshheading:11499619-Animals,
pubmed-meshheading:11499619-Anti-Inflammatory Agents, Non-Steroidal,
pubmed-meshheading:11499619-Barbiturates,
pubmed-meshheading:11499619-Biliary Tract,
pubmed-meshheading:11499619-Glucuronides,
pubmed-meshheading:11499619-Half-Life,
pubmed-meshheading:11499619-Male,
pubmed-meshheading:11499619-Rats,
pubmed-meshheading:11499619-Rats, Wistar,
pubmed-meshheading:11499619-Reproducibility of Results,
pubmed-meshheading:11499619-Sensitivity and Specificity
|
| pubmed:year |
2001
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| pubmed:articleTitle |
Metabolism of bucolome in rats. Stability and biliary excretion of bucolome N-glucuronide.
|
| pubmed:affiliation |
Department of Pharmaceutics, Meiji Pharmaceutical University, Tokyo, Japan. k-mohri@my-pharm.ac.jp
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| pubmed:publicationType |
Journal Article
|