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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
8
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pubmed:dateCreated |
1991-11-5
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pubmed:abstractText |
Aucubin, a promising hepatoprotecting iridoid glucoside, was given intravenously (iv), orally (po), intraperitoneally (ip), and hepatoportally (pv) to rats. A linear pharmacokinetic behavior was obtained after iv administation of 400-400 mg/kg of aucubin. The half-life of aucubin in the postdistributive phase (t1/2, beta), total-body plasma clearance (CLt), and volume of distribution (Vdss) were 42.5 min, 7.2 ml/min/kg, and 346.9 ml/kg, respectively, for a 40 mg/kg dose. There was no significant difference in the parameters as a reult of increasing dose. The partition coefficients of aucubin between n-octanol and buffers of pH 3.0-10.0 were low, while 18.5 +/- 1.3% of aucubin in whole blood partitioned into the blood cells. Plasma protein binding of aucubin was only 9%. The bioavailabilites of aucubin after administration at a dose of 100 mg/kg through pv, ip, and po routes were 83.5, 76.8, and 19.3%, respectively. The pH-stability profile indicated rapid degradation of aucubin at pH 1.2, 1.6, and 2.0, with degradation half-lives of 5.1, 5.8, and 14.8 hr, respectively, at 37 degrees C. Therefore, the low oral bioavailability of aucubin may be attributed to pH-instability in the gastric fluid, poor GI absorption due to low lipophilicity, and the possible metabolism in the GI mucosa and liver (so called first-pass effect).
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Blood Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Glucosides,
http://linkedlifedata.com/resource/pubmed/chemical/Iridoid Glucosides,
http://linkedlifedata.com/resource/pubmed/chemical/Iridoids,
http://linkedlifedata.com/resource/pubmed/chemical/aucubin
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pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
0724-8741
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
8
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1059-63
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:1924160-Animals,
pubmed-meshheading:1924160-Biological Availability,
pubmed-meshheading:1924160-Blood Proteins,
pubmed-meshheading:1924160-Drug Stability,
pubmed-meshheading:1924160-Glucosides,
pubmed-meshheading:1924160-Iridoid Glucosides,
pubmed-meshheading:1924160-Iridoids,
pubmed-meshheading:1924160-Male,
pubmed-meshheading:1924160-Protein Binding,
pubmed-meshheading:1924160-Rats,
pubmed-meshheading:1924160-Rats, Inbred Strains,
pubmed-meshheading:1924160-Solubility
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pubmed:year |
1991
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pubmed:articleTitle |
Pharmacokinetic study of an iridoid glucoside: aucubin.
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pubmed:affiliation |
College of Pharmacy, Seoul National University, Korea.
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pubmed:publicationType |
Journal Article
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