Source:http://linkedlifedata.com/resource/pubmed/id/16178425
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
8
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pubmed:dateCreated |
2005-9-23
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pubmed:abstractText |
The purpose of this study was to investigate the effect of morin, a flavonoid, on the pharmacokinetics of diltiazem and one of its metabolites, desacetyldiltiazem in rats. Pharmacokinetic parameters of diltiazem and desacetyldiltiazem were determined after oral administration of diltiazem (15 mg/kg) in rats pretreated with morin (1.5, 7.5, and 15 mg/kg). Compared with the control group (given diltiazem alone), pretreatment of morin significantly increased the absorption rate constant (Ka) and peak concentration (Cmax) of diltiazem (p<0.05, p<0.01). Area under the plasma concentration-time curve (AUC) of diltiazem in rats pretreated with morin were significantly higher than that in the control group (p<0.05, p<0.01), hence the absolute bioavailability (AB%) of diltiazem was significantly higher than that of the control group (p<0.05, p<0.01). Relative bioavailability (RB%) of diltiazem in rats pretreated with morin was increased by 1.36- to 2.03-fold. The terminal half-life (t1/2) and time to reach the peak concentration (Tmax) of diltiazem were not altered significantly with morin pretreatment. AUC of desacetyldiltiazem was increased significantly (p<0.05) in rats pretreated with morin at doses of 7.5 and 15 mg/ kg, but metabolite-parent ratio (MR) of desacetyldiltiazem was decreased significantly (p<0.05), implying that pretreatment of morin could be effective to inhibit the CYP 3A4-mediated metabolism of diltiazem. There were no apparent changes of Tmax and t1/2 of desacetyldiltiazem with morin pretreatment. Collectively, the pretreatment of morin significantly altered pharmacokinetics of diltiazem, which can be attributed to increased intestinal absorption as well as reduced first-pass metabolism. Based on these results, dose modification should be taken into consideration when diltiazem is used concomitantly with morin or morin-containing dietary supplements in clinical setting.
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pubmed:commentsCorrections | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Calcium Channel Blockers,
http://linkedlifedata.com/resource/pubmed/chemical/Cytochrome P-450 Enzyme System,
http://linkedlifedata.com/resource/pubmed/chemical/Diltiazem,
http://linkedlifedata.com/resource/pubmed/chemical/Flavonoids,
http://linkedlifedata.com/resource/pubmed/chemical/P-Glycoprotein,
http://linkedlifedata.com/resource/pubmed/chemical/deacetyldiltiazem,
http://linkedlifedata.com/resource/pubmed/chemical/morin
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pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
0253-6269
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
28
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
970-6
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pubmed:dateRevised |
2007-2-26
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pubmed:meshHeading |
pubmed-meshheading:16178425-Animals,
pubmed-meshheading:16178425-Biological Availability,
pubmed-meshheading:16178425-Calcium Channel Blockers,
pubmed-meshheading:16178425-Cytochrome P-450 Enzyme System,
pubmed-meshheading:16178425-Dietary Supplements,
pubmed-meshheading:16178425-Diltiazem,
pubmed-meshheading:16178425-Drug Interactions,
pubmed-meshheading:16178425-Flavonoids,
pubmed-meshheading:16178425-Intestinal Absorption,
pubmed-meshheading:16178425-Male,
pubmed-meshheading:16178425-Models, Animal,
pubmed-meshheading:16178425-P-Glycoprotein,
pubmed-meshheading:16178425-Rats,
pubmed-meshheading:16178425-Rats, Sprague-Dawley
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pubmed:year |
2005
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pubmed:articleTitle |
Effects of morin pretreatment on the pharmacokinetics of diltiazem and its major metabolite, desacetyldiltiazem in rats.
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pubmed:affiliation |
College of Pharmacy, Chosun University, 375 Seosuk-Dong, Dong-Gu, Gwangju 501-759, Korea.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Retracted Publication
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