Abstract:
:The pharmacokinetics of ketotifen fumarate (KF) was examined after administration in rabbits through four different routes (intravenous, intranasal, oral and rectal). The time-course of the plasma concentration of KF after intravenous administration (1 mg/kg dose) fitted a two-compartment open model. KF was rapidly absorbed and showed a high plasma concentration within 0.33 h after intranasal administration. The absolute bioavailability of KF after intranasal administration was 66%. After oral administration at a dose of 1 mg/kg, the plasma concentration of KF was below the detection limit of HPLC analysis. Even at 5 mg/kg, the value of the area under the plasma concentration-time curve (AUC) after oral administration of KF was significantly lower than that after intranasal administration of 1 mg/kg. Oral bioavailability was only 8%. The very low bioavailability of KF after oral administration might be due to the first-pass effect in the liver. We also prepared suppositories containing KF (1 mg/kg) for rectal administration in rabbits. After rectal administration, KF was rapidly absorbed and its bioavailability was 34%. These results indicated that the intranasal route appears the most effective for administering KF, and that rectal administration may be superior to oral administration in terms of bioavailability.
journal_name
Biol Pharm Bulljournal_title
Biological & pharmaceutical bulletinauthors
Yagi N,Taniuchi Y,Hamada K,Sudo J,Sekikawa Hdoi
10.1248/bpb.25.1614subject
Has Abstractpub_date
2002-12-01 00:00:00pages
1614-8issue
12eissn
0918-6158issn
1347-5215journal_volume
25pub_type
杂志文章abstract::Distigmine bromide (distigmine) is a reversible carbamate cholinesterase (ChE) inhibitor. Its principle clinical application is in the treatment of myasthenia gravis. Distigmine is also used as a remedy for dysuria and glaucoma. Its effectiveness in the management of dysuria has been demonstrated in several clinical r...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章,评审
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journal_title:Biological & pharmaceutical bulletin
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更新日期:2014-01-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
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journal_title:Biological & pharmaceutical bulletin
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journal_title:Biological & pharmaceutical bulletin
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journal_title:Biological & pharmaceutical bulletin
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journal_title:Biological & pharmaceutical bulletin
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journal_title:Biological & pharmaceutical bulletin
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更新日期:2010-01-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
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journal_title:Biological & pharmaceutical bulletin
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更新日期:2005-01-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
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更新日期:2015-01-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:2010-01-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章,评审
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更新日期:2004-06-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
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doi:10.1248/bpb.35.346
更新日期:2012-01-01 00:00:00