Pharmacokinetics and Safety of Indisetron Tablets in Healthy Subjects-Single Oral Dose Study-
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Accession number;05A0015060
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| Title;Pharmacokinetics and Safety of Indisetron Tablets in Healthy Subjects-Single Oral Dose Study- |
| Author;
YAMADA TADASHI
(Nisshin Flour Milling Co., Ltd.)
TADOKORO TOYOHIRO
(Nisshin Flour Milling Co., Ltd.)
NAKATA FUMIHISA
(Nisshin Flour Milling Co., Ltd.)
YONEZAWA KATSUNOBU
(Nisshin Flour Milling Co., Ltd.)
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Journal Title;Japanese Pharmacology & Therapeutics
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Journal Code:Z0947A
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ISSN:0386-3603
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VOL.32;NO.11;PAGE.807-813(2004)
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| Figure&Table&Reference;FIG.3, TBL.7, REF.2 |
| Pub. Country;Japan |
| Language;Japanese |
| Abstract;Objectives: Indisetron is a 5-hydroxytryptamine 3 receptor antagonist and an anti-emetic agent. It shows also 5-hydroxytryptamine 4 antagonistic activity in pharmacological profiles. A single oral dose study as phase I trial for healthy male volunteers was performed to show the tolerability and the pharmacokinetic profiles of indisetron tablets at doses of 4, 8, 16 and 32mg in fasting condition, and at a 16mg dose in post-prandial. Methods: The study was conducted as a manner of dose increasing stepwisely. At each dose in fasting state, subjects were assigned randomly to 6 in active drug group and 2 in placebo group, and performed under single blind. In post-prandial at a 16mg dose, 6 subjects in the administration of the same 16mg dose under fasting condition were studied unblindly. As to pharmacokinetics, the plasma and urinary concentrations of indisetron and its metabolites were measured, and then pharmacokinetic parameters were evaluated. The safety was estimated by laboratory test, vital signs, signs and symptoms. Results: 24 healthy male volunteers (the total number of subject-steps is 38) were enrolled and 20 subjects (the total number is 30) were administrated Indisetron. Adverse drug reactions were observed in 4 subjects in fasted administration of 16mg or 32mg. They were mild and not significant problems clinically. It was revealed that the Cmax and AUC0-.INF. of the plasma concentrations of indisetron were increased in dose dependent manners, and that its absorption was rapid and not influenced by meals. It was considered that bioavailability of indisetron was high as nearly 100%. Conclusions: The tolerability and the linear pharmacokinetic profiles of indisetron tablets over the dose range investigated were shown and it was revealed that the pharmacokinetics of indisetron tablets were not influenced by meals. (author abst.) |
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