Study on pharmacokinetics of radioactive labelled defibrotide after oral or intravenous administration in rats.

Abstract:

:Defibrotide (D) was labelled with 125I or with 32P. The radiolabelled compounds ([125I]-Defibrotide ([125I]-D), [32P]-Defibrotide ([32P]-D) retained the same profibrinolytic activity, in vitro, as the parent drug, suggesting that the labelling procedures had not modified the pharmacological properties of D and hence that its chemical structure was not affected significantly. After single intravenous or oral administration of [125I]-D or [32P]-D the pharmacokinetic parameters for the two labels were generally in good agreement (75%). t 1/2 alpha was in the range of minutes while t 1/2 beta was in the range of hours. Bioavailability, following single oral administration of [125I]-D or [32P]-D, was in the range of 58-70%. These data suggest that D, in spite of its macromolecular nature, is absorbed, after oral administration, fairly well.

journal_name

Thromb Res

journal_title

Thrombosis research

authors

Fisher J,Holland TK,Pescador R,Porta R,Ferro L

doi

10.1016/0049-3848(95)00213-8

subject

Has Abstract

pub_date

1996-01-01 00:00:00

pages

55-63

issue

1

eissn

0049-3848

issn

1879-2472

pii

0049-3848(95)00213-8

journal_volume

81

pub_type

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