Registration Dossier

Administrative data

Endpoint:
basic toxicokinetics in vivo
Type of information:
experimental study
Adequacy of study:
supporting study
Reliability:
2 (reliable with restrictions)
Rationale for reliability incl. deficiencies:
other: Main data provided, method acceptable

Data source

Reference
Reference Type:
publication
Title:
Unnamed
Year:
1986

Materials and methods

Objective of study:
metabolism
Principles of method if other than guideline:
Rat were treated i.p with 20 mg test substance and urine was collected for 48 h. Urinary metabolites were determiend by TLC
GLP compliance:
not specified

Test material

Reference
Name:
Unnamed
Type:
Constituent
Type:
Constituent
Radiolabelling:
not specified

Test animals

Species:
rat
Strain:
not specified
Sex:
male/female

Administration / exposure

Route of administration:
intraperitoneal
Vehicle:
other: tricaprylin
Details on exposure:
After single injection urine was collected individually for 48 h
Doses / concentrations
Remarks:
Doses / Concentrations:
20 mg/ animal
5mg/ml
no further data
No. of animals per sex per dose:
10
Control animals:
no
Details on dosing and sampling:
Urine was collected in metabolism cages at - 20 C from 0-24 and 24- 48 hours .
After thawing and filtration urines were extracted using ethyl acetate. at pH 6.5 (Extract A) and , after acidification with conc. HCl, at pH 3(Extract B). After 72 h at pH 3 at room temperature and neutralisation urines were again extracted (Extract C) and the process was repeated after repeated acidification to pH 3 (Extract D)
Extracts were then examined using TLC (UV/vis detection). Metabolites were identified by means of reference substances; Medium: Ethylacetate/diisopropylether =80/20 and Methyl-isobutyl-keton/Toluene = 20/80

Results and discussion

Toxicokinetic / pharmacokinetic studies

Details on excretion:
Besides the unchanged material the following metabolites were found:
1-Methoxy-2-N-acetylamino-5-aminobenzol (CAS-Nr. 5329-17-7),
2,5-Diacetylamino-1-methoxybenzol (CAS-Nr. 51837-64-0),
2-Amino-5-nitrophenol (CAS-Nr. 121-88-0) und
2 -N-Acetylamino-1-methoxy-5-nitrobenzol (CAS-Nr. 93-27-6)
in the urine

Metabolite characterisation studies

Metabolites identified:
yes

Applicant's summary and conclusion