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Please be aware that this old REACH registration data factsheet is no longer maintained; it remains frozen as of 19th May 2023.

The new ECHA CHEM database has been released by ECHA, and it now contains all REACH registration data. There are more details on the transition of ECHA's published data to ECHA CHEM here.

Diss Factsheets

Toxicological information

Basic toxicokinetics

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Administrative data

Endpoint:
basic toxicokinetics
Type of information:
experimental study
Adequacy of study:
supporting study
Study period:
1940
Reliability:
2 (reliable with restrictions)
Rationale for reliability incl. deficiencies:
other: The test is performed based on the scientific method

Data source

Reference
Reference Type:
publication
Title:
Unnamed
Year:
1940

Materials and methods

Objective of study:
metabolism
GLP compliance:
no

Test material

Constituent 1
Chemical structure
Reference substance name:
Sulfapyridine
EC Number:
205-642-7
EC Name:
Sulfapyridine
Cas Number:
144-83-2
Molecular formula:
C11H11N3O2S
IUPAC Name:
4-amino-N-pyridin-2-ylbenzenesulfonamide
Test material form:
not specified
Details on test material:
No data
Radiolabelling:
no

Test animals

Species:
other: rats and rabbits
Strain:
not specified
Sex:
male/female

Administration / exposure

Route of administration:
other: oral
Vehicle:
not specified
Details on exposure:
No data
Duration and frequency of treatment / exposure:
50 days; 10days
Doses / concentrations
Remarks:
Doses / Concentrations:
0.500 g/kg (50days, rats)
121.7 mgm/243.3±8.0 g(10 days, rabbits)
0.75-1.0 g/kg (10 days, rabbits)
No. of animals per sex per dose / concentration:
14 rats per dose (50days, rats)
5 rats per dose (10 days, rats)
2 rabbits (10 days, rabbits)
Control animals:
no
Positive control reference chemical:
No
Details on dosing and sampling:
No data
Statistics:
No data

Results and discussion

Main ADME results
Type:
excretion
Results:
55.4±5.0% (administrated for 10 days)

Toxicokinetic / pharmacokinetic studies

Details on absorption:
No data
Details on excretion:
average dose excreted daily(rats):55.4±5.0% for 10 days exposure.

Metabolite characterisation studies

Metabolites identified:
not measured
Details on metabolites:
No data

Applicant's summary and conclusion

Conclusions:
The average of percent of total drus excreted daily in conjugated form (the rats were administrated for 10 days) was 44.9 ±4.6 %.
In the orally administrated experiment for 50 days, the mean concentration of drug in blood of free form and conjugated form were 4.36±0.52 mgm.% and 2.62±0.19 mgm % respectively at 0.5 % group(% in food); 9.81±0.62% and 4.71 ±0.31mgm % respectively at 1.0 % group(% in food).
The amount of conjugated test subsatnce was 66% of the total in the 10 days rabbit test.
Executive summary:

Three experiments was performed to evaluate the metabolism of sulfapyridine to rats. In the first experiment, the test substance was administrated by feed to rats. 0.5% and 1% of the test substance in food was applied to rats. after 50 days, the concentration in blood of free form of test substance was 4.36(±0.52) mgm.% and 9.81(±0.62)mgm.% respectively in the two groups; the concentration in blood for conjugated form of test substance was 2.62±0.19mgm.% and 4.71 ±0.31mgm.% respectively in the two groups.

In the second experiment, the substance was administrated orally, 5 rats each recieved 500 mg/kg of free acid suspended in gum acecia solution as a single daily dose by stomach tube for 10 days. The percent of total drug excreted daily in conjugated form was 44.9( ± 4.6). In the third experiment, an aquueous suspension of test substance was injected intraperitoeally into 2 rabbits daily for 10 days. The dose of test substance given once daily was 750 to 1000 mg/kg. The amount of conjugated test subsatnce was 66% of the total.