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EC number: 617-116-8 | CAS number: 80573-04-2
- Life Cycle description
- Uses advised against
- Endpoint summary
- Appearance / physical state / colour
- Melting point / freezing point
- Boiling point
- Density
- Particle size distribution (Granulometry)
- Vapour pressure
- Partition coefficient
- Water solubility
- Solubility in organic solvents / fat solubility
- Surface tension
- Flash point
- Auto flammability
- Flammability
- Explosiveness
- Oxidising properties
- Oxidation reduction potential
- Stability in organic solvents and identity of relevant degradation products
- Storage stability and reactivity towards container material
- Stability: thermal, sunlight, metals
- pH
- Dissociation constant
- Viscosity
- Additional physico-chemical information
- Additional physico-chemical properties of nanomaterials
- Nanomaterial agglomeration / aggregation
- Nanomaterial crystalline phase
- Nanomaterial crystallite and grain size
- Nanomaterial aspect ratio / shape
- Nanomaterial specific surface area
- Nanomaterial Zeta potential
- Nanomaterial surface chemistry
- Nanomaterial dustiness
- Nanomaterial porosity
- Nanomaterial pour density
- Nanomaterial photocatalytic activity
- Nanomaterial radical formation potential
- Nanomaterial catalytic activity
- Endpoint summary
- Stability
- Biodegradation
- Bioaccumulation
- Transport and distribution
- Environmental data
- Additional information on environmental fate and behaviour
- Ecotoxicological Summary
- Aquatic toxicity
- Endpoint summary
- Short-term toxicity to fish
- Long-term toxicity to fish
- Short-term toxicity to aquatic invertebrates
- Long-term toxicity to aquatic invertebrates
- Toxicity to aquatic algae and cyanobacteria
- Toxicity to aquatic plants other than algae
- Toxicity to microorganisms
- Endocrine disrupter testing in aquatic vertebrates – in vivo
- Toxicity to other aquatic organisms
- Sediment toxicity
- Terrestrial toxicity
- Biological effects monitoring
- Biotransformation and kinetics
- Additional ecotoxological information
- Toxicological Summary
- Toxicokinetics, metabolism and distribution
- Acute Toxicity
- Irritation / corrosion
- Sensitisation
- Repeated dose toxicity
- Genetic toxicity
- Carcinogenicity
- Toxicity to reproduction
- Specific investigations
- Exposure related observations in humans
- Toxic effects on livestock and pets
- Additional toxicological data
![](https://poisoncentres.echa.europa.eu/o/diss-blank-theme/images/factsheets/A-REACH/factsheet/print_toxicological-information.png)
Basic toxicokinetics
Administrative data
- Endpoint:
- basic toxicokinetics in vivo
- Type of information:
- experimental study
- Adequacy of study:
- weight of evidence
- Study period:
- Not specified
- Reliability:
- 2 (reliable with restrictions)
- Rationale for reliability incl. deficiencies:
- data from handbook or collection of data
Data source
Reference
- Reference Type:
- review article or handbook
- Title:
- Unnamed
- Year:
- 2 000
Materials and methods
- Objective of study:
- toxicokinetics
Test guideline
- Qualifier:
- no guideline followed
- Principles of method if other than guideline:
- - Principle of test:
- Short description of test conditions: radiolabelled Basalazide sodium (BSZ) was administered to rats as a single i.v. dose at 120 mg/kg
- Parameters analysed / observed: Blood, urine and Faeces was sampled and levels of BSZ and its metabolites were determined. Tissue samples from a variety of organs were collected for distribution study. Radioactivity was determined via LSC. - GLP compliance:
- not specified
Test material
- Reference substance name:
- Benzoic acid, 5-[(1E)-[4-[[(2-carboxyethyl)amino]carbonyl]phenyl]azo]-2- hydroxy-, disodium salt, dihydrate
- Cas Number:
- 150399-21-6
- Molecular formula:
- C17H13N3O6Na2 . 2H2O
- IUPAC Name:
- Benzoic acid, 5-[(1E)-[4-[[(2-carboxyethyl)amino]carbonyl]phenyl]azo]-2- hydroxy-, disodium salt, dihydrate
- Test material form:
- solid
Constituent 1
- Specific details on test material used for the study:
- The study was performed on balsalazide disodium, but it will reach a common moiety in the blood after oral dosing , whether BSZ or BSA.
- Radiolabelling:
- yes
Test animals
- Species:
- rat
- Strain:
- not specified
- Sex:
- not specified
Administration / exposure
- Route of administration:
- oral: gavage
- Vehicle:
- not specified
- Duration and frequency of treatment / exposure:
- Single dose
Doses / concentrationsopen allclose all
- Dose / conc.:
- 120 mg/kg bw/day (actual dose received)
- Dose / conc.:
- 2 000 mg/kg bw/day (actual dose received)
- No. of animals per sex per dose / concentration:
- Not stated
- Control animals:
- no
- Positive control reference chemical:
- Not stated
- Details on dosing and sampling:
- TOXICOKINETIC / PHARMACOKINETIC STUDY (Absorption, distribution, excretion)
- Tissues and body fluids sampled: urine, faeces, blood
- Time and frequency of sampling: 1,3,6,9,12,18 and 24 hours after dosing
METABOLITE CHARACTERISATION STUDIES
- Tissues and body fluids sampled: urine, faeces, tissues,
- Time and frequency of sampling: 1,3,6,9,12,18 and 24 hours after dosing
- Method type(s) for identification HPLC-UV, Liquid scintillation counting - Statistics:
- None specified
Results and discussion
Main ADME resultsopen allclose all
- Type:
- absorption
- Results:
- Oral bioavailability was very low (0.52-0.62%)
- Type:
- distribution
- Results:
- Missing page in review document. No distribution information available
- Type:
- metabolism
- Results:
- Four metabolites were formed. 5-amino salicylic acid (ASA) which is N-acetylated to N-acetyl-5-amino-salicylic acid (NASA). 4 aminobenzoyl-5-alanine (ABA) which is N-acetylated to N-acetyl-4-aminobenzoyl-5-alanine (NABA).
- Type:
- excretion
- Results:
- Following a single oral dose, 4-ABA (one of the metabolites) was found in large quantities in Faeces and in small amounts in plasma. The majority of the applied radioactivity (approx 92%) was found in the faeces and a small (approx 5-8%) in the urine.
Toxicokinetic / pharmacokinetic studies
- Details on distribution in tissues:
- No information available.
- Details on excretion:
- Following a single oral dose, 4-ABA (one of the metabolites) was found in large quantities in Faeces and in small amounts in plasma. The majority of the applied radioactivity (approx 92%) was found in the faeces and a small (approx 5-8%) in the urine for both dose levels. In the urine, low amounts of basalazide acid (sodium salt) was recovered with the major metabolite being NABA.
Metabolite characterisation studies
- Metabolites identified:
- yes
- Details on metabolites:
- Four metabolites were reported. These were assigned as:
1) 5-aminosalicylic acid (ASA)
2) N- acetyl-5-amino-salicylic acid (NASA, derived by N-acetylation of ASA)
3) 4-aminobenzoyl-5-alanine (ABA)
4) N-acetyl-4-aminobenzoyl-5-alanine (NABA, derived by N-acetylation of ABA)
Any other information on results incl. tables
Single dose of Balsalazide to rat
Compound |
Dose of Balsalazide (mmol/kg) |
Route/group |
Cmax (nmol/ml) |
Tmax (h) |
AUC (nmol.h/ml) |
Urine (nmole/24h) |
Clr (ml/min) |
Radioactivity |
0.274 |
Oral (A) |
3.574 |
9.00 |
40.72 |
NA |
NA |
Radioactivity |
4.573 |
Oral(B) |
26.78 |
12.00 |
373.8 |
NA |
NA |
Radioactivity |
0.274 |
IV |
NA |
NA |
269.0 |
NA |
NA |
Balsalazide |
0.274 |
Oral (A) |
1.091 |
1.00 |
3.072 |
273.5 |
1.484 |
Balsalazide |
4.573 |
Oral(B) |
8.505 |
1.00 |
42.56 |
3470 |
1.359 |
Balsalazide |
0.274 |
IV |
NA |
NA |
491.9 |
18452 |
0.625 |
NABA |
0.274 |
Oral (A) |
1.838 |
9.00 |
15.73 |
1897 |
2.009 |
NABA |
4.573 |
Oral(B) |
10.71 |
12.00 |
137.0 |
10382 |
1.263 |
NABA |
0.274 |
IV |
NA |
NA |
ID |
1303 |
ID |
NASA |
0.274 |
Oral (A) |
7.585 |
9.00 |
50.75 |
6867 |
2.255 |
NASA |
4.573 |
Oral(B) |
51.28 |
9.00 |
622.0 |
75690 |
2.028 |
NASA |
0.274 |
IV |
NA |
NA |
29.16 |
5580 |
3.189 |
ABA |
0.274 |
Oral (A) |
0.310 |
9.00 |
ID |
ID |
ID |
ABA |
4.573 |
Oral(B) |
3.974 |
12.00 |
34.20 |
6238 |
3.040 |
ABA |
0.274 |
IV |
ID |
ID |
ID |
ID |
ID |
ASA |
0.274 |
Oral (A) |
1.946 |
9.00 |
ID |
ID |
ID |
ASA |
4.573 |
Oral(B) |
73.05 |
12.00 |
522.2 |
17700 |
0.565 |
ASA |
0.274 |
IV |
NA |
NA |
ID |
ID |
ID |
ID = Insufficient data to derive parameter
NA = not applicable
Applicant's summary and conclusion
- Conclusions:
- The results of the i.v. dosing are quite different to the oral dosing. After dosing, radioactivity in the plasma declines much faster than the same dose via the oral route. Excretion of a high (38% dose) percentage as intact balsalazide via urine is quite interesting as the in vitro plasma protein binding was determined to be 96-99% and protein bound molecules cannot be filtered through the kidney into urine. Clearly, in vivo the parent molecule can be excreted despite high plasma protein binding suggesting that either the plasma protein binding in vivo is much lower than in vitro indicates, or there is reversal of the binding within the kidneys.
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