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Toxicological information

Basic toxicokinetics

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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: acceptable publication

Data source

Referenceopen allclose all

Reference Type:
publication
Title:
Hippuric acid excretion after benzylamine ingestion in man
Author:
Wood SG et al.
Year:
1978
Bibliographic source:
British Medical Association, Tavistock Square, London WC1H9JR
Reference Type:
publication
Title:
Benzylamine metabolism
Author:
Wood SG et al.
Year:
1978
Bibliographic source:
The chemical environment- Fd Cosmet. Toxicol. Vol 17, no.5

Materials and methods

Objective of study:
excretion
Principles of method if other than guideline:
The fate of 14C-benzylamine after oral administration as the hydrochloride has been investigated in two human male volunteers.
GLP compliance:
not specified

Test material

Reference
Name:
Unnamed
Type:
Constituent
Details on test material:
Radiolabelled benzylamine in the form of (methylene-14C) benzylamine hydrochloride (specific activity 56 nCi/mmol). The total radioactivity was diluted with distilled water to give a final solution containing 1.00 µCi/mL. Unlabelled benzylamine hydrochloride was prepared by the dropwise addition of concentrated hydrochloric acid to a stirred solution of benzylamine in ether.
Radiolabelling:
yes

Test animals

Species:
human
Sex:
male

Administration / exposure

Route of administration:
oral: unspecified
Vehicle:
other: Each 14C-benzylamine hydrochloride dose was prepared by dissolving unlabelled benzylamine hydrochloride (100 mg) in 20 mL (10 µCi) aqueous 14C-benzylamine.
Duration and frequency of treatment / exposure:
single administration
Doses / concentrations
Remarks:
Doses / Concentrations:
Each 14C-benzylamine hydrochloride dose was prepared by dissolving unlabelled benzylamine hydrochloride (100 mg) in 20 mL (10 µCi) aqueous 14C-benzylamine.

Results and discussion

Any other information on results incl. tables

The fate of 14C-benzylamine after oral administration as the hydrochloride has been investigated in two male volunteers. Over 98% of the administered radiolabel was excreted in the urine as 14C-hippuric acid within 24 hours. The rate of urinary hippuric acid excretion was extremely rapid, with more than 90% of the dose excreted after three hours.

Urinary excretion of radioactivity following an oral dose of 14C-benzylamine hydrochloride

 Subject  Time (hr)  Total urine volume (ml)  radioactivity excreted per time interval (%dose)  Cumulative radioactivity excreted (% dose)
 A  0.5  20  66.55  66.55
   1  16  17.62  84.17
   2  64  9.55  93.72
   3  45  2.42  96.14
   4  34  1.14  97.28
   5  25  0.49  97.77
   6  25  0.37  98.14
   7  25  0.23  98.37
   8  24  0.18  98.55
   10  50  0.20  98.75
   12  105  0.16 98.91 
   24  630  0.29  99.20
 B  0.25  50  3.02  3.02
   0.50  83  25.26  28.28
   1  92  37.84  66.12
   2  122  20.07  86.19
   3  130  4.56  90.75
   4  112  2.37  93.12
   5  90  1.29  94.42
   6  57  0.86  95.28
   7  39  0.57  95.85
   8  28  0.38  96.23
   9  36  0.33  96.56
   10  47  0.29  96.85
   12  120  0.35  97.20
   24  940  0.93  98.13

Applicant's summary and conclusion