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EC number: 204-101-2
CAS number: 115-70-8
Absorption was estimated from the percent of the dermally applied
radioactivity recovered in urine and rinse, final cage wash, CO2 and
tissues, and faeces. A mean total of 27 ± 3% and 25 ± 5% of the dermally
applied dose was systemically absorbed to males and females,
respectively. The unabsorbed radioactivity of 43 ± 6% (males) and 41 ±
4% (females) was recovered from the skin wash, covering, tape strips,
frame and dosed skin.
Urinary elimination of the dermally applied dose:
Over the 168 h collection period, 19% and 15% of the administered dose
was recovered in urine of males and females, respectively. Slow and low
urinary elimination was consistent with pattern of slow penetration of
the applied dose from the dermal site of application and limited
absorption of the applied dose, as expected due to cornified layer of
cells on the skin surface that work as a barrier.
Faecal elimination of the dermally applied dose:
The 14C- BIOBAN™ CS-1246 -derived radioactivity recovered in faeces was
As expected on the basis of low absorption via the dermal route of
exposure, a lower percentage of administered radioactivity was
associated with tissues of animals receiving a single dermal dose of 14C-
BIOBAN™ CS-1246. On average, only 3% of the dermally administered
radioactivity remained in tissues at terminal sacrifice (168 h
post-dosing). Most (2.6 -2.7%) was recovered in the skin remote from the
application site and 0.8 -1.7% was recovered from skin at the site of
For males, the highest concentrations of radioactivity was found in skin
> liver > thyroid ≥ kidney.
For females, the highest concentrations of radioactivity was found in
skin > carcass > kidney = stomach tissue.
The difference in the residual radioactivity between the dose-site skin
and skin at remote from the dosed site was only 6 -fold (males) and 3
-fold (females). Such a low difference in the residual radioactivity
between the dosed site skin and skin at other sites of the body was an
indication that complete absorption has been achieved and any additional
penetration of radioactivity from the application site was not likely to
Fat and fatty tissue (e.g. brain) generally exhibited the lowest
accumulation of 14C-14C-BIOBAN™ CS-1246 -derived radiaoactivity (mostly
under the detection limit).
The absorbed 14C-BIOBAN™ CS-1246 was completely metabolised,
affording 2-amino-2-ethyl-1,3-propanediol (AEPD) as the only metabolite
above 5% of the administered dose in all urine and faecal samples
analysed from all dose groups. Four minor metabolites were also observed
above 0.5% of the administered dose, but not identified.
Kinetic parameters of 14C- BIOBAN™ CS-1246 in RBC and in plasma
The peak plasma concentration of 14C- BIOBAN™ CS-1246 among the
dermally dosed rats occurred 2 -3 h post-application. The rate of dermal
absorption was 0.14 -0.2 h-1
and elimination of absorbed radioactivity was 0.5 -1.5 h.
The clearance was relatively high 6754 -8453 mL/kg/h after dermal dosing
consistent with a low plasma AUC 0.7 -0.9 µg*h/g and a relatively rapid
elimination of absorbed radioactivity.
The test substance derived radioactivity was also present in RBC,
with Cmax concentrations ~90% of the levels seen in plasma. The rate
constant of absorption of radioactivity into RBC was faster than into
the plasma (0.03 -0.09 h-1)
and the elimination was slower. This could be an indication of binding
of radioactivity to RBC, albeit at extremly low levels (~0.01 -0.02
µg/g). The elimination of radioactivity from RBC followed a relatively
rapid (α) elimination phase and a slow elimination (β) phase.
The appearance of detectable radioactivity in RBC for extended period of
time resulted in 8 -11 fold higher AUC and 8 -12 fold slower clearance
of radioactivity from RBC than plasma.
Table 1: Kinetic parameters of 14C- BIOBAN™ CS-1246 in RBC and in
plasma (mean ± SD of 4 animals)
Mean ± SD (males)
Mean ± SD (females)
3.99 ± 0.43
3.24 ± 0.54
3.00 ± 0.54
1.71 ± 0.55
0.06 ± 0.02
0.083 ± 0.00
0.07 ± 0.02
0.09 ± 0.01
0.03 ± 0.01
0.09 ± 0.04
0.21 ± 0.07
0.14 ± 0.02
t½ elimination [h]
1.53 ± 0.76
0.47 ± 0.20
3.39 ± 1.24
4.42 ± 1.53
188 ± 46
109 ± 44
7.49 ± 1.83
6.84 ± 0.94
0.67 ± 0.24
0.86 ± 0.06
723 ± 169
876 ± 154
8453 ± 2448
6754 ± 496
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