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EC number: 204-427-5
CAS number: 120-80-9
The percutaneous penetration of Catechol,
i.e. 1,2-Benzenediol, formulated as an aqueous solution, was determined
in vitro using split-thickness skin membranes from human skin.
The skin membranes were set up in
flow-through diffusion cells and [14C] Catechol was applied onto the
skin membranes at a concentration of 1 mg/cm³. Aliquots of 64 μl of the
administration solution were applied to a skin membrane area of 0.64 cm²
corresponding to a infinite dose of 0.1 mg Catechol/cm². The receptor
fluid, i.e. aqueous saline (0.9% NaCl w/v), was delivered at a flow rate
of about 3 ml/h. The in vitro percutaneous penetration was investigated
in two groups, i.e. Groups Q1 and Q2. The Group Q1 was designed to
investigate the short term dermal penetration and Group Q2 was designed
to determine the permeability constant (Kp) for dermal penetration of
Catechol. For each objective, i.e. short term penetration (10 and 60
min) and determination of the permeability constant, at least duplicates
of valid skin membranes from at least 3 different individuals were used.
The integrity of each skin membrane preparation was checked with
Objective Subgroup Sampling
penetration Q1A1 0 – 10 minutes
– 60 minutes
constant Q2A1 0 – 6 hours : 1 hour intervals (6 intervals)
– 24 hours : 2 hour intervals (9 intervals)
The results of the short term experiments
revealed that Catechol penetrated to a very low extent through human
skin membranes within the first hour of exposure. Only 0.04 % and 0.22 %
of the applied dose penetrated through the skin membrane within 10 and
60 minutes of exposure, respectively. The bulk of test item could be
washed off at the end of the exposure period amounting to 97 % and 94 %
of the dose. After skin membrane rinse 0.28 % and 1.49 % of the dose
remained in/on the skin membranes after 10 and 60 minutes of exposure.
Within an exposure period of 24 hours, a
mean of 26.65 % of the applied [14C] Catechol penetrated through human
skin membranes. After a lag time of about 6 hours, Catechol penetrated
with a flux (penetration rate at steady state) of 1.425 μg/cm²/h through
human skin membranes. The corresponding permeability constant Kp for
Catechol was calculated to be 1.430·10-3 cm/h with a standard deviation
of 40 % (ranged from 0.712 to 2.120·10-3 cm/h) for the subjects used
(n=4). HPLC analysis of the skin membrane rinse pools revealed that
Catechol remained unchanged on the skin membranes during the exposure
In conclusion, Catechol, applied as an
aqueous solution to human skin membranes, penetrated very moderately
with a penetration rate of 1.425 μg/cm²/h after a lag time of 6 hours.
The permeability constant Kp was calculated to be 1.430 x 10E-3 cm/h.
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