Document 6RopMYbRy1M9QzMwJE9Ly8de4
AR226-3391
Repeated Dose Oral Toxicity of 8-2 Telomer B Alcohol Range-Finding Study in Rats
G.L. Kennedy,' G.S. Ladies,1J.C. O'Connor,' S.A. Gannon,' R. Jung,2H. Iwai,3M. Shinohara4
Telomer Research Toxicology Program
1 . The DuPont Company, Haskell Laboratoryfo r Health and Environmental Sciences, Newark, Delaware, USA
2. Clariant GmbH, Sulzbach, Germany 3. Daikin Industries, Inc., Osaka, Japan
H f Results
4. Asahi Glass, Co., Ltd., Tokyo, Japan
W U Abstract
Preliminary to a repeated dose toxicity assessment, a ranee-finder study involving repeated oral doses of 8-2 Teloirer B Alcohol was conducted in rats to determine die time needed to reach steady-state as determined by total organofluorine blood fluoride levels. Groups of 10 male and 5 female Crl:CD*(SD)IGS BR rats each were dosed daily with either 0 (control), 5.2 5, or 125 mg 8-2 Telotner B Alcohol/kg/day. A number of toxicology end-points such as body weights, liver and kidney weights were recorded during and at the end o f the study. Blood samples were analyzed for total fluoride levels weekly. Steady-state concentrations were reached between test days 60 and 84. At steady-state, pooled plasma samples obtained from males and females over tlte duration o f the study were analyzed for Telomer 8-2 Alcohol (parent compound), Telomer 8-2 acid, perfluorooctanoate acid (PFOA). nnd pcrfluorononanoic acid (PFNA) and total fluorine levels. The level o f parent compound detected did not exceed 0.074 ppm in either males or females. In males, PFOA represented approximately 85% of the total plasma fluorine. In females, PFOA represented approximately S%. The 8-2 acid of Telomer B Alcoliol and PFNA were also found in plasma of both males and females. Significantly lower mean body weights and increased liver weights compared to control were observed in male rats administered 125 mg/kg/day. Based on these data, tlte following doses were chosen fertile 90-day oral toxicity study: 0, 1.5.25, and 125 mg/kg/day.
|Purpose
a 90-day ora! subchronic study with 8-2
Clinical Observations
Dose (ma/kcl Findinc
0 Mnno
5 M/M.A
25 M/sna
125 Striated teeth Clipped teeth
Sex Incidence M 10/10 F 5/5
M 10/10 F 5/5
M 10/10 F 5/5
M 7/10* F 4/5* M 4/10* F 0/5
Dose
0 S 25 125
After Dosing (Test Day 81) Male Female 594 44 264 45
After Recovery
(Post-Dosinc Dav 75)
Male
Female
554 100 322 41
564 59 302 22 595 57 348 29
553 34 296 41 573 83 332 50
509* SS 291 21 549 * 37 346 31
;r B Alcohol. PFOA. nnd PFNA in Serum and Selected Tissues
Male Male PFOA Male Total
Female PFOA Female Total
Dose PFOA Converted Plasma F PFOA Converted Plasma F
(nom)
0 0.07 0.05
NM 0.0 ------- OO
NM
5 2.19 1.51
NM 0.08
0.05
NM
25
8.47*
5.83
8.11 0.54*
0.37
5.88
125 65.60* 45.16
53.24 1.85*
1.27
23.20
Tissue Analysis from Range-Finder Study (Test Day 81) 8-2 Telomer B Alcohol
C8-2A (ppm) Fat
Kidney
PFOA (ppm)
Plasma Fat Liver Kidney
PFNA (ppm) Fat 1VAT Kidney
0.07(0.01) 0.02(0.00)
NM
2.19 0.09(0.04) 696(1.94) 1.64(0.83)
0.00(0.00) 0.51(0.09) 0.00(0.00)
0.34(0.13) 0.13(0.03) 0.01(0.00)
8.47 0.35(0.12) 18.68(10.38) 8.43(4.14)
0.00(0.00) 0.91(0.23) 0.11(0.09)
1.37(055) 0.77(0.53) 0.07(0.07)
65.60 1.90(1.66) 30.69(20.68) 29.11(17.38)
0.01(0.01) 1.19(1.25) 0.86(0.62)
i Structures
FF FF H
Telotner C8-2 Alcohol
C8-2 Acid (M477)
F F F FO
Organ Weights
Dose 0 5 25 125
Liver
Kidney
(c/100e bwtl
Test Dav 81 Posl-Dosina Dav 75 Test Dav 81 Post-Dosina Dav 75
M 3.9(0.28) F-
3.0(0.13) 3.2(0.14)
0.76(0.03) -
0.65(0.06) 0.70(0.03)
M 3.7(0.20) F-
3.1(0.14) 3.2(0.33)
0.76(0.06) -
0.67(0.03) 0.7i/(0.07)
M 4.1(0.19 F-
2.9(0.13) 3.4(0.37)
0.75(0.04) -
0.69(0.05) 0.73(0.06)
M 5.5*(0.39) F
3.1(0.32) 3.6*10.05)
0.87(0.11)
0.74*(0.07) 0.78*(0.02)
* {p4X0S)diflercnlirvmcenliol
F FFO
PFNA
Total Blood Fluorine Analysis in Mule Rats Dosed with 8-2 Telomer B Alcohol
FFOA
HIMMethods
Test substance, 8-2 Telomer B Alcohol (99.2% pure) Test species: Crf:CD rat (male and female) Standard husbandry, 5-day quarantine Groups: 10 males, 5 females/group 15 males/group allowed 75-day post-dosing recovery
period]. Doses; 0,5.25.125 mg/kg Daily gavage beginning with 7-week-old rats Doses in methylceliuiose suspensions, 5 inL/kg dosing volume. Parameters measured (dosing and during recovery) Body weights (2 x/week) Cage-side exams (daily) Total fluoride/parent metabolite evaluation
Blood samples collected 1 x pre-dosing weekly during dosing Organ weights - liver, kidney Parent/Metabolite Evaluation At steady-state, pooled plasma, fat, liver, and kidney samples from each group were analyzed for
Telomer 8-2 Alcohol Perfluorooctanoic Acid (PFOA) Perfluoronanonoic acid (PFNA)
Total Blood Fluorine Analysis in Female Rats Dosed with 8-2 Telomer B Alcoliol
B llff Conclusions
Doses of Telomsr 8-2 Alcoliol were well tolerated; cumber of endpoints were altered at
125 mg/kg.
o.
Steady-state blood fluorine levels were attained between weeks 8 and 13 of dosing; males reached higher levels titan females.
Metabolites of Telotwr 8-2 Alcoliol were found in both sexes of rats.
Tiie 90-day toxicity study would employ dose levels of 0 .1 ,5 .2 5 , and 125 mg/kg.