Pesticide residues in food — 2007: Toxicological ... - ipcs inchem

354
Radioactivity in urine (%) — 57 36 29 12
Radioactivity in faeces (%) — 42 66 72 87
Peak PCM (μg equivalent/ml) — 2.8 2.3 3.4 3.6
Peak PCM-NH-COOH (μg equivalent/ml) — 0.08 0.14 0.24 0.25
Peak PCM-CH 2
OH a (μg equivalent/ml) — 1.1 0.65 1.2 0.91
Peak PA-CH 2
OH (μg equivalent/ml) — 0.24 0.13 0.32 0.22
Peak PA-COOH (μg equivalent/ml) — 0.26 0.16 0.40 0.71
Peak glucuronides (μg equivalent/ml) b — 0.06 0.08 0.15 0.96
From Sugimoto (2005a, 2005b) and Mogi (2005a)
PA, procymidone acid; PA-CH 2
OH, hydroxyprocymidone acid; PA-COOH, carboxyprocymidone acid; PCM,
procymidone; PCM-CH 2
OH, hydroxyprocymidone; PCM-NH-COOH, carboxyprocymidone.
a
Included PCM-COOH.
b
Glucuronides were of PA-CH 2
OH and PCM-CH 2
OH.
Table 2. Pharmacokinetic parameters of radioactivity in plasma of female rats and monkeys
given 14 oral doses of [phenyl- 14 C]procymidone
No. of doses Parameter Dose (mg/kg bw per day)
37.5 62.5 125 250 500
Rats
Single dose C max
(µg equivalent/ml) 11.7 15.7 29.6 42.1 —
T max
(h) 8 8 24 24 —
AUC 2–24 h
(µg equivalent/h per ml) 189 325 520 599 —
Seven doses C max
(µg equivalent/ml) 19.0 32.9 47.2 72.9 —
T max
(h) 8 8 4 8 —
AUC 2–24 h
(µg equivalent/h per ml) 301 485 693 1187 —
Fourteen doses C max
(µg equivalent/ml) 17.7 24.8 47.0 68.3 —
T max
(h) 8 8 8 8 —
AUC 2–24 h
(µg equivalent/h per ml) 269 369 689 1038 —
AUC 0-∞
(µg equivalent/h per ml) 498 599 1111 1588 —
Radioactivity in urine (%) 81 77 79 61 —
Radioactivity in faeces (%) 15 18 16 35 —
Peak PCM (μg equivalent/ml) 2.6 2.6 6.4 5.1 —
Peak PCM-NH-COOH a
— — — — —
(μg equivalent/ml)
Peak PCM-CH 2
OH (μg equivalent/ml) 9.9 9.8 32 51 —
Peak PA-CH 2
OH (μg equivalent/ml) 3.3 7.8 4.0 1.9 —
Peak PA-COOH(μg equivalent/ml) 0.3 0.5 0.6 1.4 —
Peak glucuronides (μg equivalent/ml) 0.6 0.9 0.7 2.9 —
Monkeys
Single dose C max
(µg equivalent/ml) — 2.5 5.2 5.2 9.8
T max
(h) — 4 4 8 24
AUC 2–24 h
(µg equivalent/h per ml) — 53.3 115 115 194
PROCYMIDONE 349–401 JMPR 2007