Metiazinic acid

Wistar (male, 140-160 g, carrageenan-induced paw edema)^[1]

20 mg/kg

p.o.; single dose

Reached radioactivity of 3.16 × 10^-2% of dose in edema-induced paws and 4.47 × 10^-2% of dose in control paws at 30 minutes post-administration, with a ratio of 6.96.
Reached radioactivity of 4.20 × 10^-2% of dose in edema-induced paws and 2.24 × 10^-2% of dose in control paws at 1 hour post-administration, with a ratio of 2.03.
Reached radioactivity of 4.87 × 10^-2% of dose in edema-induced paws and 2.97 × 10^-2% of dose in control paws at 3 hours post-administration, with a ratio of 1.86.
Decreased the ratio of radioactivity in edema-induced paws to control paws over time.

Wistar (male, 140-160 g, ultraviolet light-induced skin erythema)^[1]

20 mg/kg

p.o.; single dose

Reached radioactivity of 1.20 × 10⁵ dpm/g in erythema-induced skin and 4.96 × 10⁴ dpm/g in control skin at 30 minutes post-administration, with a ratio of 2.47.
Reached radioactivity of 1.85 × 10⁵ dpm/g in erythema-induced skin and 1.04 × 10⁵ dpm/g in control skin at 1 hour post-administration, with a ratio of 1.72.
Reached radioactivity of 1.24 × 10⁵ dpm/g in erythema-induced skin and 1.00 × 10⁵ dpm/g in control skin at 3 hours post-administration, with a ratio of 1.23.
Peaked radioactivity levels in both erythema-induced and control skin at 1 hour post-administration.
Decreased the ratio of radioactivity in erythema-induced skin to control skin over time.

Wistar (male, 140-160 g)^[1]

20 mg/kg

p.o.; single dose

Showed radioactivity distribution patterns consistent with those observed in rabbits, with notable accumulation in tissues including the kidneys, lungs, liver, hypophysis, and urinary bladder.

(male, 2-3 kg)^[1]

20 mg/kg; 60 mg/kg

p.o.; single dose

Reached maximum blood radioactivity concentration at 3 hours post-administration with 20 mg/kg dose.
Excreted 42.9% of administered radioactivity in urine and 19.9% in bile within 24 hours, and 56.4% in urine and 21.3% in feces within 120 hours with 20 mg/kg dose.
Reached peak kidney radioactivity of 5.90 × 10⁵ dpm/g at 3 hours post-administration with 20 mg/kg dose.
Detected 59.7% of plasma radioactivity as unchanged metiazinic acid at 6 hours post-administration with 20 mg/kg dose.
Reached maximum blood radioactivity concentration at 1 hour post-administration with 60 mg/kg dose.
Excreted 54.6% of administered radioactivity in urine within 24 hours, and 64.7% in urine and 26.6% in feces within 120 hours with 60 mg/kg dose.
Reached peak kidney radioactivity of 1.24 × 10⁶ dpm/g at 1 hour post-administration with 60 mg/kg dose.
Detected 5.8% of radioactivity as unchanged metiazinic acid and 29.2% as metiazinic acid S-oxide in 0-24 hour urine before hydrolysis, with values increasing to 8.4% and 49.1% respectively after enzymatic hydrolysis with 60 mg/kg dose.
Showed similar tissue distribution pattern between 20 mg/kg and 60 mg/kg doses.