CAS NO.: 101831-37-2
EINECS: N
Molecular Formula: C17H9Cl3N4O2
Molecular Weight: 407.64
Molecular Structure:
Property：
Diclazuril
(2,6-dichloro-α-(4-chlorophenyl)-4-(4,5-dihydro-3,5-dioxo-1,2,4-triazin-2(3H)-yl)benzeneacetonitrile)
a benzeneacetonitrile derivative is an anticoccidial
intended for oral use inlambs. The therapeutic dosage is
either a single administration of 1 mg diclazuril/kg bw (mostcommonly
at about 6-8 weeks of age) or two administrations (the first
at 3 to 4 weeks of age and the second about 3 weeks later).
Diclazuril has been
registered as an anticoccidial feed additive for broilers
with a withdrawal period of 5 days in the Council Directive
93/107/EC of 26 November 93 amending Council Directive
70/524/EEC.
Diclazuril was
previously assessed by the CVMP and an acceptable daily
intake (ADI) of 0.030 mg/kg bw (i.e. 1.8 mg/person) was
established. . The same ADI value of 0-0.03 mg/kg bw was
established by Joint WHO/FAO Expert Committee on Food
Additives (JECFA) at its 50th meeting in 1998. Both
Committees based the ADI on a NOEL of 3 mg/kg bw/day
retained from the 2-year chronic toxicity/carcinogenicity
study in mice applying a safety factor of 100.
Specifications：
|
Item |
Index |
| Description |
Yellow powder |
| Identification |
Meet the criterion |
|
Loss On Drying |
10.0% max. |
| Heavy Metals |
0.002% max. |
| Arsenic |
0.0002% max. |
| Granularity |
100% through screen
No.2 |
| Assay |
0.45%-0.55% |
Usage:
In piglets after
a single oral administration of 5 mg/kg bw of diclazuril,
the maximum plasma concentration 0.035 mg/l was observed
24 hours post administration (first sampling time).
In calves after a
single oral administration of 5 mg/kg bw of diclazuril, the
mean maximum plasma concentration 0.039 mg/l was observed 12
hours post administration. The very high value of the volume
of distribution corrected by the bioavailability factor of
100 l/kg indicates that the bioavailability is low.
Diclazuril is poorly absorbed in calves after oral
administration. The metabolism of diclazuril in pigs was
investigated with suspension cultures and primary cell
cultures of swine hepatocytes. The analyses of incubate
samples revealed that the metabolism of diclazuril was
limited. The parent compound represented more than 98 and
59% in suspension culture or in primary culture,
respectively.
In pigs, a
non-radiometric depletion study was carried out. Twenty-four
hours after a single oral administration of diclazuril at 5
mg/kg bw to 4-5 days-old piglets, 33.8 μg of diclazuril/kg
were measured in muscle, 162 μg/kg in fat + skin in natural
proportions, 45.2 μg/kg in liver and 43.1 μg/kg in kidney.
Residue levels of diclazuril were below the limit of
quantification of 25 μg/kg at day 3 for muscle, liver and
kidney and day 5 for fat + skin.
In cattle, a
non-radiometric depletion studies was carried out.
Twenty-four hours after a single oral administration of
diclazuril at 5 mg/kg bw to 3-5 days old calves, 25.8 μg of
diclazuril/kg were measured in muscle, 361 μg/kg in fat, 108
μg/kg in liver and 75.2 μg
Package and Storage:
Keep in shaded, cool 25kg fiber drum and
air places. The shelf time is 2 years.
Keyword：
Diclazuril
2,6-Dichloro-alpha-(4-chlorophenyl)-4-(4,5-dihydro-3,5-dioxo-1,2,4-triazin-2(3H)-yl)benzeneacetonitrile
