Ethanamizuril(EZL) is a novel triazine anticoccidial compound that has high anticoccidial activity in chickens. In order to treat coccidiosis rationally in poultry, a detection method was developed for ethanamizuril i...Ethanamizuril(EZL) is a novel triazine anticoccidial compound that has high anticoccidial activity in chickens. In order to treat coccidiosis rationally in poultry, a detection method was developed for ethanamizuril in broiler plasma, and then the pharmacokinetics studies were performed in broilers after oral administration of different dose levels. Ethanamizuril was administered as single oral doses at low(0.67 mg kgBW), medium(1.33 mg kgBW) and high(6.67 mg kgBW) levels in which the medium dose was that recommended in clinics. Plasma concentrations of ethanamizuril were determined using ultra-high performance liquid chromatography and the data were analyzed with a non-compartmental model. Peak plasma concentrations of ethanamizuril were(2.16±0.57),(3.91±0.71), and(23.71±5.02) mg Lat(5.17±1.80),(4.60±2.12), and(4.60±2.12) h, respectively. The terminal elimination half-lives(t) for ethanamizuril were(10.84±2.59),(10.66±2.47), and(13.34±3.10) h after oral administration at low, medium and high doses, respectively. The areas under the concentrationtime curve(AUC)) were(37.68±6.87),(73.19±9.18), and(485.76±125.10) mg Lh with mean residence times(MRT) of(14.79±3.03),(15.57±3.69), and(20.22±4.01) h at the 3 dosages, respectively. Ethanamizuril was absorbed rapidly and eliminated slowly. A comparison across the dose range indicated that the time to reach peak plasma concentration(T) values were similar while peak plasma concentration(C) and AUCwere positively correlated with increasing dosages. This study of the pharmacokinetics of an ethanamizuril solution in chickens provides a theoretical basis for the rational use in the clinic.展开更多
为研究抗球虫新化合物沙咪珠利在鸡盲肠中的药物代谢和消除情况,建立检测鸡盲肠中沙咪珠利的高效液相色谱法。检测方法以妥曲珠利亚砜为内标,X TERRA MS C18 5μm(Waters,4.6×250 mm)柱为分析柱,乙腈∶0.2%磷酸水溶液(v/v,35∶65)...为研究抗球虫新化合物沙咪珠利在鸡盲肠中的药物代谢和消除情况,建立检测鸡盲肠中沙咪珠利的高效液相色谱法。检测方法以妥曲珠利亚砜为内标,X TERRA MS C18 5μm(Waters,4.6×250 mm)柱为分析柱,乙腈∶0.2%磷酸水溶液(v/v,35∶65)为流动相等度洗脱,C18柱分离后,在251 nm波长紫外检测器检测,内标法定量。鸡盲肠样品经匀浆化后,乙腈提取、己烷除脂。结果表明,该方法在0.2~40 mg/kg添加浓度范围内检测鸡盲肠中沙咪珠利具有很好的线性关系(r2=0.994);平均相对回收率为90%~107%,日内变异系数2.37%~8.72%;日间变异系数4.09%~6.80%,具有特异性好、灵敏度高、准确性和重现性良好、操作简单等优点,能满足鸡盲肠中沙咪珠利的检测需求。展开更多
基金supported by the National Natural Science Foundation of China (31472235 and 31272607)the Natural Science Foundation of Shanghai, China (14ZR1449000)+2 种基金the Special Scientific Research Fund of Agricultural Public Welfare Profession of China (201303038)the Central Grade Public Welfare Fundamental Science Fund For Scientific Research Institute, China (2016JB08 and 2016JB04)the National Key Technology Research and Development Program of the Ministry of Science and Technology of China (2015BAD11B01-06)
文摘Ethanamizuril(EZL) is a novel triazine anticoccidial compound that has high anticoccidial activity in chickens. In order to treat coccidiosis rationally in poultry, a detection method was developed for ethanamizuril in broiler plasma, and then the pharmacokinetics studies were performed in broilers after oral administration of different dose levels. Ethanamizuril was administered as single oral doses at low(0.67 mg kgBW), medium(1.33 mg kgBW) and high(6.67 mg kgBW) levels in which the medium dose was that recommended in clinics. Plasma concentrations of ethanamizuril were determined using ultra-high performance liquid chromatography and the data were analyzed with a non-compartmental model. Peak plasma concentrations of ethanamizuril were(2.16±0.57),(3.91±0.71), and(23.71±5.02) mg Lat(5.17±1.80),(4.60±2.12), and(4.60±2.12) h, respectively. The terminal elimination half-lives(t) for ethanamizuril were(10.84±2.59),(10.66±2.47), and(13.34±3.10) h after oral administration at low, medium and high doses, respectively. The areas under the concentrationtime curve(AUC)) were(37.68±6.87),(73.19±9.18), and(485.76±125.10) mg Lh with mean residence times(MRT) of(14.79±3.03),(15.57±3.69), and(20.22±4.01) h at the 3 dosages, respectively. Ethanamizuril was absorbed rapidly and eliminated slowly. A comparison across the dose range indicated that the time to reach peak plasma concentration(T) values were similar while peak plasma concentration(C) and AUCwere positively correlated with increasing dosages. This study of the pharmacokinetics of an ethanamizuril solution in chickens provides a theoretical basis for the rational use in the clinic.
文摘为研究抗球虫新化合物沙咪珠利在鸡盲肠中的药物代谢和消除情况,建立检测鸡盲肠中沙咪珠利的高效液相色谱法。检测方法以妥曲珠利亚砜为内标,X TERRA MS C18 5μm(Waters,4.6×250 mm)柱为分析柱,乙腈∶0.2%磷酸水溶液(v/v,35∶65)为流动相等度洗脱,C18柱分离后,在251 nm波长紫外检测器检测,内标法定量。鸡盲肠样品经匀浆化后,乙腈提取、己烷除脂。结果表明,该方法在0.2~40 mg/kg添加浓度范围内检测鸡盲肠中沙咪珠利具有很好的线性关系(r2=0.994);平均相对回收率为90%~107%,日内变异系数2.37%~8.72%;日间变异系数4.09%~6.80%,具有特异性好、灵敏度高、准确性和重现性良好、操作简单等优点,能满足鸡盲肠中沙咪珠利的检测需求。
