Key Laboratory of Development and Evaluation of the Chemical and Herbal Drugs for Animal Use, College of Veterinary Medicine, China Agricultural University, Yuanmingyuan West Road No. 2, Haidian District, 100193 Beijing, China.
Vet Parasitol. 2010 Nov 24;174(1-2):72-6. doi: 10.1016/j.vetpar.2010.08.017. Epub 2010 Aug 24.
Chinese Holstein, bred by mating the Holstein-Friesian to Chinese Yellow Cattle, is a major dairy cattle breed in China. Eprinomectin is widely used in the treatment of nematode and ectoparasite infections in lactating cattle. The pharmacokinetics of eprinomectin in the plasma and milk were determined in Chinese Holstein cows following topical (at 0.5 mg kg(-1)) or oral (at 0.2 mg kg(-1)) administration. For topical administration, the concentrations of eprinomectin in plasma reached peak values (C(max)) of 16.16 ± 6.02 ng ml(-1) at 3.20 ± 1.30 days (T(max)). In milk, the C(max) values of 2.28 ± 0.85 ng ml(-1) were obtained at 3.48 ± 0.65 days. The MRT values were 5.00 ± 0.96 days for plasma and 4.65 ± 0.60 days for milk. The AUC values were 91.00 ± 25.32 ng d ml(-1) for plasma and 10.53 ± 1.55 ng d ml(-1) for milk. The ratio of AUC milk/plasma was 0.124 ± 0.041. Significant differences were found in C(max) and AUC of eprinomectin in plasma between Chinese Holstein and Prim Holstein following topical administration. It was probably due to the lower storage of body fat in Chinese Holstein than in Prim Holstein. For oral administration, the concentrations of eprinomectin reach peak values of 30.02 ± 5.73 ng ml(-1) at 1.60 ± 0.55 days in plasma and 3.14 ± 0.88 ng ml(-1) at 1.40 ± 0.27 days in milk. The MRT values for plasma and milk were 3.00 ± 0.46 and 3.18 ± 0.55 days, respectively. The AUC values were 98.46 ± 24.75 ng d ml(-1) for plasma and 10.42 ± 4.22 ng d ml(-1) for milk. The ratio of AUC milk/plasma was 0.104 ± 0.022. Compared with the topical administration, a significantly shorter MRT of eprinomectin in plasma was obtained following oral administration, which would shorten residue time of this compound in faeces and reduce its ecotoxicological effect. The low exposure of eprinomectin in milk would favor the use of eprinomectin in lactating Chinese Holstein for topical or oral administration.
中国荷斯坦牛是通过荷斯坦-弗里生牛与中国黄牛杂交培育而成的主要奶牛品种。埃普里诺菌素广泛用于治疗泌乳奶牛的线虫和外寄生虫感染。本研究采用高效液相色谱-串联质谱法测定了荷斯坦奶牛经皮(0.5mg/kg)和口服(0.2mg/kg)给予埃普里诺菌素后血浆和乳中的药代动力学参数。经皮给予埃普里诺菌素后,血浆中埃普里诺菌素的浓度在 3.20±1.30 天时达到峰值(Cmax)16.16±6.02ng/ml,达峰时间(Tmax)为 3.20±1.30 天。在乳中,Cmax 值为 2.28±0.85ng/ml,达峰时间为 3.48±0.65 天。MRT 分别为 5.00±0.96 天和 4.65±0.60 天。AUC 分别为 91.00±25.32ng·d/ml 和 10.53±1.55ng·d/ml。AUC 奶/血浆比值为 0.124±0.041。经皮给予埃普里诺菌素后,荷斯坦奶牛与荷斯坦弗里生牛相比,血浆中埃普里诺菌素的 Cmax 和 AUC 存在显著差异。这可能是由于荷斯坦奶牛体脂储存量低于荷斯坦弗里生牛。口服给予埃普里诺菌素后,血浆中埃普里诺菌素的浓度在 1.60±0.55 天达到峰值 30.02±5.73ng/ml,乳中在 1.40±0.27 天达到峰值 3.14±0.88ng/ml。血浆和乳中的 MRT 分别为 3.00±0.46 天和 3.18±0.55 天。AUC 分别为 98.46±24.75ng·d/ml 和 10.42±4.22ng·d/ml。AUC 奶/血浆比值为 0.104±0.022。与经皮给予相比,口服给予埃普里诺菌素后,血浆中埃普里诺菌素的 MRT 显著缩短,这将缩短该化合物在粪便中的残留时间,降低其生态毒理学效应。乳中埃普里诺菌素的低暴露有利于荷斯坦奶牛泌乳期经皮或口服给予埃普里诺菌素。