复方替米考星可溶性粉在鸡体内的药动学研究

Study of pharmacokinetics of Compound Tilmicosin Soluble Powder in healthy chickens

本研究比较了口服复方替米考星可溶性粉与单独肌注替米考星注射液和静注磺胺二甲嘧啶钠注射液在鸡体内药物代谢动力学特征和相对生物利用度。36只健康鸡,随机分为3组,给药剂量均为20 mg/kg,翼下静脉采血,高效液相色谱法检测鸡血浆中的药物浓度。采用药动学软件Win Nonlin 6.1的非房室模型分析方法,计算出药物的动力学参数。鸡口服复方替米考星可溶性粉、肌注替米考星注射液和静注磺胺二甲嘧啶钠注射液后的药时曲线下面积(AUC)分别为:9.49±3.64、37.17±10.82、12.40±4.11、61.31±11.38μg×h/m L。复方替米考星可溶性中替米考星相对于肌肉注射的替米考星的生物利用度为75.98%,复方制剂中磺胺二甲嘧啶钠的绝对生物利用度为60.63%。复方替米考星可溶性粉和单方药物相比,药动学参数经t检验,t_(1/2)、T_(max)、C_(max)、AUC、MRT等存在显著性差异(P<0.05)。结果表明复方替米考星可溶性粉单剂量口服给药吸收较慢,达峰时间显著延迟,平均驻留时间显著延长,有利于抗菌作用的发挥。

The pharmacokinetics and relative bioavailability of Compound Tilmicosin Soluble Powder after oral administration、Tilmicosin injection after intramuscular administration and Salfadimidine injection after intravenous administration were investigated in chickens. 36 chickens were divided to 3 groups randomly, and then received 20 mg/kg of Compound Tilmicosin Soluble Powder、Tilmicosin injection and Salfadimidine injection respectively. Blood samples were collected and analyzed by high-performance liquid chromatography（HPLC）. Pharmacokinetics parameters were estimated by the Win Nonlin6.1 software package and SPSS 16.0 analysis of the time and concentration data.. The AUC of Compound Tilmicosin Soluble Powder、Tilmicosin injection and Salfadimidine injection were respectively 9.49±3.64, 37.17±10.82, 12.40±4.11 and 61.31±11.38 μg×h/m L. The relative bioavailability of Tilmicosin after oral administration was 75.98%, and the absolute bioavailability of Salfadimidine after oral administration was 60.63%. Comparing Compound Tilmicosin Soluble Powder with Tilmicosin injection and Salfadimidine injection, statistical analysis showed that the main pharmacokinetic parameters of t1/2、Tmax、Cmax、AUC and MRT were different significantly（P0.05）. In conclusion, it appeared that Compound Tilmicosin Soluble Powder was absorbed slowly and completely, and Tmaxwas significantly delayed, and MRT was significantly prolonged, which broadens their antibacterial spectrum and benefits their pharmacodynamics.