盐酸金霉素和超级盐酸金霉素在肉鸡体内的药代动力学和组织残留量测定

Pharmacokinetics and tissue residue determination of chlortetracycline hydrochloride and super chlortetracycline hydrochloride in broiler chickens

盐酸金霉素广泛应用于家畜和家禽,然而,金霉素的低溶解度限制了其应用。该试验以20 mg/kg单剂量灌服盐酸金霉素和超级金霉素,采集各时间节点的血浆样品并用UPLC/MS/MS检测其血药浓度,计算各种药动学参数,评估盐酸金霉素和超级盐酸金霉素在肉鸡体内的ADME(Absorption distribution metabolism excretion)过程。结果表明:单剂量给药后超级盐酸金霉素的峰浓度显著高于盐酸金霉素[(4.69±1.54)μg/mL vs (1.91±0.63)μg/mL],表明超级盐酸金霉素的吸收速度快于盐酸金霉素。超级盐酸金霉素的药时曲线下面积(AUC)(Area under the concentration-time curve, AUC)也大于盐酸金霉素[(14.51±3.40) hr·μg·mL^(-1)vs (6.28±2.69) hr·μg·mL^(-1)]。表明超级盐酸金霉素到达全身血液循环的量多于盐酸金霉素,有利于提高金霉素的药效。以20 mg/kg剂量连续灌服盐酸金霉素和超级盐酸金霉素7 d后,检测肌肉和肝脏中盐酸金霉素和超级盐酸金霉素的残留量接近或低于检测限,远低于食用动物肌肉中盐酸金霉素的残留限量。因此,超级盐酸金霉素提高了盐酸金霉素的生物利用度,具有广阔的应用前景和推广价值。

Chlortetracycline hydrochloride is widely used in livestock and poultry,however,the low solubility of chlortetracycline limits its application.In this study,chlortetracycline hydrochloride and super chlortetracycline hydrochloride were administered with a single dose of 20 mg/kg,plasma samples were collected at each time point and their blood concentrations were detected by UPLC/MS/MS,and various pharmacokinetic parameters were calculated to evaluate the ADME process of chlortetracycline hydrochloride and super chlortetracycline hydrochloride in broiler chickens.The results exhibited that the peak concentration of super chlortetracycline hydrochloride was significantly higher than that of chlortetracycline hydrochloride after single dose administration[(4.69±1.54)μg/mL vs(1.91±0.63)μg/mL],indicating that the absorption rate of super chlortetracycline hydrochloride was faster than that of chlortetracycline hydrochloride.The area under the curve(AUC)of super chlortetracycline hydrochloride was also greater than that of chlortetracycline hydrochloride[(14.51±3.40)hr•μg•mL^(-1) vs(6.28±2.69)hr•μg•mL^(-1)].The results showed that the amount of super chlortetracycline hydrochloride reaching the whole body blood circulation was more than that of chlortetracycline hydrochloride,which was conducive to improving the efficacy of chlortetracycline after 7 days of continuous administration of chlortetracycline hydrochloride and super chlortetracycline hydrochloride at a dose of 20 mg/kg,the residual levels of chlortetracycline hydrochloride and super chlortetracycline hydrochloride in muscle and liver were close to or below the detection limit,which was much lower than the residual limits of chlortetracycline hydrochloride in muscle of food animals.The above results showed that super chlortetracycline hydrochloride improved the bioavailability of chlortetracycline hydrochloride and had broad application prospect and popularization value.