硫酸头孢喹肟在猪体内的药动学研究

Studies on cefquinome sulphate for injectable suspension and its pharmacokinetics in swine

建立猪血浆中硫酸头孢喹肟的SPE—HPLC测定方法，对硫酸头孢喹肟在猪体内的药动学特征进行研究。选用健康猪6头，进行单次肌肉注射2mg·kg^-1自制的2．5％硫酸头孢喹肟注射液，提取血浆药物经SPE柱净化后进行HPLC分析。色谱条件为C18反相柱，流动相。高氯酸钠-磷酸-三乙胺缓冲液（pH3．6）与乙腈混合液（体积比为90：10）。结果显示，硫酸头孢喹肟在0．05～25μg·mL^-1线性关系良好（R^2=0．9986），最低检测限为0．05μg·mL^-1。经3p97软件分析结果显示：硫酸头孢喹肟的药时数据适合一级吸收二室模型，主要药动学参数：tmax为（0．80±0．05）h，Cmax为（2．44±0．24）μg·mL^-1，AUC为（7．28±1．11）μg·mL^-1·h，T1/2β为（2．28±0．49）h。结果提示：健康猪单次肌肉沣射硫酸头孢喹肟后吸收迅速，持效时间较长，临床用药18h后仍能维持对常见病原菌的有效血药浓度。建议临床用药：2mg·kg^-1（以头孢喹肟计），1日1次。

SPE-HPLC method was established to determine cefquinome sulphate, and to study the pharmacokinetics of cefquinome sulphate iu swine plasma. Cefquinome sulphate were administrated i. m. at a dose of 2 μg · kg^-1 to six swine. After extracted with methanol, cefquinnme sulphate concentration of preparation samples were determined by HPLC/UV with solid phase extraction method. C18 was used as the revesed column, sodium perchlorate-phosphoric acid buffer （pH 3.6） ： aeetonitrile （90： 10, V/V） as the mobile phate, the eoncentration-time date were analyzed with 3p97 computer program. The results indieat that the standard eurves for cefquinome is linar in a range of 0. 05 -25 μg · mL^-1 （ R2 =0. 998 6） , the limit of detection was 0. 05 μg· mL^-1 ; the results suggest that the kinetics of the injection is fit to two compartment model with first order absorption. The main parameters of cefquinome sulphate is tmax = （0.80±0.05） h, C = （2.44±0.24） μg· mL^-1, AUC= （7.28±1.11）μg·mL^-1· h, T1/2β= （2.28± 0.49） h. We eonelud that eefquinome sulphate could be absorbed rapidly, long persistence effective time, there is enough effect after 18 h by i.m. eefquinome sulohate. 2 mg·kg^-1 and 1 day 1 time is adviced.