硫酸头孢喹肟混悬液在家兔体内的药物代谢动力学分析  

Pharmacokinetic Analysis of Cefquinome Sulfate Suspension in Rabbits

作　　者：丁媛媛 徐佳璐 刘东明 秦雨欣 董鹏伟 顾艳丽 李瑞娟 DING Yuanyuan;XU Jialu;LIU Dongming;QIN Yuxin;DONG Pengwei;GU Yanli;LI Ruijuan(College of Pharmacy,Inner Mongolia Medical University,Hohhot 010110,China)

机构地区：[1]内蒙古医科大学药学院,内蒙古呼和浩特010110

出　　处：《中国兽医杂志》2024年第12期81-86,共6页Chinese Journal of Veterinary Medicine

基　　金：内蒙古医科大学2021年度实验室开放基金项目(2021KF06);2022年全国医药学研究生教学研究课题(YXC2022-02-02)。

摘　　要：为了研究硫酸头孢喹肟混悬液在家兔体内的药物代谢动力学特征,本试验首先建立硫酸头孢喹肟血浆样品的高效液相色谱(HPLC)检测方法,通过对其专属性、精密度、回收率和稳定性的验证,确立了分析方法的可靠性;然后,将12只日本大耳白兔随机分为2个组,分别肌内注射硫酸头孢喹肟混悬液或静脉注射硫酸头孢喹肟溶液,采用HPLC法测定家兔体内硫酸头孢喹肟的质量浓度,并使用DAS 2.0软件绘制血药浓度-时间曲线,计算药物代谢动力学参数。结果显示,硫酸头孢喹肟含量测定分析方法专属性良好,在0.1~6.0 mg/L呈良好的线性关系,日内精密度低于3.48%,日间精密度低于3.47%,血浆样品的平均回收率为97.86%~103.89%,稳定性为96.82%~102.96%,符合生物样品分析要求;肌内注射和静脉注射拟合的二室模型赤池信息准则(AIC)值(-25.313和-23.907)均小于其拟合的一室模型AIC值(11.933和-3.852),2种给药方式的拟合模型均表明硫酸头孢喹肟在家兔体内的药物代谢动力学模型符合二室模型;硫酸头孢喹肟混悬液采用肌内注射给予家兔,其绝对生物利用度为84.18%。结果表明,本试验建立的HPLC检测方法操作简便、专属性强、灵敏度高,可用于家兔体内硫酸头孢喹肟血药浓度的测定和药物代谢动力学分析,硫酸头孢喹肟混悬液在家兔体内吸收迅速,可长时间维持较高的血药浓度,为该药的临床应用提供指导。To study the pharmacokinetic characteristics of cefquinome sulfate suspension in rabbits,this study first established an high-performance liquid chromatography(HPLC)detection method for cefquinome sulfate in plasma samples.The specificity,precision,recovery rate,and stability of the method were validated to confirm its reliability.Subsequently,12 Japanese white rabbits were randomly divided into two groups and were administered cefquinome sulfate either via intramuscular injection(as a suspension)or intravenous injection(as a solution).The concentration of cefquinome sulfate in rabbit plasma was measured using HPLC,and pharmacokinetic parameters were calculated by plotting the plasma concentration-time curve using DAS 2.0 software.The results showed that the method exhibited good specificity;it showed a linear relationship in the range of 0.1 to 6.0 mg/L,with intra-day precision below 3.48%and inter-day precision below 3.47%.The average recovery rate of plasma samples was between 97.86%and 103.89%,and stability was between 96.82%and 102.96%,meeting the requirements for biological sample analysis.The Akaike information criterion(AIC)values for the two-compartment model fitted to intramuscular and intravenous injection data(-25.313 and-23.907,respectively)were both lower than the AIC values for the one-compartment model(11.933 and-3.852,respectively),indicating that the pharmacokinetics of cefquinome sulfate in rabbits conformed to a two-compartment model for both administration routes.The absolute bioavailability of cefquinome sulfate suspension via intramuscular injection in rabbits was 84.18%.The results indicate that the HPLC method established in this study is simple,highly specific,and sensitive,and can be used for the determination of plasma concentration and pharmacokinetic analysis of cefquinome sulfate in rabbits.Cefquinome sulfate suspension is rapidly absorbed and can maintain a high plasma concentration over a long period in rabbits,providing guidance for its clinical application.

关 键 词：硫酸头孢喹肟 药物代谢动力学 高效液相色谱(HPLC) 家兔 

分 类 号：S859.7[农业科学—临床兽医学]