摘要
以OP-10、斯盘-80为乳化剂,油酸乙酯为油相,通过表面活性剂复配结合癸氧喹酯固体颗粒稳定乳液技术研制开发新型癸氧喹酯乳剂.与市售癸氧喹酯溶液对比研究癸氧喹酯乳液生物等效性,将实验肉鸡随机分组,并分别灌胃癸氧喹酯乳液及溶液,采用高效液相色谱的方法测定其血药浓度,采用PKSolver2.0药动学程序计算药动学参数.试验优化了癸氧喹酯血液样品的处理方法,并考察了方法专属性;结果表明,癸氧喹酯分析方法在0.16~16.33 ng·mL^(-1)之间呈良好的线性关系,回归方程:y=453.588x-94.181,r^(2)=0.9986(n=6),日内变异系数低于4.84%,日间变异系数低于7.75%;样品的平均回收率为91.6%~94.9%,完全符合生物样品分析要求;两组药动学行为均符合一级吸收一室模型,其主要药动学参数为:吸收半衰期(T_(1/2a))分别为1.45±0.07 h、1.51±0.09 h;达峰时间(T_(max))分别为6.78±0.14 h、6.95±0.21 h;峰浓度(C_(max))分别为11.385±0.052 ng/mL、10.577±0.041 ng/mL;15消除半衰期(T_(1/2β))分别为17.49±0.32 h、16.96±0.49h;药时曲线下面积(AUC_(0-t))达196.971±3.883 ng·h·mL^(-1)、182.763±4.174ng·h·mL^(-1).对两实验组AUC_(0-t)、C_(max)、T_(max)进行差异性分析,三种药代参数组间差异均不显著(P>0.05),且癸氧喹酯乳液相对溶液的生物利用度为107%;自制癸氧喹酯乳液与市售癸氧喹酯溶液具有生物等效性.
OP-10,Span 80 as emulsifier,Ethyl oleate is the oil phase,emulsion stabilization and development of new technology decoquinate emulsion by a surfactant complex binding decoquinate solid particles.The bioequivalence of decoquinate emulsion was compared with commercially available decoquinate solution.Chickens were randomized experimental,intramuscular gavageof decoquinate emulsion and solution,The plasma concentration was determined by HPLC,and the pharmacokinetic parameters were calculated by PKSolver2.0 pharmacokinetic program.The method of treating the blood samples of decoquinatewas optimized and the specificity of the method was investigated;Result showed that the decoquinate analysis method had a good linear relationship between 0.16~16.33ng/mL,and the regression equation was:y=453.588x-94.181,r^(2)=0.9986(n=6);The intraday coefficient of variation is less than 4.84%and the daytime cofficient of variation is less than 7.75%.The average recovery of the sample is 91.6%~94.9%,which is in accordance with the requirements of biological sample analysis.The pharmacokinetic parameters ofthe two groups absorption halftime(T_(1/2α))were 1.45±0.07 h、1.51±0.09h respectively,the peak time(T_(max))was6.78±0.14 h、6.95+0.21 h and the peak concentration(C_(max))were 11.385+0.052 ng/mL、10.577±0.041 ng/mL;The elimination halftime(T_(1/2β))were 17.49±0.32 h、16.96±0.49 h and the AUC_(0-t),reached 196.971±3.883 ng·h·mL^(-1)、182.763±4.174 ng·h·mL^(-1).The differences of AUC_(0-t),C_(max)and T_(max)between the two experimental groups were not significant(P>0.05);The self-made decoquinate emulsion has a bioequivalence with commercially available Decoquinatesolution.
作者
唐达
陈诚
TANG Da;CHEN Cheng(Chongqing Academy of Animal Sciences,Chongqing 402460,China)
出处
《应用化工》
CAS
CSCD
北大核心
2020年第S01期101-105,共5页
Applied Chemical Industry
基金
重庆市基础研究与前沿探索项目(cstc2018jcyjAX0789)
重庆市畜牧科学院市级财政专项资金项目(19507)
