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为建立高效液相色谱法(HPLC)测定猪血浆中地昔尼尔质量浓度的方法,探讨地昔尼尔乳剂在猪体内的药动学特征,将50g/kg地昔尼尔乳剂以45mg/kg的单剂量为6头健康猪给药(背正中线浇泼),血浆经乙腈提取,采用HPLC测定了血液中地昔尼尔浓度。本试验条件下,地昔尼尔在0.05～20μg/mL内线性良好,r2=0.999,最低检测限为0.01μg/mL;其药时数据符合一级吸收二室模型,主要药动学参数为:t1/2ka=9.836h±0.198h,t1/2α=13.649h±0.124h,t1/2β=20.745h±1.187h,tmax=17.576h±0.216h,Cmax=9.129μg/mL±0.313μg/mL,AUC=450.010μg/mL.h±2.993μg/mL.h。结果表明,该测定方法专属、准确、灵敏,适用于地昔尼尔的药动学研究;地昔尼尔乳剂经皮给药后,在猪体内的吸收、消除速率较慢,达峰浓度高。
To establish a HPLC method for the determination of dexilnil in pig plasma and to study the pharmacokinetics of dexifenil in pigs, kg single dose of 6 healthy pigs (dorsal midline pouring), the plasma was extracted with acetonitrile, the plasma concentration of clofinil was determined by HPLC. Under the experimental conditions, the linear range was 0.05 ~ 20μg / mL with r2 = 0.999 and the lowest detection limit was 0.01μg / mL. The data of the drug met the first-order absorption two-compartment model and the main pharmacokinetic parameters were : t1 / 2ka = 9.836h ± 0.198h, t1 / 2α = 13.649h ± 0.124h, t1 / 2β = 20.745h ± 1.187h, tmax = 17.576h ± 0.216h, Cmax = 9.129μg / mL ± 0.313μg / mL , AUC = 450.010 μg / mL.h ± 2.993 μg / mL.h. The results showed that the assay was specific, accurate and sensitive and suitable for the study of pharmacokinetics of dexcimene. After transdermal administration of dexshenil emulsion, the absorption and elimination rate of dexcimefil in pigs was slower and the peak concentration was higher .