比格犬体内右旋酮洛芬氨丁三醇水凝胶贴剂药代动力学研究  

Pharmacokinetics of Dexketoprofen Trometamol Hydrogel Patch in Beagle Dogs

作　　者：陈永顺 吴珍 CHEN Yongshun;WU Zhen(Taihe Hospital·Affiliated Hospital of Hubei Medical College,Shiyan,Hubei,China 442000)

机构地区：[1]湖北省十堰市太和医院·湖北医药学院附属医院,湖北十堰442000

出　　处：《中国药业》2020年第21期33-36,共4页China Pharmaceuticals

摘　　要：目的考察右旋酮洛芬氨丁三醇(DKT)水凝胶贴剂在比格犬体内的药代动力学参数。方法6只比格犬均分为DKT灌胃给药组与DKT水凝胶贴剂组,采用高效液相色谱法测定血药浓度,采用DAS 2.0软件计算药代动力学参数,并将两组间的药代动力学数据进行比较与分析。结果DKT灌胃给药和DKT水凝胶贴剂在比格犬体内的药代动力学过程符合二室模型,DKT灌胃给药(0.5 mg/kg)与DKT水凝胶贴剂腹部给药(每贴100 mg)的主要药代动力学参数,达峰时间(tmax)分别为(0.50±0.12)h和(6.02±0.14)h,峰浓度(Cmax)分别为(3.08±0.25)μg/m L和(2.98±0.22)μg/m L,分布相半衰期(t1/2α)分别为(0.29±0.11)h和(1.86±0.26)h,消除相半衰期(t1/2β)分别为(1.01±0.35)h和(10.11±0.26)h,0~24 h药时曲线下面积(AUC0→24 h)分别为(9.03±0.37)mg/(h·L)和(26.22±1.17)mg/(h·L),0~24 h平均驻留时间(MRT0→24 h)分别为(6.96±0.32)h和(8.17±0.28)h。结论与灌胃给药相比,DKT水凝胶贴剂的达峰时间和半衰期均延长,具有缓释给药特征。Objective To investigate the pharmacokinetic of dexketoprofen trometamol(DKT)hydrogel patch in beagle dogs.Methods Six beagle dogs were equally divided into the DKT intragastric administration group and the DKT hydrogel patch group.The concentration of DKT in plasma of beagle dogs was determined by the high performance liquid chromatography(HPLC)method and the pharmacokinetics parameters after administration were calculated by DAS2.0 software.The pharmacokinetic data of the two groups were compared and analyzed.Results The pharmacokinetic process in the beagle dogs of the DKT intragastric administration group and the DKT hydrogel patch group fitted the two-compartment model,and the main pharmacokinetic parameters of the DKT intragastric administration group(0.5 mg/kg)and the DKT hydrogel patch group(100 mg each patch)were as follows:tmaxwas(0.50±0.12)h and(6.02±0.14)h,Cmax was(3.08±0.25)μg/m L and(2.98±0.22)μg/m L,t1/2αwas(0.29±0.11)h and(1.86±0.26)h,t1/2βwas(1.01±0.35)h and(10.11±0.26)h,AUC0→24 hwas(9.03±0.37)mg/(h·L)and(26.22±1.17)mg/(h·L),MRT0→24 hwas(6.96±0.32)h and(8.17±0.28)h.Conclusion Compared with DKT intragastric administration,the tmaxand t1/2 of DKT hydrogel patch are prolonged significantly,which has good sustained-release characteristics.

关 键 词：右旋酮洛芬氨丁三醇 水凝胶贴剂 药代动力学 

分 类 号：R965[医药卫生—药理学] R971.1[医药卫生—药学]