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目的 研究生技霉素药代动力学过程。方法 测定狗口服生技霉素 10mg·kg-1,2 0mg·kg-1,30mg·kg-1血药浓度并与乙酰螺旋霉素比较 ;测定大鼠灌胃生技霉素 40mg·kg-1,80mg·kg-1,12 0mg·kg-1血药浓度及大鼠灌胃生技霉素 40mg·kg-1后尿、胆汁活性产物回收率。血药浓度及尿、胆汁药物浓度以微生物法测定。 3P87程序拟合计算药物动力学参数。结果 狗口服 3组剂量生技霉素 ,结果表明药物吸收较快 ,lag time为 10～ 30min ;Tmax1 43～ 2 44h ;Cmax1 0 2～ 2 94g·L-1;T1/ 2α0 48～ 1 81h ;T1/ 2 β8 40～10 5 2h ;3组剂量AUC值分别为 15 2 5 ,2 3 70 ,31 40mg·L-1·h-1,表明药物在此剂量范围内呈线形药代动力学特征 ;MRT值分别为 8 11,8 38,8 71h ,不随剂量增减而改变。大鼠口服 3组剂量生技霉素 ,Tmax1 5 7～ 2 45h ;Cmax0 39～ 3 14mg·L-1;T1/ 2α 1 36～ 1 77h ;T1/ 2 β15 6 3～2 0 6 4h ;MRT值约为 13 0h。AUC值分别为 8 44、16 5 4、37 5 8mg·L-1·h-1,同样呈线形药代动力学特征。在相同的实验条件下 ,进行狗口服 3组剂量乙酰螺旋霉素药物动力学对比实验 ,测得ASPM药物动力学参数为 :lag time为0 37～ 0 44h ;Tmax1 49～ 2 2 6h ;Cmax 0 87～ 3 34mg2 0 0 0 0 3 0 5收稿 ,2 0 0
Aim To study the pharmacokinetics of doxorubicin. Methods The blood concentrations of 10 mg · kg-1, 10 mg · kg-1 and 30 mg · kg-1 of gemcitabine in dogs were determined and compared with acetylspiramycin. The concentrations of gemcitabine 40 mg · kg- 1, 80mg · kg-1, 120mg · kg-1 blood concentration and rat stomach gentimycin 40mg · kg-1 urinary and bile product recovery. Blood concentration and urine, bile drug concentration by microbiological assay. 3P87 program fitting to calculate pharmacokinetic parameters. Results The dogs received oral administration of 3 doses of doxorubicin. The results showed that the drug absorption was rapid with a lag time of 10-30 min; Tmax1 43-2 44 h; Cmax 120-2 94 g · L -1; T1 / 2α 0 48-1 81 h; T1 / 2 β8 40 ~ 10 5 2h; The AUC values of the three groups were 15 2 5, 2 3 70 and 31 40 mg · L-1 · h-1, respectively, indicating that the drug showed linear pharmacokinetic characteristics in this dose range ; MRT values were 8 11,8 38,8 71h, not with dose changes. The rats were orally administered with 3 doses of doxorubicin, with Tmax 157 to 245 h, C max 0 39 to 3 14 mg · L -1, T1 / 2α 1 36 to 1 77 h, T1 / 2 β 15 6 3 to 2 0 6 4 h, MRT The value is about 13 0h. AUC values were 8 44,165 4,37 5 8 mg · L-1 · h-1, also linear pharmacokinetic characteristics. Under the same experimental conditions, dog oral administration of three doses of acetylspiramycin pharmacokinetic comparison test, measured ASPM pharmacokinetic parameters: lag time was 0 37 ~ 0 44h; Tmax1 49 ~ 2 2 6h; Cmax 0 87 ~ 3 34mg2 0 0 0 0 3 0 5 Received, 2 0 0