Pharmacokinetics of 5-fluorouracill and its penetration into pancreatic juice in dogs

Pharmacokinetics of 5 fluorouracil and its penetration into pancreatic juice in dogs

研究胰液中５氟脲嘧啶（５ＦＵ）的药物动力学行为及其与血药浓度的关系，并评价其穿透胰液特性．方法：杂种狗８只，手术放置胰外引流管后单剂量静注５ＦＵ２５０ｍｇ．采集血和胰液并用ＨＰＬＣ法测定药物浓度．计算药物动力学参数并作统计学分析．结果：血浆和胰液中５ＦＵ的平均Ｋ１０分别为９４ｈ－１和１０２ｈ－１（Ｐ＞００５）．血中和胰液药物消除均符合非线性模型，穿透指数为３３９±２８４．５ＦＵ由血浆向胰液穿透较迅速，胰液中的药物浓度持续高于同期血药浓度．结论：胰液中药物消除与血液相似，二者为同一动力学房室．

AIM: To study the pharmacokinetic behavior of 5 fluorouracil (5 FU) in pancreatic juice in dogs and its correlation with 5 FU in plasma, and to evaluate its penetration characteristics. METHODS: After placing a pancreatico drainage tube, 8 dogs were injected 5 FU 250 mg iv. Blood and pancreatic samples were collected and the 5 FU concentrations were determined by HPLC. The pharmacokinetic parameters were obtained with statistical analysis. RESULTS: The mean slopes of the terminal phase ( K 10 ) in plasma and pancreatic juice were 9 4 h -1 and 10 2 h -1 , respectively ( P >0 05). The pharmacokinetic behaviors of 5 FU in plasma and pancreatic juice fitted a nonlinear model. Its penetration index was 3 39±2 84. The penetration of 5 FU from blood to pancreatic juice was relatively rapid, demonstrating a consistently higher concentration in pancreatic juice than in plasma. CONCLUSIONS: The elimination phase of 5 FU in plasma was similar to that in pancreatic juice, indicating that they were in the same kinetic compartment.