Walstad R A, Wiig J N, Thurmann-Nielsen E, Halvorsen T B
Eur J Clin Pharmacol. 1986;31(3):327-31. doi: 10.1007/BF00981132.
After administration of ceftazidime as a 1 g i.v. bolus injection, its concentration was measured by HPLC at frequent intervals in serum, bile and tissue from different parts of the biliary tract in 32 patients undergoing operation for biliary tract disease. In bile from the functioning gallbladder and common bile duct, a high concentration of ceftazidime was found, mean 18.5 and 26.6 mg/l, respectively. In bile from the non-functioning gallbladder, a very low concentration was found (less than 1.5 mg/l). Ceftazidime in the gallbladder wall varied considerably with the type and degree of inflammation judged histologically; the mean level was 21.3 mg/kg. The elimination half-life of ceftazidime was 1.74 h, apparent volume of distribution 20.01 and total plasma clearance 133 ml/min. In bile from T-tube specimens a high concentration was found, the mean peak values being 27.2 mg/l. However, biliary excretion of the drug was low at less than 0.5% of the administered dose. These concentrations of ceftazidime were sufficient to inhibit the in-vitro growth of pathogens, namely the Enterobacteriaecae commonly responsible for biliary tract infection.
对32例接受胆道疾病手术的患者静脉推注1g头孢他啶后,通过高效液相色谱法(HPLC)频繁测定血清、胆汁以及胆道不同部位组织中的药物浓度。在功能正常的胆囊和胆总管胆汁中,发现头孢他啶浓度较高,平均分别为18.5mg/L和26.6mg/L。在无功能胆囊的胆汁中,浓度非常低(低于1.5mg/L)。胆囊壁中的头孢他啶含量根据组织学判断的炎症类型和程度有很大差异;平均水平为21.3mg/kg。头孢他啶的消除半衰期为1.74小时,表观分布容积为20.01,血浆总清除率为133ml/分钟。在T管标本的胆汁中发现浓度较高,平均峰值为27.2mg/L。然而,该药物的胆汁排泄率较低,低于给药剂量的0.5%。这些头孢他啶浓度足以抑制病原体的体外生长,即通常引起胆道感染的肠杆菌科细菌。