Morinaga T, Furukawa M, Nakata T, Yamada R, Itoh S, Maeda S, Itose K, Ohtsubo M
Jpn J Antibiot. 1985 Jan;38(1):128-32.
The concentration of cefoperazone (CPZ) in serum and bile was estimated after intravenous drip infusion of 1 g of the drug in 11 patients, who have performed cholecystectomy, choledocholithotomy and T-tube drainage for gallstone diseases. Administration of cefazolin (CEZ) 1 g was compared by the cross over method. After 1 g intravenous drip infusion of CPZ, the mean serum concentration was 88.3 +/- 24 micrograms/ml at 1 hour, 52 +/- 11.7 micrograms/ml at 2 hours and 36.5 +/- 10 micrograms/ml at 4 hours. The maintenance period of serum concentration was inclined to be longer in CPZ than in CEZ. After 1 g intravenous drip infusion of CPZ, the mean bile concentration reached to 810 +/- 459 micrograms/ml in 2 hours and it was maintained as high as 562 +/- 319 micrograms/ml even after 4 hours. On the other hand, after 1 g intravenous drip infusion of CEZ, the mean bile concentration was only 28.7 +/- 26 micrograms/ml in 1 hour and was low level in the progress. As compared with the highest concentration of CPZ and CEZ in same patient, the mean bile concentration of CPZ (942 +/- 525 micrograms/ml) was about 30 times higher than that of CEZ (28.6 +/- 26.3 micrograms/ml). There was no difference in the group of Gram-positive cocci between minimum inhibitory concentration (MIC) of CPZ and that of CEZ. While MIC of CEZ in the group of Gram-negative bacilli was from 0.78 to over 400 micrograms/ml, MIC of CPZ in that group was from 0.10 to 50 micrograms/ml. The value in CPZ was lower than that in CEZ at all strains. No side effects was seen in all patients.
对11例因胆结石疾病行胆囊切除术、胆总管切开取石术及T管引流术的患者静脉滴注1g头孢哌酮(CPZ)后,测定其血清和胆汁中CPZ的浓度。采用交叉对照法比较了静脉滴注1g头孢唑林(CEZ)的情况。静脉滴注1g CPZ后,1小时时血清平均浓度为88.3±24μg/ml,2小时时为52±11.7μg/ml,4小时时为36.5±10μg/ml。CPZ血清浓度的维持时间比CEZ倾向于更长。静脉滴注1g CPZ后,2小时时胆汁平均浓度达到810±459μg/ml,甚至4小时后仍维持在562±319μg/ml的高水平。另一方面,静脉滴注1g CEZ后,1小时时胆汁平均浓度仅为28.7±26μg/ml,且在后续过程中一直处于低水平。与同一患者中CPZ和CEZ的最高浓度相比,CPZ的胆汁平均浓度(942±525μg/ml)约为CEZ(28.6±26.3μg/ml)的30倍。在革兰氏阳性球菌组中,CPZ和CEZ的最低抑菌浓度(MIC)无差异。而在革兰氏阴性杆菌组中,CEZ的MIC为0.78至400μg/ml以上,CPZ的MIC为0.10至50μg/ml。在所有菌株中,CPZ的值均低于CEZ。所有患者均未出现副作用。