학술논문

Cefuroxime axetil (CXM-AX) に関する研究 / STUDIES ON CEFUROXIME AXETIL (CXM-AX)
Document Type
Journal Article
Source
CHEMOTHERAPY. 1986, 34(Supplement5):404
Subject
Language
Japanese
ISSN
0009-3165
1884-5894
Abstract
Cefuroxime axcetil (CXM-AX), an orally absorbed pro-drug of cefuroxime (CXM), was studied. The MICs of CXM were determined for 137 clinical isolates of 6 species, using plate dilution method with inoculum size of 106 cfu/ml. The MICs of CXM ranged 0.39->100 μg/ml for S. aureus, 3.13-12.5 μg/ml for E. coli, 1.56-25 μg/ml for K. pneumoniae, 1.56-100 μg/ml for P.mirabilis, 12.5-50 μg/ml for M. morganii, 6. 25->100 μg/ml for Serratia spp.CXM-AX was administered orally in a dose of 250 mg to 6 healthy male volunteers in the fasting state and after meal using crossover manner. There were differences between the pharmacokinetics of CXM-AX in the fasting state and that after meal.When CXM-AX was dosed in the fasting state and after meal, Tmax was 1.4 and 2.8 hours, Cmax was 2.9 and 3.2 μg/ml, T 1/2 was 1.1 and 1.6 hours and AUC was 9.0 and 15 μg·hr/ml, respectively. The 0-6 hour urinary excretion rate of CXM-AX was 23.4% after doses in the fasting state and 43.6% after meal.The absorption of CXM-AX was significantly better when the drug was given after meal than when it was given in the fasting.It is recommended that patients should take doses of CXM-AX shortly after meal. Twenty nine patients, including 20 with respiratory tract infections and 9 with urinary tract infections were treated with CXM-AX for 3-10 days, mainly in the dose of 250 mg t. i. d.Clinical effect was excellent in 10 cases, good in 14 cases, fair in 3 cases and poor in 2 cases. The efficacy rate was 83%.The only side effect noted was diarrhea which occured in one case.