Cefbuperazone(CBPZ)の前立腺組織内移行に関する検討

Abstract

TUR-P術前患者の36名に対し, CBPZ 1 gをone shot静注後, 摘出した前立腺組織内濃度, 血清中濃度を測定した.1) CBPZ 1 g静注後の血清中濃度は投与20分後に80.56 μg/mlの値を示し, 以後経時時に漸減し投与4時間後に9.89 μg/mlの値を示した.2)前立腺組織内濃度はTmax 24.2分, Cmax 19.34 μg/gの最高濃度を示した後, 漸減して投与後4時間に3.13 μg/gとなるカーブを示した.3)血清中濃度・前立腺組織内濃度をCBPZのMICと比較すると, P. aeruginosaを除けば, ほとんどの菌種において有効濃度を上回り, TUR-P術前投与に, また前立腺炎症性疾患において, CBPZは有効であると思われる

The concentration of Cefbuperazone (CBPZ) were determined by bioassay in the serum and prostatic tissue of 36 patients with benign prostatic hypertrophy, who underwent transurethral resection. One gram of CBPZ was injected intravenously prior to surgery. Pharmacokinetic analysis was performed using the two or three compartment model theory. The maximum serum level of CBPZ was 82.2 micrograms/ml at 30 min after the start of CBPZ administration and biological half-life was 97.3 min. CBPZ concentration in prostatic tissue reached a maximum level of 26.3 micrograms/g at 50 min following CBPZ administration. The prostatic tissue level was 28-40% of the serum level. These results suggested that intravenous administration of CBPZ would be extremely effective against pathogenic bacteria, particularly Enterobacter, E. coli, Klebsiella, Serratia, Proteus and Bacteroides, judging from its prostatic concentration.