Deguchi K, Yokota N, Koguchi M, Nakane Y, Fukayama S, Nishimura Y, Oda S, Tanaka S, Kato M, Sato K
Section of Studies, Tokyo Clinical Research Center.
Jpn J Antibiot. 1988 Sep;41(9):1194-204.
Sultamicillin (SBTPC) is a mutual prodrug in which ampicillin (ABPC) and a potent beta-lactamase inhibitor sulbactam (SBT) are ester-bound in an equimolar ratio. SBTPC is hydrolyzed during absorption after oral administration to provide ABPC and SBT for systemic circulation. In the present study, the antimicrobial activities of SBTPC against 50 isolates each of 6 species (Staphylococcus aureus, Klebsiella pneumoniae subsp. pneumoniae, Branhamella catarrhalis, Haemophilus influenzae, Streptococcus pneumoniae and Streptococcus pyogenes) of bacteria freshly obtained from upper respiratory tract infections were examined in relation to their bacterial beta-lactamase producing abilities. beta-Lactamase producing strains were identified using the acidometry disc method with benzylpenicillin (PCG) of cefazolin (CEZ) as a substrate, and their frequencies of appearance were calculated as follows: S. aureus 86%; K. pneumoniae subsp. pneumoniae 100%; B. catarrhalis 68%; H. influenzae 24%. Fourteen per cent of S. aureus strains examined were beta-lactamase positive using both PCG and CEZ acidometry discs. SBTPC, however, demonstrated excellent antimicrobial activities even against these beta-lactamase producing strains. Good activities were observed especially against those bacterial strains producing penicillinase (PCase). Average MIC80 values of SBTPC were 3.13 micrograms/ml for S. aureus and K. pneumoniae subsp. pneumoniae, 0.39 micrograms/ml for B. catarrhalis and H. influenzae, 0.05 micrograms/ml for S. pneumoniae and 0.025 micrograms/ml for S. pyogenes. As SBTPC was shown to possess excellent antimicrobial activities against PCase producing strains, the enhancement in activities of SBTPC compared to ABPC alone can be attributed to the inhibition of beta-lactamase by SBT which, as noted above, is a component of SBTPC in an equimolar ratio to ABPC.
舒他西林（SBTPC）是一种复方前体药物，其中氨苄西林（ABPC）和强效β-内酰胺酶抑制剂舒巴坦（SBT）以等摩尔比通过酯键结合。口服给药后，SBTPC在吸收过程中被水解，为全身循环提供ABPC和SBT。在本研究中，检测了SBTPC对从上呼吸道感染患者新分离出的6种细菌（金黄色葡萄球菌、肺炎克雷伯菌肺炎亚种、卡他莫拉菌、流感嗜血杆菌、肺炎链球菌和化脓性链球菌）各50株菌株的抗菌活性，并分析了其与细菌产生β-内酰胺酶能力的关系。采用以苄青霉素（PCG）或头孢唑林（CEZ）为底物的酸度计纸片法鉴定产β-内酰胺酶菌株，并计算其出现频率如下：金黄色葡萄球菌86%；肺炎克雷伯菌肺炎亚种100%；卡他莫拉菌68%；流感嗜血杆菌24%。使用PCG和CEZ酸度计纸片检测的金黄色葡萄球菌菌株中，14%为β-内酰胺酶阳性。然而，SBTPC即使对这些产β-内酰胺酶菌株也表现出优异的抗菌活性。尤其对那些产生青霉素酶（PCase）的菌株观察到良好的活性。SBTPC对金黄色葡萄球菌和肺炎克雷伯菌肺炎亚种的平均MIC80值为3.13微克/毫升，对卡他莫拉菌和流感嗜血杆菌为0.39微克/毫升，对肺炎链球菌为0.0
