Cho N, Fukunaga K, Kunii K, Deguchi K
Jpn J Antibiot. 1983 May;36(5):939-55.
T-1982 (cefbuperazone), a new cephamycin antibiotic, was studied for its MICs against clinical isolates, transfer into uterine tissues and clinical efficacy in the field of obstetrics and gynecology. The following results were obtained. The MICs of T-1982 were measured against 397 strains of 13 species. In antibacterial activity, T-1982 was equal to CTT but inferior to CMZ against Gram-positive bacteria. Against Gram-negative bacteria, T-1982 was superior to CEZ and other cephamycin antibiotics, i.e. CMZ and CTT. The activity of T-1982 was almost equal to that of CMZ and superior to that of CTT against B. fragilis. T-1982 concentrations in various uterine tissues attained the peaks of 16.8-35.9 micrograms/g at 34 minutes after intravenous administration of 1 g, the tissue/serum ratios being 34-72%. The tissue concentrations were about 3-4 micrograms/g even at 5-5.5 hours after administration. T-1982 was intravenously administered at a dose of 1 g twice daily to 5 cases with obstetrical and gynecological infections. All the cases responded to the therapy. Elevated GOT and GPT were observed in 1 case, but they returned to normal on 8 days after the therapy.
新型头孢霉素类抗生素T - 1982（头孢布宗）针对临床分离菌株的最低抑菌浓度（MIC）、在子宫组织中的药物转移情况以及在妇产科领域的临床疗效进行了研究。获得了以下结果。对13个菌种的397株菌株测定了T - 1982的MIC。在抗菌活性方面，T - 1982对革兰氏阳性菌的活性与头孢噻肟钠（CTT）相当，但低于头孢孟多（CMZ）。对革兰氏阴性菌，T - 1982优于头孢唑肟（CEZ）及其他头孢霉素类抗生素，即CMZ和CTT。T - 1982对脆弱拟杆菌的活性几乎与CMZ相当且优于CTT。静脉注射1g后34分钟，T - 1982在各种子宫组织中的浓度达到峰值，为16.8 - 35.9微克/克，组织/血清比值为34% - 72%。给药后5 - 5.5小时，组织浓度仍约为3 - 4微克/克。对5例妇产科感染患者，以每日2次、每次1g的剂量静脉注射T - 1982。所有病例对治疗均有反应。1例患者出现谷草转氨酶（GOT）和谷丙转氨酶（GPT）升高，但治疗后8天恢复正常。
