Sakai K, Ueda T, Uchino J, Hayasaka A, Shiramatsu K, Nagamachi Y, Shoda Y, Okui K, Hayata Y, Watanabe H
Jpn J Antibiot. 1987 Apr;40(4):759-811.
Clinical studies have been conducted on BRL 28500 (a formulation containing 15 parts ticarcillin (TIPC) plus 1 part clavulanic acid (CVA]. BRL 28500 was administered at doses of 1.6 g or 3.2 g b.i.d., generally for 10 days by drip infusion to patients with intraperitoneal infections or biliary tract infections. Drug concentrations in the ascites were determined. A total of 76 cases was treated with BRL 28500. These cases included 49 intraperitoneal infections (suppurative peritonitis 29, postoperative peritonitis 20) and 18 biliary tract infections (cholecystitis 5, cholangitis 13). Nine cases were excluded from evaluation according to the committee's assessment. The clinical improvement as assessed by surgeons in charge increased with the duration of continued treatment and efficacies were assessed as 57.1% on day 5, 63.1% on day 7 and 77.8% on day 10 in intraperitoneal infections. Corresponding results in biliary tract infections were 38.9%, 40.0% and 42.9%, respectively. From these results, it is clear that the degree of improvement is related to the duration of treatment. The clinical usefulness as assessed by surgeons in charge of the study was 63.8% in intraperitoneal infections (suppurative peritonitis 75.0%, postoperative peritonitis 47.4%) and 58.8% in biliary tract infections (cholecystitis 100%, cholangitis 41.7%). The overall rate of usefulness was 62.5%. The clinical efficacy rates as assessed by the committee were 81.6% in intraperitoneal infections (suppurative peritonitis 93.1%, postoperative peritonitis 65.0%) and 66.7% in biliary tract infections (cholecystitis 100%, cholangitis 53.8%). In cases where causative organisms were isolated, the efficacies were 92.9% in suppurative peritonitis, 58.8% in postoperative peritonitis, 50.0% in cholangitis and overall, 69.2%. In cases from which TIPC-resistant organisms were isolated, the overall efficacy rate was 65.4% (suppurative peritonitis 88.9%, postoperative peritonitis 58.3% and cholangitis 40.0%). Regarding bacteriological effect as assessed by the committee, the eradication rate was 76.9% in intraperitoneal infections and 40.0% in biliary tract infections (71.0% overall). In cases from whom ticarcillin-resistant organisms were isolated the corresponding rates were 68.4% and 33.3% respectively, (63.6% overall). In 4 patients with peritonitis drug levels in the ascites were determined following administration of BRL 28500 by drip infusion. Good levels of both TIPC and CVA were detected 1 to 3.5 hours after administration.(ABSTRACT TRUNCATED AT 400 WORDS)
已对BRL 28500（一种含有15份替卡西林（TIPC）加1份克拉维酸（CVA）的制剂）进行了临床研究。BRL 28500以1.6 g或3.2 g的剂量每日两次给药，通常通过静脉滴注对腹腔感染或胆道感染患者给药10天。测定了腹水中的药物浓度。共有76例患者接受了BRL 28500治疗。这些病例包括49例腹腔感染（化脓性腹膜炎29例，术后腹膜炎20例）和18例胆道感染（胆囊炎5例，胆管炎13例）。根据委员会的评估，9例患者被排除在评估之外。负责的外科医生评估的临床改善情况随持续治疗时间的延长而增加，腹腔感染在第5天的有效率为57.1%，第7天为63.1%，第10天为77.8%。胆道感染的相应结果分别为38.9%、40.0%和42.9%。从这些结果可以明显看出，改善程度与治疗持续时间有关。负责该研究的外科医生评估的临床有用性在腹腔感染中为63.8%（化脓性腹膜炎75.0%，术后腹膜炎47.4%），在胆道感染中为58.8%（胆囊炎100%，胆管炎41.7%）。总体有用率为62.5%。委员会评估的临床有效率在腹腔感染中为81.6%（化脓性腹膜炎93.1%，术后腹膜炎65.0%），在胆道感染中为66.7%（胆囊炎100%，胆管炎53.8%）。在分离出病原菌的病例中，化脓性腹膜炎的有效率为92.9%，术后腹膜炎为58.8%，胆管炎为50.0%，总体为69.2%。在分离出对TIPC耐药菌的病例中，总体有效率为65.4%（化脓性腹膜炎88.9%，术后腹膜炎58.3%，胆管炎40.0%）。关于委员会评估的细菌学效果，腹腔感染中的根除率为76.9%，胆道感染中为40.0%（总体为71.0%）。在分离出对替卡西林耐药菌的病例中，相应的根除率分别为68.4%和33.3%（总体为63.6%）。对4例腹膜炎患者在通过静脉滴注给予BRL 28500后测定了腹水中的药物水平。给药后1至3.5小时检测到TIPC和CVA的良好水平。（摘要截短于400字）
