Ceftibuten versus trimethoprim-sulfamethoxazole for oral treatment of febrile urinary tract infection in children

A randomized, open, coordinated multi-center trial compared the bacteriological and clinical efficacy and safety of orally administered ceftibuten and trimethoprim-sulfamethoxazole (TMP-SMX) in children with febrile urinary tract infection (UTI). Children aged 1 month to 12 years presenting with presumptive first-time febrile UTI were eligible for enrolment. A 2:1 assignment to treatment with ceftibuten 9 mg/kg once daily (n = 368) or TMP-SMX (3 mg + 15 mg)/kg twice daily (n = 179) for 10 days was performed. Escherichia coli was recovered in 96% of the cases. Among the E. coli isolates, 14% were resistant to TMP-SMX but none to ceftibuten. In the modified intention-to-treat population, the bacteriological elimination rates at follow-up did not differ significantly between patients treated with ceftibuten and those treated with TMP-SMX [91 vs. 95%, with a 95% confidence interval (CI) for difference of -9.7 to 1.0]. However, the clinical cure rate was significantly higher among those treated with ceftibuten (93 vs. 83%, with a 95% CI for difference of 2.4 to 17.0). Adverse events were similar for both regimens and consisted mainly of gastrointestinal disturbances. In conclusion, ceftibuten is a safe and effective drug for the empirical treatment of febrile UTI in young children.     

头孢布烯与β-内酰胺酶作用特性研究

用Ｒｉ质粒转化决明，检测转化根培养物中蒽醌化合物的产生。方法：用叶盘法转化决明外植体诱导Ｒｉ质粒转化根并用Ｓｏｕｔｈｅｒｎ杂交加以鉴定，测定转化根的生长周期，用高效液相色谱法（ｈｉｇｈ ｐｅｒｆｏｒｍａｎｃｅ ｌｉｑｕｉｄ　ｃｈｒｏｍａｔｏｇｒａｐｈｙ，ＨＰＬＣ）测定光培养及暗培养转化根中游离蒽酸化合物的质量分数。结果：决明转化根在第５～２０天为对数生长期，　Ｓｏｕｔｈｅｒｎ杂交证明了Ｒｉ质粒Ｔ－ＤＮＡ转移并整合到植物基因组中，ＨＰＬＣ结果说明暗培养转化根中芦荟大黄素等６种游离蒽醌化合物含量为光培养的２倍多。　结论：决明转化根培养周期为３５ｄ较为适宜；暗培养有利于决明转化根的生长及游离蒽醌化合物的积累。     

头孢布烯与头孢呋辛随机对照治疗急性细菌性感染临床评价

目的进一步评价头孢布烯治疗细菌性感染的安全有效性。方法采用随机对照开放试验方法。头孢布烯组２００ｍｇ，口服；头孢呋辛组７５０ｍｇ，静脉点滴；均为每１２小时一次。疗程７～１４天。结果头孢布烯组及头孢呋辛组分别有６６例及６７例可评价疗效，两组有效率分别为８７．９％及８９．６％。本次观察共分离致病菌１１０株，细菌清除率分别为９０７％及８９３％。两组安全性评价分别为６６例及７０例，不良反应发生率分别为１０．６％与１０．０％。两组经统计学处理差异无显著性（Ｐ＞０．０５）。结论采用头孢布烯治疗急性细菌性感染安全、有效     

头孢布烯治疗肺癌合并肺内感染30例临床疗效观察

探讨头孢布烯对肺癌合并肺内感染的临床效果。采用开放式，符合选择条件者３０例，口服头孢布烯２００ｍ ｇ 每日２次，连服７ｄ。于用药前后均检查痰细菌学以判定结果。结果表明，绝大部分患者用药后第３ 天症状、体征好转，第７天有１３例为显效，１５ 例有效，总有效率为９３．３％ （２８／３０）。头孢布烯对治疗肺癌合并肺内感染疗效高，副作用轻微，可于临床普遍使用。     

毛细管气相色谱法测定头孢布烯中有机溶剂残留量

目的 :建立同时测定头孢布烯中乙腈、二氯甲烷、乙酸异丙酯、甲苯和苯甲醚残留量的毛细管气相色谱法。方法 :采用HP 5毛细管柱 (30m× 0 . 5 3mm ,1 5 μm) ,柱温采用程序升温 ,检测器为FID ,载气为氮气。 结果 :各溶剂色谱的分离度均大于 1. 5 ,线性关系良好 (r >0 . 99) ,平均回收率为 96 . 5 %～ 99. 0 % ,RSD为 1. 1%～ 2 . 4 % (n =9)。结论 :毛细管气相色谱法测定头孢布烯中残留溶剂 ,方法简便 ,结果准确。     

HPLC法测定头孢布烯胶囊含量

在Ｈｙｐｅｒｓｉｌ ＢＤＳ Ｃ１８柱上,０．０５ｍｏｌ／Ｌ磷酸盐缓冲液（取磷酸二氢钠７．８ｇ,加水溶解,１０％氢氧化钠调;ｐＨ至７．０,加水至１０００ｍｌ）一乙腈（９８：２）为流动相,流速１．０ｍｌ／ｍｉｎ,室温操作,检测波长２６３ｎｍ,ＨＰＬＣ法测定头孢布烯胶囊含量,考察了色谱系统的适应性及色谱体系中各因素对色谱保留值的影响,确定的上述方法简便,准确。     

头孢布烯对淋球菌的药敏试验与治疗无合并症淋病的疗效

目的 了解头孢布对淋病奈瑟球菌的抗菌活性和治疗淋病的疗效。方法 使用孢布稀治疗了６３例无合并症淋病,并采用药敏纸片法检测上述病例的６３株淋球菌菌株对头孢布烯的药物敏感性。结果 ６３株临床淋球菌中高度敏感４８株（７６．２％）,中度敏感７株（１１．１％）,低度敏感８株（１２．７％）,临床疗效：治愈５６例（８８．９％）,有效４例（６．３％）,无效３例（４．８％）。结论 头孢布烯对淋球菌有较高的敏感性,可     

2-(2-苄氧羰基氨基噻唑-4-基)-5-(3-甲基-2-丁烯氧羰基)-2-戊烯酸的合成

对头孢布烯的关键中间体2-(2-苄氧羰基氨基噻唑-4-基)-5-(3-甲基-2-丁烯氧羰基)-2-戊烯酸(1)的合成工艺进行了研究。选用国内易得的(2-氨基噻唑-4-基)乙酸甲酯(2)作为起始原料,经过氨基保护、M ichae l加成-消除和选择性酯化三步反应制得目标化合物1,反应总收率63.0%。该工艺操作简单,生产成本低,适合工业化生产。     

Randomised trial of oral versus sequential intravenous/oral cephalosporins in children with pyelonephritis

The hypothesis was tested that oral antibiotic treatment in children with acute pyelonephritis and scintigraphy-documented lesions is equally as efficacious as sequential intravenous/oral therapy with respect to the incidence of renal scarring. A randomised multi-centre trial was conducted in 365 children aged 6 months to 16 years with bacterial growth in cultures from urine collected by catheter. The children were assigned to receive either oral ceftibuten (9 mg/kg once daily) for 14 days or intravenous ceftriaxone (50 mg/kg once daily) for 3 days followed by oral ceftibuten for 11 days. Only patients with lesions detected on acute-phase dimercaptosuccinic acid (DMSA) scintigraphy underwent follow-up scintigraphy. Efficacy was evaluated by the rate of renal scarring after 6 months on follow-up scintigraphy. Of 219 children with lesions on acute-phase scintigraphy, 152 completed the study; 80 (72 females, median age 2.2 years) were given ceftibuten and 72 (62 females, median age 1.6 years) were given ceftriaxone/ceftibuten. Patients in the intravenous/oral group had significantly higher C-reactive protein (CRP) concentrations at baseline and larger lesion(s) on acute-phase scintigraphy. Follow-up scintigraphy showed renal scarring in 21/80 children treated with ceftibuten and 33/72 with ceftriaxone/ceftibuten (p = 0.01). However, after adjustment for the confounding variables (CRP and size of acute-phase lesion), no significant difference was observed for renal scarring between the two groups (p = 0.2). Renal scarring correlated with the extent of the acute-phase lesion (r = 0.60, p < 0.0001) and the grade of vesico-ureteric reflux (r = 0.31, p = 0.03), and was more frequent in refluxing renal units (p = 0.04). The majority of patients, i.e. 44 in the oral group and 47 in the intravenous/oral group, were managed as out-patients. Side effects were not observed. From this study, we can conclude that once-daily oral ceftibuten for 14 days yielded comparable results to sequential ceftriaxone/ceftibuten treatment in children aged 6 months to 16 years with DMSA-documented acute pyelonephritis and it allowed out-patient management in the majority of these children.     

Comparison of ceftibuten vs. amoxicillin/clavulanic acid as antibiotic prophylaxis in cholecystectomy and/or biliary tract surgery

A randomized, comparative, prospective clinical trial was carried out at a tertiary care center to compare the efficacy of two antibiotic regimens in the prophylaxis of postoperative infection in patients undergoing biliary tract surgery. One hundred patients undergoing cholecystectomy or biliary tract exploration were randomly allocated to one of the following antibiotic regimens: the standard regimen of three doses of amoxicillin/clavulanic acid (1000/200 mg) given by intravenous infusion, or a single dose of ceftibuten (400 mg) given orally. Patients were monitored during their stay in the hospital and over a 2 week period as outpatients. Fifty adult patients were included in each group. Mean age was 49 years, and sex distribution was 82 women and 18 men. The groups were comparable in terms of demographic characteristics and comorbidity. There were no cases of postoperative infection in the ceftibuten group, but five cases of infection occurred in the amoxicillin/clavulanic acid group (P <0.05). No adverse effects were observed with either antibiotic. The treatment cost per patient was significantly lower for ceftibuten. The results indicate that ceftibuten is well tolerated and more effective than amoxicillin/clavulanic acid for prophylaxis following gallbladder and biliary tract surgery. In addition, ceftibuten has the advantage of being more cost-effective and easier to administer than amoxicillin/clavulanic acid so it could be considered as an alternative for antibiotic prophylaxis in these types of surgical procedures. Supported in part by Schering-Plough de México.