An observer blind trial of co-amoxiclav versus cefuroxime plus metronidazole in the prevention of postoperative wound infection after general surgery

A consecutive series of 509 patients undergoing abdominal surgery were entered into a randomized, observer and patient blind, controlled, prospective, study to evaluate the efficiency of co-amoxiclav (‘Augmentin’, SmithKline Beecham, UK) compared with cefuroxime (‘Zinacef’ Glaxo, UK) plus metronidazole (Flagyl, M&B, UK) for the prevention of postoperative wound infections. One or three doses of antibiotics were given depending on the type of surgery and operative factors. Co-amoxiclav was given to 230 patients with a total wound infection rate of 5·6% and cefuroxime plus metronidazole were given to 225 patients with a total wound infection rate of 3%. The difference between infection rates was not significant. Both groups were comparable in terms of demographic details, type and duration of surgery, risk factors associated with surgical procedures and postoperative management. Although not statistically significant, a difference in the wound infection rate for those patients undergoing colorectal surgery was seen: for the co-amoxiclav group and for the cefuroxime/ metronidazole group. The estimated cost to our hospital (October 1993) of one dose of co-amoxiclav was less that half the cost of cefuroxime and metronidazole. This study demonstrates that co-amoxiclav is an effective prophylactic antibiotic for abdominal surgery.     

头孢呋辛酯制备工艺的改进

以头孢呋辛钠为原料，从制备（R，S）-乙酸1-溴乙酯开始。经酯化反应的溶剂沉淀过程无须分离直接制得高纯度非晶型的头孢呋辛酯。本制备方法简便，适于工为化生产。     

The Relationship of Diastereomer Hydrolysis Kinetics to Shelf-Life Predictions for Cefuroxime Axetil

Cefuroxime axetil, an ester prodrug of cefuroxime, is comprised of a 50:50 mixture of diastereomers A and B. The first-order hydrolysis kinetics of cefuroxime axetil were investigated as a function of pH, temperature, buffers, and ionic strength. Chromatographically identified hydrolysis products were cefuroxime, ²-cefuroxime axetil, and ,-sulfoxides. Buffer catalysis was observed in acetate and phosphate buffers. No significant kinetic effect was observed for ionic strength in the range µ = 0.1-1.0. The pH–rate profiles for hydrolysis of cefuroxime axetil isomeric mixture were obtained at 45, 35, and 25°C. The equation defining the cefuroxime axetil hydrolysis rate constant as a function of pH was k _obs = k _H(a _H) + k _s + k _OH(K _w/a _H), exhibiting maximal stability in the pH range 3.5 to 5.5. The predicted profile at 5°C was in excellent agreement with experimental data in the pH range 3.6 to 5.5. In the pH range 1 to 9, the maximum difference observed for individual hydrolysis constants of isomers was 27%. Shelf-life estimates based on the hydrolysis rate constants for cefuroxime axetil as an isomeric mixture were shown to be equivalent to those based on individual hydrolysis rate constants for isomers A and B.     

旋光法测定注射用头孢呋辛钠的含量

目的　建立一种注射用头孢呋辛钠含量的测定方法。方法　以水为溶剂 ,采用旋光法测定。结果　在 2～ 1 0mg·ml-1的头孢呋辛钠浓度范围内 ,浓度与旋光度值呈良好的线性关系。回归方程 :C =1 4 .74 90α +0 .1 74 2 (r=0 .9999)。平均回收率1 0 0 .4 % ,RSD =1 .36 %。结论　所用方法操作简便、快捷准确 ,适合于该制剂的含量测定     

一般线性模型在药物配伍试验中的应用

目的 建立药物配伍试验数据的分析模型。方法 用一般线性模型(General Linear，GLM)分析文献报道的药物配伍试验数据。结果 方差分析表可以指出那些因素对模型有显著影响；同类亚群表可将因素内平均值无显著差异者归入同一亚群，即同一亚群内的所有平均值相互之间的差弄无显著性(P＞0．05)，而不同亚群之间则有显著性差异(P＜0．05)。结论 该模型可用于药物配伍试验的数据分析。     

注射用头孢呋辛钠的HPCE测定

建立高效毛细管电泳法测定注射用头孢呋辛钠的含量.采用毛细管柱(75 μm×60cm),运行缓冲液为30mmol/L硼砂溶液(pH9.2),检测波长254nm,阿魏酸为内标.头孢呋辛钠在6～30μg/ml浓度范围内线性关系良好(r=0.9996),平均回收率98.9%(RSD=1.82%).     

克拉霉素与头孢呋辛联合应用对肺炎链球菌和金黄色葡萄球菌的体内抗生素后效应

目的：探讨克拉霉素（CLA）与头孢呋辛（CEFU）联合应用对肺炎链球菌和金黄色葡萄球菌的体内抗生素后效应（PAE）。方法：采用琼脂平板倍比稀释法和棋盘法分别测定CLA、CEFU单用及联用时对肺炎链球菌、金黄色葡萄球菌的最小抑菌浓度（MIC）,并计算联合指数（FIC）;建立小鼠股部肺炎链球菌、金黄色葡萄球菌感染模型,并且应用平板菌落计数法测定CLA与CEFU单用及联合应用对肺炎链球菌、金黄色葡萄球菌的体内PAE。结果：CLA、CEFU单用及联用均对肺炎链球菌、金黄色葡萄球菌产生一定的PAE;两者联用的PAE长于单用时的PAE,呈浓度依赖性,联用后对肺炎链球菌体内PAE表现为相加或无关作用,对金黄色葡萄球菌体内PAE表现为无关作用。结论：CLA与CEFU联用能延长CLA、CEFU单用时的PAE。     

Clinical Efficacy and Safety of a Short Regimen of Azithromycin Sequential Therapy vs Standard Cefuroxime Sequential Therapy in the Treatment of Community-Acquired Pneumonia: An International,Randomized, Open-Label Study

Abstract

An international, randomized, open-label, comparative study was undertaken in order to assess the efficacy and safety of azithromycin and cefuroxime, short sequential vs standard sequential therapy, respectively, in the treatment of patients with community-acquired pneumonia (CAP). 180 adult patients were included in the study. 89 patients received azithromycin 500 mg intravenously (i.v.) once daily for 1-4 days followed by azithromycin 500 mg orally once daily for 3 days. 91 patients received cefuroxime 1.5 g i.v. three times daily for 1-4 days followed by cefuroxime axetil 500 mg orally twice daily for 7 days. Clinical efficacy was achieved in 67/82 (81.7%) patients treated with azithromycin, and in 73/89 (82.0%) patients treated with cefuroxime. The mean duration of total (i.v. and oral) therapy was significantly shorter for the azithromycin group than for the cefuroxime group (6.2 days vs 10.1 days). Adverse events were recorded in 38.2% of patients treated with azithromycin, and in 29.7% of patients treated with cefuroxime (p = 0.20). Shorter sequential i.v.-to-oral azithromycin therapy of patients with CAP was as effective as standard sequential i.v.-to-oral cefuroxime therapy.     

头孢呋辛、头孢曲松和头孢噻肟治疗老年社区获得性肺炎的临床评价

目的比较头孢呋辛、头孢曲松和头孢噻肟治疗老年社区获得性肺炎的临床疗效、细菌清除率和安全性特点。方法采用随机、开放、对照研究的方法．78例患者分为头孢曲松组28例．采用头孢曲松注射液，静脉滴注1g·次^-1，1次·d^-1；头孢呋辛组24例，采用头孢呋辛注射液，静脉滴注1．5g·次^-1，3次·d^-1；头孢噻肟组26例，采用头孢噻肟注射液，静脉滴注2g·次^-1，3次·d^-1；疗程10-14d，评价临床疗效和细菌学疗效。结果头孢曲松和头孢噻肟组临床疗效明显优于头孢呋辛组，其差别有显著性（P〈0．05）；头孢曲松组细菌清除率是86．7％（13／15），头孢噻肟组清除率是85．7％，头孢呋辛组是62．5％，头孢曲松组和头孢噻肟组清除率明显高于头孢呋辛组（P〈0．05）。3组均未出现严重的不良反应。结论头孢曲松和头孢噻肟临床疗效及细胞清除率均优于头孢呋辛，是治疗老年社区获得性肺炎较好的药物之一。     

头孢呋辛缓释药膜植入兔眼前房的药效学评价

目的评估植入兔眼前房的可生物降解头孢呋辛缓释药膜的抗感染效用。方法头孢呋辛缓释药膜由头孢呋辛酯(CAE)、高分子聚合物PLGA和聚乙烯吡咯烷酮按一定比例通过溶剂蒸发法制成。50只兔随机分为实验组(n=35):右眼前房植入CAE缓释药膜,对照组(n=15):右眼结膜下注射头孢呋辛125 mg,分别检测对照组注射头孢呋辛后0.5、1、2、6、24 h房水中的药物浓度以及实验组植入CAE药膜后第1、2、3、5、7、14、28天房水和血浆中的药物浓度。实验组植入药膜前后行眼压检测,植入后裂隙灯定期观察前房炎症反应,取角膜组织作扫描电镜和光镜组织学检查,以观察CAE缓释药膜的毒性作用。结果对照组注射头孢呋辛后0.5 h时房水中浓度最高为47 736.18 ng/mL,24 h后浓度极低为10.92 ng/mL;实验组于植入后1周内房水原药浓度>500 ng/mL,第28天时浓度较低为(59.20±39.05)ng/mL,血浆中药物浓度一直处于极低水平(<10 ng/mL)。实验组眼压测量、裂隙灯检查、扫描电镜及组织学检查均无明显异常发现。结论可生物降解头孢呋辛缓释药膜植入兔眼前房后,至少在1周内维持眼内有效药物浓度,而血浆中的药物浓度则极低。兔眼对植入的缓释药膜耐受良好,无明显毒副反应。