乌司他丁复合氧氟沙星对大鼠肠黏膜二胺氧化酶的影响

目的通过检测大鼠肠黏膜中的二胺氧化酶（DAO）,来评价乌司他丁复合氧氟沙星对脓毒症大鼠肠黏膜的保护作用。方法脓毒症大鼠80只,随机均分为四组：空白对照组（C组）、氧氟沙星组（O组）、乌司他丁组（U组）和氧氟沙星加乌司他丁组（O＋U组）,每组再分为12h和24h两组。O组给予氧氟沙星8mg／kg,U组给予乌司他丁15×10^4U／kg,O＋U组则同时给予氧氟沙星8mg/kg和乌司他丁15×10^4U／kg,2次／d,连续2d,C组给予生理盐水4ml／kg作为对照。在治疗后24h和48h取大鼠肠组织检测DAO,观察肠黏膜DAO的变化情况。结果肠组织DAO在治疗组中均明显升高,O组、U组与C组比较差异有统计学意义（P〈0．05）,O＋U组与C组比较差异有显著统计学意义（P〈0．01）,O＋U组与O组、U组比较差异有统计学意义（P〈0．05）,O组与U组之间差异无统计学意义（P〉0．05）。结论乌司他丁能保护肠黏膜的屏障功能,增加肠黏膜中DAO的活性,与抗感染药物合用效果更为明显。     

Influence of dose on the distribution kinetics of ciprofloxacin and ofloxacin in the isolated hindlimb of the rat

The aim of this study was to determine whether the dose influences the distribution kinetics of ciprofloxacin and ofloxacin in muscle- bone- and skin-tissues included in the isolated hindlimb of the rat. Experiments were carried out in the isolated perfused hindlimb of the rat, administering a single dose of 45, 450 or 900 microg of each quinolone as a bolus injection. Outflow perfusate samples were collected for 20 min and drug levels were determined by an HPLC technique. The mean transit time (MTT) and the distribution volume of ciprofloxacin significantly increased with the dose injected (MTT=1.47+/-0.69, 8.74+/-0.27 and 9.52+/-2.95 min for 45, 450 and 900 microg, respectively). A similar situation was observed with ofloxacin, although the increase in these parameters was less pronounced (MTT=3.65+/-0.86, 7.92+/-2.03 and 8.32+/-1.70 min for 45, 450 and 900 microg, respectively). The distribution of ciprofloxacin and ofloxacin in the rat hindlimb appears to be a dose-dependent process, at least for the dose range considered in this study. This might explain the high variability in the distribution coefficients reported for these drugs in literature.     

Single dose levofloxacin prophylaxis for prostate biopsy in patients at low risk

PURPOSE: We determine if a single 500 mg. oral tablet of levofloxacin represents adequate prophylaxis for patients at low risk who undergo transrectal prostate biopsy. MATERIALS AND METHODS: From April 2000 to May 2001 we prospectively evaluated 400 consecutive men who underwent transrectal needle biopsy of the prostate after a single 500 mg. oral dose of levofloxacin. Under an institutional review board approved protocol the drug was issued under a standing order by a clinic nurse 30 to 60 minutes before the procedure. Patients were issued 2 additional daily doses of levofloxacin if they were deemed at increased risk for infectious complications, that is if they had a large prostate more than 75 cc, diabetes mellitus, recent steroid use, severe voiding dysfunction or immune compromise. No patient received a cleansing enema before the procedure. Complications, the number of biopsy cores, prostate size and cancer detection rates were assessed. RESULTS: Only 1 of the 377 patients at low risk in whom biopsy was completed experienced a symptomatic urinary tract infection (0.27%). None of the 23 men at high risk who received additional doses of levofloxacin experienced a complication. Thus, the overall infection rate was 1 of 400 cases (0.25%) in this series. A mean of 7 biopsy cores (range 2 to 16) was obtained per patient and mean prostate volume was 49.75 cc (range 12 to 150). Prostate cancer was present in 93 patients (23%). CONCLUSIONS: A single 500 mg. dose of levofloxacin before transrectal needle biopsy of the prostate is effective and safe in patients at low risk. The administration of prophylaxis by a clinic nurse under a standing order optimizes patient compliance and physician efficiency. In patients at higher risk for infection additional antibiotic administration appears to provide adequate prophylaxis.     

氧氟沙星阴道栓的研制及临床观察

目的：提高氧氟沙星生物利用度,降低其不良反应。方法：以明胶、甘油为基质制备氧氟沙星阴道栓,建立其质量控制,并且对其进行临床观察。结果：本品制备工艺可行,质量控制能够控制本品的质量,临床疗效可靠,无不良反应。结论：本品可用于临床     

氧氟沙星涂膜剂的制备及质量控制

以壳聚糖、甘油为辅料,制备了氧氟沙星涂膜剂,实验表明,该制剂质量控制可行,符合有关要求。采用紫外分光光度法测定其含量,线性范围３．６０－７．２０μｇ／ｍｌ,平均回收率９９．９６％,ＲＳＤ为０．７１％     

氧氟沙星及其片剂的分光光度测定

在二甲亚砜－甲醇介质中氧氟沙星与三价铁离子可形成稳定的橙红色配合物,其最大吸收波长为４２０ｎｍ,可采用分光光度测定氧氟沙星及其片剂的含量,结果准确可靠。     

左旋氧氟沙星类似物的合成及其抗菌抗肿瘤活性研究

目的：设计合成有抗菌抗肿瘤活性的喹诺酮药物。方法和结果：根据推理药物设计原理,设计并合成了16个新型抗菌抗肿瘤喹诺酮类化合物,并研究其构效关系。结论：用9株细菌及4株肿瘤细胞评价了它们的体外抗菌活性(MIC值)及抗肿瘤活性(抑瘤率%)。其中,化合物16～20有较好的抗肿瘤及抗菌活性。     

RP-HPLC同时测定复方替硝唑栓中替硝唑和氧氟沙星的含量

 目的:测定复方替硝唑栓中替硝唑和氧氟沙星的含量。方法:采用RP-HPLC用Phenomenex ODS柱,以乙腈-0.2%三乙胺水溶液(40∶60)用磷酸调节pH为2.70为流动相,氯霉素为内标,检测波长为296nm。结果:替硝唑和氧氟沙星分别在20～90μg·ml^-1(r=0.9999,n=7),4～20μg·ml^-1(r=0.9998,n=7),浓度范围内呈线性关系。替硝唑和氧氟沙星平均回收率(n=4)分别为101.04%,99.20%;RSD分别为1.7%,1.5%。结论:此方法简便、快速、准确。     

Ofloxacin versus co-trimoxazole in the treatment of typhoid fever in children

Ofloxacin has been successfully used in the treatment of typhoid fever and Salmonella infections of adults for many years. However, it has rarely been tried for the typhoid fever of children. In the present study, the therapeutic efficacy of ofloxacin in the treatment of typhoid fever in children was compared to that of co-trimoxazole. Out of 41 patients with bacteriologically documented typhoid fever, those with co-trimoxazole-resistant strains received 20 mg/kg ofloxacin twice daily for 10 days, and those with co-trimoxazole-susceptible bacteria were given 60 mg/kg co-trimoxazole twice daily for 10 days. Both groups were compared according to the clinical variables (apyrexia, resolution of gastrointestinal, central nervous system reactions and articular symptoms) and the time when cultures became negative. All patients in both groups were cured without relapse. Apyrexia, resolution of gastrointestinal, central nervous system reactions and articular symptoms were obtained in a significantly shorter time with ofloxacin than with co-trimoxazole (P < 0.05). The interval between onset of therapy and the time when cultures became negative was significantly shorter in the ofloxacin group than in the co-trimoxazole group (P = 0.005). Ofloxacin seems to be a good alternative in the treatment of typhoid fever caused by co-trimoxazole resistant salmonellae in children aged less than 16 years. It is well tolerated by the patients and it causes no side effects with short-term usage.     

活性肠球菌M74与氧氟沙星治疗急性感染性腹泻的比较

目的：研究微生态制剂活性肠球菌Ｍ７４与氧氟沙星治疗急性感染性腹泻效果的比较。方法：６７例急性感染性腹泻病人（男性４７例,女性２０例;年龄３９±４ａ）随机分为２组：Ｍ７４组３６例,服活性肠球菌制剂０．５ｇｔｉｄ;氧氟沙星组３１例,服用氧氟沙星０．２ｇ,ｔｉｄ。疗程均７ｄ。结果：Ｍ７４组显效率８１％,有效率１９％;氧氟沙星组显效率和有效率分别是９０％和１０％。２组疗效无统计学差异（Ｐ＞０．０５）。结论：活性肠球菌Ｍ７４制剂治疗急性感染性腹泻效果良好,无严重并发症和不良反应。