加替沙星治疗社区获得性下呼吸道感染

目的评价加替沙星治疗社区获得性下呼吸道感染的疗效和安全性。方法前瞻性、非对照、开放性Ⅳ期药物临床试验。加替沙星400 mg/d口服,疗程7~14 d。结果2004年2月—2005年2月,共入选36例下呼吸道感染患者,其中失访2例,中途停药2例,剔除1例。安全性可评价病例34例;治疗效果可评价病例31例,其中男7例,女24例,年龄23~69岁,平均44.8岁;肺炎18例,慢性支气管炎急性发作13例;治愈28例,显效1例,进步2例,有效率93.5%。筛选痰培养细菌15株,阳性率44%,治疗结束全部清除,清除率100%。4例出现不良事件,表现为输液局部发痒、口服药物后出现呼吸困难、胃肠道反应和失眠,不良反应发生率11.8%。结论加替沙星口服每日1次给药,治疗社区获得性下呼吸道感染疗效确凿,安全性高。     

Effects of gatifloxacin and levofloxacin on rates of hypoglycemia and hyperglycemia among elderly hospitalized patients

STUDY OBJECTIVES: To compare rates of hypoglycemia and hyperglycemia among elderly hospitalized patients with normal blood glucose concentrations at baseline who were receiving either gatifloxacin or levofloxacin, and to determine if appropriateness of their doses, according to their package inserts, was associated with hypoglycemia or hyperglycemia. DESIGN: Retrospective cohort study. SETTING: Integrated Veterans Administration (VA) health care system. PATIENTS: Nine hundred thirty-seven elderly (>or= 65 yrs) patients with documented blood glucose levels of 65-140 mg/dl before receiving a fluoroquinolone. MEASUREMENTS AND MAIN RESULTS: Between January 2003 and April 2004, 405 patients receiving levofloxacin met study criteria. In April 2004, gatifloxacin was substituted for levofloxacin on the formulary of this VA system. Thus, between April 2004 and December 2004, 532 patients received gatifloxacin. All blood glucose concentrations during hospitalization that were measured during fluoroquinolone therapy or within 72 hours of completion of therapy were reviewed. Demographic characteristics, comorbidities, insulin and oral hypoglycemic therapies, disease severity, blood glucose levels, and outcomes were recorded and compared between groups. The two groups were similar at baseline for all characteristics examined except previous hospitalization. In the logistic regression, gatifloxacin was independently associated with both hypoglycemia (adjusted odds ratio [AOR] 2.5, 95% confidence interval [CI] 1.2-5.7, p=0.04) and hyperglycemia (AOR 2.4, 95% CI 1.5-3.6, p<0.001). Improper dosage adjustment based on renal function was not associated with higher rates of hypoglycemia and hyperglycemia for either drug. Of the 532 patients receiving gatifloxacin, 465 (87.4%) received appropriate doses, yet gatifloxacin was associated with higher rates of hypoglycemia and hyperglycemia compared with patients receiving levofloxacin. CONCLUSIONS: Higher rates of both hypoglycemia and hyperglycemia were noted among elderly hospitalized patients who received gatifloxacin compared with those receiving levofloxacin, irrespective of dosing.     

加替沙星聚乳酸纳米粒的包封率测定

目的建立加替沙星聚乳酸纳米粒的包封率测定方法。方法采用葡聚糖凝胶柱层析法,以水为洗脱剂,以l mL.min·1的流速洗脱,采用反相高效液相色谱法测定药物含量,计算包封率。色谱柱为C18柱（150 mm×4.6 mm,5μm）,流动相为0.02 mol.L·1枸橼酸溶液（内含0.6%三乙胺）-甲醇（60∶40）,检测波长为290 nm,流速为1.0 mL.min-1,进样量20μL。结果加替沙星在2.051-60.14μg.mL·1内线性关系良好（r=0.999 9）。平均柱回收率为98.8%,RSD=0.71%;测得3批纳米粒的平均包封率为82.1%,RSD为2.2%。结论建立的方法可用于加替沙星聚乳酸纳米粒的包封率测定。     

加替沙星分散片生物等效性研究

目的研究加替沙星分散片在健康志愿者体内的药物动力学特征及相对生物利用度。方法采用双交叉试验设计自身对照试验法,将20名健康志愿者随机分成2组,单次空服加替沙星分散片（受试制剂）或加替沙星片（参比制剂）400mg,采用高效液相色谱法测定其血药浓度。结果试验制剂和参比制剂的达峰时间（Tmax）分别为（1.813±0.949）h和（1.413±0.718）h,峰浓度（Cmax）分别为（3958.814±598.317）ng/mL和（4098.321±838.365）ng/mL,0-t药时曲线下面积（AUC0-t）分别为（42330.694±5478.929）ng·h/mL和（42927.761±5237.192）ng·h/mL。受试制剂的相对生物利用度为（98.9±8.9）%。结论受试制剂加替沙星分散片与参比制剂生物等效。     

加替沙星致血糖异常及其合理应用

目的减少加替沙星致血糖代谢紊乱的不良反应的发生,促进其合理应用。方法检索近年来国内外医药学期刊报道的加替沙星引起血糖代谢紊乱的案例,结合国外对加替沙星的评价、加替沙星致血糖代谢紊乱的机理,进行分析、总结,提出加替沙星合理应用的建议。结果与结论应加强对加替沙星引起血糖代谢紊乱的重视,临床使用中密切监测血糖,合理应用。     

盐酸加替沙星对兔体内茶碱药动学的影响

目的:研究盐酸加替沙星对家兔体内茶碱药动学的影响.方法:6只家兔于第1,6天单次静脉注射氨茶碱10 mg·kg-1,第2～6天灌服盐酸加替沙星20 mg·kg-1,qd.用氨茶碱后各时间点采静脉血,测定茶碱血清浓度,数据用3P97药动学软件处理,计算参数,并用t检验进行统计处理.兔血清氨茶碱浓度以HPLC法测定.结果:氨茶碱在兔体内的药动学过程呈二室模型,t1/2分别为(0.21±0.04)h和(0.33±0.21 )h;t1/2β分别为(4.4±0.8)h和(4.8±1.1)h ;AUC分别为(72.9±10.6)g·h·mL-1和(80.7±20.3)g·h·mL-1;CL分别为(139.7±21.7)mL··h-1·kg-1和(131.4±36.3)mL·h-1·kg-1;V(c)分别为(495.3±26.55)mL·kg-1和(462.86±34.71)mL·kg-1.结论:所有参数经双侧t检验,差异无显著性(P>0.05),合用加替沙星对家兔体内氨茶碱药动学无影响.     

喹诺酮类抗菌药的研究进展

综述了近年喹诺酮类抗菌药的抗菌活性和临床应用进展，包括近年上市的第四代喹诺酮类抗菌药莫西沙星、加替沙星、吉米沙星和巴洛沙星，与结构经进一步深入修饰的喹诺酮类抗菌药如帕珠沙星和鲁利沙星，还概述了正在研发中的新药。     

加替沙星氯化钠注射液治疗细菌性感染的临床分析

目的：评价加替沙星氯化钠注射液治疗细菌性感染的临床疗效和安全性。方法：以加替沙星氯化钠注射液为试验药，左氧氟沙星氯化钠注射液为对照药，用随机双盲对照的试验方法，治疗细菌性感染，加替沙星和左氧氟沙星剂量均为200mg／次，2次／d，静脉滴注，疗程5～10d。结果：加替沙星总有效率和痊愈率分别为95．1％和85．4％，细菌清除率为86．4％；左氧氟沙星总有效率和痊愈率分别为91．1％和80．2％，细菌清除率为82．2％。二者不良反应发生率分别为11．65％和12．87％，两组比较均无显著差异（P〉0．05）。结论：加替沙星氯化钠注射液治疗细菌性感染疗效确切，患者耐受性良好。     

复方加替沙星阴道泡腾片的制备及毒理学研究

目的:研究复方加替沙星阴道泡腾片(CGVE)的制备及其对豚鼠的毒性作用.方法:研制了CGVE.对豚鼠分别采用单次及多次阴道给药,进行急性毒性和刺激性试验,观察其全身状态有无异常及阴道组织有无红斑和水肿等.结果:豚鼠给药前、后全身状态无明显变化,刺激反应评分为0分.结论:CGVE对豚鼠阴道给药未见明显毒性反应.