Penetration of pefloxacin and its desmethyl metabolite into the uroepithelium after a 800-MG single oral dose in human patients

Penetration of pefloxacin into the uroepithelium was studied in 20 patients (10 men and 10 women) receiving a single oral dose of 800 mg. Samples of serum, urine, and uroepithelium were taken 1.8 h (mean) after the dose. Pefloxacin and its active metabolite, norfloxacin, were assayed by liquid chromatography, and the microbiologically active compounds were quantified by a microbiological assay. Both procedures were correlated (r>0.7); nevertheless, slight differences detected in concentrations depended on the levels of norfloxacin achieved in the biological samples. The serum and tissue concentrations were higher than the concentration of bactericide (4 g·ml^–1), except in one case. The uroepithelium concentration of pefloxacin was proportional to the serum concentration (r=0.79). The urinary concentrations ranged from 1.2 g·ml^–1 to 82.4 g·ml^–1. The mean norfloxacin/pefloxacin ratios were 3% in serum, 8% in uroepithelium, and 44% in urine. The mean uroepithelium/serum concentration ratios were 1 for pefloxacin and 2.3 for norfloxacin. This result shows that, at a time close to that of the maximum concentration, there is good penetration of pefloxacin and norfloxacin into the uroepithelium.     

复方奥硝唑甲磺酸培氟沙星缓释牙栓对大鼠龈沟液中天冬氨酸转氨酶水平的影响

目的:了解复方奥硝唑甲磺酸培氟沙星缓释牙栓对大鼠牙周组织及其龈沟液中天冬氨酸转氨酶水平的影响,以观察该药对大鼠牙周炎的治疗效果.方法:将90只SD大鼠随机分成A、B、C、D、E 5组,其中B、C、D、E 4组用细丝线结扎实验牙的牙颈部并给予高糖饮食,形成牙周炎动物模型,E组使用复方奥硝唑甲磺酸培氟沙星缓释牙栓治疗大鼠实验性牙周炎模型,而D组使用甲硝唑棒治疗.比较B、C、D、E 4组的各项牙周临床指数及其龈沟液中天冬氨酸转氨酶水平变化,评价疗效.结果:E组和D组用药后,各项指标与用药前相比均明显改善,经统计学处理差异非常显著(P＜0.01).结论:复方奥硝唑甲磺酸培氟沙星缓释牙栓对大鼠牙周炎有良好的治疗作用;龈沟液中天冬氨酸转氨酶水平的变化可作为判断大鼠牙周炎近期疗效的客观指标.     

培氟沙星与左氧氟沙星治疗下呼吸道感染的疗效评价

目的比较培氟沙星与左氧氟沙星治疗下呼吸道感染的疗效、不良反应.方法117例下呼吸道感染患者分成2组:培氟沙星治疗组60例,0.4g,2次/d,静点;左氧氟沙星治疗组57例,0.3g,2次/d,静点,疗程均为7～14d.结果培氟沙星和左氧氟沙星治疗下呼吸道感染的有效率分别为90.0%和87.7%,痊愈率分别为76.8%和77.2%,均无显著性差异.结论培氟沙星和左氧氟沙星治疗下呼吸道感染临床疗效和不良反应相仿.     

甲磺酸培氟沙星凝胶的研制与质量控制

目的研制甲磺酸培氟沙星凝胶。方法用CMC-Na作凝胶基质制备甲磺酸培氟沙星凝胶,采用紫外分光光度法直接进行含量测定,检测波长277 nm,线性范围2~14μg/mL,r=0.999 9,建立性状、鉴别、酸碱度、含量测定等质控方法,并对制剂进行质量控制。结果含量测定回收率为99.54%~100.41%,RSD=1.98%(n=6),pH值6.0~8.0,凝胶稳定无变化。结论该凝胶制备工艺简单,稳定性好,质量可控,适于临床应用。     

HPLC法测定甲磺酸培氟沙星注射剂中有关物质及含量

目的：建立科学合理的高效液相色谱法(HPLC)测定甲磺酸培氟沙星注射剂的有关物质及含量。方法：用方法Ⅰ和方法Ⅱ测定所有样品,综合考虑分离效果、稳定性、含量测定结果、有在物质测定结果等几方面。选择方法Ⅰ为转正标准的HPLC条件,色谱条件为C_(18)色谱柱,以0.04mol·L~(-1)磷酸二氢钾-乙腈-0.05mol·L~(-1)四丁基溴化铵(80∶9∶8)(磷酸调节pH为2.5)为流动相；流速为1.0ml·min~(-1)；检测波长277nm；进样量为20μl。结果：用方法Ⅰ和方法Ⅱ测定所有样品的有关物质,各杂质分离良好,最大杂质含量均未过1.0%,总杂质含量均未过1.0%；在0.072～287μg·ml~(-1)范围内,线性关系良好,稳定性好,注射液粉针和注射液含量测定的回收率分别为100.6%和99.6%,RSD分别为0.9%和0.8%。结论：方法Ⅰ灵敏度高,线性范围宽,回收率高,可作为转正标准的HPLC方法。     

甲磺酸培氟沙星凝胶剂的研制

目的:研究甲磷酸培氟沙星凝胶剂的处方、制备工艺、质量控制及稳定性。方法:采用CMC-Na为基质制成凝胶剂,用双波长紫外分光光度法测定甲磺酸培氟沙星的含量。结果:平均回收率为100.0％,RSD为0.2％,稳定性好,临床疗效较好。结论:该制剂适合于临床应用。     

Quinolones and colonization resistance in human volunteers

The suppression of alimentary canal flora by the three quinolones nalidixic acid, ciprofloxacin and pefloxacin was investigated in fifteen volunteers. They received the three quinolone compounds in tablet form both uncoated and colon-coated.Escherichia coli suppression was poor under nalidixic acid, but complete under ciprofloxacin and pefloxacin for both administration forms. The indigenous anaerobic flora contributing to the control of aerobicStreptococcus faecalis andCandida albicans in the intestines ('colonization resistance') was not affected by nalidixic acid and pefloxacin, and only slightly by ciprofloxacin. Out of the three quinolone compounds, only colon-coated pefloxacin was associated with a considerable absorption rate at colonie level. Using these criteria of successfulEscherichia coli clearing from the intestinal canal - left the indigenous flora more or less intact (in a 'selective' way) - and a good absorption rate, pefloxacin is found to be superior to ciprofloxacin and nalidixic acid. These results suggest that a colon-coated tablet with a low dose of pefloxacin is a promising administration form in the therapy of recurrent urinary tract infections and diarrhoeal diseases and in the prevention of gut colonization in immunocompromised hosts.     

甲磺酸培氟沙星人体药代动力学研究

目的 研究甲磺酸培氟沙星人体内药代动力学,为该药的临床评价提供依据.方法10名健康志愿者单剂量口服400mg甲磺酸培氟沙星后,采用HPLC法测定血药浓度,并拟合药代动力学参数.结果 8名受试者药时曲线为二室模型,2名为一室模型,平均达峰时间为1.19±0.48h,消除半衰期为11.61±2.53h,药时曲线下面积51.82±17.10μg·h·ml~(-1),吸收速率常数个体差异明显(1.69～923h~(-1)).结论 甲磷酸培氟沙星吸收迅速,半衰期长,体内分布广,有利于深部组织感染的治疗.     

三种国产氟喹诺酮药物体外抗菌作用

测试了国产氟哌酸、氟啶酸和甲氟哌酸等三种氟喹诺酮类药物(FQs)对8种共80株细菌的体外抗菌活性(MIC)及其对大肠杆菌2280杀菌作用的量效关系,结果表明,主种药物对大肠杆菌,阴沟扦菌、志贺氏菌属、沙门菌属、克雷白氏肺炎杆菌和金萄菌具有强大的抗菌活性(MIC90多≤1ug/ml)。对绿脓杆菌的作用较弱(MIC90为2—4ug/ml4株变形杆菌对三种FQS药物也较敏感(MIC为0、25—2ug/ml),但1株耐利福平杆菌的MIC为9ug/ml,提示利福平与FQS药物之间可能存在交叉耐药性。三种药物对大肠杆菌2280的杀菌量效关系呈双相变化,最强杀菌浓度为1—2ug/ml。本文对其临床意义进行了讨论。     

甲磺酸培氟沙星的示波极谱滴定法研究

对甲磺酸培氟沙星含量的示波极谱滴定法测定进行了研究。在 pH5 2的HCl NaAc缓冲溶液中 ,四苯硼钠 (Na TPB)与甲磺酸培氟沙星作用可生成 1∶1定量沉淀 ,过滤弃去初滤液 ,用硫酸亚铊标准溶液滴定续滤液中过量的Na TPB ,通过示波极谱图 (dE/dt=f(E)曲线 )上TPB的切口消失指示滴定终点。本法操作简单、快速 ,终点直观 ,应用于多批原料药样品的测定 ,获得了满意的结果 ,其回收率为 99 4 6 %～ 1 0 0 4 % ,相对误差 <± 0 .6 % ,与部颁标准非水滴定法测得的结果基本一致。