氧氟沙星胶囊生物利用度和药物动力学的研究

目的 :考察氧氟沙星胶囊的人体相对生物利用度及药代动力学 ,生物等效性 ,从而评价其临床疗效。方法 :泰利必妥片为对照品 ,选 10名志愿受试者 ,随机分成 2组 ,自身交叉服用 ,以高效液相色谱法检测血药、尿药浓度及生物利用度 ,进而对主要动力学参数进行分析。结果 :交叉口服氧氟沙星胶囊和泰利必妥片后 2组药物动力学特性接近 ,药动学参数基本一致 ,试验药品的相对生物利用度平均为 (10 6 2 3± 5 3 6) %。结论 :氧氟沙星胶囊和泰利必妥片生物等效。     

基于多药耐药相关蛋白2(Abcc2/Mrp2)在大鼠肾脏表达性别差异的氧氟沙星药动学变化(英文)

本研究旨在探讨基于多药耐药相关蛋白2(Abcc2/Mrp2)在大鼠肾脏表达性别差异的氧氟沙星的药代动力学变化。采用高效液相色谱法(HPLC)分别测定经尾静脉注射给予氧氟沙星(30 mg.kg1)后大鼠血浆和尿液中氧氟沙星的浓度;通过免疫组化法和流式细胞术分别对雄性和雌性大鼠肾脏Mrp2的表达进行定性和定量分析。结果表明在雄性大鼠体内,氧氟沙星药时曲线下面积(AUC)明显小于雌性大鼠,而尿排总量明显大于雌性大鼠;Mrp2在雄性大鼠肾脏中的表达显著高于雌性大鼠。因此,氧氟沙星药动学性别差异可能是由Mrp2在雄性和雌性大鼠肾脏中的表达差异所引起的。     

氧氟沙星片工艺的研究

目的　筛选氧氟沙星片最佳处方和制备工艺。方法　采用正交试验法考察羧甲基淀粉钠 (CMS Na)、十二烷基硫酸钠(SDS)的用量和制片压力对氧氟沙星片的质量影响。结果　制备的氧氟沙星片各项指标符合规定 ,5min溶出度 >80 %。结论　本法处方合理 ,工艺简单 ,适用于工业化生产     

A randomized prospective comparison of oral versus intraperitoneal ofloxacin as the primary treatment of CAPD peritonitis

Summary: Oral ofloxacin has been successfully used in our centres for the primary treatment of peritonitis complicating continous ambulatory peritoneal dialysis (CAPD). In view of the progressive rise in the resistance rate to ofloxacin among peritoneal bacterial isolates, a study was conducted to determine if oral ofloxacin remains a viable first line treatment for CAPD peritonitis in our centres and if the result can be improved by changing from an oral to an intraperitoneal (i.p.) route. In patients on three 2 L daily CAPD exchanges, ofloxacin given at the i.p. dosage of 200 mg loading followed by 25 mg/L of peritoneal dialysate achieved overnight trough peritoneal levels which are at least four times the minimal 90% inhibitory concentration (MIC90) of most bacterial pathogens without significant accumulation in the systemic circulation. This i.p. dosage was therefore chosen for the clinical study and the result was compared to that using ofloxacin given in the oral dosage of 400 mg loading followed by 300 mg once daily as maintenance. of all the recruited episodes, 35 were eligible for analysis. the overall primary cure rate including primary failures and relapses was 55.6% (10/18) in the oral treatment group and 70.6% (12/17) in the i.p. treatment group. the corresponding figures for gram positive bacterial (g +) infections were 36.4% and 50%, for gram negative bacterial (g -) infections were 66.7 and 80% and for culture negative infections were 75 and 80%. In culture positive cases, all treatment failures were due to resistant infections which were observed in 42.3% of all bacterial isolates, 47.1% of g + isolates and 33.3% of g - isolates. Due to the high background level of bacterial resistance among our CAPD population, ofloxacin monotherapy given either by the oral or the i.p. route can no longer be recommended for the primary treatment of CAPD peritonitis.     

用NONMEM法估算氧氟沙星片的相对生物利用度(英文)

用NONMEM法估算国产和日本进口的氧氟沙星片的相对生物利用度(F),在健康志愿者中两种片剂的生物利用度无显著性差异,NONMEM法(97.3±5.0％)与传统方法(98.2±3.6％)得到一致的结论,用NONMEM法分析在临床病人中收集的零散数据,得到呼吸道和泌尿道感染病入国产氧氟沙星片的相对生物利用度为91.7±8.0％.     

The measurement of ofloxacin in hair as an index of exposure

Summary Several strands of hair were collected from each of patients who had been taking ofloxacin against bacterial infections some time in the past. In 10 out of total 14 subjects studied the drug was detected only in the hair portions corresponding to the administration period with the assumption of the hair growth rate of about 1 cm/month. Even in a subject who had received 300 mg/day of ofloxacin only for two days the drug could be detected in the corresponding portion. In 3 subjects the drug was detected in some other portion(s) than the corresponding ones. This might be due to the uncertainty of having used the drug on the other occasion. Only in one subject the dosage history could not be deduced from the drug distribution along hair length.In 3 subjects, who had taken the drug within 1 month, hair samples were collected every month for 3 or 4 consecutive months. The front of drug appearance in hair was clearly shown to move outwards along hair shaft every month at a pace of 1–1.5 cm/month.These results suggest that ofloxacin is excreted into human scalp hair, captured there and moves outwards along the hair shaft at its own growth rate. This leads to the concept that the distribution of ofloxacin along hair length can be used for knowing the individual exposure or non-exposure to the drug, and even for knowing hair growth rate when the innoculation(s) of the drug is strictly supervised and recorded.     

氧氟沙星治疗下呼吸道感染

下呼吸道感染37例(男16例,女21例;年龄44±13a)采用氧氟沙星治疗,剂量为200mg,tid,po,疗程为11±4d。37例患者经痰培养者26例,经纤维支气管镜刷取标本培养者11例。分离出致病菌19种,54株,其中革兰阴性杆菌11种26株(48％)。结果:治愈22例,有效10例(总有效率86％),病原菌清除率为80％,不良反应轻微。     

重庆市肺结核患者异烟肼与丙硫异烟胺耐药状况分析

目的 了解重庆市结核分枝杆菌异烟肼(INH)、丙硫异烟胺(Pto)及其交叉耐药情况,为重庆市耐药结核病的防控提供参考。方法 根据重庆市2015-2017年39个区县培养阳性菌株的传统药敏试验结果,收集288例INH或Pto任意耐药菌株,分析其耐药情况。结果 288例菌株中,INH耐药菌株285例,Pto耐药菌株19例,交叉耐药菌株16例。复治患者INH 或Pto的耐药率均高于初治患者,年龄15~44岁患者Pto耐药率显著高于INH组。Pto耐药组Pre-XDR-TB及Ofx耐药率显著高于INH组。交叉耐药菌株中,年龄15~44岁组交叉耐药率较高,且 MDR-TB发生率高达93.8%。结论 重庆市INH与Pto耐药情况已较为严重,医生在为INH耐药患者制定化疗方案时应根据药敏结果,应谨慎选择Pto进行替代治疗,以避免更多耐药的发生。     

浙江省杭州市结核分枝杆菌氧氟沙星耐药研究

目的 了解杭州市结核分枝杆菌对氧氟沙星的耐药情况及耐药菌株gyrA基因的突变特点。 方法 收集2010年4月至2012年6月杭州市各结核病定点医院分离培养的临床菌株,进行一线抗结核药物、氧氟沙星和卡那霉素敏感性检测,测定氧氟沙星耐药菌株gyrA基因的喹诺酮类药物耐药决定区(QRDR)序列。 结果 收集的1242株临床菌株中, 67株(5.39%)对氧氟沙星耐药,其中32株(47.76%)对氧氟沙星单耐药,23株为耐多药结核病(MDR-TB)菌株,占MDR-TB菌株的22.77%。选取55株耐药株进行gyrA序列分析,其中33株(60%)携带gyrA基因突变位点。突变位点包括第90和94位密码子,突变率分别为27.27%和32.73%。 结论 杭州市氧氟沙星单耐药患者的比例较高,MDR-TB患者中氧氟沙星耐药情况较严重,需加强结核患者的早期发现和用药管理。     

国产和进口氧氟沙星治疗伤寒和副伤寒的疗效比较

伤寒、副伤寒共54例,以国产氧氟沙星治疗26例(男性13例,女性13例;年龄26±s 7a),用进口氧氟沙星治疗28例(男性19例,女性9例;年龄28±9a)。剂量均为300mg, po, bid。疗程7d。结果:2组临床有效率均为100％,细菌阴转率分别为96％和100％。随访2mo均未见复发病例。提示2药治疗伤寒、副伤寒的疗效相同(P>0.05)。