替硝唑葡萄糖注射液的稳定性研究

采用反相ＨＰＬＣ法测定替硝唑葡萄糖注射液中替硝唑的含量，用加温加速实验研究该制剂的热稳定动力学。结果表明，替硝唑的热降解反应为一级动力学过程，在５０、６５、８０、９５℃时的降解速度常数分别为５．５８×１０－４、２．６６×１０－３、８．１０×１０－３、２．８２×１０－２ｄ－１，为８．３年，半衰期为３９．５年。     

A systematic review on the treatment of giardiasis

To assess the efficacy of treatment of parasitological excretion of cysts and trophozoites and symptoms of patients with giardiasis, a systematic review of published randomized clinicial trials was conducted through extensive searches in Medline, Embase and Current Contents from 1966 till 1996 as well as manual reviews of 28 journals. The methodological quality of all trials was assessed by guidelines of the Cochrane Collaboration. Thirty‐one trials were included, only one of which had no serious methodological flaws. The mean score of parasitological examination was 4.8 out of a possible 15. There was a considerable effect in cure rate of treatment versus placebo (odds 9.3, 95%CI 4.69–18.4), but all 3 trials in this comparison had serious flaws. Metronidazole treatment over more than 3 days seems to achieve a better parasitological cure rate than other long treatment courses (pooled odds 2.6, 95% 1.7–3.8), but trials are clinically and statistically heterogeneous. Single‐dose therapy is as effective as longer treatment courses (pooled odds 0.67, 95% 0.31–1.44). Within the single‐dose regimens tinidazole (2 g) reaches a higher parasitological cure rate than other short therapies (pooled odds 55, 95% CI 3.7–8.3) with relatively few side‐effects. Placebo‐controlled trials with parasitological and clincial outcomes are needed.     

替硝唑的合成

以甲硝唑为原料，经过氯化、硫醚化和气化反应合成了替硝唑，经元素分析和１Ｈ－ＮＭＲ证实了结构。     

高效液相色谱法测定替硝唑栓的含量

建立反相高效液相色谱法测定替硝唑栓中替硝唑的含量。采用lichrosorbC1 8色谱柱 (5μm ,4 6mm×2 0 0mm) ,甲醇 -水 (2 7∶73)为流动相 ,流速为 0 9ml·min-1 ,检测波长为 31 7nm。替硝唑在 1 6～ 48μg·m1 -1 范围内线性关系良好 ,r=0 9999,平均回收率 99 6 % ,RSD =1 1 8%。该法简便、快速、专属性好 ,结果准确、可靠     

γ-闪烁扫描法确定替硝唑结肠释放片人体内释药部位的研究

 目的确定替硝唑结肠释放片在人体内释药部位。方法以氧化钐为标记物，利用γ-闪烁扫描技术对替硝唑结肠释放片在人体内的释药部位进行跟踪监测。结果替硝唑结肠释放片在2名志愿者胃肠道内的崩解部位均为升结肠,药片崩解时间为7～8 h。结论替硝唑结肠释放片在人体胃肠道内具有结肠定位释药效果,达到了预期的设计目的。     

替硝唑结肠给药系统的研制

依据时控型结肠给药系统原理，以替硝唑为模型药物．利用于压包衣和薄膜包衣双层包衣的方法制备了结肠给药系统，并对影响药物释放的因素(如EC粒度，HPMC粘度，时控层厚度，片刑硬度等)、肠衣层性能和药物释放稳定性等进行了考查。结果表明，HPMC粘度增加使药物释放滞后时间延长,但高粘度HPMC会导致药物释放无明显突跃点；包芯片硬度40～60N、片重0．26～0．28g的片剂药物释放较稳定。加速试验(3个月)结果表明,药物释放稳定性良好。     

甲硝唑与替硝唑治疗滴虫性阴道炎的成本-效果分析

目的评价甲硝唑与替硝唑两种药品治疗滴虫性阴道炎的疗效、不良反应及成本-效果[1,2].方法将60例滴虫性阴道炎患者随机分成2组,分别口服甲硝唑(治疗组)和替硝唑(对照组),对甲硝唑与替硝唑治疗滴虫性阴道炎的疗效、不良反应并运用药物经济学成本效果分析法及成本进行评价.结果甲硝唑与替硝唑治疗滴虫性阴道炎的总有效率基本相同,分别为93.33%和96.67%(P＞0.05);不良反应发生率分别为30.00%和6.67%(P＜0.05);成本-效果比分别为0.0557和0.2772(P＜0.01).结论甲硝唑与替硝唑均能有效治疗滴虫性阴道炎.不良反应发生率甲硝唑与替硝唑有显著性差异.成本-效果比甲硝唑优于替硝唑.     

复方左氧氟沙星滴鼻液的制备和临床应用

目的：建立复方左氧氟沙星滴鼻液的制备和质控方法，并观察临床疗效。方法：以盐酸左氧氟沙星和替硝唑为主药制成滴鼻剂，采用紫外分光光度法测定主药含量，留样考察其稳定性，并临床应用于鼻炎、鼻窦炎共239例，观察疗效。结果：本制剂中两主药平均回收率分别为98．24％和98．88％，RSD为1．2％和0．6％(n=6)，治疗鼻炎、鼻窦炎患者，总有效率为89．96％。结论：该滴鼻液制备工艺简单，性质稳定，疗效明显，含量测定方法快速准确，适于医院制备和应用。     

HPLC测定人体血浆中替硝唑浓度

目的:建立替硝唑血药浓度测定方法,用于复方替硝唑片血药浓度研究。方法:采用高效液相色谱法。色谱柱为C18柱,流动相为12%乙腈水溶液(pH7.0),检测波长318nm。结果:样品组分在0.2～20μg.ml-1线性良好(r=0.9998),最低血浆药物检测浓度为0.02μg.ml-1。回收率为94.4%～98.3%,日内及日间RSD<5%。结论:本法简便、迅速、灵敏、准确,适合于临床药学研究需要。