阿奇霉素分散片与其普通片溶出度比较考察

目的　考察阿奇霉素分散片的溶出度。方法　以硫酸溶液 (75→ 10 0 )为显色剂 ,用分光光度法测定其溶出度 ,并与阿奇霉素普通片比较。结果　测定 3批样品的累积溶出百分率在 10min内可达 90 % ,但批与批之间存在差异。结论　阿奇霉素分散片的溶出度比普通片快。     

阿奇霉素分散片的制备与溶出度测定

目的 研究阿奇霉素分散片的制备工艺. 方法 以阿奇霉素为主药,羟丙基纤维素和交联羧甲纤维素钠为辅料,制成阿奇霉素分散片,并采用紫外分光光度法测定其溶出度. 结果 通过对阿奇霉素分散片含量测定、线性关系、稳定性、回收率、重现性、溶出限度、溶出度均一性实验的研究,建立了可控制其质量的溶出度测定方法 . 结论 所研发的阿奇霉素分散片制备工艺简单,质量稳定,分散性能良好,检测方法 快速便捷.     

阿奇霉素分散片的制备及质量研究

目的 制备阿奇霉素分散片。方法 以崩解时间为指标比较不同崩解剂的作用，以正交试验设计确定最佳处方，并与普通片进行了体外溶出度的比较。结果 崩解剂以交联聚乙烯吡咯烷酮效果最优，最佳处方崩解时间为92．1s，溶出速度远大于普通片，其崩解时间、分散均匀度达到中国药典(2000年版二部)要求，稳定性试验表明制剂质量稳定。结论 研制的阿奇霉素分散片溶出迅速。     

阿奇霉素分散片的制备及质量研究

目的　制备阿奇霉素分散片。方法　以崩解时间为指标比较不同崩解剂的作用 ,以正交试验设计确定最佳处方 ,并与普通片进行了体外溶出度的比较。结果　崩解剂以交联聚乙烯吡咯烷酮效果最优 ,最佳处方崩解时间为 92 1s,溶出速度远大于普通片 ,其崩解时间、分散均匀度达到中国药典 (2 0 0 0年版二部 )要求 ,稳定性试验表明制剂质量稳定。结论　研制的阿奇霉素分散片溶出迅速     

阿奇霉素分散片的稳定性研究

目的对阿奇霉素分散片进行质量控制和确定其有效期。方法以加速试验和长期试验的阿奇霉素分散片为研究对象,观察其外观性状并测定其崩解时限,通过薄层方法检查其有关物质,用硫酸显色测定其溶出度,微生物效价测定法检测其含量。结果各批阿奇霉素分散片的性状、崩解时限、有关物质、溶出度及含量均符合规定。结论阿奇霉素分散片在加速试验和长期试验条件下稳定,因长期试验12个月内其含量无明显变化,可初步确定其有效期为2年。     

阿奇霉素片（分散片）的溶出度测定方法研究

目的对阿奇霉素片（分散片）溶出度检查方法进行改进和研究，使溶出度检查的方法更为简便，结果更为合理。方法分别以0．1mol·L^-1盐酸溶液与pH6．0的磷酸盐缓冲液为溶出介质，采用不同浓度的硫酸作为显色剂，对同批样品的溶出度检查结果进行比较：结果以两种溶液为溶出介质的溶出度检查结果无明显差异，不同浓度的硫酸对测定结果有显著影响。结论实验表明以0．1mol·L^-1盐酸溶液为溶出介质，显色硫酸的浓度确定为（90→100），能够符合片剂在胃中的溶出情况，不同批号阿奇霉素片剂溶出度测定结果重现性良好。     

四厂家阿奇霉素片溶出度考察

目的比较4厂家阿奇霉素片的溶出度，为临床用药提供参考。方法依据2005年版《中国药典（二部）》阿奇霉素片溶出度项下有关规定进行溶出度的测定。结果4厂家产品在45min时的累积溶出百分率均〉75％，但溶出度参数则差异明显（P〈0．01）。结论各厂家的阿奇霉素片的溶出度均符合《中国药典》规定，但溶出度参数有极显著性差异.     

阿奇霉素片溶出度测定

以0.1mol/L盐酸溶液为溶制,采用浆法继以硫酸显色分光光度法测定阿奇霉素片溶出度。方法可行,并能符合药片在胃中的实际溶出情况。测定的三批片剂溶出度均超过75%,但批与批之间存在差异。     

阿奇霉素分散片溶出度方法的改进

目的　改进测定阿奇霉素分散片溶出度的方法。方法　采用浆法,以0. 1mol/L盐酸为溶出介质,转速为5 0rpm/min ,9- 羟基占吨显色,5 4 0nm波长测定比色液的吸收度。结果　2 0分钟内溶出量不少于标示量的75 % ,比色液在5～30 μg范围内线性关系良好。结论　本法可用于阿奇霉素分散片的溶出度的测定     

阿奇霉素片溶出度的研究

目的：比较4个不同厂家阿奇霉素片含量及体外溶出度,证明含量基本一致的前提下,阿奇霉素在人工胃液中受酸性破坏导致影响人体吸收量,从而影响疗效。方法：采用抗生素管碟法测定4厂家阿奇霉素片的含量,采用紫外分光光度法测定4厂家阿奇霉素片的溶出度。结果：阿奇霉素片经人工胃液破坏会影响其含量,从而影响其疗效,比较4个厂家阿奇霉素片溶出度用管碟法测定含量反映其不同厂家不同时间内的溶出度。结论：阿奇霉素片经人工胃液破坏其含量呈曲线降低趋势,说明阿奇霉素片在胃里溶出的越少,对阿奇霉素片的含量影响越小,相应的疗效也就越好。选用阿奇霉素片时注意产品质量。     

阿奇霉素与诺氟沙星治疗小儿急性肠胃炎的临床效果对比

目的 对比分析阿奇霉素与诺氟沙星治疗小儿急性肠胃炎的临床效果。方法 选择2014年1月-2015年1月在成都市龙泉驿区妇幼保健院进行诊治的小儿急性肠胃炎患者100例,随机分为阿奇霉素组与诺氟沙星组,每组各50例。阿奇霉素组静脉注射阿奇霉素治疗,根据患儿体质量每次10 mg/kg,每天1次;诺氟沙星组静脉注射诺氟沙星注射液治疗,每次150 mg,每天2次。比较两组的临床治疗效果,住院时间、呕吐缓解时间、发热缓解时间、腹泻缓解时间以及腹痛缓解时间。结果 阿奇霉素组的有效率为98.00%（49/50）,明显高于诺氟沙星组的78.00%（39/50）,差异有统计学意义（P<0.05）。阿奇霉素组患儿的住院时间、呕吐缓解时间、发热缓解时间、腹泻缓解时间以及腹痛缓解时间均明显短于诺氟沙星组,差异有统计学意义（P<0.05）。阿奇霉素组的不良反应发生率为4.00%（2/50）,与诺氟沙星组的6.00%（3/50）相比无明显差异。结论 阿奇霉素对小儿急性肠胃炎的临床治疗效果明显优于诺氟沙星,安全有效,具有较高的临床应用价值。     

不同厂家阿奇霉素片溶出度评价

目的:建立阿奇霉素片的溶出度测定方法,并对不同生产厂家的阿奇霉素片溶出度进行考察及比较,为临床用药提供参考。方法:参考2005年版《中国药典》相关标准对5厂家5个批次的阿奇霉素片的含量和累积溶出百分率进行检测,再按威布尔分布模型原理计算溶出参数。结果:所有片剂在45min内溶出量均在75%以上,符合要求,但各样品溶出参数的方差分析结果具有显著性差异(P<0.01)。结论:建立的溶出度测定方法简便、可靠;不同厂家阿奇霉素片溶出度有差异,临床用药时应加强监控。     

Safety and effectiveness of azithromycin in the treatment of respiratory infections in children

Abstract

Objectives:

To describe clinical effectiveness of azithromycin in the management of respiratory tract infections in children up to 12 years of age; to examine duration of symptoms after commencement of therapy and to mark adverse events possibly caused by treatment with azithromycin.     

川芎嗪联合阿奇霉素对红霉素耐药性大叶肺炎患儿的疗效及细胞因子的影响

目的 考察川芎嗪联合阿奇霉素对红霉素耐药性大叶肺炎患儿的疗效及细胞因子的影响。方法 选择180例红霉素耐药大叶性肺炎患儿为研究对象,随机分为阿奇霉素组和联合组,每组90例。阿奇霉素组给予静脉滴注10 mg/kg的注射用阿奇霉素,连用3～5 d,患儿体温恢复,且外周血白细胞恢复后,给予口服10 mg/kg的阿奇霉素干混悬剂,1次/d,连续治疗10 d。联合组在此基础上给予静脉滴注40 mg的盐酸川芎嗪注射液,1次/d,连续治疗10 d。观察比较两组的疗效、免疫球蛋白水平及炎性因子水平。结果 治疗后,阿基霉素组的有效率为77.78%,联合组为87.78%,两组有效率有显著差异（P<0.05）。治疗前,两组患儿CD3⁺、CD4⁺、CD8⁺、CD4⁺/CD8⁺水平均无显著差异;治疗后,两组患儿CD3⁺、CD4⁺、CD4⁺/CD8⁺水平均显著升高,CD8⁺水平显著降低,同组治疗前后比较差异有统计学意义（P<0.05）;其中联合组患儿CD3⁺、CD4⁺、CD4⁺/CD8⁺水平均显著高于对照组,CD8⁺水平显著低于对照组,组间差异均有统计学意义（P<0.05）。治疗前,两组患儿IL-6、IL-8、IL-10水平均无显著性差异;治疗后,两组患者IL-6、IL-8、IL-10水平均显著降低,同组治疗前后比较差异有统计学意义（P<0.05）;其中联合组显著低于对照组,组间差异有统计学意义（P<0.05）。结论 川芎嗪联合阿奇霉素对红霉素耐药大叶肺炎患儿有较好的疗效,其治疗作用的发挥与调节机体免疫环境有关,能增加免疫力,减轻炎症反应,从而促进患儿的康复。     

Levofloxacin versus azithromycin on the oropharyngeal carriage and selection of antibacterial- resistant streptococci in the microflora of healthy adults

ABSTRACT

Objective: To determine the proportion of subjects with oropharyngeal streptococci resistant to either levofloxacin or azithromycin prior to and during antibacterial exposure, and to follow temporal changes in the proportion of resistant and susceptible isolates through 6 weeks post-exposure. This randomized, open-label, single-center study is registered with ClinicalTrials.gov (identifier: NCT00821?782).

Research design and methods: A total of 143 healthy volunteers (levofloxacin, n?=?71; azithromycin, n?=?72) without antibacterial exposure in the previous 90 days received either levofloxacin 750?mg once daily for 5 days or azithromycin 500?mg once daily on day 1 and 250?mg once daily on days 2 through 5. Oropharyngeal cultures were obtained pre-exposure, at day 5, and at 2, 4, and 6 weeks post-dosing. Bacterial strains were identified and the minimum inhibitory concentrations for levofloxacin and azithromycin were determined.

Results: At study entry 117 streptococci were isolated from 72 subjects randomized to azithromycin and 53 (45.3%) were azithromycin-resistant. None of the 121 streptococci isolated from 71 subjects randomized to.levofloxacin were colonized by a levofloxacin-resistant microorganism prior to dosing. At the end of dosing, the number of subjects with resistant streptococci (S. mitis, S. salivarius, S. sanguis, or alpha streptococcus species [spp.]) increased in azithromycin-exposed subjects and resistant isolates remained through 6 weeks post-dosing. In contrast, a small number of levofloxacin-resistant streptococci were observed at the end of dosing but decreased by week 2 post-dosing and continued to decrease through the 6-week evaluation period (p?<?0.001 azithromycin vs. levofloxacin for S. mitis, S. salivarius, S. sanguis and alpha streptococcus spp. at week 6). Limitations of this study included the fact that, since previous antibiotic use was self-reported, genetic typing was not done. The results of this study may not be completely generalizable, because subjects in this study received study drug under directly-observed conditions, thus ensuring compliance.

Conclusions: Both antibacterial agents were well tolerated. Levofloxacin 750?mg administered for 5 days was associated with less microbial resistance than that observed with azithromycin in healthy subjects.

Trial registration: ClinicalTrials.gov identifier: NCT00821782.     

The effect of erythromycin and clarithromycin versus azithromycin on serum valproate concentration

IntroductionUnlike azithromycin, erythromycin and clarithromycin strongly inhibit CYP450, which metabolizes valproic acid. The aim of this study was to evaluate the impact of macrolide administration on serum valproate trough levels.MethodsThis retrospective cohort study included hospitalized adult patients who concomitantly received valproate with a macrolide. Patients who received a carbapenem, those who do not have a baseline and/or post-levels, and those who received different doses of valproate were excluded. The change in serum valproate trough level from baseline to after the occurrence of co-administration (post-level) was compared in patients who received either erythromycin or clarithromycin versus those who received azithromycin.ResultsA total of thirteen patients were included in the comparison. The mean ± SD for change in serum valproate trough levels was significantly higher in the erythromycin/clarithromycin group than the azithromycin group (209.1 ± 105.9 µmol/L [equivalent to 30.1 ± 15.2 mg/L] vs. 12.7 ± 52.1 µmol/L [equivalent to 1.8 ± 7.5 mg/L]; P = 0.002).ConclusionThis study found a significantly higher increase in serum trough levels of valproate after co-administration of erythromycin/clarithromycin versus azithromycin. Clinicians should consider avoiding co-administration of erythromycin and clarithromycin with valproate if possible or close monitoring of valproate levels with dose reduction.     

Comparison of azithromycin and moxifloxacin against bacterial isolates causing conjunctivitis

ABSTRACT

Objective: To examine in vitro resistance to azithromycin and moxifloxacin in bacterial conjunctivitis isolates.

Methods: MIC₉₀s (Minimum Inhibitory Concentration) and resistance rates to azithromycin and moxifloxacin were determined based upon microtiter broth dilution and/or antimicrobial gradient test strips in a multicenter phase III study and confirmed externally.

Results: The most common isolates collected from bacterial conjunctivitis patients in the phase III study were Haemophilus influenzae (40.6%), followed by Staphylococcus epidermidis (19.3 %), Propionibacterium acnes (17.3%), Streptococcus pneumoniae (16.8%), and Staphylococcus aureus (0.06%). MIC₉₀s for all of these organisms were well below established resistance breakpoints for moxifloxacin, indicating no bacterial resistance. On the other hand, the MIC₉₀ for H. influenzae was 3-fold higher than the resistance breakpoint for azithromycin, ≥ 128-fold higher for S. epidermidis, 16-fold higher for S. pneumoniae and ≥ 128-fold higher for S. aureus, indicating moderate to very high bacterial resistance to azithromycin.

Conclusions: Resistance to azithromycin is more common than resistance to moxifloxacin in clinical isolates causing bacterial conjunctivitis.     

阿奇霉素胶囊溶出度测定方法的改进

目的:以茜素红荷移分光光度法改进阿奇霉素胶囊溶出度的测定方法.方法:依<中国药典>二部附录X C溶出度测定方法项下二法,以600 mL pH 5.0的磷酸盐缓冲液为溶剂,转速为100 r·min-1.经45 min取样,以茜素红荷移分光光度法在524 nm处测定阿奇霉素胶囊的溶出度,限度为75%.结果:阿奇霉素在12.5～62.0 mg·L-1范围内线性关系良好(r=0.991 3),平均回收率为100.3%.结论:该方法准确、简便,可用于阿奇霉素胶囊溶出度的测定.