琥乙红霉素片溶出度检查方法的探讨

目的：改进琥乙红霉素片溶出度测定方法。方法：用对照品代替自身对照溶液测定琥乙红霉素片溶出度。结果：测定结果与含量符合规定与否相一致。结论：改进方法更能真实、客观反映样品的内在质量。     

阿奇霉素治疗成人肺炎支原体肺炎的临床研究

目的：探讨阿奇霉素治疗成人肺炎支原体肺炎的临床疗效,为临床治疗提供参考资料。方法：将120例成人肺炎支原体肺炎患者随机分为观察组和对照组各60例,观察组采用阿奇霉素治疗,对照组采用红霉素治疗,疗程均为2～3周;比较两组患者的临床疗效。结果：观察组痊愈53例,显效7例,总有效率100%,对照组痊愈32例,显效12例,有效16例,总有效率为73.33%,两组比较差异具有统计学意义（P＜0.05）;对照组患者的胃肠道反应及注射部位疼痛发生率明显高于观察组（P＜0.05）;两组均未见严重的药品不良反应。结论：阿奇霉素治疗成人肺炎支原体肺炎临床疗效显著,安全性高,值得临床应用推广。     

红霉素与阿奇霉素治疗小儿支原体肺炎的最小成本分析

目的：探讨红霉素与阿奇霉素治疗小儿支原体肺炎的成本和效果。方法：运用药物经济学最小成本分析法对红霉素与阿奇霉素治疗小儿支原体肺炎方案进行回顾性分析。结果：两种治疗方案总有效率均为96.66％,差异无统计学意义（P〉0.05）;病原体清除率红霉素组为53.33％,阿奇霉素组为76.67％,差异有统计学意义（P〈0.05）;治疗成本,红霉素组为383.37元,阿奇霉素组为306.27元,差异有统计学意义（P〈0.05）。结论：阿奇霉素与红霉素在治疗小儿支原体肺炎感染方面均有较好疗效,但前者疗效优于后者,具有成本少、清除支原体功能更强、缩短病程、不良反应少的特点,值得在儿童中推广应用。     

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.     

Effect of compression force on the crystal properties of erythromycin acistrate tablets

The crystal properties of compressed and powdered erythromycin acistrate tablets were studied by the X-ray powder diffraction (XRPD) method. Detailed analysis of X-ray powder diffraction line profiles was performed. Diffraction peak intensities and full width at half maximum (FWHM) values of the peaks corresponding to three different crystal lattice directions were determined. Crystallite size was calculated by Scherrer's equation using the data of integral breadth of the peaks. The preferred orientation of the crystallites is also discussed. According to the results, the crystallite size increased on the tablet surface after a small compression force (4 kN) in all crystal lattice directions studied. Even small compression forces caused recrystallization. With higher compression forces (8–18 kN) the crystallite size and the FWHM values remained rather constant. After the compression force of 18 kN the peaks in different crystal lattice directions behaved differently. In the lattice directions of diffraction maxima 2 and 3, the effect was the same with the small (4 kN) and the high compression force (22 kN). Further recrystallization occurred with 22 kN. However, in the crystal lattice direction of diffraction maximum 1 at the compression force of 8 kN the crystallite broke and crystallinity decreased. These were not seen in the powdered tablet samples. It could be concluded that the effect of compression force on the crystal properties of erythromycin acistrate tablets was seen on the tablet surface but not in the powdered tablets. Compression force also affected the preferred orientation of crystallites on the tablet surface and especially in the lattice direction of diffraction maximum 3. This was not seen in the powdered tablets.     

消炎痛,红霉素预防胆囊结石形成的实验研究

为进一步探讨胆汁成份异常、胆囊动力学变化和胆囊结石形成之间的内在联系，对家兔胆囊结石动物模型进行了胆囊动力学研究。结果显示：除胆汁成份异常外，胆囊动力学变化参与了胆囊结石形成。消炎痛能减少胆汁粘蛋白含量抑制胆固醇成核过程而防止胆囊结石形成；而红霉素能通过促进胆囊收缩同时减少胆汁粘蛋白含量和促进胆囊排空，从而更有效地防止胆囊结石形成。提示：改善致石胆汁引起的胆囊动力学变化较改变胆汁成分更有利于防止胆囊结石形成。     

红霉素在几种缓冲液中的溶解度

红霉素在水中溶解度同其解离度有一定关系，当ｐＨ＜６．０时红霉素以盐的形式存在，其溶解度随ｐＨ值降低而迅速增大。在酸性范围内，红霉素的溶解度随温度升高而增大，这与游离碱的反温度溶解特性不同，不同温度下的溶解度随ｐＨ变化曲线相交于ｐＫａ为８．６附近。     

早期药物干预对慢性阻塞性肺疾病大鼠转化生长因子β1的表达影响

目的:观察慢性阻塞性肺疾病(COPD)大鼠模型的TGF-β1的表达变化和早期药物干预对其表达的影响.方法:利用烟薰和气道内多次滴入脂多糖(LPS)建立大鼠COPD模型(B组).早期给予冬虫夏草(C组),红霉素(D组),吸入布地奈德(E组)等分组干预.小动物肺功能仪测定气道阻力(RL)和动态顺应性(Cdyn).采用免疫组织化学法和逆转录-聚合酶链反应(RT-PCR)法检测TGF-β1蛋白及mRNA.结果:模型组基本符合人类COPD病理生理变化.外周细支气管平滑肌层和细胞外基质胶原较正常组(A组)大鼠明显增多.C组与B组比RL减少(P＜0.01),D组、E组与B组比RL亦减少,但Cdyn增加(P＜0.01).B组细支气管上皮、肺泡巨噬细胞和小动脉内皮的TGF-β1蛋白及mRNA的表达高于A组(P<0.01),C组与B组无明显差异,而D组、E组与B组相比,TGF-β1蛋白及mRNA的抑制明显,主要表现在细支气管上皮,但两者抑制程度并无明显差异(P>0.05).气道阻力与细支气管黏膜上皮TGF-β1蛋白,支气管肺组织的TGF-β1mRNA均呈正相关(r＝0.510、P＜0.01,r＝0.367、P＜0.05).结论:慢性烟薰和气道内滴入LPS能构建含有气道重塑特征的COPD大鼠模型.早期应用红霉素,吸入布地奈德可明显抑制气道TGF-β1的表达,影响COPD大鼠气道重塑的发生发展,而冬虫夏草未见此作用.     

红霉素逆转口腔鳞癌多药耐药的临床研究

目的；研究红霉素逆转口腔鳞癌多药耐药（MDR）的临床疗效。方法：采用免疫组化SP法检测口腔鳞癌P－糖蛋白（P－gp)表达，并依P－gp表达随机分组，给以单纯化疗或加红霉素治疗。结果：P－gp阳性治疗组CR＋PR11例（73．3％），P－gp阳性对照组3例（20．0％），两组比较差异有显著性（P＜0．05），P-gp阴性治疗组及对照组疗效无差异（P＞0．05）。结论：红霉素对逆转口腔鳞癌MDR具有明确作用。     

安美汀、红霉素对铜绿假单胞菌菌膜的作用研究

目的 :观察安美汀、红霉素在体外对铜绿假单胞菌菌膜的作用。方法 ;将聚乙烯膜和绿脓杆菌置LB培养基中培养 4 8h ,扫描电镜观察有菌膜形成时取出聚乙烯膜 ,漂洗后分别放入含有不同浓度安美汀和红霉素的LB培养基中 ,2 4h后观察菌膜情况 ,并将培养液接种至LB琼脂平板观察是否有菌落形成。结果 :聚乙烯膜和铜绿假单胞菌共培养 4 8h ,扫描电镜观察到有菌膜形成 ;浓度为 10 0、30 0和 5 0 0 μg/ml的安美汀和浓度为 5 0、10 0和 30 0 μg/ml的红霉素作用 2 4h,聚乙烯膜上的铜绿假单胞菌菌膜均消失 ,培养液接种至LB琼脂平板无菌落形成。结论 :聚乙烯膜和铜绿假单胞菌共培养 4 8h可成功制作铜绿假单胞菌菌膜的体外模型 ;较高浓度的安美汀和红霉素对伴有菌膜形成的铜绿假单胞菌有杀灭作用