阿奇霉素-离子交换树脂复合物的制备及其掩味与调控释药作用

为掩盖阿奇霉素(azithromycin,AZI)苦味和个性化调控药物释放速度以减少胃肠道刺激,分别以羟丙基纤维素(hydroxypropyl cellulose,HPC)和尤特奇RS100修饰制备速释型AZI-Amberlite^TM IRP64/HPC和缓释型AZI-Amberlite^TM IRP69/RS100进而组合以实现控制释放。对AZI-离子交换树脂复合物的载药量、药物利用率进行测定,通过差示扫描量热分析和X射线衍射对AZI-离子交换树脂复合物进行结构表征,测定其润湿度、掩味效果、体外溶出和释放行为。结果显示,形成的AZI-离子交换树脂复合物改变了药物原有的结晶状态,2.5%HPC修饰的AZI-Amberlite^TM IRP64/HPC和0.5%RS100修饰的AZI-Amberlite^TM IRP69/RS100掩味效果良好,两者以对应AZI含量为13∶67的比例组合可以实现AZI在前10 min的快速释放和后期的6 h内平稳释药。结果表明,经表面修饰制得的AZI-离子交换树脂复合物及其...     

阿奇霉素胶囊的人体相对生物利用度研究

目的研究国产阿奇霉素胶囊的相对生物利用度。方法采用双周双制剂交叉试验设计，让20名健康男性志愿者随机单剂量口服国产四川维奥阿奇霉素胶囊和四川明欣阿奇霉素胶囊，剂量均为500mg，剂间间隔为2周。用微生物杯碟法测定血清中阿奇霉素浓度，并计算相对生物利用度。结果受试制剂和参比制剂的药代动力学参数无统计学差异，消除半衰期（t1/2B）分别为（53．29±19．33）h和（51．21±17．04）h，峰浓度（Cmax）分别为（0．360±0．118）μg／mL和（0．367±0．132）μg／mL，达峰时间（tmax）分别为（2．30±0．67）h和（2．30±0．86）h，AUC0-τ，分别为（5．42±1．89）μg·h／mL和（5．84±2．29）μg·h／mL。结论受试制剂阿奇霉素胶囊的相对生物利用度为（92．81±11．79）％，与参比制剂具有生物等效性。     

孟鲁司特联合阿奇霉素治疗儿童肺炎支原体肺炎的疗效观察

目的探讨孟鲁司特联合阿奇霉素治疗儿童肺炎支原体肺炎临床效果。方法将86倒肺炎支原体肺炎感染患儿随机分为两组,对照组43例给予阿奇霉素静脉滴注序贯口服治疗,观察组45例在对照组的基础上加用孟鲁司特口服,并比较两组的临床效果。结果观察组的总有效率为97．67％,而对照组为86．05％,两组相比较差异有统计学意（P〈0．05）,观察组的发热消失时间、咳嗽消失时间、肺部音消失时间、平均住院时间均低于对照组（均P〈O．05）。结论孟鲁司特联合阿奇霉素治疗儿童肺炎支原体肺炎可有效改善肺炎支原体肺炎患儿临床症状,安全可靠,缩短病程,提高儿童肺炎支原体肺炎感染的防治水平。     

Single-dose azithromycin for the treatment of children with acute otitis media

Azithromycin is an azalide with in vitro activity against otitis media pathogens, good middle ear penetration and a prolonged half-life. A total of four clinical trials have evaluated the clinical success rate, safety and compliance of single-dose azithromycin (30 mg/kg) in the treatment of children with otitis media. Among all the patients treated with single-dose azithromycin (30 mg/kg), and presented previously in four published clinical trials, end-of-treatment clinical success was 88% (544 out of 619) and maintained clinical success at the end-of-study was 82% (498 out of 610). Three of the four studies included a mandatory baseline tympanocentesis. The overall end-of-treatment and end-of-study clinical success rates among all culture-positive patients was 84% (222 out of 263) and 80% (210 out of 263), respectively. Per pathogen end-of-treatment clinical success rates observed were 91% (125 out of 137) among patients with Streptococcus pneumoniae, 77% (75 out of 97) among patients with Haemophilus influenzae, 100% (14 out of 14) among patients with Moraxella catarrhalis, 64% (seven out of 11) among patients with baseline Streptococcus pyogenes and 25% (one out of four) among patients with a S. pneumoniae and H. influenzae mixed infection. Clinical success was observed in 90% (106 out of 118) of patients with baseline macrolide-susceptible S. pneumoniae and in 67% (14 out of 21) among patients with baseline macrolide-resistant S. pneumoniae (p = 0.01). Adverse events were uncommon, mostly mild and transitory gastrointestinal complaints, and in the two larger comparative trials, were less frequent than the rates observed with the comparator agents. Compliance was excellent (99–100%). Single-dose azithromycin (30 mg/kg) represents an alternative for the treatment of pediatric patients with uncomplicated acute otitis media, particularly in those geographic regions where high-level S. pneumoniae macrolide resistance is uncommon, and for those patients that require directly observed therapy or when compliance may be a problem.     

Treatment of Tularemia in Pregnant Woman,France

A pregnant woman who had oropharyngeal tularemia underwent treatment with azithromycin and lymph node resection and recovered without obstetrical complication or infection in the child. Azithromycin represents a first-line treatment option for tularemia during pregnancy in regions where the infecting strains of Francisella tularensis have no natural resistance to macrolides.     

The dilemma of monotherapy or combination therapy in community‐acquired pneumonia

Scope

To study the factors associated with mortality in hospitalized patients with community‐acquired pneumonia treated with monotherapy or combination therapy.

Methods

PubMed and Scopus were searched. Patients receiving macrolides, β‐lactams and fluoroquinolones, as monotherapy or in combination, were included. Meta‐analyses and meta‐regressions were performed.

Results

Fifty studies were included. Overall, monotherapy was not associated with higher mortality than combination (RR 1.14, 95% CI 0.99‐1.32, I² 84%). Monotherapy was associated with higher mortality than combination in North American and retrospective studies. β‐lactam monotherapy was associated with higher mortality than β‐lactam/macrolide combination in the primary (1.32, 1.12‐1.56, I² 85%) and most sensitivity analyses. There was no difference in mortality between fluoroquinolone monotherapy and β‐lactam/macrolide combination (0.98, 0.78‐1.23, I² 73%). In meta‐regressions, the moderators that could partially explain the observed statistical heterogeneity were the frequency of cancer patients (P = .03) and Pneumonia Severity Index score IV (P = .008).

Conclusion

Due to the considerable heterogeneity and inclusion of unadjusted data, it is difficult to recommend a specific antibiotic regimen over another. Specific antibiotic regimens, study design and the characteristics of the population under study seem to influence the reported outcomes.     

埃索美拉唑和阿奇霉素联合治疗幽门螺杆菌感染的疗效观察

【目的】观察埃索美拉唑和阿奇霉素联合治疗，幽门螺杆菌（Hp）感染的疗效。【方法】120例Hp阳性患者，随机分为治疗组（A组）和对照组（B组）。A组给予埃索美拉唑20mg，阿奇霉素0．25g，均2；k／d，共7d；B组给予经典Hp根除治疗方案：奥美拉唑20mg，阿莫西林1．0g，替硝唑0．4g，均2；k／d，共7d；7d后分别继续单独使用埃索美拉唑或奥美拉唑20mg，1；k／d，连续7d。于用药前1d，用药后d1，d3，d7，按标准对上腹痛，反酸进行评分，其中上腹痛从严重程度和发作频率两个方面进行评估。记录患者有无出现不良反应。治疗结束后4周做^14C—UBT检查，了解Hp根除情况。【结果】A组上腹痛消失率用药d1为56．1％，d3为89.4％；B组用药d1为21.4％，d。为60．7％，两组比较差异有显著性（P〈0．05）；A组反酸消失率用药d1为59．6％，d3为93．0％；对照组用药d1为19.6％，d3为64．3％，两组比较差异有显著性（P〈0.05）；服药d7，A组上腹痛、反酸消失率分别为98．2％、98.2％，B组亦分别为96．4％、94.6％，两组比较差异无显著性（P〉0.05）。A组、B组HP根除率分别为91．2％（52／57）、91．1％（51／56）（P〉0．05）。不良反应发生率两组分别为8.7％（5／57），10．7％（6／56），所有患者均未出现明显不良反应。【结论】埃索美拉唑和阿奇霉素二联疗法是一种高效、安全、经济的根除HP方案。     

Azithromycin maintenance therapy in patients with cystic fibrosis: a dose advice based on a review of pharmacokinetics, efficacy, and side effects

Azithromycin maintenance therapy results in improvement of respiratory function in patients with cystic fibrosis (CF). In azithromycin maintenance therapy, several dosing schemes are applied. In this review, we combine current knowledge about azithromycin pharmacokinetics with the dosing schedules used in clinical trials in order to come to a dosing advise which could be generally applicable. We used data from a recently updated Cochrane meta analysis (2011), the reports of clinical trials and pharmacokinetic studies. Based on these data, it was concluded that a dose level of 22-30 mg/kg/week is the lowest dose level with proven efficacy. Due to the extended half-life in patients with CF, the weekly dose of azithromycin can be divided in one to seven dosing moments, depending on patient preference and gastro-intestinal tolerance. No important side effects or interactions with other CF-related drugs have been documented so far.