小鼠血清及组织中阿奇霉素的HPLC-MS测定

建立了HPLC-MS法测定小鼠血清及组织中阿奇霉素的含量。以罗红霉素为内标，采用C8柱，流动相为乙腈-5mmol／L甲酸铵溶液（含0．3％三乙胺）（75：25）。HPLC-ESI-MS法选择离子检测模式，选择检测的离子为m／z748．8（阿奇霉素，[M＋H]^＋）和858．7（罗红霉素，[M＋Na]^＋），碎片电压分别为150V和130V。阿奇霉素在5～3200ng／ml浓度范围内线性关系良好，提取回收率均在70％以上。     

阿奇霉素分散片的人体药物动力学和生物等效性研究

20名健康男性志愿者交叉口服两种国产阿奇霉素分散片的受试制剂和参比制剂500mg,以HPLC-MS法测定血浆中阿奇霉素的浓度,研究人体药物动力学参数和生物等效性。采用C_8柱,流动相为甲醇-0．02mol／L乙酸铵溶液(70:30), 受试制剂和参比制剂的C_(max)分别为(472．14±216．37)和(432．96±131．80)ng／ml t_(1／2)分别为(68．63±12．93)和(70．63± 15．61)h;T_(max)分别为(2．18±0．89)和(2．25±0．84)h; AUC_(o→144h)分别为(4268．52±1252．89)和(4370．32±807．82)ng·h·ml~(-1)。经方差分析和双单侧t检验,说明两片剂具有生物等效性,受试制剂的相对生物利用度为(97．1±22．7)％。     

国产阿奇霉素在健康人体内的药代动力学

采用微生物法，对１６名男性健康志愿者单剂口服国产阿奇霉素胶囊后的药代动力学进行了研究。口服后不同时间收集血、尿标本。检测菌为藤黄八叠球菌２８００１。测定结果用３Ｐ８７软件经微机处理。结果：口服本品后药时曲线符合二室模型，主要药动学参数，峰时间为（１９６±０７８）ｈ，峰浓度为（１０２±０４０）ｍｇ／Ｌ，药时曲线下面积为（１６２６±３１９）ｍｇ·ｈ·Ｌ－１，消除半衰期为（４７４１±５３３）ｈ，１９２ｈ尿累积排出率为（１３１１±２２９）％。结果提示：国产阿奇霉素体内过程与进口阿奇霉素相仿     

Trachoma decline and widespread use of antimicrobial drugs

Trachoma is disappearing in many parts of the world, even in the absence of specific control programs. Following mass antimicrobial drug treatments for trachoma in western Nepal, the prevalence of trachoma declined far more rapidly than could be attributed to the control program alone. Pharmacy surveys in the same region found that children received more antichlamydial drugs from sources outside the trachoma program than they did from the program itself. We demonstrate that high background antimicrobial drug use may be responsible for much of the observed decline in trachoma and discuss its potential role in eliminating this infectious disease.     

Cell Handling,Membrane-Binding Properties and Membrane-Penetration Modeling Approaches of Pivampicillin and Phthalimidomethylampicillin,Two Basic Esters of Ampicillin,in Comparison with Chloroquine and Azithromycin

Purpose. The purpose of this work was to examine and understand the cellular pharmacokinetics of two basic esters of ampicillin, pivaloyloxymethyl (PIVA) and phthalimidomethyl (PIMA), in comparison with lysosomotropic drugs (chloroquine, azithromycin). Methods. Cell culture studies (J774 macrophages) were undertaken to study uptake and release kinetics and to assess the influence of concentration, pH, proton ionophore (monensin), and MRP and P-gp inhibitors (probenecid, gemfibrozil, cyclosporin A, GF 120918). Equilibrium dialysis with liposomes were performed to directly asses the extent of drug binding to bilayers. Conformational analysis modeling of the drug penetration in bilayers was conducted to rationalize the experimental observations. Results. PIVA and PIMA showed properties in almost complete contrast with those of chloroquine and azithromycin, i.e., fast apparent accumulation and fast release at 4°C as well as at 37°C, saturation of uptake (apparent K _d 40 M), no influence of monensin, MRP, or P-gp inhibitors; tight binding to liposomes (K _d approx. 40 M); and sharp increase in calculated free energy when forced in the hydrophobic domain. Conclusions. Although they are weak organic bases, PIVA and PIMA show none of the properties of lysosomotropic agents. We hypothesize that they remain locked onto the pericellular membrane and may never penetrate cells as such in significant amounts.     

Potentially fatal interaction between azithromycin and disopyramide

A patient on disopyramide developed disopyramide toxicity when treated concurrently with azithromycin. Evidence of toxicity included an elevated serum disopyramide level and ventricular tachycardia requiring cardioversion. The azalide antibiotic presumably inhibited dealkylation of disopyramide to its major metabolite, mono-N-dealkyldisopyramide. Physicians should avoid using azithromycin in patients on disopyramide. If this drug combination is unavoidable, disopyramide levels must be closely monitored.     

阿奇霉素治疗支原体肺炎临床疗效观察

目的观察阿奇霉素治疗支原体肺炎的疗效。方法138例支原体肺炎患者在常规对症治疗的基础上，治疗组（n=78）予阿奇霉素10mg／（kg·d），ivgtt，Qd。对照组（n=60）采用白霉素ZOmg／（kg·d），ivgtt，Qd，5～7天后观察两组疗效。结果治疗组洛愈率达80．8％，显著高于对照组55．0％，两组均未见严重的药物不良反应。结论阿奇霉素静滴治疗支原体肺炎疗效显著。     

阿奇霉素致嗅觉和味觉障碍

1例52岁女性患者,因上呼吸道感染自行服用阿奇霉素0.5g,1次/d.3d后患者出现嗅觉和味觉障碍,立即停用阿奇霉素.然而停药2周后,患者的嗅觉、味觉仍未恢复.     

盆炎降支颗粒剂联用阿奇霉素治疗女性生殖道解脲支原体感染的临床观察

【目的】观察盆炎降支颗粒剂联用阿奇霉素治疗女性生殖道解脲支原体感染的临床疗效。【方法】将2010年1月至2010年12月本院收治的生殖道解脲支原体感染女性患者60例随机分为观察组30例（盆炎降支颗粒剂联合阿奇霉素）和对照组30例（阿奇霉素），对两组的临床疗效进行对比。【结果】观察组总有效率100％，对照组总有效率83．33％，观察组明显优于对照组（P〈0．05）；观察组在改善临床症状方面优于对照组，特别对白带异常、外阴瘙痒、腰腹疼痛、小便不适等症状具有良好的改善作用。【结论】盆炎降支颗粒剂与阿奇霉索联用是治疗女性生殖道解脲支原体感染的有效治疗方法，在改善临床症状方面优于单用阿奇霉素，且具有减少阴道菌群失调的优势。