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L-苏糖酸阿奇霉素抗菌效应及急性毒性研究
引用本文:胡晓,李响敏,刘大仁,胡雪飞,李文,杨媛. L-苏糖酸阿奇霉素抗菌效应及急性毒性研究[J]. 矿产勘查, 2011, 0(12): 1-4,10
作者姓名:胡晓  李响敏  刘大仁  胡雪飞  李文  杨媛
作者单位:[1]南昌大学医学院临床药理研究所,南昌330006 [2]南昌大学中德联合研究院,南昌330047 [3]南昌大学期刊社,南昌330006 [4]南昌大学第一附属医院检验科,南昌330006
基金项目:江西省科技支撑计划项目(2007BS12505)
摘    要:目的观察L-苏糖酸阿奇霉素的抗菌效应及其急性毒性。方法肉汤稀释法检测药物对临床分离的常见致病菌最小抑菌浓度(MIC)和最低杀菌浓度(MBC)以评价其体外抗菌作用。以金黄色葡菌球菌及耐甲氧西林金黄色葡菌球菌感染小鼠建立动物模型,阿奇霉素灌胃给药对感染动物进行治疗评价其体内抗菌作用并测定小鼠LD50评价其急性毒性。结果体外实验显示L-苏糖酸阿奇霉素和乳糖酸阿奇霉素对革兰阳性球菌、革兰阴性球菌和革兰阴性杆菌的MIC50、MIC90、MBC50和MBC 90基本一致,均对耐药菌无效;低剂量(37.5mg.kg-1)L-阿苏糖酸阿奇霉素和乳糖酸阿奇霉素对金黄色葡萄球菌敏感株感染小鼠的保护率分别为55%和15%,经χ2检验差异有统计学意义(P〈0.05);小鼠腹腔注射L-苏糖酸阿奇霉素和乳糖酸阿奇霉素的LD50分别为(1 308.6±203.2)mg.kg-1和(1 193.1±161.4)mg.kg-1,经t检验差异有统计学意义(P〈0.05)。结论 L-苏糖酸阿奇霉素和乳糖酸阿奇霉素体外抗菌活性相似,低剂量L-苏糖酸阿奇霉素对金葡菌感染小鼠有更强的保护作用且对小鼠的急性毒性小于乳糖酸阿奇霉素。

关 键 词:L-苏糖酸阿奇霉素  抗菌效应  急性毒性  动物,实验  小鼠

Antibacterial Effect and Acute Toxicity of Azithromycin L-threonate
HU Xiaoa,LI Xiang-minb,LIU Da-renc,HU Xue-feid,LI Wena,YANG Yuan. Antibacterial Effect and Acute Toxicity of Azithromycin L-threonate[J]. Mineral Exploration, 2011, 0(12): 1-4,10
Authors:HU Xiaoa  LI Xiang-minb  LIU Da-renc  HU Xue-feid  LI Wena  YANG Yuan
Affiliation:a (a.Institute of Clinical Pharmacology of Medical College,Nanchang University, Nanchang 330006,China;b.Jiangxi-OAI Joint Research Institute, Nanchang University,Nanchang 330047,China;c.Pediodical Press, Nanchang 330006,China;d.Department of Clinical Laboralology, the First Affiliated Hospital,Nanchang,University,Nanchang 330006,China)
Abstract:Objective To investigate the antibacterial effect and acute toxicity of azithromycin L-threonate.Methods The minimal inhibitory concentration(MIC)and minimal bactericidal concentration(MBC) were detected to investigate the antibacterial activity of azithromycin L-threonate by broth dilution method.The mouse infection model was established using Staphylococcus aureus and Methicillin-resistant Staphylococcus aureus.The antibacterial effect and acute toxicity(LD50) of azithromycin were evaluated after intragastric administration of azithromycin L-threonate.Results The MIC50,MIC90,MBC50 and MBC90 of Azithromycin L-threonate against gram-positive cocci,gram-negative cocci and gram-negative bacilli were similar to azithromycin lactobionate.Drug-resistant bacteria were less sensitive to both azithromycin L-threonate and azithromycin lactobionate.The protective rate of 37.5 mg·kg-1azithromycin L-threonate(55%) was significantly higher than that of 37.5 mg·kg-1azithromycin lactobionate(15%) in mice infected with sensitive strains of Staphylococcus aureus.In addition,LD50 valuesof azithromycin L-threonate [(1 308.6±203.2)mg·kg-1] were obviously greater than those of azithromycin lactobionate [(1 193.1±161.4)mg·kg-1](P0.05).Conclusion The antibacterial activity of azithromycin L-threonate is similar to azithromycin lactobionate.But,low-dose azithromycin L-threonate is more protective against Staphylococcus aureuson and has lower acute toxicity than azithromycin lactobionate.
Keywords:azithromycin L-threonate  antibacterial effect  acute toxicity  animals  laboratory  mice
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