盐酸米诺环素软膏治疗口腔常见病的临床应用进展

盐酸米诺环素软膏是一种新型的半合成四环素,近年来在口腔常见病的治疗和研究中备受关注。对其在慢性牙周炎、牙周牙髓联合病变、窦道型根尖周炎、智齿冠周炎、种植体周围炎、干槽症等临床治疗中的应用进行综述,为盐酸米诺环素软膏在口腔疾病治疗中的进一步推广应用提供依据。     

米诺环素文献循证计量分析

目的 了解米诺环素(四环素类广谱抗生素)的研究现状和方向.方法 在Cnld、PubMed、Web of Science数据库中检索所有米诺环素方面的文献,按照文献的发表年份、作者、研究机构、文献出版来源、相关关键词等进行统计分析.结果 国内外米诺环素相关文献总数为8463篇,其中中文2448篇,外文6015篇.米诺环素的研究文献呈逐年增长的趋势,自1994年开始大幅增长.近年来研究发现,它在治疗多重耐药菌如MRSA、泛耐药鲍曼不动杆菌方面有较好的抗菌作用,对细菌生物被膜的形成也有一定的抑制作用.此外,其有一些非抗菌的生物学活性,如抗炎作用、免疫抑制作用、抗胶原酶活性、神经保护作用等.结论 米诺环素文献近10年来显著增加,主要研究热点是其抗耐药菌作用、抗细菌生物被膜作用、抗非典型致病原作用以及抗炎等新的生物学效应.     

Metabolism of minocycline in humans

Metabolites of tetracycline antibiotics have not previously been isolated from human excreta. It is now demonstrated that minocycline is the first tetracycline to be metabolized in man. A two-step liquid chromatographic procedure was used to isolate three metabolites from human urine. The principal metabolite was tentatively identified as 9-hydroxyminocycline by mass spectral and spectrophotometric analysis and comparison with a synthetic compound. The latter was prepared by incubation of minocycline in a modified Udenfriend system, simulating an enzymatic oxygenase. Two other major metabolites are probably mono-N-demethylated derivatives. Substantial amounts of 4-epiminocycline, which probably resulted from minocycline epimerization rather than biotransformation, were also present.     

盐酸米诺环素软膏应用时机对超声龈下刮治治疗慢性牙周炎效果的影响

目的探讨盐酸米诺环素软膏应用时机对超声龈下刮治治疗慢性牙周病效果的影响。方法选取2013年4月~2015年2月在我院择期行超声龈下刮治治疗的中重度慢性牙周炎患者69例,按随机数字表法分为A组(n=31)和B组(n=38),分别于龈下刮治前0.5~1h和龈下刮治完成后次日予盐酸米诺环素软膏牙周袋内注射,1次/周,连用4周。分别于牙周治疗前、治疗后2个月时,检测菌斑指数(PI)、牙龈指数(GI)、探诊出血(BOP)、探诊深度(PD),并进行组间比较。结果治疗前,两组患者PI、GI、BOP%、PD比较,差异均无统计学意义(P0.05),治疗后2个月均明显降低(P0.05);治疗后2个月,A组患者PI、PD、BOP%均明显低于B组(P0.05),而组间GI、AL比较,差异无统计学意义(P0.05)。结论超声龈下刮治同时予牙周袋内注射盐酸米诺环素软膏可较大程度地发挥抗菌作用,有助于提高对慢性牙周炎的治疗效果,优于刮治后用药。     

米诺环素的药效学研究

国产米诺环素（ｍｉｎｏｃｙｃｌｉｎｅ，ＭＩＮＯ）的体内外抗菌活性研究结果表明：ＭＩＮＯ是一个对革兰氏阳性菌和革兰氏阴性菌均有较强抗菌活性的广谱抗生素，对金葡球菌、表葡球菌的抗菌活性优于四环素（ＴＣ）、青霉素（ＰＣＧ）、麦迪霉素（ＭＤＭ）、庆大霉素（ＧＭ）和依诺沙星（ＥＮＸ），并对耐四环素金葡球菌和表葡球菌有很强的抗菌活性。ＭＩＮＯ对化脓性链球菌的抗菌活性优于ＴＣ、ＭＤＭ、ＧＭ、ＥＮＸ，弱于ＰＣＧ；对大肠杆菌、肺炎克雷伯氏菌的抗菌活性优于ＴＣ、ＧＭ，弱于ＥＮＸ；对变形杆菌的抗菌活性优于ＴＣ，弱于ＧＭ、ＥＮＸ。口服ＭＩＮＯ对金葡球菌感染小鼠的ＥＤ５０为０．９９ｍｇ／ｋｇ，优于强力霉素（ＤＯＸＹ）和ＴＣ；对大肠杆菌感染小鼠的ＥＤ５０为１０．９６ｍｇ／ｋｇ，优于ＴＣ，与ＤＯＸＹ的ＥＤ５０无显著性差异；对耐ＴＣ金葡球菌感染小鼠的ＥＤ５０为０．６５ｍｇ／ｋｇ，明显优于ＤＯＸＹ和ＴＣ。杀菌试验表明：ＭＩＮＯ在２～４ＭＩＣ时，对金葡球菌和大肠杆菌具有杀菌作用。     

Ophthalmic drug discovery

Millions of people suffer from a wide variety of ocular diseases, many of which lead to irreversible blindness. The leading causes of irreversible blindness in the elderly--age-related macular degeneration and glaucoma--will continue to effect more individuals as the worldwide population continues to age. Although there are therapies for treating glaucoma, as well as ongoing clinical trials of treatments for age-related macular degeneration, there still is a great need for more efficacious treatments that halt or even reverse ocular diseases. The eye has special attributes that allow local drug delivery and non-invasive clinical assessment of disease, but it is also a highly complex and unique organ, which makes understanding disease pathogenesis and ocular drug discovery challenging. As we learn more about the cellular mechanisms involved in age-related macular degeneration and glaucoma, potentially, new drug targets will emerge. This review provides insight into some of the new approaches to therapy.     

Improved LC of minocycline drug substance

An isocratic liquid chromatographic method is described for the separation of minocycline and its impurities. This method uses XTerra RP-18, 5 microm (25 cm x 4.6 mm I.D.), a silica-based stationary phase with reduced silanol activity. A mobile phase composed of acetonitrile-0.2 M tetrabutylammonium hydrogen sulphate pH 6.5-0.2 M ethylenediaminetetraacetic acid pH 6.5-water (20:20:20:40; v/v/v/v) was used at a flow rate of 1 ml/min. The column temperature was set at 35 degrees C. UV detection was performed at 280 nm. Optimisation of the separation method and a robustness study were performed by means of a central composite experimental design. The method allows to separate minocycline from known impurities. Some unidentified impurities are also separated. The total time of analysis is less than 20 min.     

Clinical pharmacokinetics of doxycycline and minocycline

Doxycycline and minocycline are second-generation tetracyclines. They are readily absorbed, distributed throughout the organism as a function of their lipophilicity and eliminated in both the urine and the faeces. The influence of age, renal disease, malnutrition and hyperlipidaemia is reviewed, together with the main pharmacokinetic interactions.     

眼科抗感染类基本药物在2家眼科专科医院应用的调查分析

目的:为调整我国眼科抗感染类基本药物提供参考。方法:收集某市级眼科专科医院和某县级眼科专科医院2009年眼科抗感染类基本药物应用数据(包括药品名称、规格、剂型、单价、用量和销售金额),采用表格进行信息数据的统计处理。并通过中国知网查询1989-2011年国内期刊公开发表的眼科用药分析及常见的眼科抗感染药物不良反应的文献,对其进行分析。结果:本次调查中,我国《国家基本药物目录.基层医疗卫生机构配备使用部分》(2009年)中的氯霉素滴眼液和《世界卫生组织基本药物示范目录》(17版)中的四环素眼药膏和庆大霉素溶液均未使用;红霉素、左氧氟沙星和阿昔洛韦则都得到了广泛应用;妥布霉素及其复方制剂,则在金额和数量排序中居首位。文献资料显示,红霉素眼膏、左氧氟沙星、阿昔洛韦和妥布霉素不良反应的报道较少,氯霉素和庆大霉素在眼科用药中的不良反应报道较多,由于眼科疾病谱的变化,四环素近年来使用较少。结论:2009年版基本药物目录收录的红霉素眼膏、左氧氟沙星滴眼液和阿昔洛韦滴眼液符合我国基本药物目录的遴选原则;另外,本着"临床首选"的原则建议收录妥布霉素滴眼液。     

盐酸米诺环素胶囊的质量评价

目的对国产盐酸米诺环素胶囊的质量现状进行评价。方法采用法定标准检验与探索性研究相结合,对国家药品计划抽验的159批次样品与调研企业收集样品进行检验与统计分析。结果法定标准检验结果显示159批次盐酸米诺环素胶囊合格率100%。探索性研究建立新的有关物质HPLC测定方法分离效果更好,对产品有关物质质量的评价更全面准确;本品以差向米诺环素为主要杂质,抽验样品中杂质的种类及个数基本相同,但不同内容物性状胶囊的杂质含量存在差异;无复合袋包装的产品更易吸潮及降解;国内外原料为同一晶型;不同内容物性状胶囊的溶出行为存在差异。结论国内盐酸米诺环素胶囊质量总体良好,现行质量标准需进一步修订完善。建议企业对制剂生产工艺进行优化,选用阻隔性能优良的包材,以保证产品质量。