依诺沙星治疗感染性疾病的临床研究

依诺沙星(Enoxacin,ENX)是一种新的喹诺酮类抗菌剂,其抗菌谱广,口服吸收快,本文报道用ENX治疗各种细菌性感染101例,其中71例与诺氟沙星(Norfloxacin,NFX)治疗组60例作对照,年龄17～91岁(>65岁者8例),男70例,女91例,药物剂量均为0.3～0.6克每日三次,疗程7～14天,结果随机对照组ENX与NFX疗效各为94.37％,83.3％(P<0.05),有显著差异,其中对伤寒病治疗ENX优于NFX,两组细菌清除率各为95.5％,94.8％(P>0.05),无显著差异。不良反应各为9.86％和11.7％。ENX治疗各种细菌感染101例,有效率为96.0％,细菌清除率为95.8％,不良反应主要为消化道反应,另皮疹3例,白细胞及血小板下降各1例,未见肝肾功损害。体外抗菌活性表明ENX对肠杆菌科有高度的抗菌活性,包括对氨苄青霉素、庆大霉素、头孢唑林、氯霉素耐药菌均有较强的抗菌活性,对绿脓杆菌、金葡球菌及表葡球菌也有良好的抗菌作用,表明依诺沙星是一抗菌谱广、抗菌活性强、使用安全有效的抗菌药物。     

依诺沙星滴耳液的研制及临床疗效

依诺沙星滴耳液的研制及临床疗效Ｐｒｅｐａｒａｔｉｏｎａｎｄｃｌｉｎｉｃａｌｅｆｆｉｃａｃｙｏｆｅｎｏｘａｃｉｎｅａｒｄｒｏｐｓ王志朝，夏众源，汤韧，王晓卫，姜加维，张萍ＷａｎｇＺｈｉｃｈａｏ；ＸｉａＺｈｏｎｇｙｕａｎ；ＴａｎｇＲｅｎ；ＷａｎｇＸｉａｏ...     

依诺沙星修饰碳糊电极的制作及应用

碳糊电极以其制作简单、可更新表面 ,且有较好的选择性和较高的灵敏度而倍受人们的青睐。目前常见的化学修饰碳糊电极多为伏安型 ,而电位型的较少见。本文研制了用硝酸汞和依诺沙星生成的配合物作电活性物质修饰碳糊电极。该电极对溶液中的依诺沙星有良好的线性响应和较低的检出限 ;用该电极测定了市售药片中的依诺沙星含量 ,结果较好。1　试剂与仪器石墨粉 (光谱纯 ) ,液体石蜡 (ＣＰ) ,Ｈｇ(ＮＯ3) 2 (Ａ .Ｒ) ,依诺沙星对照品 (浙江省药品检验所提供 ,纯度 99.5 % ) ;依诺沙星片 (浙江海正药业公司提供 ) ;ｐＨＳ - 3ｃ型精密酸度计。2　…     

依诺沙星的药理作用与临床应用

本文介绍依诺沙星的国外研究概况、抗菌谱、抗菌机理、药物动力学、药效学、临床疗效、毒性、不良反应及使用注意事项。     

依诺沙星与氯霉素治疗伤寒的比较

４８例伤寒患者随机分为氯霉素组２４例（男性１１例，女性１３例；年龄３８．６±ｓ１．８ａ）和依诺沙星组２４例（男性１５例，女性９例；年龄２６．２±１．６力。氯霉素１．Ｏ－１．５ｇ，加入１０％葡萄糖液５００ｍＬ中静脉滴注，ｑｄ。依诺沙星０．２ｇ，ｔｉｄ，ｐｏ，均２１ｄ为一个疗程。结果：氯霉素组有效率为６２％（依诺沙星组为９６％），退热时间、中毒症状清退时间较氯霉素组缩短（Ｐ＜０．０１）。     

依诺沙星钴配合物的制备及其抗菌活性研究

目的 合成依诺沙星与钴的配合物,并研究其抗菌活性.方法 以水热法合成配合物,用固体培养基平板药物敏感性试验测定配合物的体外抗菌活性.结果 依诺沙星钴配合物对金黄色葡萄球菌、肺炎链球菌、绿脓杆菌、白色念珠球菌均有抗菌活性,对金黄色葡萄球菌和绿脓杆菌的抗菌活性强于配体本身.结论 依诺沙星钴配合物能在一定程度上提高了抗菌活性,可为开发新药提供依据.     

依诺沙星片剂及胶囊剂近红外光谱模型的研究

目的:建立依诺沙星片剂及胶囊剂的近红外光谱模型。方法:通过对7家生产企业的依诺沙星片和7家生产企业的依诺沙星胶囊进行近红外扫描,对两种依诺沙星制剂分别建立了各企业近红外一致性检验模型和近红外通用型定量模型。结果:一致性检验模型可对各企业产品进行较好的区分,定量模型的验证异常点数在可接受范围内。结论:依诺沙星片剂及胶囊剂的一致性检验模型和定量模型均可达到快速分析的要求。为依诺沙星片剂及胶囊剂的快速分析提供了参考。     

依诺沙星与镍配合物的制备及其抗菌活性

依诺沙星（enoxaein,Ex）是一种结构上与萘啶酸有关的第三代氟代喹诺酮药,其抗菌谱广,抗菌作用强,人体对依诺沙星的耐受性好,不易产生耐药现象,对全身性感染和急、慢性尿道感染有效。许多金属离子可与喹诺酮分子中的3-位羧基和4-位酮基配位形成配合物,与药物协同而使其具有更强的抗菌活性。本文利用溶剂热法合成了依诺沙星与镍的配合物并对其进行了体外抑菌活性实验。     

依诺沙星注射液治疗盆腔炎的效果分析

目的分析依诺沙星注射液治疗盆腔炎的临床效果。方法选取我院在2010年2月至2012年2月共收治的60例盆腔炎患者,将其随机平均分为观察组和实验组,观察组30例患者每天静脉注射依诺沙星200mL,对照组的30例患者每天静脉注射左氧氟沙星200mL,两组患者的疗程均为10d,比较观察组和对照组患者的临床治疗效果。结果观察组治愈的患者16例,显效的患者8例,有效的患者6例,总有效率100%;对照组治愈的患者9例,显效的患者7例,有效的患者2例,无效的患者12例,总有效率60%。两组的总有效率存在着显著的差异(P<0.05)。结论依诺沙星注射液对于治疗盆腔炎有着显著效果,值得临床推广使用。     

氧氟沙星、依诺沙星和诺氟沙星治疗伤寒疗效比较

用氧氟沙星(65例)0.6g/d,依诺沙星(57例)0.6g/d,诺氟沙星(65例)0.8-1.2g/d治疗伤寒。开始退热时间依次为2.6±1.0d,3.8±1.2d,5.3±1.8d,热退到正常时间4.4±1.4d,7.6±2.6d,10±3d,疗程7.5±1.1d,10.6±2.6d,13±3d,有效率依次为100％,90％,63％。结果提示:氧氟沙星疗效显著优于依诺沙星和诺氟沙星,是临床治疗伤寒的满意药物。     

夹心型钨锑酸阴离子插层镁铝水滑石的制备与表征

目的：制备一种新型多阴离子插层水滑石类无机复合功能材料（Sb2W18Co3-LDHs）。方法：采用离子交换法制备Sb2W18Co3-LDHs,使用X-射线粉末衍射和红外光谱对样品进行了表征。结果：夹心型钨锑酸阴离子（Sb2W18Co3）成功插入到Mg-Al-LDHs层间,取代了层间原有的硝酸根离子,制备了新型的Sb2W18Co3-LDHs。结论：夹心型锑钨酸盐成功应用于水滑石复合材料中。     

Mg,Al layered double hydroxides with intercalated indomethacin: synthesis, characterization, and pharmacological study

Magnesium aluminium layered double hydroxides (LDH) with a molar Mg/Al ratio of 2.0 have been prepared with intercalated indomethacin following two routes: reconstruction from a previously calcined Mg(2)Al-CO(3) LDH, and coprecipitation from the corresponding chlorides. The solids have been characterized by powder X-ray diffraction, FTIR, and (13)C CP/MAS NMR spectroscopies and thermal stability (differential thermal analysis and thermogravimetric analysis). Intercalation of the drug is attained by both routes; however, while coprecipitation leads to a single layered structure, contamination with another layered MgAl-CO(3) phase occurs by the reconstruction method. The amount of drug intercalated, as well as the height of the gallery, are larger by the coprecipitation than by the reconstruction one. The data obtained support a somewhat tilted, upwards orientation of the drug molecules forming an interdigited bilayer, in the case of the sample prepared by coprecipitation, with the carboxylate groups pointing towards the hydroxyl layers. However, in the case of the sample prepared by reconstruction, the molecules are forming a tilted, upwards monolayer. The solids prepared are stable up to 250 degrees C. Pharmacological studies in vivo show that intercalation of the drug in the LDH reduces the ulcerating damage of the drug.     

Preparation,characterization, in vitro drug release and anti-inflammatory of thymoquinone-loaded chitosan nanocomposite

In this study, we formulated Thymoquinone-loaded nanocomposites (TQ-NCs) using high-pressure homogenizer without sodium tripolyphosphate. The TQ-NCs were characterized and their anti-inflammatory determined by the response of the LPS-stimulated macrophage RAW 264.7 cells in the production of nitric oxide, prostaglandin E2, tumor necrosis factor-α, interleukin-6, and interleukin-1β. The physicochemical properties of TQ-NC were determined using different machines. TQ was fully incorporated in the highly thermal stable nanoparticles. The nanoparticles showed rapid release of TQ in the acidic medium of the gastric juice. In medium of pH 6.8, TQ-NC exhibited sustained release of TQ over a period of 100 h. The results suggest that TQ-NC nanoparticles have potential application as parenterally administered therapeutic compound. TQ-NC effectively reduce production of inflammatory cytokines by the LPS-stimulated RAW 264.7 cells, indicating that they have anti-inflammatory properties. In conclusion, TQ-NC nanoparticles have the characteristics of efficient carrier for TQ and an effective anti-inflammatory therapeutic compound.     

盐酸非那吡啶的合成及其热稳定性初步研究

目的研究盐酸非那吡啶的制备工艺及其热稳定性。方法以苯胺为原料,经重氮化、偶合、中和、成盐得盐酸非那呲啶;用热重分析法(TG)和差示扫描量热法(DSC)对其热稳定性进行初步研究。结果本工艺路线4步总收率为71.5%;在氮气氛(氮气流量为20 mL.min-1)、10 K.min-1的升温条件下,将盐酸非那吡啶加热到235℃才开始发生剧烈分解,至287.4℃时,有50.79%的盐酸非那呲啶发生分解。结论本制备方法简单,适合于大量制备。本品的热稳定性较好。     

Intercalation of hydrophilic and hydrophobic antibiotics in layered double hydroxides

Four pharmaceutically active molecules, each representing a different class of antibiotic, were intercalated in layered double hydroxides. Two of them, gramicidin and amphotericin B, are hydrophobic, surface active drugs that were incorporated in artificial membranes formed in the interlayer of the inorganic host. The other two, ampicillin and nalidixic acid, are water soluble, commonly used antibiotics that were directly intercalated by using simple ion exchange reactions. The synthetic nanohybrid materials were characterized by various methods, as X-ray diffraction, infrared spectroscopy and ultraviolet-visible spectroscopy that verified the successful intercalation of the antibiotics and provided information regarding the interlayer structure of the nanohybrids. The reversible interaction of the antibiotic molecules with the inorganic host leads to release of the active drugs under the appropriate conditions. The release studies showed that the synthetic nanohybrids can successfully serve as controlled release systems for different kinds of antibiotics.     

Immobilization of ibuprofen and copper-ibuprofen drugs on layered double hydroxides

The immobilization of the NSAID ibuprofen (Hibp) and the Cu(II)-ibp compound on magnesium-aluminum layered double hydroxides (Mg3Al-LDH) is described. Ibuprofen was intercalated on LDHs by three routes (ion exchange, co-precipitation, and reconstruction). The organic drug and the Cu(II)-ibp were also immobilized by adsorption on LDH external surfaces. Materials were characterized by elemental analysis, UV/VIS, FTIR, and Raman spectroscopies, powder X-ray diffractometry (XRD), thermogravimetry, and electronic paramagnetic resonance (EPR). Mg3Al-(ibp)(cop) (30% w/w of drug/material) and Mg3Al-(ibp)(ie) (33%) materials exhibit bilayer arrangements of ibp anions intercalated between the host layers. Mg3Al-(ibp)(rec) and Mg3Al-(ibp)(ads) contain 13% and 6.2% of ibuprofenate, respectively. Mg3Al-(Cu-ibp)(ads) exhibits two Cu centers in different environments interacting with host layers. Pharmacological potential of materials are compared considering the amounts of immobilized drugs and their buffering properties. Mg3Al-(ibp)(ie) and Mg3Al-(ibp)(cop) exhibit poor buffering property, but contain high ibp amounts. Mg3Al-(ibp)(ads) despite having buffering property, contains low amount of ibuprofen. Mg3Al-(ibp)(rec) combines significant amount of immobilized ibp with good buffering property. Mg3Al-(Cu-ibp)(ads), due to the buffering property, may be an interesting new formulation aiming to decrease gastric irritation.     

Synthesis and properties of cordycepin intercalates of Mg-Al-nitrate layered double hydroxides

Layered double hydroxides (LDHs) were investigated as cordycepin delivery nanocarriers for the first time in this study. Negatively charged biomolecule-cordycepin was intercalated in the gallery spaces of [Mg-Al-NO(3)] as the charge-compensating species, which was confirmed by the results of XRD, FT-IR, TEM, CZE and electrophoretic mobility. Cell experiment suggested that the new bio-LDH nanohybrid could prevent cordycepin decomposition by adenosine deaminase. This new formulation could possibly be used as a novel form cordycepin intravenous injection.     

Drug silica nanocomposite: preparation,characterization and skin permeation studies

The aim of this work was to evaluate silica nanocomposites as topical drug delivery systems for the model drug, caffeine. Preparation, characterization, and skin permeation properties of caffeine-silica nanocomposites are described. Caffeine was loaded into the nanocomposites by grinding the drug with mesoporous silica in a ball mill up to 10?h and the efficiency of the process was studied by XRPD. Formulations were characterized by several methods that include FTIR, XRPD, SEM and TEM. The successful loading of caffeine was demonstrated by XRPD and FTIR. Morphology was studied by SEM that showed particle size reduction while TEM demonstrated formation of both core-shell and multilayered caffeine-silica structures. Solid-state NMR spectra excluded chemical interactions between caffeine and silica matrix, thus confirming that no solid state reactions occurred during the grinding process. Influence of drug inclusion in silica nanocomposite on the in vitro caffeine diffusion into and through the skin was investigated in comparison with a caffeine gel formulation (reference), using newborn pig skin and vertical Franz diffusion cells. Results from the in vitro skin permeation experiments showed that inclusion into the nanocomposite reduced and delayed caffeine permeation from the silica nanocomposite in comparison with the reference, independently from the amount of the tested formulation.