差示紫外分光光度法测定左氧氟沙星制剂的含量

左氧氟沙星(levofloxacin,LVFX)是第三代氟喹诺酮类抗菌药物氧氟沙星的左旋体,其抗菌活性约为氧氟沙星的二倍.对革兰阴性和革兰阳性细菌的MIC90值比氧氟沙星低50%;对甲氧西林敏感和耐药的金葡球菌的平均MIC90是环丙沙星的25%～50%[1].左氧氟沙星主要作用机制为抑制细菌DNA转移酶(细菌拓扑异构酶)的活性,阻碍细菌DNA复制.适用于敏感细菌所引起的呼吸系统、泌尿生殖系统及软组织感染.左氧氟沙星的含量测定方法有紫外分光光度法[2]、高效液相色谱法[3]等、差示紫外分光光度法尚未见报道.本文用差示紫外分光光度法测定甲磺酸左氧氟沙星片及盐酸左氧氟沙星葡萄糖注射液的含量,为该药提供了又一含量测定方法,方法简便、快速,结果满意.……     

差示紫外分光光度法测定左氧氟沙星制剂的含量

左氧氟沙星(levofloxacin,LVFX)是第三代氟喹诺酮类抗菌药物氧氟沙星的左旋体,其抗菌活性约为氧氟沙星的二倍.对革兰阴性和革兰阳性细菌的MIC90值比氧氟沙星低50%;对甲氧西林敏感和耐药的金葡球菌的平均MIC90是环丙沙星的25%～50%[1].左氧氟沙星主要作用机制为抑制细菌DNA转移酶(细菌拓扑异构酶)的活性,阻碍细菌DNA复制.适用于敏感细菌所引起的呼吸系统、泌尿生殖系统及软组织感染.左氧氟沙星的含量测定方法有紫外分光光度法[2]、高效液相色谱法[3]等、差示紫外分光光度法尚未见报道.本文用差示紫外分光光度法测定甲磺酸左氧氟沙星片及盐酸左氧氟沙星葡萄糖注射液的含量,为该药提供了又一含量测定方法,方法简便、快速,结果满意.     

左氧氟沙星治疗下呼吸道感染30例

左氧氟沙星是新型氟喹诺酮类药物 ,具有抗菌谱广、抗菌活性强、体内分布广的特点[1] 。我们自 2 0 0 2年 4～ 9月用左氧氟沙星序贯治疗社区获得性下呼吸道感染 3 0例 ,取得较好的临床效果 ,现报告如下。材料与方法1　病例选择3 0例均为临床确诊的社区获得性下呼吸道感染并收住入院的中度感染者。年龄 1 9～ 83岁 ,平均60岁。男 1 4例 ,女 1 6例。2　药品、剂量和疗程左氧氟沙星注射液及口服片剂 (商品名 :可乐必妥 ,日本第一制药 (北京 )有限公司 ,批号 :0 2 0 9Ｃ40 ) ,规格 :0 .3 ｇ/ 1 0 0ｍＬ静滴 ,ｑｄ,5～ 7ｄ后临床症状控制好转改为…     

左氧氟沙星地塞米松滴眼液的制备

<正>左氧氟沙星(levofloxacin)属第3代氟喹诺酮类抗菌药,为氧氟沙星的左旋光学活性异构体,对包括厌氧菌在内的革兰阳性菌及革兰阴性菌有较强的抗菌活性[1],眼科中主要用于角膜炎、结膜炎[2]、白内障术后[3]、结膜炎、麦粒肿、泪囊炎等,地塞米松(dcxamethasonc)可抑制各种因素引起的炎症反     

左氧氟沙星滴耳液的制备及质量控制

左氧氟沙星是氧氟沙星的左旋光学异构体 ,是氧氟沙星的活性部分 ,其抗菌活性是氧氟沙星的两倍。目前国内上市有注射液、片剂、胶囊剂 ,未见滴耳剂的报道。为满足临床需要 ,我院研制了左氧氟沙星滴耳液 ,现报道如下 :1 仪器与试药ＤＵ - 5 0型分光光度计 (Ｂｅｃｋｍａｎ) ,ＴＧ32 8Ａ分析天平 (上海长江科学仪器厂 ) ;盐酸左氧氟沙星 (江苏昆山制药总厂 ) ,甘油、乙醇均符合 95版药典标准 ,其余试剂均为分析纯。2 处方及制备2 1　处方　盐酸左氧氟沙星 3 0 ｇ ,甘油 2 0 0ｍｌ,氢氧化钠试液适量 ,35 %乙醇加至 10 0 0ｍｌ。2 2　制法　取…     

左氧氟沙星治疗肠道细菌感染的临床观察

左氧氟沙星抗菌活性约为氧氟沙星、环丙沙星、氟罗沙星、洛美沙星的 2～ 8倍 ,且使用方便 ,不良反应少 ,适于治疗包括厌氧菌在内的革兰阳性菌及革兰阴性菌引起的各种感染[1] 。我们观察左氧氟沙星治疗肠道细菌感染 88例 ,结果总结如下。1　病例与方法1 .1病例情况　肠道细菌感染患者 88例 (男 64,女2 4 ) ,年龄 (31 .0 3± 1 3.2 2 ) y,体重 (57.56± 6.86)kg。其中急性细菌性痢疾 55例 ,副溶血弧菌肠炎 6例 ,沙门菌肠炎 2例 ,豚鼠气单孢菌肠炎 1例 ,霍乱 2例 ,伤寒 2 2例。主要表现为发热、腹痛、腹泻及里急后重等。用药前体温增高有 69例 …     

左氧氟沙星的不良反应(二)

左氧氟沙星是第三代喹诺酮类抗菌药物 ,抗菌谱广 ,抗菌力强 ,广泛应用于临床。现将其不良反应简述如下。1　过敏反应患者 ,男 ,53岁 ,因支气管炎给予左氧氟沙星 0 .2ｇ,ｂｉｄ ,用药第 3天 ,出现全身皮肤潮红、瘙痒 ,眼睑、嘴唇水肿、气紧等症状 ,停药后经对症治疗 ,次日上述症状消失。 3个月后因前列腺炎第 2次服用左氧氟沙星 ,2ｈ后出现上述不良反应[1 ] 。2　耳鸣视物模糊患者 ,女 ,2 5岁 ,因发热寒战 ,咳嗽咽痛给予左氧氟沙星 2 0 0ｍｇ,静脉点滴 ,第 9天 ,患者出现头晕、耳鸣 ,感觉眼前光线逐渐变暗 ,次日感觉视物模糊至全黑 ,约 0 .5…     

抗菌新药普利沙星

普利沙星(prulifloxacin,PUFX)系日本新药公司研制的喹诺酮类抗菌药物,它是NM394的前体药物,代号为NM441,并与明治制果公司共同进行开发。今将本品简要介绍如下。 普利沙星的化学名为: (±)-6-氟-1-甲基-7-[4-(5-甲基-2-氧-1,3-二氧杂环戊烯-4-基)甲基-1-哌嗪基]-4-氧-4氢-[1,3]噻嗪[3,2-α]喹啉-3-羧酸 抗菌力 本品对革兰阳性菌和革兰阴性菌有广谱抗菌,特别是对以绿脓杆菌为首的革兰阴性菌的抗菌力强。 本品的抗菌力与诺氟沙星、氧氟沙星、左氟沙星、环丙     

左氧氟沙星致老年人不良反应25例分析

盐酸左氧氟沙星(levofloxacin,LOFLX)是新一代光学活性氟喹诺酮类抗菌药物,具有抗菌谱广,抗菌作用强的特点,适用于治疗包括厌氧菌在内的革兰阳性菌及革兰阴性菌引起的感染。其抗菌活性是氧氟沙星的2倍,耐药性低,安全性好。与其他喹诺酮类药物相比,其毒性小,不良反应常见为消化道反应,如厌食、恶心、便秘、腹泻,其发生率较低,一般耐受良好。此外有中枢兴奋,如失眠,头晕等。近年来,有文献报道左氧氟沙星出现不良反应,尤其对老年患者不良反应更为突出。本文对25例左氧氟沙星致老年人不良反应(ADR)进行分析探讨。1方法通过网络及手工检索,收…     

氟喹诺酮类药物的副作用

近20年来相继有新的氟喹诺酮类药物上市,其中诺氟沙星(norfloxacin)、环丙沙星(ciprofloxacin)及氧氟沙星(ofloxacin)对革兰阴性菌有较强的抗菌活性.近来开发的左氧氟沙星(levofloxacin)、加替沙星(gatifloxacin)及莫西沙星(moxifloxacin)提高了对革兰阳性菌及非典型病原菌的抗菌活性,但对铜绿假单胞菌的抗菌活性仍不及环丙沙星.克林沙星(clinafloxacin)、替马沙星(temafloxacin)、曲伐沙星(trovafloxacin)、格帕沙星(grepafloxacin)、培氟沙星(pefloxacin)、依诺沙星(enoxacin)、司帕沙星(sparfloxacin)及洛美沙星(lomefloxacin)等新开发的氟喹诺酮类药物均因各种毒副作用,未能继续或限用于临床.现在将临床常用的氟喹诺酮类药物分为4组:第1组:诺氟沙星;第2组:环丙沙星及氧氟沙星;第3组:左氧氟沙星;第4组:加替沙星及莫西沙星.大量研究表明:这6种药物均具良好耐受性,能相对安全地用于临床.虽然年龄不是发生副作用的独立危险因素,但老年人仍可能更多地发生各种氟喹诺酮类药物副作用,特别是当伴有肾功能不全及某些合并症时更应予以关注[1].     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

Lung disease and PKCs

The lung offers a rich opportunity for development of therapeutic strategies focused on isozymes of protein kinase C (PKCs). PKCs are important in many cellular responses in the lung, and existing therapies for pulmonary disorders are inadequate. The lung poses unique challenges as it interfaces with air and blood, contains a pulmonary and systemic circulation, and consists of many cell types. Key structures are bronchial and pulmonary vessels, branching airways, and distal air sacs defined by alveolar walls containing capillaries and interstitial space. The cellular composition of each vessel, airway, and alveolar wall is heterogeneous. Injurious environmental stimuli signal through PKCs and cause a variety of disorders. Edema formation and pulmonary hypertension (PHTN) result from derangements in endothelial, smooth muscle (SM), and/or adventitial fibroblast cell phenotype. Asthma, chronic obstructive pulmonary disease (COPD), and lung cancer are characterized by distinctive pathological changes in airway epithelial, SM, and mucous-generating cells. Acute and chronic pneumonitis and fibrosis occur in the alveolar space and interstitium with type 2 pneumocytes and interstitial fibroblasts/myofibroblasts playing a prominent role. At each site, inflammatory, immune, and vascular progenitor cells contribute to the injury and repair process. Many strategies have been used to investigate PKCs in lung injury. Isolated organ preparations and whole animal studies are powerful approaches especially when genetically engineered mice are used. More analysis of PKC isozymes in normal and diseased human lung tissue and cells is needed to complement this work. Since opposing or counter-regulatory effects of selected PKCs in the same cell or tissue have been found, it may be desirable to target more than one PKC isozyme and potentially in different directions. Because multiple signaling pathways contribute to the key cellular responses important in lung biology, therapeutic strategies targeting PKCs may be more effective if combined with inhibitors of other pathways for additive or synergistic effect. Mechanisms that regulate PKC activity, including phosphorylation and interaction with isozyme-specific binding proteins, are also potential therapeutic targets. Key isotypes of PKC involved in lung pathophysiology are summarized and current and evolving therapeutic approaches to target them are identified.     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

Gender-related symptoms and correlates of alcohol dependence among men and women with a lifetime diagnosis of alcohol use disorders

This study explored gender-related symptoms and correlates of alcohol dependence in a crosssectional study of 150 men and 150 women with a lifetime diagnosis of alcohol use disorders (AUD). Participants were recruited in equal numbers from treatment settings, correctional centres and the general community. Standardized measures were used to determine participants' use of substances, history of psychiatric disorders and psychosocial stress, their sensation seeking and family history of substance use and mental health disorders. Multivariate analyses were used to detect patterns of variables associated with gender and the lifetime severity of AUD. Men had a longer history of severe AUD than women. Women had similar levels of alcohol dependence and medical and psychological sequelae as men, despite 6 fewer years of AUD. More women than men had a history of severe psychosocial stress, severe dependence on other substances and antecedent mental health problems, especially mood and anxiety disorders. There were differences in family history of alcohol-related problems approximating same-gender aggregation. The severity of a lifetime AUD was predicted by its earlier age at onset and the occurrence of other disorders, especially anxiety, among both men and women. The limitations in the generalizability of these findings due to sample idiosyncrasies are discussed.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.