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…     

氟喹诺酮类药物的临床应用

氟喹诺酮类药物 (ＦＱＮＳ)的作用机制是抑制细菌ＤＮＡ螺旋酶 ,故与其他抗菌药无交叉耐药性。近十年来 ,此类药物使用迅猛发展 ,以环丙沙星为例 ,1 996年全球销售额达 1 5亿美元 ,治疗人数 1 .5亿 ,占当年抗菌药首位[1 ] 。ＦＱＮＳ最常用品种有诺氟沙星、氧氟沙星、环丙沙星等 ,诺氟沙星主要用于肠道、泌尿道感染 ,某些地区[2 ] 伤寒杆菌仍对其具有较高敏感性。环丙沙星是ＦＱＮＳ中对革兰阴性杆菌活性最强的一种 ,其抗菌谱甚至比头孢哌酮 舒巴坦更广[3 ] ,氧氟沙星对革兰阳性球菌作用更强。由于许多ＦＱＮＳ口服生物利用度好(氧氟沙星口服生物利用度 99% ,左氧氟沙星达到 1 0 0 % [4] ) ,临床上可以静脉用药 1～ 2ｄ改为口服 ,大大减少了用药程序。最近研究发现[5] ,许多药物的抗菌活性与药物的高峰浓度密切相关 ,体内抗菌药物在一定时间内达到有效血药浓度即有稳定的杀菌效果 ,即抗生素后效应 (ＰＡＥ)。ＦＱＮＳ具有较长的血药半衰期和ＰＡＥ ,常用品种中以环丙沙星和氧氟沙星最长 ,对一般轻度感染每日用药 1次即可 ,临床使用方便、有效 ,减少了不良反应的发生和细菌耐药性。新品种如司...     

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.

     

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.     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.     

Glycofection: The Ubiquitous Roles of Sugar Bound on Glycoplexes

Glycofection (transfection by using sugar-substituted polylysine) was assessed in order to provide an alternative to viral vectors for the transfer of genes into vascular smooth muscle cells. A rabbit vascular smooth muscle cell line (Rb-1 cells) was selectively transfected by using glycoplexes (glycosylated polylysine/pSV2LUC complexes) in the presence of 10 mu M of the fusogenic peptide GALA. A sugar-specific transfection was obtained when the glycofection was conducted for 1 h with glycoplexes containing either alpha Gal, alpha -Glc, alpha -GalNAc, beta -GlcNAc, or beta -GalNAc residues. The gene expression was high after transfection, with glycoplexes bearing alpha Gal, alpha -GalNAc, or beta -GalNAc residues that were weakly internalized, and low with glycoplexes carrying Lact or Rha residues that were well taken up by cells. These results suggest that 1) glycofection can be a good approach for a selective transfer of genes intovascular smooth muscle cells, 2) an efficient uptake of the glycoplexes is not the unique limiting step for an efficient transfection, and 3) the sugar-dependent trafficking of the glycoplexes inside the cells may account for the transfection efficiency.     

直肠癌下切缘病理组织学分析

目的探讨直肠癌逆向浸润与下切缘的安全距离的关系。方法对36例直肠癌Miles手术和Dixon手术后标本的肿瘤下缘1.0cm、2.0cm、3.0cm的肠壁及对应的系膜病理组织学检查,观察直肠癌逆向浸润或转移的距离。结果36例直肠癌标本距癌肿下缘1.0 cm、2.0cm、3.0cm的肠壁及对应的系膜病理组织学检查均为阴性,结论直肠癌远恻逆向浸润或转移未见超过1.0cm,因此认为保肛手术时切除肿瘤远侧肠管(包括系膜)2.0cm是安全的。