奥门丁与头孢拉定随机对照治疗细菌性感染

奥格门丁是棒酸与羟氨苄青霉素的复方制剂，内含羟氨苄青霉素１．０ｇ，棒酸０．２ｇ。本组所用奥格门丁静脉注射针剂为英国比切姆公司原粉，由华北制药厂生产提供。本组试验共治疗细菌性感染４２例，其中１６例试验药奥格门丁与对照药头孢拉定１６例进行随机对照临床试验试验，两组临床痊愈显效率分别为８７．５％与８１．３％，细菌消除率分别为８３．３％与８１．３％；奥格门丁共观察２６例（开放１０例，随机对照１６例），临床     

爱维治注射液

用国产环丙氟哌酸与对照药头孢氨苄，氟哌酸进行随机对照临床试验，剂量分别为：环丙氟哌酸和氟哌酸400－800mg/d，头孢氨苄3－6g/d,2-3次／d；口服，疗程7－14天，环丙氟哌酸与头孢氨苄对照治疗呼吸道及皮肤软组织等感染22例，痊愈显效率分别为90．9％和81．8％，细菌消除率分别为100％和77．8％，本组试验药与对照药统计处理均无显著性差异，环丙氟哌酸和氟哌酸治疗泌尿系统感染48例，痊愈显效率分别为95．8％与91．6％，细菌消除率分别为100％和92％，本组试验药与对照药统计处理均无显著性差异。试验药环丙氟哌酸共治疗35例，痊愈显效率为94．3％，细菌消除率为100％。，不良反应发生率为8．3％。     

克拉维酸钾羟氨苄青霉素分散片的人体生物利用度

目的 :研究克拉维酸钾羟氨苄青霉素分散片在健康志愿者体内的相对生物利用度。方法 :交叉口服单剂量克拉维酸钾羟氨苄青霉素分散片 (受试制剂 )和克拉维酸钾羟氨苄青霉素片 (参比制剂 ) ,用反相高效液相色谱法测定人血清中克拉维酸钾和羟氨苄青霉素的浓度。使用NDST程序对各药物动力学参数进行方差分析和双单侧t检验。结果 :受试制剂的克拉维酸钾和羟氨苄青霉素的AUC0→ 8,cmax,tmax,T1/ 2 分别为 (3 18± 1 5 8)h·μg·mL-1,(1 5 0± 0 90 ) μg·mL-1,(1 33± 0 5 9)h ,(1 0 2±0 34 )h和 (13 6 6± 1 16 )h·μg·mL-1,(6 5 5± 1 46 ) μg·mL-1,(1 0 3± 0 42 )h ,(1 15± 0 32 )h ;参比制剂的克拉维酸钾和羟氨苄青霉素的AUC0→ 8,cmax,tmax,T1/ 2 分别为 (2 76± 0 84)h·μg·mL-1,(1 32± 0 47)h·μg·mL-1,(1 5 3± 0 71)h ,(1 2 8± 0 5 1)h和(11 0 3± 1 5 3)h·μg·mL-1,(5 0 8± 1 2 8) μg·mL-1,(1 0 5± 0 2 6 )h ,(1 0 4± 0 47)h。受试制剂中克拉维酸钾和羟氨苄青霉素的相对生物利用度分别为 112 80 %和 12 6 14%。克拉维酸钾的AUC0→ 8和cmax在 2药间比较无显著差异 ,而羟氨苄青霉素的AUC0→ 8和cmax具显著差异 ,受试制剂中较高。结论 :受试制剂和参比制剂不具生     

奥格门汀的药理及临床应用

奥格门汀(Augmentin)又名安灭菌,系克拉维酸(棒酸)强化羟氨苄青霉素,是英国比切姆公司研究的一项成果。1991年该公司同华北制药厂合作生产。奥门汀是由羟氨苄青霉素(1.0g)和β—内酰胺酶抑制剂—克拉维酸(0.2g)复合而成。本文就奥格门汀的药理及临     

β-内酰胺酶抑制剂棒酸和羟氨苄青霉素联合应用治疗β-内 酰胺酶产生菌卡他奈瑟氏菌引起的支气管肺部感染

棒酸(clavulanic acid)是从带棒链霉菌分离得到的一个新的β-内酰胺酶抑制剂。当它和其他β-内酰胺抗生素,尤其是和羟氨苄青霉素联合应用时,呈现显著的协同抗菌作用。作者联合应用棒酸和羟氨苄青霉素成功的治疗了三例产生β-内酰胺酶的卡他奈瑟氏菌引起的呼吸系统感染。作者报道的三例病人均为退休的患有矽肺病的煤矿工人,具有慢性支气管急性加重的临床表现,其临床特征为:咳脓性痰、咳嗽加剧、呼吸困难及发热。作者通过气管穿刺分离致病菌。用捧酸和羟氨苄青霉素的复合制剂——BRL25000(每片含羟氨苄青霉素25Cmg和棒酸     

反相高效液相色谱法测定人体血浆中克拉维酸钾羟氨苄青霉素的含量

目的 :采用反相高效液相色谱法同时测定服用克拉维酸钾羟氨苄青霉素颗粒剂和片剂后人血浆中的克拉维酸和羟氨苄青霉素的浓度。方法 :以ODS柱为分析柱 ,磷酸盐缓冲液 -三乙胺缓冲液 -甲醇 ( 87∶1 3∶2 5) ,用磷酸调 pH至 3作流动相 ,柱温 :3 5℃ ;检测波长 :2 2 2nm。 结果 :本法中羟氨苄青霉素的平均回收率为 99 0 1 %～ 99 75% ,RSD为 1 7%～ 3 2 % ;克拉维酸钾的平均回收率为 97 95%～ 1 0 0 0 % ,RSD为 0 8%～ 2 0 %。 2种药物的日内和日间RSD小于 6 4 % ,血浆中的标准曲线相关良好 ,克拉维酸和羟氨苄青霉素在血浆中的最低检测浓度分别为 0 2 4和 0 2 5μg·mL- 1。结论 :以此条件可对克拉维酸钾羟氨苄青霉素进行药代动力学参数研究     

酶抑制剂对β-内酰胺抗生素体外抗菌作用的影响

本文报导两种酶抑制剂——棒酸与青霉烷砜,分别和青霉素G、氨苄青霉素、羟氨苄青霉素、头孢哌酮4种β-内酰胺抗生素联合对产酶金黄色葡萄球菌、大肠杆菌、绿脓杆菌等82株耐药细菌的协同作用。棒酸的抑酶活性一般强于青霉烷砜;两种酶抑制剂浓度愈高,抗生素对细菌的MIC愈低;就胞外酶(金葡菌)和胞内酶(大肠杆菌)而言,酶抑制剂的作用对前者更为明显。     

一种耐β-内酰胺酶的抗生素复合剂:羟氨苄青霉素-棒酸钾盐‘Augmentin’

棒酸(Clavulanic acid)是由Str.clavuligerus 产生的β-内酰胺酶抑制剂。细菌对青霉素类和头孢菌素类耐药最主要原因之一,就是通过产生β-内酰胺酶破坏上述抗生素的β-内酰胺环,使药物失活。棒酸能渗入到细菌的胞壁与胞内和胞外的β-内酰胺酶相结合,形成一种无活性的非可逆性的酶产物。棒酸单独使用时,对大多数细菌只有较弱的抗菌活性,而与羟氨苄青霉素(Amoxicillin,下简称AM)联用     

羟氨苄青霉素,梅毒和HIV感染

本文采用双盲、安慰剂对照试验,用羟氨苄青霉素对有梅毒既往史的HIV(人体免疫缺陷病毒)阳性患者进行了重新治疗,患者每日2次给予羟氨苄青霉素3g加丙磺舒0.5g,共3周,并口服制霉菌素混悬液以防口腔念珠菌病,对照组以乳糖代替羟氨苄青霉素。对使用Zidovudine或治疗不足14天者不进行分析评价。结果,总共24人有23人用药后参加评价。服用羟氨苄青霉素的12人(治疗组),6     

优立新的体外抗菌活性及其对感染病人的临床应用研究

本文报道优立新对临床分离的72株细菌的体外抗菌活性,与氨苄青霉素比较证实,优立新的抗菌活性明显优于氨苄青霉素。临床观察治疗各种细菌感染16例,痊愈及显效10例,好转4例,2例无效,不良反应少见。     

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.

     

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.     

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.     

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.     

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.