苯妥英锌对大鼠血脂的影响

考察了大鼠口服苯妥英锌或苯妥英钠１５ｍｇ／（ｋｇ·ｄ）４５ｄ对血脂的影响。服药前后比较，苯妥英锌使大鼠血清ＨＤＬ－Ｃ和ＨＤＬ－Ｃ／ＴＣ分别上升８％和１７％（ｐ＜０．０５），（ＬＤＬ＋ＶＬＤＬ）－Ｃ下降３４％（ｐ＜０．０１）；苯妥英钠则使大鼠血清ＨＤＬ－Ｃ和ＨＤＬ－Ｃ／ＴＣ分别下降３７％（ｐ＜０．０１）和２１％（ｐ＜０．０５），（ＬＤＬ＋ＶＬＤＬ）－Ｃ上升３０％（ｐ＜０．０５）。     

脂必妥对大鼠高脂血症模型血脂水平的影响

目的：研究脂必妥的降脂疗效。方法：通过对大鼠腹腔注射脂酶抑制剂——１０％泰洛沙泊溶液（３ｍＬ／ｋｇ）后７ｍｉｎ，分别用脂必妥２．５９，１．２９，０．６５ｇ／ｋｇ，及洛伐他汀１０ｍｇ／ｋｇ灌胃给药。结果：脂必妥２．５９ｇ／ｋｇ组及洛伐他汀组（１０ｍｇ／ｋｇ）的胆固醇（ＴＣ）值分别降低３３％（Ｐ＜０．０１）及３１％（Ｐ＜０．０１），组间比较Ｐ＞０．０５；低密度脂蛋白胆固醇（ＬＤＬ－ｃｈ）值分别降低５０％（Ｐ＜０．０１）及４４％（Ｐ＜０．０１）；脂必妥１．２９ｇ／ｋｇ组亦能降低ＴＣ及ＬＤＬ－ｃｈ值１８％（Ｐ＜０．０５）及２６％（Ｐ＜０．０５）；小剂量０．６５ｇ／ｋｇ的脂必妥仅能降低ＴＣ１４％（Ｐ＜０．０５）；各组对三酰甘油（ＴＧ）值均无显著降低作用（Ｐ＞０．０５）。结论：脂必妥有显著降低血脂过多大鼠ＴＣ及ＬＤＬ－ｃｈ值的作用。     

盐酸克林霉素棕榈酸酯颗粒剂治疗细菌性感染临床疗效观察

采用随机对照开放临床试验，对克林霉素棕榈酸酯（ＣＬ－ＰＩ）颗粒剂进行了临床疗效评价，共治疗各种细菌性感染１１２例，其中５０例与盐酸克林霉素（ＣＬ）胶囊随机对照。结果显示随机对照组ＣＬ－ＰＩ和ＣＬ有效率分别为９６．００％（４８／５０）和９６．７２％（５９／６１）（Ｐ＞０．０５），细菌阴转率分别为９１．１１％（４１／４５）和９６．３６％（５３／５５）（Ｐ＞０．０５），均无显著性差异。ＣＬ－ＰＩ开放组治疗感染５０例，有效率为８８．００％（４４／５０），细菌阴转率为９３．６２％（４４／４７）。ＣＬ－ＰＩ单独治疗厌氧菌感染１２例，有效率为８３．３３％（１０／１２），细菌阴转率为９１．６７％（１１／１２），ＣＬ－ＰＩ组总不良反应发生率为１５．１８％（１７／１１２），主要表现为胃肠道反应。个别病人有皮疹，未见肝肾功能损害和伪膜性肠炎的发生。     

高效毛细管电泳测定盐酸小檗碱脂质体包封率

目的：建立一个快速、简便且经济的盐酸小檗碱脂质体包封率测定方法。方法：采用高效毛细管电泳法，分析条件为，石英毛细管，７０ｃｍ×７５μｍｉｄ；温度，２０℃，运行缓冲液，１０ｍｍｏｌ／Ｌ磷酸氢二钠（０１ｍｏｌ／Ｌ氢氧化钠调至ｐＨ１０８１）；运行电压，３０ｋｖ；检测波长，２５４ｎｍ。结果：线性范围１００～５０００ｍｇ／Ｌ，ｒ＝０９９８９，平均回收率９８７％（ｎ＝５），ＲＳＤ＝３５１％，薄膜分散法的包封率（１９５±２３）％远高于乙醇注入法的包封率（８３±３７）％。结论：本法适用于盐酸小檗碱脂质体包封率测定     

二氢小檗碱在家兔体内的口服药代动力学研究

本实验应用反相高效液相色谱法研究了家兔灌胃二氢小檗碱的吸收情况及药代动力学参数。结果表明，在本实验条件下，家兔灌胃二氢小檗碱有一定的吸收，其药－时曲线符合一室模型。药代动力学参数ｋａ１．０４９ｈ－１，ｋｅ０．２９８ｈ－１，Ｔ１／２（ｋａ）０．６６１ｈ，Ｔ１／２（ｋｅ）２．３２８ｈ，Ｔ（ｐｅａｋ）１．６７６ｈ，Ｃ（ｍａｘ）２４１．７３μｇ．Ｌ－１，ＡＵＣ１３３７．３２μｇ．ｈ－１．Ｌ－１。血清中二氢小檗碱最低检测浓度为２０μｇ．Ｌ－１。     

非胰岛素依赖型糖尿病患者血清D—二聚体的变化及其意义

为探讨非胰岛素依赖型糖尿病（ＮＩＤＤＭ）患者凝血及纤溶活性，采用ＥＬＩＳＡ双抗体夹心法测定了３５例ＮＩＤＤＭ患者的血清Ｄ－二聚体，结果：ＮＩＤＤＭ患者血清Ｄ－二聚体水平为１．６３ｍｇ／Ｌ±０．１４ｍｇ／Ｌ），明显高于正常对照组（０．３３ｍｇ／Ｌ±０．０９ｍｇ／Ｌ）（Ｐ〈０．０５）；有血管病变组Ｄ－二聚体为２．６２ｍｇ／Ｌ±０．６８ｍｇ／Ｌ，高于无血管病变组（０．６９ｍｇ／Ｌ±０．６８ｍｇ／Ｌ），差     

磷灰石析出法治疗牙本质过敏的临床研究

目的 观察碳酸氢钠和氟化钠混合液治疗牙本质过敏的临床疗效。方法 实验组使１ｍｏｌ／Ｌ浓度碳酸氢钠和０．４８ｍｏｌ／Ｌ浓度氟化钠混合液治疗;对照组用０．４８ｍｏｌ／Ｌ浓度的氟化钠溶液治疗,记录第三次治疗后的疗效。结果 实验组：显效５８例（９６．６７％）、有效２例（３．３３％）、无效０例（０．００％）,总有效６０例（１００．００％）。对照组：显效２４例（４０．００％）、有效３３例（５５．００％）、无效３例（５．００％）,总有效５７例（９５．００％）。两组总有效率无显著差异（Ｐ〉０．０５）。两组显效率有显著差异（Ｐ〈０．０２）。结论 １ｍｏｌ／Ｌ浓度的碳酸氢钠和。０．４８ｍｏｌ／Ｌ浓度的氟化钠混合液,是一种强有效的牙本质脱敏剂。     

洛美沙星治疗淋病临床疗效对比观察

观察了国产洛美沙星与氧氟沙星随机对照治疗无合并症淋病１０１例的临床疗效及不良反应。洛美沙星组５８例，氧氟沙星组４３例。男性病人８７例服用洛美沙星或氧氟沙星２００ｍｇ，每日２次，２天；女性病人１４例服４００ｍｇ，每日２次，２天。两药临床治愈率分别为９３．１％（５４／５８）和９０．７％（３９／４３），无显著性差异（Ｐ＞０．０５）。细菌清除率分别为９６．６％（５６／５８）和９３．０２％（４０／４３）。其不良反应发生率分别为１．７％（１／５８）和２．３％（１／４３），反应轻微。洛美沙星、氧氟沙星、环丙沙星、头孢曲松、青霉素和大观霉素对５６株淋球菌的ＭＩＣ＿（５０）／ＭＩＣ＿（９０）（ｍｇ／Ｌ）为０．０６／０．２５、０．０６／０．１２５、０．０６／０．１２５、０．０６／０．２５、０．５／１．０和１６／３２。     

反相高效液相色谱法测定天门冬氨酸洛美沙星及其注射液的含量

建立了天门冬氨酸洛美沙星及其注射液的高效液相色谱法．在ＯＤＳ柱上，以０．０５ｍｏｌ／Ｌ柠檬酸—乙腈（８０∶２０，用三乙胺调ｐＨ至４．０）为流动相，于２５８ｎｍ波长检测，流速１．０ｍＬ／ｍｉｎ，苯甲酸钠作内标，天门冬氨酸洛美沙星和内标的保留时间分别为６．４和１０．９ｍｉｎ．线性范围为０．０５～０．３ｇ／Ｌ，平均回收率为９９．４％（ｎ＝６），ＲＳＤ＝０．４％．     

HPLC法测定吗氯贝胺片的含量

建立了测定片剂中吗氯贝胺的ＨＰＬＣ方法，色谱条件为ＷａｔｅｒｓＣ１８色谱柱，乙腈－０．０５ｍｏｌ／Ｌ醋酸铵溶液－冰醋酸（２５：７５：１．５）为流动相，２５４ｎｍ检测波长，咖啡因为内标，该法简便，灵敏，准确，吗氯贝胺在１９．８～１９８．０ｍｇ／Ｌ浓度内线性关系良好（ｒ＝０．９９９９），平均回收率为１００．０％，（ＲＳＤ＝０．１７％，ｎ＝５）。     

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.     

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.     

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.