盐酸氨溴索与维生素B6注射液的配伍考察

目的考察在25±2℃下8h内,盐酸氨溴索注射液与维生素B6注射液的配伍稳定性。方法采用紫外双波长分光光度法测定配伍后0、2、4、6、8h时盐酸氨溴索和维生素B6的含量变化,同时观察其紫外吸收光谱、外观、pH值等变化。结果25±2℃下8h内,盐酸氨溴索注射液与维生素B6注射液配伍后含量、紫外吸收光谱、外观、pH几乎无变化。结论8h内盐酸氨溴索与维生素B6注射液配伍基本稳定。     

盐酸氨溴索注射液与注射用加替沙星的配伍稳定性考察

目的：考察25℃与37℃下,盐酸氨溴索注射液与注射用加替沙星在0．9％氯化钠注射液中的配伍稳定性。方法：采用RP-HPLC-二极管阵列检测器测定盐酸氨溴索与加替沙星在0．9％氯化钠注射液中配伍后8h内各时间段的含量,同时测定pH,观察配伍液的外观变化。结果：在25℃与37℃下、8h内,配伍液外观、pH及含量均无明显变化。结论：盐酸氨溴索注射液与注射用加替沙星在0．9％氯化钠注射液中8h,pH、外观、含量基本无变化,微粒检测等尚有待进一步试验。     

注射用头孢替安与盐酸氨溴索注射液的配伍稳定性考察

目的:考察室温下注射用盐酸头孢替安与盐酸氨溴索注射液在0.9%氯化钠注射液中的配伍稳定性。方法:采用反相高效液相色谱法-二极管阵列检测器测定配伍液0～8h头孢替安与盐酸氨溴索的含量,同时测定pH值,并观察配伍液的外观变化。结果:在室温((20±1)℃)下、8h内,配伍液外观、pH值及含量均变化明显。结论:在室温((20±1)℃)下,在盐酸头孢替安与盐酸氨溴索注射液不宜在0.9%氯化钠注射液中配伍使用。     

头孢替唑钠与盐酸氨溴索在0．9％氯化钠注射液中配伍稳定性考察

目的：考察室温（25±1）℃下,注射用头孢替唑钠与盐酸氨溴索注射液在0．9％氯化钠注射液中的配伍稳定性。方法：采用反相高效液相色谱法-二极管阵列检测器测定头孢替唑钠与盐酸氨溴索配伍后8h内各时间段的含量,同时测定pH,观察配伍液的外观变化。结果：8h内配伍液外观、pH及含量均无明显变化。结论：在室温（25±1）℃8h内,注射用头孢替唑钠与盐酸氨溴索注射液在0．9％氯化钠注射液中配伍时二者含量和pH稳定。     

反相高效液相色谱法-二极管阵列检测器考察盐酸氨溴索注射液与注射用头孢唑肟钠配伍稳定性

目的考察盐酸氨溴索注射液与注射用头孢唑肟钠分别在5％葡萄糖注射液和0．9％氯化钠注射液中的配伍稳定性。方法在室温[（22±1）℃]下,采用反相高效液相色谱法-二极管阵列检测器测定盐酸氨溴索与头孢唑肟钠配伍后0～6h内的含量变化,并观察配伍液的外观及pH。结果6h内混合液外观、pH无明显变化,盐酸氨溴索在5％葡萄糖注射液其含量在0～6h内变化为：100％、99．5％、99．2％、98．8％、99％、98．2％、98．6％;在0．9％氯化钠注射液中0～6h内变化为：100％、99．1％、99．5％、99．4％、100．7％、100．3％、100．1％。头孢唑肟在5％葡萄糖注射液中其含量为100％、100．2％、100．5％、99．8％、98．3％、99．3％、99％;在0．9％氯化钠注射液其含量为100％、99．5％、99．7％、99．3％、99．8％、98．9％、98．6％,表明该配伍试验基本稳定。结论在室温[（22±1）℃]条件下,盐酸氨溴索注射液与注射用头孢唑肟钠在5％葡萄糖注射液和0．9％氯化钠注射液中6h内配伍稳定。     

以甲硝唑为基础配伍的2组抗胆道感染药物的稳定性研究

目的　探讨甲硝唑葡萄糖注射液 (甲硝唑G)与头孢唑啉钠、头孢曲松钠配伍的稳定性及贮存期。方法　借紫外分光光度法测定甲硝唑、头孢唑啉钠、头孢曲松钠的含量 ;用经典恒温法、留样观察法考察甲硝唑G 头孢唑啉钠及甲硝唑G 头孢曲松钠配伍液的含量、pH值及外观的变化。结果　甲硝唑、头孢唑啉钠、头孢曲松钠的线性范围分别为 2 0 1～ 2 0 0 8mg·L-1、5 0 7～ 30 4 2mg·L-1、4 0 3～ 2 0 16mg·L-1;平均回收率依次为 (99 5 8± 1 6 3) %、(99 78± 1 2 3) %、(99 93± 0 96 ) % ;70℃ ,8h内的热分解产物不干扰测定。恒温加速试验时 ,配伍液中甲硝唑稳定 ;头孢唑啉钠、头孢曲松钠降解均遵循一级动力学反应 ,2 0℃的T0 9分别为 2 6 0 8d和 6 0 7d ,T1/ 2 为 171 5 4d和 39 95d ;溶液颜色有随温度、时间递增而加深的趋势。室温 (2 0℃±1℃ ) ,0～ 12 0h内留样观察 ,配伍前后药物残存率 >95 % ,pH值、外观均无明显改变。 结论　高温 (5 0、6 0、70℃ )下 ,甲硝唑稳定 ,头孢唑啉钠、头孢曲松钠随温度、时间递增而逐渐降解 ;室温下 ,0～ 12 0h内 ,2组配伍液的含量变化在允许范围内 (<5 % ) ,pH值、外观无明显变化 ,可以配伍使用     

阿奇霉素与氨溴索的配伍稳定性考察

目的:考察注射用乳糖酸阿奇霉素与盐酸氨溴索注射液的配伍稳定性.方法:观察注射用乳糖酸阿奇霉素与盐酸氨溴索注射液配伍后于室温避光放置24h内的外观、pH及不溶性微粒的变化,并采用高效液相色谱法测定配伍液中阿奇霉素、氨溴索的含量.结果:室温、避光条件下,注射用乳糖酸阿奇霉素、盐酸氨溴索注射液加入5％葡萄糖注射液和0.9％氯化钠注射液中,在24h内配伍液的外观、pH均无明显变化,微粒数目不断减少,含量测定结果显示氨溴索在以5％葡萄糖为溶媒的配伍液和以0.9％氯化钠为溶媒的配伍液中,24h内含量无明显变化;阿奇霉素以5％葡萄糖为溶媒的配伍液中24h内含量无明显变化,但在以0.9％氯化钠为溶媒的配伍液中16 h后含量有所下降.结论:最终浓度分别为4.31,1.03或小于4.31,1.03 mg·ml-1的乳糖酸阿奇霉素和盐酸氨溴索以5％葡萄糖为溶媒的配伍液在24 h内使用较安全,以0.9％氯化钠为溶媒的配伍液建议在8h内使用.     

盐酸氨溴索注射液在果糖注射液中的配伍稳定性研究

目的考察25℃和37℃下盐酸氨溴索注射液在果糖注射液中配伍的稳定性。方法采用高效液相色谱法测定氨溴索与果糖注射液配伍一定时间后的含量,同时观察外观变化并测定其pH值。结果药物在25℃和37℃果糖注射液中配伍后,0-8 h内其外观、pH值及含量均无明显变化。结论两药液配伍后在8 h内稳定,可配伍使用。     

盐酸氨溴索注射液在果糖注射液中的配伍稳定性研究

目的 考察25 ℃和37 ℃下盐酸氨溴索注射液在果糖注射液中配伍的稳定性。方法 采用高效液相色谱法测定氨溴索与果糖注射液配伍一定时间后的含量,同时观察外观变化并测定其pH值。结果 药物在25 ℃和37 ℃果糖注射液中配伍后,0~8 h内其外观、pH值及含量均无明显变化。结论 两药液配伍后在8 h内稳定,可配伍使用。     

头孢哌酮钠在输液中与临床常用7种注射剂稳定性探讨

目的探讨头孢哌酮钠在0．9％氯化钠溶液中与维生素C等7种注射剂配伍的稳定性．为临床舍理用药提供依据。方法选择在25℃‘室温’时观察配伍液的外观、pH及头孢哌酮钠的紫外光谱的变化,用紫外分光光度法测定头孢哌酮钠的含量。结果配伍液在实验鼋件下与盐酸氨溴索产生白色沉淀;与氨荼碱配伍时超过5h含量无明显变化．但颜色呈淡黄色,其它配伍液的外观、pH值及含量无明显变化。结论在25℃时,头孢哌酮钠与盐酸氨溴索不能配伍使用,与氨荼碱配伍时最好5h内使用,与其它5种注射剂配伍在6h内稳定,可以配伍使用。     

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.