注射用美洛西林钠在四种常用输液中的稳定性实验

目的：研究注射用美洛西林钠在5％葡萄糖注射液等四种输液中的稳定性,为临床合理用药提供科学依据。方法：在室温(24℃左右)条件下,于0、0．5、l、2h考察配伍液的外观、pH值及美洛西林钠含量的变化。结果：与四种输液配伍后,其外观及pH值变化不大,但美洛西林钠含量下降。0、5h时含量下降10％左右。结论：美洛西林钠在四种常用输液中稳定性较差,临床应用以采用静脉注射为宜。     

3%氯化钠注射液细菌内毒素检查方法的考查

目的:考察不同温度(25℃、37℃)下6h内,美洛西林钠与木糖醇的配伍稳定性。方法:用紫外分光光度法测定配伍液中关洛西林含量,并观察外观、pH值的变化。结果:美洛西林钠与木糖醇输液配伍后6 h内,其外观,pH值以及含量均无明显变化。结论:美洛西林在上述条件下可以与木糖醇输液配伍使用。     

美洛西林钠与左氧氟沙星配伍稳定性及不溶性微粒的研究

目的　观察注射用美洛西林钠与左氧氟沙星注射液配伍的稳定性。方法　采用紫外分光光度法 ,测定美洛西林钠与左氧氟沙星注射液在配伍前后的 pH值和含量变化情况。 结果　 1 8℃～ 2 2℃、38℃±1℃下 8h内 ,配伍液外观澄明无色变 ,pH值、两药含量及不溶性微粒均无明显变化。 结论　 1 8℃～ 2 2℃、38℃± 1℃下 8h内 ,注射用美洛西林钠与左氧氟沙星注射液可以配伍使用     

美洛西林钠在果糖注射液和转化糖注射液中的稳定性考察

目的 考察美洛西林钠在果糖注射液和转化糖注射液中的稳定性.方法采用高效液相色谱法测定美洛西林钠与果糖注射液和转化糖注射液配伍一定时间后的含量.并观察其外观、pH值的变化.结果美洛西林钠与这两种注射液配伍,6h内其含量变化不大,溶液澄清,PH值稳定.结论 美洛西林钠可与果糖注射液和转化糖注射液配伍使用.     

头孢地嗪钠与5种输液的配伍稳定性考察

目的考察注射用头孢地嗪钠在5种常用输液（灭菌注射用水、0.9％氯化钠注射液、复方氯化钠注射液、5％葡萄糖注射液、10％葡萄糖注射液）中的稳定性。方法采用紫外分光光度法测定配伍后输液中头孢地嗪钠的含量，考察混合液的外观性状和pH值变化。结果头孢地嗪钠和5种输液混合后，在室温4h内配伍溶液的外观性状、pH值无明显变化。头孢地嗪钠含量仅有微小变化。基本保持稳定。结论室温4h内注射用头孢地嗪钠与5种输液可以配伍使用。     

美洛西林钠与4种常用输液配伍稳定性考察

目的:探讨美洛西林钠在5%葡萄糖、10%葡萄糖、0.9%氯化钠、葡萄糖氯化钠4种输液中的稳定性.方法:用高效液相色谱法测定配伍液中美洛西林钠的含量,并观察其外观、pH值的变化.结果:美洛西林钠在4种输液中的含量与温度有关,温度越高,含量下降越快.在5%葡萄糖注射液中2 h内含量为101%(25℃)、95.3%(35℃);在10%葡萄糖注射液中4 h内含量为98.9%(25℃)、95.4%(35℃),在0.9%氯化钠注射液中8 h内含量为100.4%(25℃)、97.6%(35℃);在葡萄糖氯化钠注射液中12 h内含量为98.4%(25℃)、97.5%(35℃).结论:美洛西林钠与4种输液可以配伍应用.     

盐酸洛美沙星在常用输液中的稳定性考察

目的测定注射用盐酸洛关沙星在5种输液中的稳定性。方法应用紫外分光光度法，将临床用量的盐酸洛美沙星溶于输液中，再稀释到待测浓度，观察其外观并测定pH值、含量、微粒、回收率等。结果在25℃和其他条件平行的情况下，盐酸洛关沙星与氯化钠注射液和葡萄糖氯化钠注射液配伍会出现白色浑浊，与5％及10％葡萄糖注射液、乳酸钠注射液这3种输液配伍后外观无明显变化。结论临床上，盐酸洛关沙星与0．9％氯化钠注射液和葡萄糖氯化钠注射液不宜配伍，与其他3种输液可以配伍。     

美洛西林钠与卡络磺钠在5%葡萄糖注射液中配伍稳定性考察

目的:考察室温(25℃)下注射用美洛西林钠与注射用卡络磺钠在5%葡萄糖注射液中的配伍稳定性。方法:采用反相高效液相色谱法-二极管阵列检测器分别测定美洛西林钠与卡络磺钠在5%葡萄糖注射液中配伍后0～4 h内的含量及pH变化,并观察配伍液的外观变化。结果:4 h内注射用美洛西林钠与注射用卡络磺钠在5%葡萄糖注射液中配伍液外观、pH及含量均无明显变化。结论:在室温(25℃)下,注射用美洛西林钠与注射用卡络磺钠在5%葡萄糖注射液中4 h内配伍稳定。     

美洛西林的钠在八种输液中的稳定性

用紫外分光光度法注射用美洛西林钠的含量,并考察其在八种常用输液中的稳定性。结果：注射用美洛西林钠与低分子右旋糖酐４０－－葡萄糖注射液、复方氨基酸注射液、葡萄糖氯化钠注射液、氯化钠注射液、乳酸钠林格注射液、１０％葡萄糖注射液、５％葡萄糖注射液配伍在２０℃条件下Ｔ０．９０大于或拉近４小时,而与碳酸氢钠注射液配伍显示出极不稳定,２４小时内含量下降到８２．７％。     

头孢尼西钠与4种输液配伍的稳定性

目的考察头孢尼西钠与4种输液配伍的稳定性。方法采用紫外分光光度法测定5%葡萄糖注射液、10%葡萄糖注射液、葡萄糖氯化钠注射液和0.9%氯化钠注射液中头孢尼西钠的含量。考察混合液的外观性状和pH值变化，测定配伍后头孢尼西钠的含量。结果头孢尼西钠与4种输液混合后，溶液的pH值和外观性状无明显变化，头孢尼西钠的含量稳定。 结论头孢尼西钠和4种输液配伍后在5 h内稳定性无明显变化。     

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.     

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.     

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.