利巴韦林和氟罗沙星葡萄糖注射液的配伍稳定性考察

目的:建立3％氯化钠注射液的细菌内毒素检查法。方法:确定3％氯化钠注射液的细菌内毒素限值,并进行干扰实验,考察确立3％氯化钠注射液细菌内毒素检查法。结果:3％氯化钠注射液原液不干扰鲎试剂与细菌内毒素的凝胶反应。结论:可用细菌内毒素检查法替代家兔法对3％氯化钠注射液的热原检查。     

甘油氯化钠注射液细菌内毒素检查法的研究

目的介绍细菌内毒素法对甘油氯化钠注射液热原的研究。方法应用鲎试剂检查甘油氯化钠注射液的热原,观察甘油氯化钠注射液对细菌内毒素检查法的干扰现象。结果甘油氯化钠注射液稀释2倍对细菌内毒素检查法无干扰行为。结论对甘油氯化钠注射液进行2倍稀释以0.5EU/ml的鲎试剂检查其热原是可行的。     

依托米酯注射液细菌内毒素检测法的实验研究

目的建立依托米酯注射液的细菌内毒素检查方法。方法用两个生产厂的鲎试剂对依托米酯注射液进行干扰试验研究。结果依托米酯注射液对细菌内毒素检查无干扰作用。结论可以用细菌内毒素检查法(凝胶法)代替家兔热原检查法控制其热原。     

盐酸罂粟碱氯化钠注射液细菌内毒素检测法实验研究

目的：建立盐酸罂粟碱氯化钠注射液的细茵内毒素检查方法。方法：用两个生产厂的鲎试剂对盐酸罂粟碱氯化钠注射液进行干扰试验研究。结果：盐酸罂粟碱氯化钠注射液对细茵内毒素检查无干扰作用。结论：可以用细茵内毒素检查法(凝胶法)代替家兔热原检查法控制其热原。     

细胞色素C注射液细菌内毒素检测法研究

目的: 建立细胞色素C注射液的细菌内毒素检查方法.方法: 用两个生产厂的鲎试剂对细胞色素C注射液进行干扰试验研究.结果: 细胞色素C注射液对细菌内毒素检查无干扰作用.结论: 可以用细菌内毒素检查法(凝胶法)代替家兔热原检查法控制其热原.     

环丙沙星氯化钠注射液细菌内毒素检查法的研究

目的：探讨环丙沙星氯化钠注射液应用于细菌内毒素检查法的可行性。方法：制定实验,不同灵敏度的鲎试剂对环丙沙星氯化钠注射液进行干扰试验,将细菌内毒素检查法和热原检查法结果进行比较。结果：环丙沙星氯化钠注射液液稀释2倍后,对细菌内毒素检查无干扰作用,细菌内毒素检查法和热原检查法经比较完全相符。结论：通过系列实验,说明环丙沙星氯化钠注射液细菌内毒素检查法可替代热原检查法。     

鲎试剂法检测肝脑清注射液中细菌内毒素

目的: 探讨肝脑清注射液中细菌内毒素鲎试剂检查法.方法: 用不同厂家的鲎试剂对不同批号的肝脑清注射液分别进行干扰试验,考察确立肝脑清注射液细菌内毒素检查法.结果: 肝脑清注射液不干扰鲎试剂与细菌内毒素的凝集反应.结论: 肝脑清注射液可以用鲎试剂检查法取代家兔热原检查法.     

盐酸氨溴索葡萄糖注射液的细菌内毒素检测

目的:建立盐酸氨溴索葡萄糖注射液的细菌内毒素检查方法.方法:用两个生产厂家的鲎试剂对盐酸氨溴索葡萄糖注射液进行干扰试验研究.结果:盐酸氨溴索葡萄糖注射液对细菌内毒素检查无干扰.结论:可以用细菌内毒素检查法(凝胶法)代替家兔热原检查法控制盐酸氨溴索葡萄糖注射液的热原.     

环磷腺苷注射液细菌内毒素检查方法探讨

目的:探讨环磷腺苷注射液细菌内毒素检查方法替代家兔热原检查法的可行性。方法:采用凝胶法,进行干扰预试验及干扰试验,其中干扰试验采用两个厂家生产的鲎试剂;用灵敏度为0.25 EU·ml^-1鲎试剂和环磷腺苷注射液62.5倍稀释液进行细菌内毒素检查。结果:环磷腺苷注射液稀释62.5倍时对鲎试剂与内毒素的凝集反应无干扰作用。结论:环磷腺苷注射液可用细菌内毒素检查法,替代原有的家兔热原检查法。     

曲克芦丁氯化钠注射液的细菌内毒素检查法

目的:探讨曲克芦丁氯化钠注射液的细菌内毒素检查法.方法:采用不同厂家、不同批号、不同灵敏度的鲎试剂进行干扰试验.结果:选用灵敏度为0.25 EU/mL(0.125 EU/mL)的鲎试剂,曲克芦丁氯化钠注射液经2倍(或4倍)稀释,不会对细菌内毒素检查产生干扰.结论:曲克芦丁氯化钠注射液的内毒素检查法可取代热原检查法.     

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.     

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.     

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.