多烯紫杉醇注射液细菌内毒素检查方法探讨

目的 :通过试验探讨采用干扰初筛法检测多烯紫杉醇注射液中细菌内毒素方法的可行性。方法 :运用干扰初筛法对供试品进行干扰试验和内毒素限量检查。结果 :选用 0 .12 5EU·ml-1以上灵敏度的鲎试剂可以消除供试品对内毒素检查的干扰 ,并且干扰初筛试验法一步就可以确定出多烯紫杉醇注射液对内毒素检查无干扰的有效稀释范围以及所需的鲎试剂灵敏度范围。结论 :采用干扰初筛法检查多烯紫杉醇注射液中细菌内毒素不但可以大大减少通常内毒素检查中的工作量 ,而且切实可行。     

蟾蜍注射液细菌内毒素检查法的建立

目的:探讨用鲎试剂检查蟾蜍注射液细菌内毒素的可行性.方法:根据<中国药典>2000年版二部细菌内毒素检查方法及指导原则进行实验.将蟾蜍注射液经30倍稀释,用标示灵敏度为0.5 EU·ml-1的鲎试剂检测其细菌内毒素.结果:蟾蜍注射液30倍稀释液对鲎试剂的细菌内毒素检查无干扰.结论:鲎试剂可用于蟾蜍注射液的细菌内毒素检查.     

氧氟沙星注射液细菌内毒素检查的研究

目的：探讨用鲎试剂检查氧氟沙星注射液细菌内毒素的可行性。方法：对家兔热原检查合格的氧氟沙星注射液作细菌内毒素检查的干扰试验。结果：氧氟沙星对鲎试剂的细菌内毒素检查无干扰.结论：鲎试剂可用于氧氟沙星注射液的细菌内毒素检查。     

紫杉醇脂质体细菌内毒素的检测

对注射用紫杉醇脂质体中的细菌内毒素检查方法进行了研究.以60%乙醇溶液作为溶剂破坏脂质体后进行试验.结果表明,60%的乙醇溶液对细菌内毒素的活性无明显影响;4%的乙醇溶液和0.17mg/ml的供试品溶液对鲎试剂和细菌内毒素的凝集反应无明显干扰.     

注射用L-缬氨酸细菌内毒素检查法的研究

目的通过鲎试剂的干扰试验,研究注射用L-缬氨酸原料中细菌内毒素检查法的可行性。方法依据中国药典2000年版中细菌内毒素检查法进行操作。结果在16倍稀释级下,L-缬氨酸(c=2.5%)对鲎试剂无干扰,检测细菌内毒素的鲎试剂灵敏度≤0.5 EU.mL-1结论L-缬氨酸用灵敏度为0.5 EU.mL-1的鲎试剂检查其细菌内毒素方法可行,供注射用L-缬氨酸细菌内毒素应小于0.04 EU.mg-1,显著高于中国药典2005年版的规定(5 EU.mg-1)。     

注射用头孢唑啉钠细菌内毒素检查方法研究

目的　 通过试验确定注射用头孢唑林钠细菌内毒素的具体检测方法。 方法 　选择相应灵敏度的鲎试剂 ,进行干扰试验 ,研究细菌内毒素检查方法。 结果 　用灵敏度 0 12 5EU/ml的鲎试剂 ,进行细菌内毒素检查 ,没有出现干扰作用。 结论 　注射用头孢唑林钠的热原检查可用细菌内毒素检查法     

注射用氨苄西林钠细菌内毒素检查方法研究

目的:通过试验确定注射用氨苄西林钠细菌内毒素的具体检测方法。方法:选择相应灵敏度的鲎试剂,进行干扰试验,研究细菌内毒素检查方法。结果:用灵敏度0.125EU.m-l 1的鲎试剂,同时将供试品2倍稀释,进行细菌内毒素检查,没有出现干扰作用。结论:氨苄西林钠的热原检查可用细菌内毒素检测法。     

注射用木糖醇原料中细菌内毒素检查方法的研究

目的通过对供注射用木糖醇原料,作鲎试剂的干扰试验,确定用细菌内毒素检查法,检测注射用木糖醇原料中细菌内毒素方法的可行性.方法按中国药典2000年版附录中的细菌内毒素检查法进行试验操作.用不同厂家的鲎试剂对不同批号的注射用木糖醇原料分别进行干扰试验,考察确立注射用木糖醇原料的细菌内毒素检查法.结果将供注射用木糖醇用无热原水稀释制成0.1g/mL以下(10倍)浓度的溶液后,无干扰作用,结果准确可靠.结论供注射用木糖醇原料用细菌内毒素检测方法是可行的,结果安全可靠.可以替代热原检查法.     

奥拉西坦注射液细菌内毒素检查

目的:建立奥拉西坦注射液细菌内毒素的检查法.方法:用不同厂家、不同批号、不同灵敏度的鲎试剂对奥拉西坦注射液进行干扰实验.结果:用标示灵敏度为0.125 EU/ml的鲎试剂,奥拉西坦注射液稀释20倍后,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取代奥拉西坦注射液的热原检查.     

细菌内毒素法检查碳酸氢钠注射液热原的研究

目的:研究用细菌内毒素法检查碳酸氢钠注射液的热原.方法:应用鲎试剂检查碳酸氢钠注射液中的热原,考察了碳酸氢钠注射液对细菌内毒素检查法的干扰行为.结果:碳酸氢钠注射液稀释2.5倍,对细菌内毒素检查法无干扰作用.结论:选用鲎试剂,细菌内毒素检查可代替碳酸氢钠注射液热原检查法.     

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.     

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.     

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.