正交试验法优选骨炎宁颗粒的提取工艺

目的：选择骨炎宁颗粒的最佳水煎工艺条件。方法：以浸膏得率和总绿原酸含量为考察指标，应用L9（34）正交试验法确定最佳水煎工艺。结果：骨炎宁颗粒最佳水煎工艺条件为加8倍量水，煎煮60min，煎煮2次。结论：该工艺稳定可行。     

赤芍片提取工艺的研究

目的:筛选赤芍片水煎提取的最佳工艺条件。方法:应用正交试验得到最佳提取条件。结果:赤芍加水首次10倍量,煎煮2小时。第二次加水8倍量,煎煮1小时。结论:此提取条件最佳。     

消萎灵颗粒制备工艺研究

目的研究消萎灵颗粒制备工艺,确定最佳的制备工艺条件,并拟定质量标准。方法应用正交试验研究消萎灵提取工艺,运用水煎法和喷雾干燥制粒技术进行工艺制备,通过原药材鉴别、颗粒检查和微生物限度控制消萎灵质量。结果最佳制备工艺为:处方量药材加12倍量水,煎煮提取2次,每次2.0 h,喷雾干燥制粒。结论该制备工艺可行、重现性良好。     

产舒康颗粒提取工艺研究

目的:探讨产舒康颗粒提取工艺条件.方法:正交试验设计,以薄层扫描法测定不同工艺颗粒中阿魏酸含量.结果:最佳工艺为药材粗颗粒(过5目筛 ),以16倍量水煎煮2次,每次1 h.结论:该工艺能充分提取药材中的有效成分.     

正交试验法优选保肝醒酒胶囊水煎工艺

目的:优选保肝醒酒胶囊的水煎工艺。方法:以浸膏得率和总绿原酸含量为指标,采用L_9(3~4)正交试验进行优选。结果:水煎工艺影响因素依次是:煎煮次数>煎煮时间>加水量,最佳制备条件为加12倍的水,煎煮3次,每次0.5 h。结论:该优化的制备工艺易于操作,合理可行。     

正交试验法优选淫黄颗粒的提取工艺

目的优选淫黄颗粒的最佳水煎提取工艺。方法采用正交试验法，以提取液中淫羊藿苷的含量为考察指标，对影响水煎提取效果的加水量、浸泡时间、煎煮时间、煎煮次数等4个因素进行研究。结果煎煮次数对提取效果的影响最明显，最佳工艺为浸泡30min，煎煮3次，每次1．5h，每次加8倍量水。结论该实验所优选的工艺稳定，可行。     

补肾壮骨胶囊提取工艺的优选

目的：优选补肾壮骨胶囊提取工艺的最佳条件。方法：用正交设计法以方中君药淫羊藿药材的主要成分淫羊藿苷的总量为指标，对其水煎工艺及醇沉工艺进行筛选。结果：优选出补肾壮骨胶囊水煎醇沉工艺，重复试验结果满意。结论：补肾壮骨胶囊水煎工艺的最佳条件为A2B3C2D2，即加12倍量水先浸泡40min，再煎煮2次，每次煎煮90min。醇沉工艺的最佳条件为A282Dl，即浓缩药液比例至1：1(药液：药材量)后醇沉(55％乙醇醇沉)12h。     

正交试验法优选痛风颗粒水提工艺条件

目的:正交试验法优选痛风颗粒水提工艺条件。方法:采用高效液相色谱法测定绿原酸含量并进行方法学考察;以绿原酸含量及干浸膏收率为综合评价指标,选取影响水溶性成分提取率的蒸馏水的量、煎煮提取时间及煎煮次数作为考察因素,应用L9(3~4)正交试验设计选取最佳水提工艺条件。结果:最佳水提工艺条件为加8倍量的水,煎煮3次,每次1 h。结论:优选所得提取工艺条件稳定可行,可为痛风颗粒的工业生产提供试验依据。     

祛风胜湿颗粒提取工艺优选

目的 优选祛风胜湿颗粒最佳的提取工艺.方法 采用L9（3）4正交试验设计,以异欧前胡素含量及干浸膏得率为考察指标,筛选祛风胜湿颗粒的醇提最佳工艺条件;以甘草酸单铵盐含量及干浸膏得率为考察指标,筛选祛风胜湿颗粒的水提最佳工艺条件;采用单因素试验,优选防风、川芎、藁本和蔓荆子4味药材的最佳提取工艺.结果 优选的祛风胜湿颗粒醇提最佳工艺条件为加10倍量70％乙醇,回流提取2次,每次2h;挥发油的提取工艺条件为加8倍量水提取4h;水提最佳工艺条件为加10倍量水,煎煮2次,每次1h.结论 优选的生产工艺合理、可靠,适合现代化大生产.     

知柏地黄泡腾颗粒的提取工艺研究

目的:优选知柏地黄泡腾颗粒提取工艺的最佳条件。方法:采用正交试验法L9(34),对影响知柏地黄泡腾颗粒提取工艺的主要因素进行了研究。结果:优选出知柏地黄泡腾颗粒的提取工艺:方中山茱萸、泽泻采用乙醇提取,最佳工艺为使用8倍量的90%乙醇,加热回流提取2次,每次1 h;药渣和方中其他药味采用水煎煮提取,最佳工艺为15倍量的水,煎煮3次,每次1 h。结论:该提取工艺合理可行。     

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.