正交设计法优选补肾壮骨颗粒的制备工艺

目的优选补肾壮骨颗粒的最佳制备工艺。方法分别以干膏中淫羊藿苷和柚皮苷的含量为指标,采用正交试验法优选制备工艺。结果淫羊藿、水蛭2味药材粉碎成粗粉,用8倍量70%的乙醇为溶媒,加热回流提取1次,提取90 min,淫羊藿苷得率最高。其余药材粗粉与药渣一起加水煎煮3次,每次用8倍量水煎煮60 min,柚皮苷得率最高。结论经正交设计优化的补肾壮骨颗粒的制备工艺可行。     

正交试验优选强脊壮督颗粒的提取工艺

目的：优选强脊壮督颗粒的提取工艺。方法：采用L9（3^4）正交试验，以淫羊藿苷含量为指标，以醇质量分数、醇用量、提取时间和提取次数为考察因素，筛选强脊壮督颗粒的最佳醇提取工艺条件；以出膏率为指标，以加水量、煎煮时间和煎煮次数为考察因素，筛选强脊壮督颗粒的最佳水提取工艺条件。结果：最佳醇提取工艺条件为加8倍药材量60％乙醇，回流提取2次，每次2h；最佳水提取工艺条件为加10倍药材量水，煎煮3次，每次煎煮2h。结论：优选得到的提取工艺稳定、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。     

正交设计法研究补肾壮骨胶囊醇提工艺

目的 优选补肾壮骨胶囊醇提工艺的最佳条件。方法 用正交设计法以补骨脂素含量、异补骨脂素的含量为指标对醇提工艺进行筛选。结果 优选出补肾壮骨胶囊醇提工艺,重复试验结果满意。结论 补肾壮骨胶囊醇提工艺的最佳条件为A1B2C2D2,即加10倍量60％乙醇,回流提取2次,每次提取60min,     

醒脑益智颗粒水提醇沉制备工艺研究

目的：研究醒脑益智颗粒的水提醇沉制备工艺。方法：以阿魏酸含量为考察指标，通过L9（3^4）正交试验设计优选水提醇沉的制备工艺条件，确定醒脑益智颗粒的最佳制备工艺。结果：水提醇沉制备工艺影响因素依次为：加水量（A）〉煎煮次数（C）〉醇沉质量分数（D）〉煎煮时间（B），最佳制备工艺条件为A3B1C3D2，即处方药材加10倍量水，煎煮3次，每次0．5h，醇沉质量分数为50％。结论：该制备工艺合理，有效成分提取率高。     

扶肾颗粒制备工艺研究

目的:优选扶肾颗粒制备工艺。方法:以干膏率和淫羊藿苷含量作为考察指标,采用正交试验法优化扶肾颗粒的提取工艺和醇沉精制工艺,以吸湿百分率为指标考察颗粒辅料。结果:最佳制备工艺条件加10倍水,煎煮3次,每次2h;最佳醇沉浓度是60%;最佳制粒工艺条件为:药材提取物-糊精以1:2的比例湿法制粒。结论:优选项的制备工艺合理,有效成分提取率较好。     

芍石护睛胶囊醇沉工艺的优选

目的:优选芍石护睛胶囊的醇沉最佳工艺条件。方法:HPLC法测定醇沉液中芍药苷的含量;采用正交试验法考察醇沉前水煎液相对密度、醇沉浓度、醇沉时间3因素对醇沉工艺有效成分含量的影响。结果:醇沉前水煎液相对密度对醇沉工艺有显著影响(P<0.05)。芍石护睛胶囊醇沉工艺最佳条件即煎煮液浓缩密度为1.10～1.15,加入乙醇使含醇量为70%,醇沉时间为12h。结论:该工艺缩短了生产周期,降低了生产成本,适用于实际生产。     

正交试验优选补气通脉胶囊制备工艺

目的:优选补气通脉胶囊的制备工艺。方法:以大鼠血液流变学指标考察醇沉条件。以药材的浸泡时间、提取次数、加水量、煎煮时间为考察因素,以黄芪甲苷含量为考察指标优选黄芪最佳提取工艺。以丹参素含量为考察指标优选丹参、川芎、枳壳、红花最佳提取工艺。结果:药材最佳提取方法为采用水提取70%醇沉。黄芪最佳提取工艺为浸泡30 min,煎煮2次,每次90 min,按1∶10加水。丹参、川芎、枳壳、红花最佳提取工艺为煎煮90 min,共煎煮2次,按1∶8加水。结论:该生产工艺方法可行、稳定,符合临床需要。     

芪黄胶囊的制备工艺研究

目的优选芪黄胶囊的最佳提取工艺。方法采用正交实验法对煎煮过程中提取次数、提取时间、加水量3个因素选取分别选择3个水平进行正交试验，通过考察提取液中淫羊藿苷的含量，用直观法和方差分析法分析结果。结果最佳提取工艺为A282C2，即加9倍量水提取2次，每次提取时间为1．5h。结论该优选最佳方案能保证芪黄胶囊的质量。     

正交设计优选复方护肺颗粒水煮醇沉提取工艺

目的：优选复方护肺颗粒中当归、川芎、陈皮、五味子等药材的最佳水煮醇沉工艺。方法：采用正交设计法考察当归、川芎、陈皮、五味子等药材的水煮醇沉工艺条件,以平均干膏收率（％）和干浸膏中橙皮苷的含量（mg）为考察指标筛选最佳条件。结果：最佳水煮醇沉工艺条件为：当归、陈皮等几味中药提取挥发油后的药渣加水煎煮2次,第1次加8倍量水煎煮1h,第2次加6倍量水煎煮0．5h,药液合并,浓缩至相当于每1ml含1．0g生药,加乙醇至含醇量60％（v／v）,静置。结论：正交设计法优选复方护肺颗粒中当归、川芎、陈皮、五味子等药材的水煮醇沉提取工艺,效率高、工艺稳定。     

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.

---

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.