均匀设计法对芍药苷的含量测定

本实验采用均匀设计实验法,以出膏率和紫外分光光度法测定的芍药苷回收率为指标,考察水量（A）、煎煮时间（B）和醇沉浓度（C）3个因素,得出最佳工艺为A3B1C2即加水煎2次,第一次加水14倍,煎煮90分钟,第二次加水12倍,煎煮60分钟,醇沉浓度为80%可基本提取完全.本提取工艺研究具有实用价值,适合大生产使用.     

芩杏口服液提取工艺的优选

目的 :优选芩杏口服液的提取工艺。方法 :以黄芩苷的含量为指标 ,应用L9(34)正交试验设计筛选最佳提取工艺条件。结果 :影响提取的主次因素 :B >A >D >C(A为加水量 ;B为煎煮次数 ;C为煎煮时间 ;D为醇沉浓度 )。最佳提取条件为 :加水 12倍 ,煎煮 3次 ,每次煎煮 30min ,醇沉浓度为 6 0 %。结论 :优选得到的工艺稳定可行。     

加味生化口服液提取工艺的优选

目的:优选加味生化口服液的提取工艺.方法:以盐酸水苏碱含量为指标,应用L9(34)正交试验设计筛选最佳提取工艺条件.结果:影响提取的主要因素依次为A＞B＞C＞D(A为煎煮次数,B为加水量,C为煎煮时间,D为醇沉浓度),最佳提取条件为:加水12倍,煎煮3次,每次煎煮60min,醇沉浓度50%.结论:优选得到的工艺稳定可行.     

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。     

复方鼻咽洗剂制备工艺研究

目的:根据临床需要研制复方鼻咽洗剂,并进行制备工艺的研究.方法:采用提取挥发油和水煎浓缩后醇、水沉法制备,分别以干膏提取率和绿原酸含量评价提取与精制工艺的指标,采用L9(33)和L9(34)正交设计试验分别筛选较优的提取和精制工艺条件.结果:最佳提取工艺为A2B1C2,即药材加8倍量水煎煮两次,每次1.5 h;最佳精制工艺为A1B2C2D3,即提取液浓缩的相对密度为1.25、醇沉液的含醇浓度为65%、醇沉液浓缩的相对密度为1.10、水沉的加水倍数为10倍量.结论:工艺合理、可行,质量可控.     

胃长康胶囊制备工艺研究

目的：为胃长康胶囊的生产工艺提供依据。方法：采用正交试验法，对胃长康胶囊的制备工艺及影响因素(A为煎煮次数；B为煎煮时间；C为加水量)进行研究，用薄层扫描法测定黄芪甲苷含量作为指标，确定最佳提取工艺。结果：A、B、C 3个因素对胃长康胶囊中黄芪甲苷的提取均有显著性的影响。结论：最佳提取条件为A3B1C3，即加水煎煮提取3次(2.0，1.5，1.5 h)，第1次加10倍量水，其余加6倍量水，并可以此工艺制成胶囊剂。     

降压益肾颗粒的提取工艺考察

目的：对降压益肾颗粒提取工艺进行优选。方法：采用正交试验法，以总黄酮含量和浸膏收率为指标，考察加水量、浸泡时间、煎煮时间和煎煮次数4因素及醇沉浓度对浸膏收率和有效成分的影响。结果：优化的提取工艺为用药材10倍量水，浸泡1h，每次煎煮1．5h，煎煮3次，醇沉浓度70％。结论：此工艺有效成分提取率高，重现性好，稳定可行。     

头痛安胶囊提取工艺研究

目的 筛选头痛安胶囊提取工艺参数。方法：以人参皂甙Rb1为指标成分。分光光度法为含量测定方法。采用正交设计,优选提取工艺,结果 加水倍数、提取时间、煎煮次数和醇沉浓度对方中人参皂甙Rb1的含量无显著影响。结论 头痛安胶囊最佳提取工艺条件为加水12倍。煎煮1h提取3次,醇沉浓度65%。     

银马解毒颗粒水提取工艺研究

目的优选银马解毒颗粒的水提工艺。方法采用L9（3^4）正交试验设计，以加水量、煎煮时间、煎煮次数、醇沉浓度为主要考察因素，以金银花的绿原酸和甘草的甘草酸铵总含量作为选择指标。结果水提醇沉制备工艺影响因素影响大小依次为煎煮次数、煎煮时间、醇沉浓度、加水量；最佳提取工艺为处方药材加10倍量水，每次煎煮1h，煎煮2次，醇沉浓度为40％。结论按优选的工艺条件放大试验，工艺稳定，结果满意。     

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。     

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.     

Pharmacological treatment of COVID-19: an opinion paper

The precocity and efficacy of the vaccines developed so far against COVID-19 has been the most significant and saving advance against the pandemic. The development of vaccines has not prevented, during the whole period of the pandemic, the constant search for therapeutic medicines, both among existing drugs with different indications and in the development of new drugs. The Scientific Committee of the COVID-19 of the Illustrious College of Physicians of Madrid wanted to offer an early, simplified and critical approach to these new drugs, to new developments in immunotherapy and to what has been learned from the immune response modulators already known and which have proven effective against the virus, in order to help understand the current situation.     

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.