骨炎宁颗粒的制备及其对大鼠免疫功能的影响

目的 选择骨炎宁颗粒的最佳制备工艺; 探讨骨炎宁颗粒对实验性大鼠红细胞免疫功能的影响. 方法 应用正交实验法, 采用喷雾干燥制粒机制粒并在流化床上进行干燥, 以浸膏浓缩的相对比例、进/出口风温及入塔风压为考察因素, 每个因素3个水平, 以颗粒的成品率及半成品颗粒的含水量为考察指标; 建立大鼠胫骨化脓性骨髓炎模型, 观察白细胞（WBC）、C3b受体花环率、红细胞（RBC）、红细胞免疫复合物花环率和血清溶酶体含量. 结果 3因素中以浸膏浓缩的相对比例（A）和入塔风压（C）的影响较显著, 而进/出口风温（B）的影响不显著. 骨炎宁颗粒喷雾干燥的最佳工艺条件为A₃B₁C₃. 即浸膏浓缩的相对比例为1：1.20, 进/出口风温为90～100/50～60 ℃, 入塔风压为负压1 800 Pa; 免疫学指标方面骨炎宁组与模型组之间差异有极显著性（P<0.01）, 骨炎宁效果优于青霉素（P<0.05）. 结论 优选的骨炎宁颗粒工艺可靠, 药理实验表明骨炎宁颗粒有明显的抗炎和提高机体免疫力作用.     

正交试验法优选骨炎宁颗粒的喷雾制粒工艺

目的：选择骨炎宁颗粒喷雾制粒的最佳工艺条件。方法：应用正交试验法，采用喷雾干燥制粒机制粒并在流化床上进行干燥，以浸膏浓缩的相对比例、进风温度及入塔风压为考察因素，每个因素3个水平，以颗粒的成品率及半成品颗粒的含水量为考察指标。结果：三因素中以浸膏浓缩的相对比例A和入塔风压C的影响较显著（P〈0．05），而进风温度B的影响不显著。结论：骨炎宁颗粒喷雾制粒的最佳工艺条件为A3B1C3。即浓缩的相对比例为1：1．20，进风温度为90℃，入塔风压为负压1800Pa。     

去脂胶囊喷雾干燥工艺优选

目的 建立去脂胶囊的最佳喷雾干燥工艺.方法 采用正交试验法,以入塔风温、出塔风温、浸膏比重等为影响因素,以喷雾干燥粉中醇浸出含量、出粉率为考察指标.结果 去脂胶囊的最佳喷雾干燥工艺为A2B2C3,即入塔风温为190～200 ℃,出塔风温为105～115 ℃,相对密度为1.15.结论 A2B2C3喷雾干燥条件,所得醇浸出物量、出粉率综合评分最高,该工艺条件比较稳定.     

去脂胶囊喷雾干燥工艺优选

目的建立去脂胶囊的最佳喷雾干燥工艺。方法采用正交试验法,以入塔风温、出塔风温、浸膏比重等为影响因素,以喷雾干燥粉中醇浸出含量、出粉率为考察指标。结果去脂胶囊的最佳喷雾干燥工艺为A2B2C3,即入塔风温为190~200℃,出塔风温为105~115℃,相对密度为1.15。结论A2B2C3喷雾干燥条件,所得醇浸出物量、出粉率综合评分最高,该工艺条件比较稳定。     

柴藿颗粒浸膏喷雾干燥工艺研究

目的:优选柴藿颗粒浸膏喷雾干燥的最佳工艺条件.方法:采用L9(34)正交实验法对影响浸膏喷雾干燥的工艺条件:浸膏密度(A)、喷雾速度(B)、出口温度(C)进行考察,每个因素三个水平,并以柴藿颗粒浸膏喷雾干燥的出粉率为考察指标.结果:柴藿颗粒浸膏喷雾干燥最佳工艺条件为A1B3C2,即浸膏密度0.8 g/mL、喷雾速度2 mL/min、出口温度80℃.结论:该工艺稳定、有效、可控,为中试生产工艺提供了科学的理论依据.     

愈痫灵颗粒喷雾干燥工艺的考察

目的：优选愈痫灵颗粒喷雾干燥适宜的工艺条件。方法：应用正交设计法，以干粉重量、水分含量以及黄芩苷、阿魏酸含量为考察指标，对影响愈痫灵颗粒喷雾干燥的因素进行考察，利用多指标实验全概率公式评分法进行数据处理。结果：正交试验法设计的三个因素中，浓缩液运动黏度的差异有显著性（P〈0.05）．入塔风温与进药速度的差异无显著性（P〉0．05）。工艺条件：浸膏运动黏度为0．04，入塔风温为160℃，进药速度为30％。结论：该工艺合理可行，可为工业化生产提供理论依据。     

正交试验研究功血宁颗粒的提取工艺

目的优选功血宁颗粒的最佳提取工艺。方法采用正交试验设计,以黄芪甲苷为指标,选择加水量、煎煮时间、煎煮次数三个因素,考察对提取效果的影响。结果最佳工艺组合确定为A3B2C2,即黄芪等八味药材加水煎煮2次,每次加入8倍量水,煎煮2 h。结论优选出的提取工艺为功血宁颗粒的制备提供了依据。     

正交试验优选双花抗病毒口服液提取工艺

目的：优选双花抗病毒口服液的提取工艺。方法：采用L9（34）正交试验筛选提取工艺;以加水量（A）、提取时间（B）、浸泡时间（C）作为考察因素,以挥发油提取量为指标,优选广藿香、鱼腥草、连翘3味药材的挥发油提取工艺;以加水量（A）、浸泡时间（B）、提取时间（C）、提取次数（D）为考察因素,以绿原酸和连翘苷含量为指标,优选药材的水提工艺。结果：挥发油最佳提取工艺为：加10倍量水,直接提取4小时;水提取最佳工艺为：加8倍量水,浸泡0.5小时,煎煮2次,每次1.5小时。结论：优选得到的提取工艺质量稳定、可行。     

正交试验优化复方枳参胶囊处方药材的提取工艺

摘 要：目的 研究影响复方枳参胶囊提取效果的各种因素,确定最佳提取工艺。方法 采用正交试验设计,以浸膏收率和槲皮素提取率为指标,考察回流提取时间（A）、乙醇体积分数（B）、提取次数（C）和乙醇用量[乙醇体积（mL）/药材量（g）,D]4个因素对提取效果的影响,优选出复方枳参胶囊的提取工艺。结果 在所考察的4个因素中,对复方枳参胶囊提取效果的影响程度依次为：B＞D＞C＞A,即乙醇体积分数＞乙醇用量＞提取次数＞回流提取时间,确定出最佳提取工艺为 B2D3C2A3,即10倍于药材量（g）的70%乙醇（mL）,回流提取2次,每次2 h 为最佳提取工艺。结论 本实验优选出的提取工艺适用于复方枳参胶囊的提取。     

血栓康胶囊喷雾干燥工艺研究

目的:选择血栓康胶囊喷雾干燥的最佳工艺条件。方法:应用正交实验法,以每小时药粉产量为考察指标,同时兼顾药粉中的有效成分,对影响血栓康胶囊喷雾干燥过程的因素进行考察。结果:正交实验设计的三个因素中,浸膏的相对密度影响最显著,入塔风压的影响较显著。结论:最佳工艺条件:入塔风温165℃,入塔风压-1550Pa,浸膏相对密度为1.28,采用喷雾干燥的工艺生产出的血栓康胶囊,有效成分黄芪甲甙的含量明显高于湿法制粒的含量。     

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.     

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.