康妇炎片中挥发油的提取及β-CD包合工艺研究

目的：优选康妇炎片剂中苍术、当归、川芎、香附挥发油的提取及β-CD包合工艺。方法：以苍术、当归、川芎、香附挥发油出油量为指标优选提取工艺；以挥发油的包合率为指标优选B-CD包合工艺。结果：优选挥发油提取工艺条件为：苍术、当归、川芎、香附药材加10倍量水，蒸馏4h；包合物最佳包合工艺为：采用饱和水溶液法，β-CD与油量为10：1，40℃搅拌1h。结论：该工艺可用于苍术、当归、川芎、香附挥发油的提取及包合。     

化痰降气胶囊制备工艺研究

目的：优选化痰降气胶囊最佳制备工艺。方法：采用正交试验法，以浸膏得率及盐酸麻黄碱含量为指标，优选药材乙醇提取工艺；以挥发油含量为提取工艺筛选指标；以挥发油利用率和包合物收率为包合工艺评价指标。结果：药材提取最佳工艺为：以70％乙醇为提取溶媒，加液量8倍，提取2次，时间分别为2h，1h；挥发油最佳提取条件搭配为：10倍水，浸泡1h，提取4h，当归挥发油包合最佳工艺为：每1ml挥发油用10gβ-环湖精（β-CD），100ml水，60℃搅拌包合2h。结论：正交试验法为制备化痰降气胶囊提供依据。     

超临界CO2萃取川芎挥发油的工艺研究

目的:优选超临界CO_2萃取川芎挥发油的最佳工艺条件。方法:以川芎挥发油出油率和阿魏酸的含量为评价指标,采用正交试验优化超临界CO_2萃取川芎挥发油的工艺条件。结果:超临界CO_2萃取川芎油的最佳条件:萃取温度50℃,萃取压力35 MPa,萃取时间2 h,CO_2流量20 L·min~(-1)。结论:该优选提取工艺条件稳定可行。     

正交试验法优选冠心康胶囊挥发油提取工艺条件

目的:优选冠心康胶囊中川芎、当归、桂枝挥发油的提取工艺条件。方法:采用水蒸气蒸馏法提取川芎、当归、桂枝挥发油,以挥发油的收率作为评价指标,选择加水量、浸泡时间及提取时间等为主要影响因素,应用L9(34)正交试验设计选取最佳提取工艺条件。结果:水蒸气蒸馏法提取川芎、当归、桂枝挥发油最佳工艺条件为加8倍量的水,浸泡0.5h,蒸馏提取7h。结论:优选所得提取工艺条件稳定可行。     

紫苏、辛夷混合挥发油提取与包合工艺研究

目的：优选辛夷、紫苏挥发油提取和包合的最佳工艺。方法：利用正交实验设计超临界流体萃取辛夷、紫苏挥发油,选择萃取的温度、压力、时间和二氧化碳（CO2）流量为考察因素,以挥发油提取率为考察指标,优选最佳提取工艺;应用响应面法优选挥发油包合工艺,以挥发油与β-环糊精（β-CD）的比例、包合温度和包合时间为考察因素,以包合物得率和挥发油包合率为指标优选挥发油包合工艺。结果：超临界CO2萃取辛夷、紫苏挥发油的最佳工艺：萃取的温度为40℃,压力为30 MPa,时间为1.5 h,CO2流量为60 kg·h-1;挥发油包合的最佳工艺：挥发油与β-CD之比为1∶8,包合温度为60℃,包合时间4 h。结论：本研究确定了辛夷、紫苏挥发油超临界CO2萃取的最佳工艺及包合工艺,优化了工艺参数,经验证表明本工艺稳定、可行。     

姜黄提取工艺研究

目的：优选姜黄提取工艺.方法：采用单因素法,以姜黄挥发油收率为评价指标,优选姜黄挥发油提取工艺条件;采用正交试验法,以姜黄素、干膏率为评价指标,优选姜黄醇提工艺条件.结果：姜黄挥发油提取工艺条件为：粉碎过一号筛,加8倍水,蒸馏提取7 h;姜黄醇提的工艺条件为：加80%乙醇,提取3次,每次加药材8倍量乙醇,提取60 min.结论：优选的姜黄提取工艺条件稳定可行.     

人参当归颗粒剂中挥发油的提取及包合工艺研究

目的探讨人参当归颗粒剂中挥发油提取及包合的最佳工艺条件。方法采用正交设计试验,以挥发油总质量为评价提取工艺的指标。以包舍物收率、挥发油包合率为评价包合工艺的指标。结果挥发油的最佳提取工艺条件为药材加6倍量水、浸泡1h、加热至沸腾回流8h,挥发油的最佳包合工艺为挥发油与β-环糊精按1：6投料、包合温度45℃、磁力搅拌2h。结论所优选的最佳提取工艺和包合工艺稳定、可行。     

牡丹皮挥发油提取方法的研究

目的：优选牡丹皮原药材中挥发油的提取工艺。方法：采用共水蒸馏、间接水蒸气蒸馏和超临界CO2萃取三种提取方法提取牡丹皮中的挥发油,比较了不同提取方法对挥发油的出油率和丹皮酚含量的影响,并通过正交试验优化了提取工艺条件。结果：确定最佳提取方法为超临界CO2萃取,最佳萃取工艺为萃取温度50℃,萃取压力50 MPa,萃取3 h。结论：优选得到的工艺简便易行、稳定性好,为牡丹皮进一步开发研究提供了依据。     

正交试验法优选血府逐瘀滴丸的提取工艺

目的：确定血府逐瘀滴丸的乙醇渗漉提取最佳工艺条件。方法：以当归、川芎中阿魏酸的提取效果和转移率为评价指标,通过正交实验对血府逐瘀滴丸的乙醇渗漉提取工艺条件进行优选。结果：筛选的最佳工艺为药材加入13倍量65%乙醇,静置浸泡24 h,以10 ml/min流速渗漉提取。结论：优化的提取工艺条件可为工业化生产提供实验依据。     

超临界流体萃取肉桂挥发油工艺研究

目的：探讨肉桂挥发油的最佳提取工艺。方法：采用超临界CO2萃取技术提取挥发油。结果：最佳工艺条件为：萃取温度45℃、萃取压力45MPa、萃取时间2．5h、CO2流量20kg·h^-1。结论：优选的提取工艺条件稳定、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.     

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.