参芪五味子胶囊提取工艺研究

目的优选参芪五味子胶囊中五味子的提取工艺。方法采用正交设计试验法,分别以五味子甲素的含量和浸膏得率为指标,对五味子的提取工艺进行优选。结果五味子的最佳提取工艺为,以60%乙醇为溶剂,浸渍24 h后,以药材的10倍量体积进行渗漉,渗漉速度为0.3 mL/min。结论试验结果为确定参芪五味子胶囊中五味子的提取工艺提供了试验依据。     

渗漉法提取五味子的工艺研究

目的筛选渗漉法提取五味子中木脂素的最佳工艺。方法用正交实验设计,以乙醇浓度、浸泡时间、渗漉速度、收集渗漉液体积和为因素,用分光光度计对五味子中木脂素进行测定,以五味子甲素为评价指标优化提取工艺。结果与结论五味子的最佳提取工艺为80%乙醇浸泡24h渗漉速度为6mL/kg.min,收集8倍的渗漉液。     

肝酶安胶囊中五味子提取工艺的研究

目的优选肝酶安胶囊中五味子的提取工艺研究。方法应用正交设计法,筛选最佳工艺条件。结果最佳提取工艺是加12倍量45%乙醇,以每分钟1~3 kg/m L的速度进行渗漉。结论优选出的肝酶安胶囊中五味子的最佳提取工艺稳定可行。     

五味子不同产地、部位及提取工艺对木脂素成分含量影响的研究

目的：探究五味子药材不同产地、不同部位及不同提取方式对木脂素成分含量的影响,为本厂含有五味子的品种选择适宜的药材产地及工艺提供科学的理论依据。方法：采用高效液相色谱法（ HPLC）测定不同产地、不同部位五味子中五味子醇甲、五味子酯甲、五味子甲素和五味子乙素的含量;同时,分别考查不同提取工艺（水煮、不同乙醇体积分数热回流、渗漉）对木脂素类含量的影响,使用正交试验方法进一步优化确定五味子渗漉工艺对四种木脂素类成分的最佳提取条件。结果：不同产地五味子木脂素成分都主要集中在种仁中,果皮中的含量较少;以乙醇热回流及渗漉提取工艺对木脂素成分的含量提取效果好,正交试验中以乙醇体积分数的影响最为显著,其次是提取倍数。结论：五味子中有效成分主要存在于种仁中,在大生产工艺中,需将五味子破碎,有利于有效成分的煎出;在提取工艺中,提示在工业化生产过程中,尽量选取体积分数较大的乙醇,以便提取完全。     

正交试验优化补肾健骨片中青风藤的提取工艺

目的:研究补肾健骨片中青风藤乙醇提取的最佳工艺。方法:以乙醇为溶剂采用浸渍法、连续渗漉法、回流法对药材进行提取工艺优选;以青藤碱含量为指标,以乙醇浓度、乙醇用量、药材粒度、pH值为考察因素,优选提取工艺。结果:最佳提取工艺为采用连续渗漉法,药材粉碎过10目筛,氨水调节pH8～9的12倍量75%乙醇提取。结论:本工艺稳定、操作简便、质量可控,可用于工业化大生产。     

复方参芪五味咀嚼片制备中五味子与人参的醇提工艺

目的研究复方参芪五味咀嚼片制备中五味子和人参的最佳醇提取工艺。方法以五味子醇甲和人参皂苷Rg1含量为指标,结合出膏率,进行L9(34)正交试验,筛选最佳工艺条件。并用高效液相色谱法测定五味子醇甲和人参皂苷Rg1的含量。色谱条件如下,五味子醇甲:Dikma Diamonsil-C18(250 mm×4.6 mm,5μm),流动相为甲醇-水(57.5:42.5),检测波长为250 nm,流速为1.0 mL.min-1;人参皂苷Rg1:Dikma Diamonsil-C18(200 mm×4.6 mm,5μm),流动相为乙腈-水(20:80),检测波长为203 nm,流速为1.0 mL.min-1。结果复方参芪五味咀嚼片制备中五味子和人参最佳醇提取工艺为10倍量90%乙醇回流提取3次,每次1.5 h。结论该实验所得最佳提取工艺能为参芪五味咀嚼片的研制和中试生产提供依据。     

正交试验优选姜黄的渗漉提取工艺

目的筛选姜黄药材的最佳渗漉提取工艺。方法采用正交实验对渗漉提取工艺进行研究。结果最佳渗漉提取工艺为药材粗粉用6倍量80%乙醇渗漉提取,渗漉流速为9mL/(min.kg)。结论此方法可作为姜黄药材的最佳渗漉提取工艺。     

南五味子提取工艺研究

目的五味子是我厂联苯双酯片的主要成份之一,其主要有效成分在一般制备过程中不易提取出来,严重影响了联苯双酯片的质量和临床疗效。为了提高联苯双酯片的质量、对五味子有效成分的提取工艺进行研究,尤其是提取工艺的最佳条件。方法采用正交设计法选定乙醇浓度、提取次数和溶媒用量4个因素,每个因素选定3个水平作为考察内容。实验采用分光光度法、高效液相色谱法(HPLC)测定各条件下南五味子提取液中的百分含量,并以总木脂素及五味子甲、甲素为考察指标。结果最佳提取方案为AB C D,即使用4倍量的80%乙醇,回流提取3次,每次1.5 h。结论为提高工业生产联苯双酯片中南五味子中的含量提供了科学依据。     

正交试验优选苦参总生物碱提取工艺

目的:优选苦参总生物碱的最佳提取工艺。方法:以酸水浓度、溶剂用量、渗漉液流速为考察因素,以苦参中苦参碱、氧化苦参碱含量之和以及总生物碱含量的综合评分为评价指标,采用正交试验优选最佳工艺条件。结果:优选的最佳提取工艺为采用10倍量的0.2%盐酸溶液进行渗漉提取,渗漉速度为3mL·min-1·kg-1。结论:酸水渗漉法操作简便、提取率高,可用于苦参总生物碱的提取。     

正交试验法优选五味子甲素和五味子乙素的超声提取工艺

目的:通过正交试验确定了五味子甲素和五味子乙素的超声提取工艺。方法:采用超声提取法提取五味子甲素和五味子乙素,以提取溶剂、超声时间、超声次数、溶剂用量为因素,以五味子甲素和五味子乙素提取率为考察指标,采用L9(34)正交表设计,用正交实验确定最佳提取条件,采用HPLC法分析2种成分。结果:在所考察的因素中,以五味子甲素与五味子乙素含量的均值为主要指标,确定最佳超声提取工艺为:以8倍体积甲醇为溶剂,超声提取3次,每次10min。结论:确定五味子最佳超声提取工艺,此法简单、快速、提取效率高;HPLC分析方法准确,灵敏度高,重现性好,可用于五味子有效成分的分析。     

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.     

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.     

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.