基于指标成分和药效学优选定痛宁颗粒的醇沉工艺

摘 要 目的：优选定痛宁颗粒的醇沉工艺,结合药效学角度考察醇沉工艺的合理性。方法: 以干膏得率和芍药苷、阿魏酸转移率的综合评分为指标,通过L9(34)正交试验考察醇沉浓度、清膏相对密度和醇沉时间对醇沉工艺的影响,采用小鼠生化指标变化比较定痛宁颗粒水提清膏醇沉前后的药效。结果: 最佳醇沉工艺条件为提取液浓缩至相对密度的清膏1.10 g·ml-1（25℃）,加入一定量的90%乙醇使药液含醇量达70%,冷藏静置18 h。醇沉前后药效未发生明显变化。结论: 优选的水提醇沉工艺稳定可行,在保持药效的基础上达到了较好的纯化效果,为定痛宁颗粒的科学生产提供了实验依据。     

正交试验优选咽炎宁颗粒提取工艺

目的优选咽炎宁颗粒的提取工艺。方法应用高效液相法测定射干苷的含量;采用正交设计法考察煎煮次数、煎煮时间、加水量三因素对水提工艺提取成分提取率的影响;考察醇沉浓度、醇沉前水提液相对密度、醇沉时间三因素对醇沉工艺有效成分含量的影响。结果加水量对水提工艺有显著影响(P<0.05);醇沉浓度对醇沉工艺有显著影响(P<0.05)。结论最佳水提醇沉工艺为药材加10倍量水,煎煮2次,每次1.5 h;水提液浓缩至相对密度为1.15,加入乙醇使含醇量至60%,静置48 h。     

经舒宁颗粒提取纯化工艺优选

摘 要 目的:优选经舒宁颗粒的提取纯化工艺。方法: 以芍药苷的转移率和浸膏得率作为评价指标,采用正交试验对水提条件进行优选,以醇沉前后芍药苷的转移率和干膏量对醇沉条件进行考察。结果:优选出最佳的工艺条件是8倍量的水,提取3次,每次2.5 h,醇沉浓度为70%。结论:优选出的工艺稳定,可行,适合该制剂的批量生产。     

铁皮石斛滴眼液的制备工艺研究

摘 要 目的： 优选铁皮石斛多糖提取、纯化及滴眼剂配制的工艺参数,为工业化生产提供依据。方法: 采用硫酸 苯酚比色法测定铁皮石斛样品中的多糖含量;采用单因素和正交试验优选水提、醇沉的工艺参数;采用等级一致性检验法优选滴眼液的配制参数。结果: 最佳水提工艺为：铁皮石斛鲜药材经冷冻干燥（-55℃、-0.01 Mpa）后,粉碎、过40目筛,过筛后粉末加30倍量水浸泡1 h,提取3次,提取时间分别为3,2.5,2 h,第2、3次提取加水量分别为25倍和20倍,提取温度为85℃。最佳醇沉工艺为：提取液浓缩至固液比为1∶3时,加乙醇使含醇量达85%,静置24 h。滴眼液配制参数为：采用3%聚氧乙烯氢化蓖麻油作为稳定剂,0.25%苯甲酸钠和0.25%尼泊金乙酯作为防腐剂。结论:优选的铁皮石斛多糖提取、纯化及滴眼剂配制工艺合理可行、重复性好,适合于工业化生产。     

正交试验优选麻芎平喘颗粒中药材的提取工艺

目的:优选麻芎平喘颗粒中药材的提取工艺。方法:采用正交试验,以盐酸麻黄碱质量分数为评价指标,考察加水量、煎煮时间和煎煮次数对水提工艺的影响;以盐酸麻黄碱保留率、固形物减少率为评价指标,考察药液相对密度、醇沉浓度、醇沉时间对醇沉工艺的影响。结果:最佳水提醇沉工艺为加12倍量水,煎煮3次,分别为80、60、60 min,提取液浓缩至相对密度为1.25,冷却后加入乙醇使含醇量为60%,放置24 h,除去沉淀。结论:优选的水提醇沉工艺稳定、可行,重现性好,可用于麻芎平喘颗粒中药材的提取。     

益精明目口服液的制备工艺考察

摘 要 目的： 考察益精明目口服液的提取工艺。方法: 采用硫酸 蒽酮法测定口服液中总多糖含量,并以总多糖提取率为评价指标,通过单因素试验法考察浸泡时间、加水量、煎煮时间、煎煮次数及醇沉浓度对多糖含量的影响,筛选最佳工艺参数。结果: 蒽酮 硫酸法测定总多糖含量,线性范围为10.4～104.0 mg·L^-1,r=0.999 5,平均加样回收率为99.94%,RSD=2.31%（n=9）;所得最佳提取工艺为加10倍量水,浸泡25 min,煎煮2次,每次25 min,40%浓度乙醇醇沉。结论: 蒽酮 硫酸法简单快速,准确率高;所建立的制备工艺简单可行,稳定可控,为进一步制定质量标准及产业化开发奠定了基础。     

镇惊泻火颗粒的制备工艺研究

摘 要 目的： 研究镇惊泻火颗粒的制备工艺。方法: 采用正交试验,以干浸膏得率、甘草苷和丹酚酸B的含量为指标,对镇惊泻火颗粒的提取、纯化工艺进行研究;以合格颗粒得率为指标,对颗粒的成型工艺进行研究,优选制剂的制备工艺。结果: 铁落先煎60 min,其余各药加8倍量水,浸泡90 min,加入先煎铁落液,煎煮提取90 min,共3次。合并浓缩至相对密度1.3左右（60℃热测）,加蒸馏水至稀释比为1:2（V/V）,加乙醇至含醇量50%,24 h后滤过。滤液回收乙醇后浓缩至相对密度1.3 （60℃热测）,60℃下干燥粉碎得干浸膏。以淀粉作稀释剂,干浸膏与辅料比例1：0.8,90%乙醇为润湿剂制软材,过20目筛制粒,60℃干燥3 h,烘干,整粒,即得。结论:优选的镇惊泻火颗粒制备工艺稳定可行。     

四味生津颗粒的提取工艺实验研究

目的优选四味生津颗粒的最佳提取工艺。方法水提工艺及醇沉工艺都以芍药苷和甘草酸的总量为考察指标进行正交实验。结果四味生津颗粒的最佳水提工艺为:加水10倍量,煎煮3次,每次2 h;最佳醇沉工艺为:水提液浓缩至清膏相对密度为1.05,醇浓度为70%,静置24 h。结论优选出的提取工艺稳定可行。     

复方血通蒲颗粒的提取纯化工艺研究

目的研究复方血通蒲颗粒制备工艺,优选最佳提取、纯化工艺条件。方法以葛根素含量、含固量为检测指标,用正交试验考察了3种因素（加水量、煎煮时间、煎煮次数）对其水煎煮工艺的影响,同时比较了不同的醇沉浓度的去杂效果。结果复方XTP颗粒最佳水提工艺条件为先加12倍量水,煎煮1.5h,再加10倍量水,煎煮1h,煎煮2次;去杂工艺中以60%乙醇沉为佳。结论制备工艺合理。     

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。     

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.