裂叶荨麻提取物微囊的制备工艺

目的：研究裂叶荨麻提取物微囊的制备工艺。方法：采用正交设计法对裂叶荨麻提取物微囊的制备工艺进行研究。结果：当囊心、囊材比为0．5：1．25，成囊温度为70℃，搅拌速度为800r·min^-1时，含量及产量较高。结论：该工艺简单，可靠。     

阴道用替硝唑缓释微囊的制备及其体外释放度考察

目的：制备替硝唑缓释微囊，考察其在体外的释放度。方法：以明胶、阿拉伯胶为囊材，采用复凝聚法制备替硝唑缓释微囊，正交试验优化制备工艺，采用紫外分光光度法测定含量。以100mL，pH4．5的乳酸溶液为释放介质，温度（37±0．5）℃，转速50r·min^-1测定其体外释放度。结果：替硝唑缓释微囊的最佳制备工艺为囊心囊材质量比为1：1，温度50℃，甲醛用量为2mL·120mL）^-1。（甲醛用量／系统体积），体外缓释时间为240min。结论：替硝唑缓释微囊的制备工艺简单、成囊性和重复性好，替硝唑微囊具有明显的缓释效果。     

马来酸氨氯地平微囊制备工艺研究

目的：研究马来酸氨氯地平微囊的最佳制备工艺,以扩大马来酸氨氯地平的临床应用范围。方法采用物理化学法制备马来酸氨氯地平微囊,通过正交试验,以包封率和载药量为指标综合评价制备工艺,筛选最佳工艺条件。结果优选后的马来酸氨氯地平微囊的最佳制备工艺条件为：采用囊材与药物比例为1∶1．5、油水相比例为3∶1、聚维酮用量为0．2g,此时包封率为88．03％、微囊载药量为54．80％,综合评分71．41％。结论马来酸氨氯地平微囊的工艺稳定可靠,重现性良好,为临床生产缓控制剂提供基础。     

正交法研究盐酸克林霉素-乙基纤维素微囊的处方工艺

目的 制备盐酸克林霉素微囊,选择最优处方工艺。方法 以乙基纤维素为囊材,采用液中干燥法制备盐酸克林霉素微囊。采用四因素三水平正交实验设计考察药物与囊材的比例、油水相比例、表面活性剂用量、抗粘剂用量对微囊粒径、载药量和包封率的影响。结果 确定处方药物与囊材的比例为3：2,油水相比例为3：1,司盘用量为0．5％．滑石粉与囊材的质量比为1：1为最佳处方工艺。结论 本法处方合理,制备工艺可行,有良好的应用前景。     

番茄红素-橄榄油微囊的制备及稳定性研究

目的：利用微囊化技术提高番茄红素的稳定性。方法：以明胶和阿拉伯胶为混合壁材,用复凝聚法制备番茄红素-橄榄油微囊,通过电镜扫描和粒径测定法评价微囊的体外特征,并在光照和热破坏条件下考察其稳定性。结果：初步确定微囊制备的最佳工艺：以橄榄油为油相,囊材溶液质量浓度为0．05g·mL^-1,成囊时体系pH值为4．0、温度为45℃;选用高剪切乳化机进行乳化,转速为3000r·min^-1,乳化时间为5min;以冷冻干燥法进行微囊干燥。由此制得的微囊圆整度好,平均粒径约7μm,均匀度为0．0899,包封率为81．8％;在强光（4500h）或高温（60℃）下放置10天,其含量基本稳定。结论：番茄红素-橄榄油微囊制备工艺简易,成品稳定性好,值得进一步研究开发。     

用正交法对阿司匹林微囊制备工艺的研究

本文用正交设计法对阿司匹林微囊的制备工艺进行了研究，结果表明用单凝聚法制备阿司匹林微囊；其包裹率与囊心囊材比和成囊温度有显著性关系，而搅拌速度则能影响微囊的粒径，当囊心囊材比为1：4，成囊温度50℃，搅拌速度为600r／min时，包裹率最高，囊径最小。同时以一阶导数光谱法测定微囊中阿司匹林含量，方法简单方便，结果准确。     

利用喷雾干燥法制备肠溶微囊的研究

目的采用喷雾干燥法制备肠溶微囊，建立微囊质量评价方法。方法采用丙烯酸树脂Ⅱ号为包衣材料，蓖麻油为增塑剂，乙醇为溶剂，阿司匹林为囊心物，将囊材与囊心物按1：2和1：4的比例喷雾干燥制成微囊。结果经扫描电镜和差示量热扫描法测定表明，微囊包囊形成，囊心物、囊材按1：4较好，微囊能迅速在人工肠液中释放，45分钟释药达75％，而肠溶片45分钟释药低于60％。结论喷雾干燥法制备肠溶微囊方法简单，工艺稳定，改变丙烯酸树脂Ⅱ号比例可控制药物释放速率。     

正交法研究双嘧达莫微囊的制备工艺

目的 :研究双嘧达莫微囊的制备工艺。方法 :用正交设计法对双嘧达莫微囊的制备工艺进行研究。结果 :用单凝聚法制备双嘧达莫微囊 ,其包裹率与囊心囊材比有显著性差异 (P<0.05) ,而搅拌速度能影响微囊的粒径 ,当囊心囊材比为1∶4、成囊温度50℃、搅拌速度为400r/min时 ,包裹率最高 ,囊径最小。结论 :该法工艺简单、可靠     

双嘧达莫缓释微囊的制备与体外评价

目的:研究以明胶和阿拉伯胶为囊材,将双嘧达莫微囊化的制备工艺。方法:以微囊的药物包封率为制备工艺优化指标,利用复凝聚法,通过正交实验得出微囊的最佳制备工艺条件。结果:囊材与囊心物的质量比2∶1,搅拌转速140r·min-1,固化时间3h、成囊pH4.0、成囊温度为50℃为最佳工艺条件。结论:以最佳制备工艺条件制备含药微囊,重复性好,工艺稳定,同时体外溶出实验表明,该微囊具有较好的缓释作用。     

盐酸黄连素肠溶微囊的制备及评价

目的：以聚丙烯酸树脂Ⅱ号为囊材，制备盐酸黄连素肠溶微囊，并测定其体外溶出度。方法：采用溶剂挥发法制备盐酸黄连素肠溶微囊，通过正交实验进行优化，以微囊的包封率及栽药量为指标。结果：应用优化工艺制备的盐酸黄连素肠溶微囊，栽药量为11．18％，包封率为85．00％，盐酸黄连素肠溶微囊在pH为6．8、7．4的溶出介质中60min内溶出度超过70％。结论：采用溶剂挥发法制备盐酸黄连素肠溶微囊，工艺稳定可靠，操作简便，栽药量高，具有肠溶特性，显示出良好的应用前景。     

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.     

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.     

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.     

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.