双黄连气雾剂中黄芩苷含量降低影响因素探讨

目的 通过对双黄连气雾剂黄芩苷含量的影响因素进行分析，确定最佳制备工艺。方法 考察气雾阀门处理方法、灌装抛射剂装量对制剂中黄芩苷含量的影响。结果 气雾阀门直接使用（不处理）、抛射剂装量为7.0～7.2 g时，黄芩苷含量降低最小。结论 双黄连气雾剂最优制备工艺为气雾阀门直接使用、抛射剂装量7.0～7.2 g。     

金喉含片制备工艺研究

目的研究了金喉含片的工艺制备过程,确定最佳工艺参数。方法采用正交试验,考察岗梅和金牛草两味药水提工艺方法和制剂成型工艺,分别以水提干膏收率和制粒、外观、口感为指标优化了工艺参数。结果确定最佳水提工艺方法:药材分别加10、12倍量水,第一次煎煮2h,第二次煎煮2h。最佳成型工艺为:每1个处方填充剂(蔗糖:乳糖)配比为4∶1,主药与所有辅料配比为1∶1.94,加0.5%甜菊素做矫味剂。每片重0.5g。结论本试验采用的方法和指标适合于金喉含片的制备工艺。     

正交试验优选龙胆中龙胆碱提取工艺

目的:优选龙胆中龙胆碱的最佳提取工艺。方法:以龙胆碱含量为指标,以氨水浓度、乙醇浓度、醇氨比例、提取时间为考察因素,采用正交试验优选最佳提取工艺。结果:最佳提取工艺为龙胆药材加10倍量的溶剂(95%乙醇-20%氨水(3∶1)),80℃回流提取2次,每次1h。结论:该工艺稳定、合理、可行,适用于工业化生产。     

金喉含片制备工艺研究

目的研究了金喉含片的工艺制备过程,确定最佳工艺参数。方法采用正交试验,考察岗梅和金牛草两味药水提工艺方法和制剂成型工艺,分别以水提干膏收率和制粒、外观、口感为指标优化了工艺参数。结果确定最佳水提工艺方法：药材分别加10、12倍量水,第一次煎煮2h,第二次煎煮2h。最佳成型工艺为：每1个处方填充剂（蔗糖：乳糖）配比为4∶1,主药与所有辅料配比为1∶1.94,加0.5%甜菊素做矫味剂。每片重0.5g。结论本试验采用的方法和指标适合于金喉含片的制备工艺。     

头皮脂溢搽剂制备工艺研究

目的:研究头皮脂溢搽剂的制备工艺。方法:采用正交试验设计L9(34),以60%乙醇为溶剂,以盐酸小檗碱含量为考察指标,以提取方法、提取时间、溶剂用量和提取次数为考察因素,确定最佳制备工艺。结果:最佳制备工艺为采用浸渍法,提取时间为48h,60%乙醇用量1500mL,提取次数为2次。结论:本工艺稳定、可行,可为头皮脂溢搽剂的工业化生产提供理论依据。     

以氯氟烃（CFC）和氢氟烷（HFA）为抛射剂的沙丁胺醇气雾剂的特性比较

目的：比较分别以氯氟烃（CFC）和氢氟烷（HFA）为抛射剂的沙丁胺醇气雾剂的特性。方法：测定使用2种抛射剂的沙丁胺醇气雾剂的每揿主药含量和含量均匀度，使用8级Anderson多级圆盘撞击取样器测定空气动力学雾粒大小分布、测定其温度下降效应及年泄漏率等项目。结果：2种气雾剂各3批样品的lO瓶的每揿主药含量均在标示量的80％～120％之间；以CFC为抛射剂的气雾剂的质量中间空气动力学直径（MMAD）为3．82～3．98斗m，以HFA为抛射剂的气雾剂的MMAD为3．40—3．41μm;使用HFA为抛射剂的气雾剂，其温度下降值比使用CFC为抛射剂的气雾剂大；年泄漏率均小于1．8％。结论：2种气雾剂在体外具有相似的特性；所建立的气雾剂体外质鼍评价项目为CFC抛射剂替代品的研究提供了参考。     

环孢素A自微乳软胶囊的制备及质量控制

目的：制备环孢素A自微乳软胶囊,确定纳米粒径测定方法,控制产品质量。方法：通过测定环孢素A溶解度,以及以自微乳化后的粒径、自乳化时间和色泽为指标,对油相、潜溶剂、乳化剂、助乳化剂进行筛选,制备环孢素A自微乳软胶囊;通过稳定性、精密度等方法学试验,确定自微乳化后乳滴直径测定方法,控制产品质量。结果与结论：油相、潜溶剂、乳化剂、助乳化剂比例为1∶2∶2∶2时可获得优良的自乳化效果,软胶囊平均自微乳粒径为25 nm,因此提高了环孢素生物利用度,减少了服用量。     

微波辐射-溶剂回流提取农吉利中农吉利甲素

目的 利用微波辐射引起农吉利药材细胞破壁,研究在微波辐射-溶剂回流提取中各因素对生物碱农吉利甲素提取的影响,探讨其最佳实验条件及工艺方法,以提高其提取效率。方法 采用微波辐射处理含有一定水分的药材,再以甲醇为溶剂回流提取农吉利中农吉利甲素,用高效液相方法测定提取液的含量。结果 微波辐射-溶剂回流提取农吉利甲素的实验条件为：药材颗粒度80目,加水量21.0 mL,微波功率40%,辐射时间2 min,提取温度80 ℃,提取时间2 h,料液比1∶20。结论 经过微波辐射农吉利药材,再溶剂回流提取,农吉利甲素的提取率明显提高,优于直接溶剂回流提取和超声提取方法,且方法简单,操作简便。     

坎地沙坦酯自微乳软胶囊的制备

目的通过坎地沙坦酯自微乳软胶囊的制备工艺研究,确定其最佳工艺条件。方法采用伪三元相图优化了软胶囊内容物的配方,并制备和优化了载药自微乳软胶囊的工艺。结果内容物以乙酸乙酯为油相,RH40为乳化剂,聚乙二醇400为助乳化剂,且三者最佳配比为9∶14∶7。软胶囊囊壳材料最佳配比为明胶∶甘油∶水=1∶0.5∶1,且评价了坎地沙坦酯自微乳软胶囊的相关特性。结论本工艺简单、稳定、可靠。     

玄丹巴布剂的醇提工艺研究

目的用正交法优选玄丹巴布剂药材的最佳提取工艺条件。方法以延胡索乙素、淫羊藿苷的含量及出膏率为试验指标,应用L9(34)正交试验法。结果最佳提取条件为:体积分数70%乙醇提取2次,第1次加10倍量溶剂提取2h,第2次加8倍量溶剂提取1h。结论验证试验表明,最佳提取工艺为A1B2C3D2。说明优选工艺稳定、可靠。     

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.