白金降脂减肥滴丸的成型工艺研究

目的:确立白金降脂减肥滴丸的最佳成型工艺.方法:采用正交试验法,以滴丸的丸形、溶散时间以及滴丸的质量差异系数为评价指标,优选药物与基质配比、药液温度、滴速以及滴头的口径,确定最佳滴制条件.结果:原料药与基质以1:6:1.5-1:8:2配比,药液温度为(80±1)℃,滴速为50滴/min,滴口内外径为1.32/2.28 mm的滴头为最佳滴制条件.结论:白金降脂减肥滴丸滴制方法简单、操作容易切实可行,成品率高,质量稳定.     

草乌甲素滴丸成型工艺研究

目的 确立草乌甲素滴丸的最佳成型工艺.方法 采用正交试验法,以滴丸的丸形、溶散时间以及滴丸的质量差异系数为评价指标,优选药物与基质配比、药液温度、滴速以及滴头的口径,确定最佳滴制条件.结果 原料药与基质以1∶6∶1.5～1∶8∶2配比,药液温度为(80±1)℃,滴速为50滴/min,滴口内外径为1.32/2.28 mm的滴头为最佳滴制条件.结论 草乌甲素滴丸滴制方法简单、操作容易切实可行,成品率高,质量稳定.     

灯盏花素滴丸成型工艺研究

目的了解不同基质与冷却剂、不同药物与基质的比例、不同药液的温度、不同滴头的内外径大小、不同的滴速和滴距以及冷却剂的温度对滴丸滴制的难易程度、丸形、沉降状况以及成丸的溶散时间和滴丸的重量差异系数的影响.方法以滴制的难易程度、丸形、沉降状况以及成丸的溶散时间和滴丸的重量差异系数作为评价标准,对基质和冷却剂的种类、药物与基质的比例、药液温度的选择用正交试验法,对滴头的内外径大小、滴速、滴距以及冷却剂温度的选择用筛选法,优选出最佳试验方案和滴制条件.结果以聚乙二醇6000:聚乙二醇4000(1:4)混合液作为基质,冷却剂选择二甲基硅油:液体石蜡(3:2),原料灯盏花素与基质以1:5配比,药液温度为80℃的试验方案为最佳试验方案;以冷却温度为0～5℃,滴口内外径为4.5/7.0mm的滴头,滴口距冷却液面为5cm,滴速30滴/min的滴制条件为最佳滴制条件.结论本试验优选出的试验方案和滴制条件滴制成的滴丸,成品率高,符合滴丸剂的质量标准.     

参芍双苷滴丸的成型工艺探讨

目的:确立参芍双苷滴丸的最佳成型工艺。方法:采用正交试验法,以滴丸的丸形、溶散时间以及滴丸的重量差异系数为评价指标,优选药物与基质的配比、药液的温度、滴头口径以及滴速,确定最佳滴制条件。结果:最佳条件为参芍双苷原料药与基质比为1∶1.5,药液温度为80℃,滴管内外径为2.14mm/3.18mm,滴速为(30±2)滴/min。结论:本试验优选出的滴制条件切实可行,成品率高。     

灯盏花素滴丸成型工艺研究

目的了解不同基质与冷却剂、不同药物与基质的比例、不同药液的温度、不同滴头的内外径大小、不同的滴速和漓距以及冷却剂的温度对滴丸漓制的难易程度、丸形、沉降状况以及成丸的溶散时间和滴丸的重量差异系数的影响。方法以漓制的难易程度、丸形、沉降状况以及成丸的溶散时间和滴丸的重量差异系数作为评价标准，对基质和冷却剂的种类、药物与基质的比例、药液温度的选择用正交试验法，对滴头的内外径大小、滴速、滴距以及冷却剂温度的选择用筛选法，优选出最佳试验方案和滴制条件。结果以聚乙二醇6000：聚乙二醇4000(1：4)混合液作为基质，冷却剂选择二甲基硅油：液体石蜡(3：2)，原料灯盏花素与基质以l：5配比，药液温度为80℃的试验方案为最佳试验方案；以冷却温度为0～5℃，滴口内外径为4．5／7．0mm的滴头。滴口距冷却液面为5cm，滴速30滴／min的滴制条件为最佳滴制条件。结论本试验优选出的试验方案和滴制奈件滴制成的滴丸。成品率高，符合滴丸剂的质量标准，     

正交试验优选断血流滴丸成型工艺

目的:优选断血流滴丸的成型工艺。方法:采用正交试验,以基质种类、浸膏与基质的比例、药液滴制温度为考察因素,以丸重差异RSD值、溶散时限和滴丸成型率为指标,并进行综合评分,优选成型工艺;以滴距、滴速和滴头内外口径为考察因素,以丸重变异系数为指标,优选滴制条件。结果:优选的成型工艺为以PEG6000为基质,浸膏与基质的比例为1∶3,药液滴制温度为75℃;优选的滴制条件为滴距10cm,滴速50～60滴.min-1,滴头内外口径5.0mm、3.0mm。结论:该工艺为断血流滴丸的制备提供了试验依据。     

正交试验优选复方岩白菜素滴丸制备工艺

目的:确立复方岩白菜素滴丸的最佳制备工艺。方法:采用L9(34)正交试验,以滴丸的溶散时限和外观评分为指标,以基质种类、药物与基质的用量比、药液温度、冷凝剂种类为考察因素,优选最佳成型工艺;以滴丸重量变异系数为指标,以滴头口径、滴速、冷却剂温度、滴距为考察因素,优选最佳滴制工艺。结果:最佳制备工艺是基质为聚乙二醇6000,药物与基质配比为1∶2,药液温度为(70±0.5)℃,冷却剂为液体石蜡,滴头内外径为2.0mm/3.0mm,滴速为60d·min-1,滴距为6cm,冷却剂温度为(10±0.5)℃。结论:该制备工艺稳定、可行、重现性好,所得制剂成型性好。     

山楂叶总黄酮滴丸的制备工艺优化

目的:确立山楂叶总黄酮滴丸的最佳成型工艺.方法:采用正交试验法,以滴丸的外观质量、溶散时间以及滴丸的重量差异系数为评价指标,优选药物与基质的配比、混合基质配比、药液的温度以及冷却剂温度,确定最佳滴制条件.结果:最佳条件为山楂叶总黄酮与基质比为1∶5,混合基质配比PEG 4000∶PEG 6000=1∶2,药液温度为85℃,冷却剂温度为10℃.结论:本方法确定的山楂总黄酮滴丸制备工艺稳定可行.     

正交试验优选左金滴丸的成型工艺

目的:优选左金滴丸的成型工艺。方法:采用正交试验,以基质种类、药物与基质的比例、药液温度、冷却剂种类为考察因素,以混合状况、成型情况、溶散时间为指标选取基质和冷却剂;以冷却剂温度、滴头的内外径大小、滴距、滴速为考察因素,以丸重差异变异系数为指标选取滴制条件。结果:最佳成型工艺为以聚乙二醇4000为基质,液体石蜡为冷却剂,冷却温度为12℃,滴头的内外径大小为3.5/4.9mm,滴距为10cm,滴速为25滴.min-1。结论:该工艺稳定、重现性好,所得制剂成型好,可为左金滴丸的生产提供参考依据。     

正交试验优选杜仲叶滴丸的成型工艺

目的:优选杜仲叶滴丸的成型工艺。方法:在单因素考察的基础上,以滴丸的外观质量、丸重差异变异系数、溶散时限为指标,以提取物与基质比例、冷凝液温度、滴速和滴头口径为考察因素,采用正交试验优选最佳成型工艺。结果:最佳成型工艺为提取物与基质比例为1:2,冷凝液温度为14℃,滴速为30d.min-1,滴头口径为2.50mm/3.62mm。结论:优选的工艺合理、可行,所制得的滴丸形状圆滑,大小均匀,符合滴丸的质量要求。     

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.