薄层色谱法检查雌三醇栓剂中的有关物质

目的建立雌三醇栓中有关物质的检查方法。方法采用薄层色谱法。结果所建方法简便可行,能将有关物质和原药能完全分离,且重复性好。结论所用方法可有效的控制雌三醇栓剂中的有关物质。     

薄层色谱法检查磷酸伯氨喹的有关物质及对映异构体的研究

目的:建立磷酸伯氨喹的有关物质检查法及鉴定其对映异构体.方法:采用薄层色谱法常用的硅胶GF254薄层板,以醋酸乙酯-异丙醇-浓氨溶液(43:35:5)为展开剂,以自身对照法检查磷酸伯氨喹原料的有关物质.采用正相高效液相色谱法,以Waters 5 μm硅胶柱为色谱柱,检测波长为261 nm,流动相为氯仿-正己烷-甲醇-浓氨溶液(45:45:10:0.1),流速为2 mL/min,确认其对映异构体.结果:有关物质均能达到较好分离,最低检出限可达0.3μg.薄层色谱中主斑点上方杂质斑点经鉴定为其对映异构体.结论:薄层色谱法较<英国药典>的高效液相色谱法更简便、快速,灵敏度较高,适用于磷酸伯氨喹的有关物质检查.     

薄层色谱法测定阿德福韦酯有关物质

目的：建立阿德福韦酯有关物质薄层色谱检查法。方法：反相薄层色谱法，甲醇-水(3：1)为展开剂，在紫外光254nm下检视。结果：经方法学验证本法能有效分离并检测阿德福韦酯中的有关物质。最小检测限为0．1μg。结论：反相薄层色谱法避免了阿德福韦酯在硅胶薄层色谱法中发生分解的现象，且分离效果好，检测灵敏度高。     

萃取-薄层色谱法检测克拉霉素注射液中的有关物质

目的 建立萃取-薄层色谱法(TLC)检查克拉霉素注射液中的有关物质及分解产物。方法 用乙酸乙酯萃取，萃取液浓缩至干，氯仿定容，TLC法检查。TLC条件为氯仿-甲醇-氨溶液(120：20：0．2)作展开剂；硫酸铈2．0g与钼酸钠2．5g，加入10％硫酸溶液使成100ml为显色剂。结果 对杂质的最小萃取量2．5μg，萃取率大于96％；所选展开剂对有关物质及分解产物均可实现清晰分离，显色剂的最低检出限2μg；平行萃取、检查三次的结果相同。结论 本法对杂质萃取、分离、检出的效果良好，具有重复性，可有效地用于存在辅料干扰的克拉霉素注射液中的有关物质检查。     

中国药典2020年版药用辅料二丁基羟基甲苯质量标准有关物质检查修订建议

摘要 目的：针对《中国药典》2020年版四部二丁基羟基甲苯质量标准中有关物质检查项采用的薄层色谱法专属性差、重复性不强、耗时较长等问题,建立有关物质测定的高效液相色谱分析方法,对该辅料质量标准进行修订。方法：将薄层色谱法检查有关物质修订为高效液相色谱法,并进行方法学验证。结果：按修订后方法进行有关物质检查,9种指定杂质具有良好分离度,4批样品均符合规定。结论：修订后有关物质检查方法操作简单,灵敏度高,实验结果准确可靠,可替代《中国药典》2020年版四部二丁基羟基甲苯质量标准现有有关物质检查方法。     

薄层色谱法测定尼索地平中的有关物质

目的：建立测定尼索地平有关物质的薄层色谱方法。方法：采用GF254薄层板，以氯仿-丙酮-氨水（190：5：1）为展开剂，在紫外灯254nm下检视。结果：尼索地平与其有关物质斑点完全分离。结论：此法操作简便、快速、准确。     

HPLC法测定替加氟注射液的有关物质

目的:建立以高效液相色谱法测定替加氟注射液中有关物质的方法。方法:色谱柱为Kromasil C18,柱温为30℃,流动相为甲醇-水(25∶75),检测波长为282nm,流速为1.0mL·min-1,进样量为20μL。结果:有关物质与主药色谱达到有效分离,样品中有关物质的含量分别为2.35%、2.37%、2.24%。结论:与薄层色谱法相比,本方法更准确、灵敏度更高,可用于该制剂的有关物质检查。     

薄层色谱法检查甲磺酸双氢麦角毒碱片中的有关物质

目的 采用TLC法检查甲磺酸双氢麦角毒碱片中的有关物质.方法 使用硅胶G薄层板,以氨水饱和的氯仿-甲醇(9:1)为展开剂,1％对二甲氨基苯甲醛为显色剂.结果 该方法能有效分离并检测甲磺酸双氢麦角毒碱片中的有关物质.结论 所用方法专属性好、灵敏度高,可用于甲磺酸双氢麦角毒碱片中有关物质的检查.     

两种薄层板对阿奇霉素片中有关物质检查结果的实验对比

目的探讨不同薄层板对阿奇霉素片有关物质检查产生的结果。方法同一供试品溶液分别采用自制板和预制板展开。结果两种薄层板实验结果基本一致，预制板分离效果比自制板好。结论两种薄层板均可用于阿奇霉素片的有关物质的检查。     

反相薄层色谱法在药物分析中的应用研究进展

目的本文简要概述了反相薄层色谱法在药物分析中的应用研究进展。方法通过查阅国内外相关文献资料,对反相薄层色谱的原理及应用研究加以综述。结果反相薄层色谱法可用于中药材鉴别、有关物质检查和手性药物分离。结论反相薄层色谱法具有设备简单,操作简便等特点,可广泛应用于药物分析中。     

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.

---

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.