茜素红荷移分光光度法测定阿奇霉素片的溶出度

目的建立茜素红荷移分光光度法测定阿奇霉素片溶出度的方法。方法采用中国药典附录XC第三法，以250ml pH5的磷酸盐缓冲液为溶剂，转速为100r／min，经45min取样，茜素红荷移分光光度法在538nm处测定阿奇霉素的溶出度，限度为标示量的75％。结果阿奇霉素在51～25μg／ml范围内线性关系良好（r=0．9996），平均回收率为99．2％。结论该方法准确、简便。可用于阿奇霉素片溶出度的测定。     

盐酸硫必利片的溶出度方法研究

目的建立测定盐酸硫必利片溶出度方法。方法采用中国药典2005年版二部附录XC溶出度测定第一法，以0．1mol·L^-1盐酸为溶媒，转速为75r·min^-1，取样时间为30min，在287nm波长处测定其溶出度。结果盐酸硫必利检测浓度的线性范围为16～144μg·mL^-1（r=0．9999）；平均回收率为98．77％，RSD=0．3%（n=9），7批样品30min溶出度均在90％以上。结论本方法操作简便，结果准确，可用于盐酸硫必利片的溶出度测定。     

利福平片溶出度检查方法的改进

目的改进利福平片的溶出度检查方法。方法分别用桨法、篮法两种溶出装置,调整转速进行试验,分别采用过滤、离心两种样品后处理方法,调整供试品溶液的测定浓度,比较试验结果。结果利福平片较为适宜的溶出度检查方法为：以盐酸溶液（9→1000）为溶出介质,采用篮法装置,转速为100r／min,于45min取样,用离心方式处理供试品溶液并用磷酸盐缓冲液制成每ml中约含利福平30pg的溶液,随行对照品,采用可见一紫外分光光度法在溶液制备后30min内于474nm波长处进行测定。其溶液浓度在15～45μg／ml的范围内与吸光度呈良好的线性关系,以溶液浓度为横坐标,吸光度为纵坐标绘制标准曲线,其回归方程为：Y=0．0350X＋0．0262,r=1．0000;测定平均回收率为99．2％,RSD=1．0％,n=9。结论本法溶出条件科学合理,测定方法具有良好的线性、回收率和精密度。     

加替沙星片溶出度的测定

目的建立加替沙星片的溶出度测定方法。方法以0．1mol／L盐酸为溶出介质，转篮法(转速100r／min，45min取样)，检测波长325nm，紫外分光光度法测定。结果加替沙星片在线性范围1．519～9．114μg／ml浓度和吸收度之间具有良好的线性关系(r=0.9997)，平均回收率为100．55％，RSD为0．846％，三批样品的溶出度均大于90％。结论该法操作简便，快速，可作为评价制剂工艺是否合理和稳定的一项指标。     

盐酸三氟拉嗪片溶出度的测定方法

目的：建立盐酸三氟拉嗪片的溶出度测定方法。方法：按2000年版《中国药典(二部)》附录溶出度测定项下第三法，以盐酸溶液(1：20)为介质，转速75r／min，用紫外分光光度法检测，测定波长为256nm。结果：在1．90～11．38μg／mL范围内，浓度与吸收度里良好的线性关系(r＝0.9998)，平均回收率为99．2％，RSD＝0．99％(n＝6)。规定45min的溶出量不得少于标示量的80％。结论：方法简单、准确，能有效控制盐酸三氟拉嗪片的质量，并可作为质量控制标准之一。     

异福酰胺胶囊溶出度测定方法

目的：建立复方制剂异福酰胺胶囊中利福平溶出度测定方法。方法：以紫外－可见分光光度法测定难溶性成分利福平的溶出量作为异福酰胺胶囊溶出度测定指标。结果：该方法测得利福平平均回收率为98．90％，RSD为0．66％，结论：该方法辅料及异烟肼，吡嗪酰胺无干扰，方法简捷，结果准确。     

自身对照法测定复方黄连素片溶出度

目的:建立自身对照法测定复方黄连素片溶出度。方法:采用自身对照法(UV)测定复方黄连素片的溶出度。采用篮法,溶出介质为纯化水(900 mL),转速100 r.min-1,取样时间90 min。结果:复方黄连素片溶出度测定自身对照法在1.2～9.0μg.mL-1浓度范围内呈线性(r=0.9995,n=5),回收率98.9%,RSD=0.03%。结论:本法简便、准确、可行,可作为复方黄连素片的质量标准中控制项目之一。     

HPLC法测定宗胺因片中氯唑沙宗、乙水杨胺和咖啡因的溶出度

目的：建立高效液相色谱法，测定复方制剂宗胺因片的溶出度。方法：照《中国药典》2005年版（二部）溶出度测定第二法，以0．1mol·L^-1盐酸溶液1000mL为溶出介质，转速为100r·min^-1，45min时取样。以高效液相色谱法，C18柱为固定相，以甲醇-水（48：52）为流动相，检测波长：280nm。测定宗胺因片的溶出度。结果：线性范围为氯唑沙宗0．0825～0．742μg（r=0．9999）；乙水杨胺0．165—0.923μg（r=1．0000）；咖啡因0．0263～0．131μg（r=0．9999），平均回收率为氯唑沙宗100．1％（RSD％=0．4％，n=9）；乙水杨胺99．7％（RSD％=0．8％，n=9）；咖啡因99．3％（RSD％=1．2％，n=9）。结论：本方法简便、快速，专属性强。     

高效液相色谱法测定萘丁美酮分散片的溶出度

目的建立测定萘丁美酮分散片溶出度的高效液相色谱（HPLC）法。方法以0．5％十二烷基硫酸钠溶液为溶出介质,转速为50r／min,取样时间为45min,采用桨法测定萘丁美酮分散片的溶出度。结果萘丁美酮检测质量浓度的线性范围为20～100μg／mL（r=0．9999）,平均回收率为99．56％,RSD=1．13％（n=9）,3批样品45min平均溶出度均在90％以上。结论该方法操作简便,结果准确可靠。     

复方头孢克洛片溶出度测定方法研究

目的建立复方头孢克洛片溶出度的测定方法。方法按2005年版《中国药典（二部）》附录溶出度测定法第一法，分别以水、稀盐酸、磷酸盐缓冲溶液等3种溶出介质进行溶出试验，采用高效液相色谱（HPLC）法测定溶出介质中头孢克洛的质量浓度。结果头孢克洛质量浓度在100-800μg／mL范围内与峰面积具有良好的线性关系，平均回收率为99．89％，RSD=1．11％（n=9）；复方头孢克洛片45min时的溶出量大于标示量的90％。结论所建立的溶出度测定方法简单、准确、可靠，可作为复方头孢克洛片的质量控制方法。     

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.