普卢利沙星片溶出度测定方法研究

目的:建立紫外分光光度法测定普卢利沙星片溶出度。方法:以0.1 mol·L~(-1)盐酸作为溶剂,测定波长274 nm。结果:线性范围为1～10μg·mL~(-1),r=0.9999,平均回收率为100.0%(n=9)。结论:本方法简便,结果准确。     

盐酸克林霉素胶囊溶出度测定方法研究

目的：建立紫外分光光度法测定盐酸克林霉素胶囊溶出度的方法。方法：以0．1mol／L的盐酸作为溶出介质,转速为100r·min-1,紫外分光光度法测定溶出量,检测波长为201nm。结果：在12．1—72．7μg/ml内呈良好的线性关系,r=0．9990,精密度RSD为0．12％（n=6）。结论：本方法简单快速,准确稳定,可用于盐酸克林霉素胶囊溶出度。     

氟哌酸胶囊溶出度测定方法的试验

目的：探讨紫外分光光度法测定氟哌酸胶囊含量的条件、方法和氟哌酸胶囊溶出度的测定。方法：用紫外分光光度法测定氟哌酸胶囊含量及转篮法测定其溶出度。结果：在２７３ｎｍ 波长处有最大吸收（５μｇ／ｍｌ,０４ ％ 氢氧化钠溶液） ,其吸收系数平均值（ Ｅ１ ％１ ｃｍ ） 为１０９５ , 线性关系良好（ ｒ ＝０９９９８） 。２０ｍｉｎ 溶出率（ ％ ） 均在８０ ％ 。结论：氟哌酸胶囊含量测定可采用紫外分光光度法,简便易行,快速准确。同时可用于氟哌酸胶囊溶出度测定。     

维生素B4片溶出度测定方法研究

目的对维生素B4片的溶出度测定方法进行研究。方法采用紫外分光光度法测定维生素B4片的溶出度，测定波长为（262±1）nm。结果维生素B4质量浓度在4～16μg／mL范围内与吸收度线性关系良好，r=0．9997（n=6），平均回收率为99．59％，RSD=0．8％（n=9）。结论该方法灵敏，结果准确可靠，重现性好，可用于维生素B4片的溶出度测定。     

紫外分光光度法测定普卢利沙星片中主药的含量

目的:建立以紫外分光光度法测定普卢利沙星片中主药含量的方法。方法:以0.1mol.L-1盐酸溶液为溶剂,测定波长为274nm。结果:普卢利沙星检测浓度在1~10μg.mL-1范围内线性关系良好(r=0.9999),平均回收率为100.0%(RSD=0.31%,n=9)。结论:本方法操作简便,检测结果准确。     

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。     

齐墩果酸微囊的制备及溶出度的测定

目的：制备齐墩果酸微囊并进行体外溶出度的测定。方法：采用紫外分光光度法测定自制的齐墩果酸微囊的含量，测定波长为210nm。结果：齐墩果酸质量浓度在4～120mg·L^-1范围内线性关系良好（r=0．9999），其平均回收率为99．56％（RSD为1．15％）。同时测定齐墩果酸微囊和市售齐墩果酸片剂的体外溶出度大小，齐墩果酸微囊30min时溶出度为（76．2±1．9）％，片剂的溶出度为（15．8±1．0）％（P〈0．01）。结论：齐墩果酸微囊制备方法简单，可显著提高齐墩果酸的体外溶出度。     

司帕沙星栓的制备及质量控制

目的：研究司帕沙星栓的制备方法及质量控制标准。方法：采用紫外分光光度法进行含量测定，测定波长为292nm，同时对制剂稳定性进行了初步考察。结果：平均回收率为100．9％，RSD为0．79％（n=9)。结论：该制剂工艺简单，质量稳定，以紫外分光光度法测定其含量，具有简便，快速之特点。     

紫外分光光度法测定双苯氟嗪片的含量、含量均匀度及溶出度

目的:建立紫外分光光度法测定双苯氟嗪片含量、含量均匀度及溶出度的方法.方法:采用紫外分光光度法测定含量、含量均匀度和溶出度.溶剂为0.1 mol·L-1的盐酸溶液;测定波长为248 nm;含量及含量均匀度的测定浓度为12.5 μg·mL-1,溶出度的测定浓度为10μg·mL-1.采用对照品比较法计算含量、含量均匀度和溶出度.结果:双苯氟嗪在4～28 μg·mL-1的范围内线性关系良好,r=0.999 9(n=7).平均回收率为99.7%,RSD为0.16%(n=9).结论:该法简便,准确,可作为双苯氟嗪片含量、含量均匀度及溶出度的测定方法.     

紫外分光光度法测定氧氟沙星胶囊的含量

本文报道了以0.1mol／L盐酸溶液为溶剂，采用紫外分光光度法测定氧氟沙星胶囊的含量的方法，其平均回收率99.51％，RSD=0．60％，n=9；样品含量测定的平均RSD为0．90％，n=6。     

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.     

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.     

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.