反相高效液相色谱法测定富马酸酮替芬滴鼻液的含量

目的建立测定富马酸酮替芬滴鼻液中富马酸酮替芬含量的反相高效液相色谱法。方法采用Agilent SB-C18色谱柱(250 mm×4.6 mm,5μm),流动相为甲醇-0.1%磷酸溶液(50∶50),流速1.0 mL/min,测定波长301 nm,柱温为室温。结果富马酸酮替芬进样量在0.020 26～1.013 0μg范围内与峰面积线性关系良好,r=0.999 9(n=5);平均加样回收率为99.51%,RSD为1.56%(n=9)。结论所用方法操作简便、准确可靠,可作为富马酸酮替芬滴鼻液的质量控制方法。     

HPLC法测定复方酮替芬滴鼻液中3组分的含量

目的：测定复方酮替芬滴鼻剂中主要成分的含量。方法：采用HPLC法。色谱柱Dia-monsil C18柱（4．6mm×150mm,5μm）;流动相为乙腈-1％乙酸胺溶液（pH5．5）=10：90;流速为1mL·min^-1;检测波长为240nm;柱温为室温。结果：富马酸酮替芬在40．0-160．0μg·mL^-1的范围内,其浓度与峰面积呈良好的线性关系,得回归方程A=1．178C-5．193,r=0．9995（n=7）,平均回收率为100．61％,RSD=0．49％（n=5）。盐酸麻黄碱在200．0-800．0μg·mL^-1的范围内,其浓度与峰面积呈良好的线性关系,得回归方程A=0．3680C-6．455,r=0．9993（n=7）,平均回收率为99．99％,RSD=0．38％（n=5）。呋喃西林在8．0-30．0μg·mL^-1的范围内,其浓度与峰面积呈良好的线性关系,得回归方程A=66．58x-4．103,C=0．9998（n=7）,呋喃西林的平均回收率为98．69％,RSD=0．92％（n=5）。结论：本方法建立的高效液相色谱法操作简单,准确、专属性强、重现性好,可作为复方酮替芬滴鼻剂中酮替芬、麻黄碱、呋喃西林的含量测定。     

复方酮替芬滴鼻液的制备及质量控制

目的:制订复方酮替芬滴鼻液的制备方法及质量标准.方法:用分光光度法测定主药富马酸酮替芬和盐酸麻黄碱含量.结果:处方设计合理,质控方法切实可行.结论:该滴鼻液制备简便,质量可控,能保证药品质量.     

HPLC法测定富马酸酮替芬片的含量

目的:建立富马酸酮替芬片含量测定的HPLC方法.方法:色谱柱:Hypersil ODS C18(5μm,4.6 mm×200mm),流动相:水-甲醇-三乙胺(375:625:0.35),检测波长:300 nnm.结果:富马酸酮替芬在0.01～0.6 mg·ml-1范围内线性关系良好(r=0.999 9,n=5).平均回归率为100.9%,RSD=2.2%.结论:本方法简便,结果准确,重复性好,适用于富马酸酮替芬片的质量控制.     

酮替芬麻黄碱喷鼻剂的制备及质量控制

目的探讨酮替芬麻黄碱喷鼻剂的制备方法及质量标准。方法采用紫外分光光度法测定富马酸酮替芬含量,旋光法测定盐酸麻黄碱含量;以经典恒温加速实验预测该制剂的有效期。结果富马酸酮替芬在7.5~25mg·L-1范围内吸收度与浓度呈良好线性相关,r=0.9999,平均回收率99.99%,RSD为0.41%(n=5);t0.9309d;盐酸麻黄碱t0.9为411d。结论本制剂配制方法简单,质量可控,稳定性较好,有效期暂定为10个月。     

HPLC法测定富马酸酮替芬片的含量及含量均匀度

目的建立高效液相色谱法测定富马酸酮替芬片的含量及含量均匀度的方法。方法采用Shim-pack VP-ODS C18柱(150mm×4.6mm,5μm);以乙腈-0.04mol.L-1磷酸二氢钾(28∶72)为流动相,磷酸调pH 3.5;流速1mL.min-1;检测波长300nm;柱温为30℃。结果富马酸酮替芬在9.75～97.50μg.mL-1的范围内线性关系良好(r=0.999 6),平均加样回收率为99.3%,RSD为0.4%(n=6)。结论高效液相法简便、快速,重复性良好。     

富马酸酮替芬溶液

本品为富马酸酮替芬的含糖溶液。含富马酸酮替芬以酮替芬(C₁₉H₁₉NOS)计,应为标示量的90.0~110%。[性状]本品为黄色粘稠液体;味香甜。     

HPLC法检测富马酸酮替芬滴眼液中的有关物质

目的 建立用HPLC法检测富马酸酮替芬滴眼液中的有关物质。方法 用十八烷基硅烷键合硅胶为填充剂;以水-三乙胺(500∶0.175)为流动相A,以甲醇-三乙胺(500∶0.175)为流动相B;检测波长为297 nm,柱温为40℃;进样量:20μL。结果该色谱系统能完全分离经光照、高温破坏所产生的杂质峰、辅料峰及主峰。富马酸酮替芬的检测限为2 ng,本方法可检测到0.02%的杂质。结论 本法专属性强,操作简便,灵敏,可用于富马酸酮替芬滴眼液中的有关物质检查。     

富马酸酮替芬片溶出度的测定

目的建立富马酸酮替芬片溶出度测定方法。方法采用浆法,以水900 m L为溶出介质,转速50 r·min-1,Inertsil ODS-SP色谱柱(4.6 mm×250 mm,5μm),以甲醇-水-三乙胺(950∶50∶0.02)为流动相,检测波长:300 nm。结果富马酸酮替芬的浓度在0.1~25μg·m L-1内与峰面积线性关系良好,回收率为99.9%,RSD为0.1%。结论该溶出度实验条件可以较客观地反映产品的内在品质,对不同来源的同一制剂具有显著的区分力。     

毛细管电泳法测定富马酸酮替芬糖浆中富马酸酮替芬的含量

目的:建立毛细管电泳法测定富马酸酮替芬糖浆剂中富马酸酮替芬的含量。方法:以50 mmol·L-1磷酸二氢钾缓冲液为运行缓冲液,运行电压为30 kV,检测波长为301 nm。结果:富马酸酮替芬(以酮替芬计)在16.08～80.40μg·mL-1浓度范围内有良好的线性关系(r=0.9995),回收率为100.1%(n=9)。结论:此方法可用于富马酸酮替芬糖浆剂的含量测定。     

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.     

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.     

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.