氯诺昔康注射液的HPLC测定

建立了HPLC法测定氯诺昔康注射液的含量和有关物质.色谱柱为Shimadzu VIP-ODS柱,流动相为0.05mol/L乙酸钠溶液(pH 6.0)-甲醇(45:55),检测波长379nm.线性范围为9.6～22.4μg/ml(r=0.9999).回收率100.1%～101.1%,检测限为8.13ng/ml.     

超临界流体色谱法手性拆分盐酸罗哌卡因及其右旋异构体

目的:建立盐酸罗哌卡因注射液中异构体的超临界色谱检测方法.方法:DMCEL CHIRALPAK AS 色谱柱(250 mm×4.6 mm,5 μm),柱温:40 ℃,检测波长:220 nm,流速:2.0 ml/min,背压12 MPa,流动相:超临界二氧化碳-无水乙醇(80∶20).结果:盐酸罗哌卡因及其异构体在0.001~0.005 mg/ml范围内具有良好的线性关系(r=0.999),盐酸罗哌卡因定量限为0.002 mg/ml (相当于0.02%),最低检测限为0.001 mg/ml (相当于0.01%);异构体定量限为0.001 mg/ml (相当于0.01%),最低检测限为0.000 5 mg/ml (相当于0.005%).结论:该方法操作简便,结果准确,可用于盐酸罗哌卡因注射液中异构体的含量测定.     

HPLC法测定阿苯达唑颗粒的含量

目的:建立阿苯达唑颗粒含量的高效液相测定方法.方法:色谱柱为Waters C18 柱(4.6mmx150mm,5μm),流动相为甲醇一水(75:25),流速为1.0ml/min,检测波长为295nm,柱温为30℃.结果:阿苯达唑在1- 20μg/ml浓度范围内呈良好线性关系(r=1.0),平均加样回收率为100.1%(...     

杏贝止咳颗粒中苦杏仁苷的HPLC测定

建立了杏贝止咳颗粒中苦杏仁苷的HPLC测定法.色谱柱Kromasil Ci8柱,以甲醇-水(24:76)为流动相,流速1.0ml/min,检测波长218nm.在13.32～428μg/ml浓度范围内,线性关系良好(r=0.9997),平均回收率98.8%,RSD为1.36%.     

阿托伐他汀钙自微乳的HPLC测定

建立了HPLC法测定阿托伐他汀钙自微乳制剂含量.采用C18色谱柱,乙腈-0.05%乙酸(65:35)为流动相,检测波长248nm,流速1.0ml/min.检测限0.12μg/ml.线性范围1～100μg/ml(r=0.9998),回收率为98.9%～99.5%.     

阿奇霉素片的HPLC测定

建立了HPLC法测定阿奇霉素片的含量.采用ODS色谱柱,流动相为甲醇-水(9:1,含0.3%三乙胺,pH 8.0),流速0.5ml/min,检测波长215nm.线性范围为0.6～3mg/ml(r=0.9991),平均回收率为101.2%,RSD 1.2%.     

高效液相色谱法测定消肿止痛酊中盐酸巴马汀的含量

目的 建立消肿止痛酊中盐酸巴马汀的高效液相色谱含量测定方法.方法 采用色谱柱:岛津VP-ODS C18:柱(5 μm,4.6 mm ×250 mm),流动相:乙腈-0.5%磷酸(20:80),检测波长:345 nm,柱温:40℃,流速:1 ml/min.结果 盐酸巴马汀在0.200 4-4.008 0μg/ml范围内浓...     

盐酸头孢吡肟中N-甲基吡咯烷的离子色谱-电导检测法测定

建立了直接进样离子色谱电导检测法测定盐酸头孢吡肟中的N-甲基吡咯烷.选用高容量阳离子交换柱,进样量25 μl,流动相为9 mmol/L硝酸(含15%乙腈),流速0.9 ml/min,35 min内洗脱所有成分.N-甲基吡咯烷在0.9～25μg/ml浓度范围内线性关系良好(r=0.999 7),检出限为0.095μg/ml,回收率为95.3%.     

HPLC法测定林可霉素利多卡因凝胶的含量

目的:用高效液相色谱法同时测定盐酸林可霉素利多卡因凝胶中林可霉素和利多卡因的含量.方法:流动相为0.05,ol/L硼砂溶液(用85%磷酸溶液调节pH值至5.7)-甲醇-乙腈(75:15:10);色谱柱为C18柱;紫外检测波长为214nm;流速1ml/min;柱温30℃.结果:林可霉素在8.2～513μg/ml范围内线性关系良好,r=0.9999,平均回收率为100.9%(n=6),RSD为1.03%;利多卡因在7.8～487μg/ml范围内线性关系良好,r=0.9994,平均回收率为98.8%(n=6),RSD为1.51%.结论:该方法灵敏度高,线性范围广,具有高的专属性,快速简便,重现性好.     

高效液相色谱法测定洛伐他汀含量及有关物质

目的建立高效液相色谱法测定洛伐他汀的含量和有关物质.方法色谱柱为Symmetry Shield RP8(4.6 mm×150mm,5μm),流动相为乙腈-0.1%磷酸(65:35),流速为1.5 ml/min,柱温为30℃.结果该方法的线性范围为30～450μg/ml(r=0.9998),在线性范围内的高、中、低浓度的平均加样回收率分别为99.8%、99.4%、100.1%,RSD均不大于0.70%(n=5),最低检测限为3 ng.结论本方法适用于洛伐他汀含量及有关物质的测定.     

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.     

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.