高效液相色谱法测定氯霉素地塞米松搽剂中二组份的含量

目的建立一种快速、准确的高效液相色谱法测定氯霉素地塞米松搽剂中的氯霉素和醋酸地塞米松含量的方法。方法色谱柱岛津VP-ODS(5μm,150mm×4.6mm)流动相:甲醇-水(70∶30);流速:1mL.m in-1;检测波长:240nm;柱温:室温;进样量:20μL。结果氯霉素进样量在5.00μg~30.00μg范围内线性良好,r=0.99999。平均回收率为99.70%,RSD=0.68%(n=9);醋酸地塞米松进样量在0.13μg~0.75μg范围内线性良好,r=0.99999。平均回收率为99.97%,RSD=1.38%(n=9)结论试验结果表明本法简便快速,重现性好,结果准确可靠,可以作为氯霉素地塞米松搽剂中氯霉素和醋酸地塞米松含量测定的方法。     

高效液相色谱法测定复方醋酸地塞米松搽剂中2组分的含量

目的建立高效液相色谱法测定复方醋酸地塞米松搽剂中地塞米松、樟脑的含量。方法 CAPCELL PAK C18色谱柱(4.6 mm×150 mm,5μm),流动相:乙腈-水(65∶35,V/V),柱温:30℃,流速:1.0 mL.min-1,检测波长:298 nm。结果地塞米松、樟脑进样量分别在0.375～6.00μg(r=0.999 9)、9.69～155.04μg(r=0.999 9)范围内有良好线性关系,平均回收率分别为(100.75±0.83)%、(99.61±0.71)%,RSD分别为0.81%、0.69%(n=9)。结论本方法简便、准确、重复性好,可用于复方醋酸地塞米松搽剂的质量控制。     

HPLC法测定醋酸地塞米松搽剂中醋酸地塞米松的含量

目的建立高效液相色谱法测定醋酸地塞米松搽剂中醋酸地塞米松的含量.方法采用Agilent高效液相色谱仪,流动相为乙腈-水(40∶60),流速1.5mL·min-1,检测波长240 nm,柱温:35℃.结果醋酸地塞米松在7.812～85.932μg·mL-1范围内,线性关系良好,r=0.999 9,回收率为99.3%.结论本法可准确测定醋酸地塞米松搽剂中醋酸地塞米松的含量,适用于产品的质量控制.     

高效液相色谱法测定复方地塞米松搽剂中盐酸达克罗宁的含量分析

目的建立采用高效液相色谱法测定复方地塞米松搽剂中盐酸达克罗宁的含量的方法。方法采用Kromasil C18柱(4.6mm×250mm,5μm),HPLC反相法进行分离,紫外检测器检测,流动相为乙腈-水-冰醋酸-三乙胺(45∶55∶0.5∶0.5);流速:1.5mL·min-1;测定波长:279nm;柱温:40℃:进样:20μL。结果该方法没有受到处方中基质干扰。盐酸达克罗宁的线性范围为0.1003～0.7021μg(r=0.9998,n=6),平均回收率分别为98.8%,RSD为0.97%(n=9)。结论该方法操作简便、准确、快速、重现性好,可用于复方地塞米松搽剂中盐酸达克罗宁的含量测定。     

高效液相色谱法测定盐酸氟西汀的含量

目的建立测定盐酸氟西汀含量的高效液相色谱法。方法选用Agilent Eclipse XDB-C8柱(4.6 mm×250mm,5μm);流动相:四氢呋喃-甲醇-三乙胺缓冲液(取三乙胺10ml,置1 000ml量筒中,加水980ml,用磷酸调节pH值至6.0)(301060);流速为1.0ml/min;检测波长:227nm;进样量:10μl;柱温:25℃。结果方法的线性范围为55.17~165.51μg/ml(r=0.999 9);最低检测限:0.15μg/ml;回收率在99.9%~100.0%之间,重复性RSD为0.1%(n=6)。结论方法简便灵敏,结果准确可靠,可用于盐酸氟西汀的质量控制。     

复方地塞米松搽剂的制备及质量控制

目的:制备复方地塞米松搽剂并建立其质量控制方法。方法:以氮酮为促透剂、乙醇为溶剂制备复方地塞米松搽剂,采用高效液相色谱法测定制剂中主药醋酸地塞米松和维生素E的含量。结果:醋酸地塞米松、维生素E检测浓度分别在2~40μg/ml、80~800μg/ml范围内呈良好线性关系,平均回收率分别为100·5%(RSD=0·82%)、98·6%(RSD=0·59%)。结论:该制剂处方合理,质量控制方法简便、准确。     

HPLC法测定氯霉素地塞米松搽剂的含量

目的:建立HPLC法测定氯霉素地塞米松搽剂中氯霉素和醋酸地塞米松的含量。方法:色谱柱为C18柱(4.6mm×250mm,5μm),流动相为甲醇-水(68∶32),流速为1.0ml·min-1,检测波长为240nm。结果:氯霉素在400~1200μg·ml-1(r=1.000)范围内线性关系良好,平均回收率为100.1%(n=9),RSD为0.32%;醋酸地塞米松在10~30μg·ml-1(r=1.000)范围内线性关系良好,平均回收率为100.8%(n=9),RSD为0.71%。结论:该方法简便、准确、快速,可同时测定两组分的含量。     

高效液相色谱法测定地塞米松透剂中醋酸地塞米松的含量

目的:制备地塞米松透剂;建立高效液相色谱法测定醋酸地塞米松含量的方法。方法:采用 Nova—Pak C_(18)柱;流动相:甲醇-水(70:30);流速:1ml·min~(-1);检测波长:240nm。结果:浓度在20～200μg/ml 范围内线性良好(r=0.9999)。平均回收率99.7%,RSD 为0.67%。结论:该方法简便,准确,重现性好,适用于醋酸地塞米松透剂的质量控制。     

醋酸地塞米松搽剂的含量测定及方法学考查

目的采用HPLC法测定醋酸地塞米松搽剂中醋酸地塞米松的含量测定并进行方法学考察。方法用十八烷基硅烷键合硅胶为填充剂,甲醇-水(70∶30)为流动相,检测波长为240nm,柱温:25℃,流速:1.0mL/min,理论板数按醋酸地塞米松峰计算为7423,醋酸地塞米松峰和其它物质的分离度均>1.5。结果醋酸地塞米松的检测量为10～80μg范围内时呈良好线性关系,标准曲线:y=0.3075x+0.0318(r=0.9999),平均回收率为:99.00%,RSD=0.47%。结论该方法快速、简便、可靠、准确度高、重复性好,处方中其他成分对测定亦无干扰,分离效果好,可用于醋酸地塞米松搽剂的含量测定。     

HPLC法测定菌克软膏中醋酸地塞米松的含量

目的：建立反相高效液相色谱法测定菌克软膏中醋酸地塞米松的含量。方法：色谱柱为Lichrospher C18（150mm×4.6 mm,5μm）,流动相为甲醇-0.05 mol/L磷酸水溶液（70∶30）,流速为1.0 ml/min,检测波长为240 nm,进样量20μl,柱温为30℃。结果：醋酸地塞米松在0.042 8~0.856 0μg范围内呈良好的线性关系（r=0.999 9,n=6）,平均回收率为98.1%,RSD为1.48%。结论：所建立的方法简便、准确、重复性好,可用于菌克软膏中醋酸地塞米松的含量测定。     

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.