高效液相色谱法同时测定复方甲硝唑搽剂中甲硝唑和氯霉素含量

目的建立同时测定复方甲硝唑搽剂中甲硝唑和氯霉素含量的高效液相色谱法。方法采用高效液相色谱仪,色谱柱为AgilentZorbax Eclipse XDB-C18柱(250 mm×4.6 mm,5μm),以甲醇-水-冰醋酸(45∶55∶0.1)为流动相,检测波长为277 nm,流速为1.0 mL/min,柱温为30℃。结果甲硝唑和氯霉素的进样量线性范围分别为214.10～2 141.00μg(r=0.999 9)和55.96～559.60μg(r=0.999 9),平均回收率分别为98.09%(RSD=0.73%)和98.48%(RSD=0.87%)。结论该方法两种成分分离效果好,可同时测定,方法简便快速,结果准确可靠,可作为复方甲硝唑搽剂的质量控制方法。     

高效液相色谱法测定康肤霜中甲硝唑和氯霉素含量

目的建立测定康肤霜中甲硝唑和氯霉素含量的高效液相色谱法。方法色谱柱为VP-ODS C18柱(150 mm×4.6 mm,5μm),流动相为0.1%庚烷磺酸钠溶液(取0.1%庚烷磺酸钠溶液500 mL与二甲基甲酰胺5 mL、冰醋酸0.5 mL,混匀)-乙腈(75∶25),流速为1.0 mL/min,检测波长为272 nm,进样量为20μL。结果甲硝唑与氯霉素进样量分别在50～500μg和25～250μg范围内与峰面积线性关系良好,r分别为0.999 8和0.999 9(n=6),平均回收率分别为99.39%和99.40%,RSD分别为0.68%和0.28%(n=9)。结论该法简便、结果准确、重复性好,可用于康肤霜的质量控制。     

高效液相色谱法测定氯霉素甲硝唑搽剂的含量

目的建立高效液相色谱法同时测定氯霉素甲硝唑搽剂中两组分含量。方法采用高效液相色谱法测定氯霉素和甲硝唑的含量。色谱条件为:Agilent Extend-C18色谱柱(4.6×250mm),流动相:甲醇-水-冰醋酸(45∶55∶0.1),流速1.0mL/m in,检测波长280nm,柱温30℃,进样量10μL。结果线性范围分别是:氯霉素49.82μg/mL~498.20μg/mL,r=0.9999;甲硝唑39.74μg/mL~397.40μg/mL,r=0.9999;平均回收率±RSD分别为99.42%±0.97%,99.83%±0.70%。结论本法简便,快速,准确,适用于该制剂中氯霉素和甲硝唑含量测定。     

高效液相色谱法测定复方氯霉素阴道栓中2种成分的含量

目的建立测定复方氯霉素阴道栓中氯霉素、甲硝唑含量的高效液相色谱（HPLC）法。方法色谱柱为AgilentTC-C18柱（250mm×4.6mm,5μm）,流动相为甲醇-水（50∶50）,流速1.0mL/min,检测波长277nm。结果氯霉素、甲硝唑质量浓度分别在4.008～40.08μg/mL（r=0.9998）和4.024～40.24μg/mL（r=0.9998）范围内与峰面积线性关系良好,平均回收率分别为99.24%和98.73%,RSD分别为0.27%和0.47%（n=6）。结论HPLC法分离度好,快速、简便。     

RP-HPLC法测定氯霉素滴眼液中氯霉素及二醇物的含量

目的:测定氯霉素滴眼液中氯霉素和二醇物的含量.方法:采用RP-HPLC法.色谱系统:色谱柱:Kromasil ODS-1(250×4.6mm)流动相为水-甲醇-冰醋酸(55:45:0.1)[1],流速约为1ml·min-1,检测波长为278nm.结果:氯霉素与二醇物的平均回收率分别为100.6%、100.8%,RSD值分别为0.23%、1.49%.氟霉素线性范围为12.5μg·ml-1～300μg·ml-1,二醇物线性范围为1μg·ml-1～24μg·ml-1.结论:该法快速,简单,准确.可作为该制剂的质量控制标准.     

RP-HPLC法测定氯霉素及注射液的有关物质和含量

目的:采用RP-HPLC法测定氯霉素及注射液的有关物质和含量.方法:用Kromasil C18色谱柱(10μm,4.6mm×200mm),以[0.1%庚烷磺酸钠溶液-二甲基甲酰胺-冰醋酸(500:5:0.5),pH3.2]-乙腈(70:30)为流动相;检测波长为272nm;流速为1.0ml·min-1.结果:氯霉素在0.02～1mg·ml-1范围内呈良好的线性关系,回归方程为Y=16813344X 5465(r=0.9999),氯霉素二醇物在1～40μg·ml-1范围内呈良好的线性关系,回归方程为Y=54695X 541(r=0.9999);平均回收率为99.3%,RSD=0.5%(n=5).结论:所用方法简便、准确、专属性好,可用于氯霉素及注射液的二醇物检测和氯霉素的含量测定.     

九分喷雾剂中士的宁和马钱子碱的含量测定

目的:建立九分喷雾剂中士的宁和马钱子碱的含量测定方法.方法:采用反相高效液相色谱法(RP-HPLC法).色谱柱为NucledurC18柱(5μm,4.6 mm×250 mm);流动相为甲醇-水(65:35),1000 mL溶液中含十二烷基磺酸钠1g、磷酸二氢钾0.4 g;检测波长:254 nm.结果:士的宁和马钱子碱回归方程分别为Y=15.51 2 772.70X(r=0.999 5),Y=6.44 1 848.65X(r=0.999 2);线性范围分别为0.174 7～0.873 6μg,0.108 8～0.544 4μg;平均回收率分别为98.92%,99.43%;RSD分别为1.70%,2.58%.结论:RP-HPLC法可作为九分喷雾剂的质量控制方法之一.     

高效液相色谱法测定面刺霜中甲硝唑、氯霉素的含量

目的:建立同时测定面刺霜中甲硝唑和氯霉素含量的方法。方法:采用高效液相色谱法,色谱柱为Diamonsil C18(250mm ×4.6mm,5μm),流动相为甲醇(?)水(50:50),检测波长为280nm.结果:甲硝唑、氯霉素在10.0～250.0μg/ml浓度范围内均有良好的线性关系,相关系数均为0.9 998,平均回收率分别为100.54％、100.53％,相对标准差分别为0.79％,0.56％ 结论:本方法分离度好、快速、简便,可用于含甲硝唑、氯霉素霜剂的质量控制。     

反相高效液相色谱法测定利巴韦林注射液的含量

目的建立利巴韦林注射液含量测定的反相高效液相色谱(RP-HPLC)法。方法色谱柱为HypersilC18柱(250mm×4.6mm,10μm),以水为流动相,检测波长为207nm。结果利巴韦林质量浓度在20.24～80.96μg/mL范围内与峰面积线性关系良好(r=0.9998),平均回收率为100.09%,RSD=1.26%(n=9)。结论RP-HPLC法简便、快速、准确、专属,适用于利巴韦林及其制剂的质量控制。     

高效液相色谱法测定鼻窦炎口服液中黄芩苷的含量

目的:探讨鼻窦炎口服液中黄芩苷的含量测定方法.方法:采用高效液相色谱法(RP-HPLC法),固定相为Shimpack CLC-ODS色谱柱(5μm,6.0 mm×150 mm),流动相是甲醇-水-磷酸(47:53:0.2),检测波长为278 nm.结果:黄芩苷的线性范围为0.157～1.01μg(r=0.999 9),加样回收率为98.59%,RSD为1 46%(n=9).结论:RP-HPLC法简便、快速、准确,可作为控制鼻窦炎口服液质量的方法.     

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.     

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.     

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.