高效液相色谱法同时检测盐酸林可霉素和硝酸咪康唑

目的采用高效液相色谱法同时测定盐酸林可霉素和硝酸咪康唑。方法Hypersil-CN色谱柱(4.6mm×200mm,5μm);流动相:0.05mol.L-1硼砂溶液(用磷酸调节pH至6.0)-甲醇(85∶15);检测波长214nm;流速1.0mL.min-1。结果盐酸林可霉素和硝酸咪康唑的线性范围分别为0.08~3.2mg.mL-1(r=0.9999)和0.08~1.6mg.mL-1(r=0.9993),平均回收率分别为100.0%、99.4%。结论该法简便准确,可用于盐酸林可霉素和硝酸咪康唑复方制剂含量的同时测定。     

HPLC法测定复方硝酸咪康唑软膏中硝酸咪康唑和丙酸倍氯米松的含量

目的 建立高效液相色谱法同时测定复方硝酸咪康唑软膏中的硝酸咪康唑和丙酸倍氯米松的含量.方法 采用Hypersil ODS2 柱(4.6 mm×150 mm,5μm);流动相为0.5%醋酸铵∶甲醇∶乙腈(15∶42.5∶42.5);流速为1.0ml·min-1,检测波长240 nm.结果 硝酸咪康唑在0.976～2.278mg·mL-1范围岗位线性关系良好(r=0.9992),丙致倍氯米松在5.17～12.07μg·mL-1范围内线性关系良好(r=0.9997),硝酸咪康唑和丙酸倍氯米松的回收率分别为99.3%和98.7%.结论 本法快速、简便、准确,可有效地控制复方硝酸咪康唑软膏的质量.     

菌克软膏的制备及质量控制

目的:制备菌克软膏并建立质控标准.方法:采用HPLC法进行定性鉴别并同时测定处方中盐酸林可霉素和硝酸咪康唑的含量.结果:盐酸林可霉素的平均回收率为101.23%,RSD为0.93%;硝酸咪康唑的平均回收率为99.89%,RSD为0.57%.结论:该制剂处方合理,工艺简单,质量可控.     

HPLC测定硝酸咪康唑尿素乳膏中硝酸咪康唑的含量

目的 建立高效液相色谱法测定硝酸咪康唑尿素乳膏中硝酸咪康唑的含量.方法Agilent TC-C18(4.6mm×150 mm,5μm)色谱柱;流动相0.5%醋酸铵溶液·乙腈和甲醇(11)混合液(16.583.5);流速1.0 mL·min-1;检测波长230 nm.结果硝酸咪康唑在0.192 8～1.928 4 mg·mL-1的浓度内线性关系良好(r=0.999 1),平均回收率为98.21%.RSD=1.41%(n=9).结论 此法操作简便、结果准确、精密度好,可用于硝酸咪康唑尿素乳膏的质量控制.     

HPLC法测定克白酊中补骨脂素、异补骨脂素和盐酸异丙嗪的含量

目的建立高效液相色谱法(HPLC)测定克白酊中补骨脂素、异补骨脂素和盐酸异丙嗪的含量测定方法。方法采用HPLC对补骨脂素、异补骨脂素和盐酸异丙嗪的含量进行测定。结果克白酊中补骨脂素含量在10~100μg/ml范围内线性关系良好(r=0.9999),平均回收率99.0%(n=6),精密度RSD=0.13%;异补骨脂素含量在10~100μg/ml范围内线性关系良好(r=1),平均回收率99.6%(n=6),精密度RSD=0.10%;盐酸异丙嗪含量在10~80μg/ml范围内线性关系良好(r=0.9997),平均回收率101.1%(n=6),精密度RSD=2.04%。结论该方法简单,结果准确、重现性好,可作为该制剂的质量控制方法。     

RP-HPLC测定复方麻黄碱滴鼻液中盐酸麻黄碱、盐酸林可霉素和地塞米松磷酸钠含量的方法学研究

目的 建立反相高效液相色谱法测定复方麻黄碱滴鼻液中盐酸麻黄碱、盐酸林可霉素和地塞米松磷酸钠含量的方法.方法采用Dikma C18(150 mm x4.6 mm,5μm)色谱柱,甲醇-0.05mol·L-1硼砂缓冲液(用磷酸调节pH值至6.0)(4753)为流动相,检测波长为241nm.结果盐酸麻黄碱、盐酸林可霉素、羟苯乙酯(尼泊金乙酯)和地塞米松磷酸钠的分离度完全达到要求.盐酸麻黄碱浓度在2.55～30.63 mg·mL-1内线性关系良好(r=0.999 9);盐酸林可霉素在2.58～30.98 mg·mL-1内线性关系良好(r=0.999 6);地塞米松磷酸钠在49.53～594.30 μg·mL-1内线性关系良好(r=1.000 0);平均回收率分别为99.75%(RSD为0.77%)、102.11%(RSD为0.94%)、99.69%(RSD为0.72%).结论 本方法准确、专属、简便、快速,能有效地控制产品的质量.     

HPLC法测定消炎霜中硝酸咪康唑和丙酸氯倍他索的含量

目的建立了高效液相色谱法测定消炎霜中硝酸咪康唑和丙酸氯倍他索的含量。方法用十八烷基硅烷键合硅胶为填充剂;以甲醇-乙腈-0.5%醋酸铵溶液（38∶38∶24）为流动相;检测波长为240nm;进样量20μL。结果硝酸咪康唑和丙酸氯倍他索在0.06mg·mL-1~2.0mg·mL-1及1.5μg·mL-1~100.0μg·mL-1范围内呈良好的线性关系;硝酸咪康唑和丙酸氯倍他索精密度RSD分别为0.57%和0.77%;平均回收率（n=9）分别为98.81%和99.82%。结论本方法准确可靠,专属性强。     

HPLC法测定芩宁软膏中黄芩苷及盐酸达克罗宁的含量

目的建立高效液相色谱法测定芩宁软膏中黄芩苷及盐酸达克罗宁的含量。方法用C18柱,以乙腈-0.02mol.L-1KH2PO4磷酸调节pH至3.0(30∶70)为流动相,检测波长为282nm。结果黄芩苷及盐酸达克罗宁分别在25~125μg.mL-1(r=0.9999,n=5),7.5~37.5μg.mL-1(r=0.9999,n=5)范围内呈良好的线性关系,其平均回收率(n=5)分别为99.5%、100.5%,RSD分别为0.51%、0.92%(n=6)。结论此方法简便、快速、准确。     

RP-HPLC法同时测定复方曲安奈德乳膏中醋酸曲安奈德和硝酸咪康唑的含量

目的建立同时测定复方曲安奈德乳膏中醋酸曲安奈德和硝酸咪康唑含量的方法。方法采用RP-HPLC法。色谱柱为SunFire C18柱,流动相为甲醇-水(70∶30),检测波长为230nm,流速为1.0mL.min-1,柱温为30℃。结果醋酸曲安奈德和硝酸咪康唑质量浓度分别在0.008 4～0.050 4mg.mL-1(r=0.999 7)和0.049 8～0.298 8mg.mL-1(r=0.9998)范围内与峰面积积分值线性关系良好。平均回收率分别是98.3%,RSD为1.6%(n=9);98.6%,RSD为1.5%(n=9)。结论该方法准确、方便、快速,可用于复方曲安奈德乳膏中醋酸曲安奈德和硝酸咪康唑含量的测定。     

HPLC法测定复方硝酸咪康唑软膏中硝酸咪康唑的含量

目的 　测定复方硝酸咪康唑软膏中硝酸咪康唑的含量。方法 　采用高效液相色谱法。色谱柱 :Hypersil ODS( 15 0 mm× 4.6mm,5 μm) ;流动相 :甲醇 -( 0 .0 3 m ol· L - 1、p H6.0 )磷酸二氢钾溶液 ( 80∶ 2 0 ) ;流速 :1.2 ml· min- 1 ;检测波长 :2 3 8nm;进样量 10μL。结果 　硝酸咪康唑在 0 .5～ 8.0 mg· m L- 1 范围内线性关系良好 ( r=0 .9997) ,平均回收率为 99.6% ,RSD( n=6)为 0 .7%～ 1.2 %。结论 　该法操作简便快速 ,结果准确性高 ,可用于测定复方硝酸咪康唑软膏的中间产品及成品的质量分析。     

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.     

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.     

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.