高效液相色谱法测定克痔栓中盐酸小檗碱的含量

目的:建立高效液相色谱法测定克痔栓中盐酸小檗碱含量的方法.方法:色谱柱为Eclipse XDB-C8,流动相为乙腈-0.05mol·L-1磷酸二氢钠溶液(pH 3)(30:70),检测波长:345nm,流速:1.0 mL·min-1.结果:盐酸小檗碱在0.096～0.64 μg范围内线性关系良好(r=0.999 9),平均回收率为98.2%,RSD =1.1%(n=5).结论:该方法简便可靠,可用于克痔栓的质量控制.     

克痔栓的制备及质量控制

目的:制备能消除或缓解痔疮发作期症状的克痔栓,并制订其质量控制标准.方法:由血竭、白及、黄柏、冰片4味中药为主药,半合成脂肪酸(36型)为栓剂基质制成栓剂,采用高效液相色谱法测定处方中主药血竭中血竭素的含量来控制该制剂的质量,同时用薄层色谱法(TLC)对制剂中的血竭、黄柏进行鉴别.结果:高、中、低3种浓度的平均回收率分别为99.8%,102.1%,101.3%,RSD分别为2.0%,1.8%,2.1%.结论:克痔栓制备工艺简单,质量控制方法可行,性质稳定,可满足临床需要.     

克痔栓的质量控制

目的:建立克痔栓的质量控制标准.方法:采用高效液相色谱法(HPLC)测定主药血竭中血竭素的含量,同时用薄层色谱法(TLC)对制剂中的血竭、黄柏进行鉴别.结果:HPLC线性关系良好,平均回收率为100.7%,RSD为1.32%.薄层图谱斑点清晰,阴性对照无干扰.结论:方法可靠,结果重现性好,可有效地控制该制剂质量.     

高效液相色谱法测定回生第一丹胶囊中血竭素的含量

目的运用反相高效液相色谱法测定回生第一丹胶囊中血竭素的含量.方法采用Zorbax C18柱,乙腈-0.05mol·L-1磷酸二氢钠溶液(50:50)为流动相,检测波长为440nm.结果血竭素平均回收率为100.1%,RSD为1.5%(n=6).结论 本法简便、快速、重现性好,可作为产品的定量分析方法.     

HPLC法测定大七厘散中血竭素的含量

目的:建立血竭素的含量测定方法。方法:HPLC 法,色谱柱为 DiamonsilTM C_(18)(250 mm×4.6 mm,5μm);流动相为乙腈-0.05 mol·L~(-1)磷酸二氢钠溶液(35:65);检测波长为440nm;柱温35℃;流量1 ml·min~(-1)。结果:血竭素含量在2.96～14.80μg·ml~(-1)范围内具有良好线性关系(r=0.999 8),平均回收率为98.54%,RSD=1.36%。结论:本法简便、快速、准确,可用于大七厘散的质量控制。     

HPLC法测定薄荷护表膏中血竭素的含量

目的建立薄荷护表膏中血竭素的含量测定方法。方法薄荷护表膏经3%磷酸甲醇研磨提取、稀盐酸溶解后,用HPLC法测定血竭素含量。色谱柱为Phenomenex C18柱,流动相为乙腈-0.05mol·L-1磷酸二氢钠溶液(32:68),检测波长为440nm,流速为1.0mL·min-1。结果血竭素的平均回收率为99.16%,RSD为2.45%(n=6)。结论本方法简便、准确。可用于测定薄荷护表膏中血竭素的含量     

UPLC测定跌打丸中血竭素与姜黄素的含量

摘 要 目的：建立跌打丸中血竭素和姜黄素的UPLC含量测定方法。方法: 采用超高效液相色谱法,色谱柱为Waters Acquity UPLC BEHC₁₈(100 mm×2.1 mm,1.7 μm)柱,流动相为乙腈-0.05 mol·L^-1磷酸二氢钠溶液(50∶50),血竭素检测波长为440 nm,姜黄素检测波长为431 nm,柱温为30℃,流速为0.1 ml·min^-1。结果: 血竭素在0.001 8～0.036 4μg(r=0.999 9),姜黄素在0.000 8～0.015 6 μg(r=0.999 9)之间呈良好的线性关系。血竭素平均加样回收率为97.94%（RSD=0.89%）,姜黄素平均加样回收率为98.45%（RSD=0.91%）。结论:该方法简便快速,重复性好,可用于跌打丸中血竭素和姜黄素的含量测定。     

RP-HPLC测定祛风除湿膏中血竭素的含量

目的:建立祛风除湿膏中血竭素含量的测定方法。方法:采用反相高效液相色谱法(RP-HPLC)对贴膏中血竭素含量进行测定。结果:以乙腈-0.5moL·L~(-1)磷酸二氢钠溶液(41:59)为流动相,血竭素分离度良好,阴性对照无干扰,血竭素在6.5μg·mL~(-1)~65μg·mL~(-1)范围内线性关系良好,R=0.9995。平均加样回收率为99.01%(RSD 3.81%)。结论:所建立的测定方法简便、可靠、重现性好,可用于祛风除湿膏的质量控制。     

安阳固本膏中血竭素的HPLC含量测定

目的 建立以HPLC测定安阳固本膏中血竭素的含量方法.方法:色谱柱为Diamonsil C18(200 mm×4.6 mm,5μm),流动相为乙腈-0.05 mol/L磷酸二氢钠溶液(45∶55),流速为1.0 ml/min,检测波长为440 nm.结果 血竭素进样量在0.04357~0.26144μg范围内线性关系良好(r=0.9998),平均加样回收率为97.8%,RSD=0.4%(n=6).结论 本方法操作简便、快速、准确,可作为血竭素的定量分析方法.     

龙石膏中钙元素ICP-AES测定及血竭素HPLC含量测定方法研究

目的 建立龙石膏中钙元素和血竭素的定量分析方法.方法 采用微波消解法消解样品,ICP-AES测定龙石膏中钙元素含量,采用HPLC测定血竭素的含量.结果 龙石膏中钙元素含量40.272 6 mg·g-1,回归方程Y=5 916.7X+330.31,相关系数r=0.999 8;血竭素的含量2.144 2 mg·g-1,回归...     

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.