尿囊素乳膏的制备及含量测定

目的制备尿囊素乳膏并建立含量测定方法,制定质量标准。方法采用高效液相色谱法测定尿囊素含量,用SupelcosilLc-18-DB柱,以甲醇-0.02mol/L磷酸二氢钠溶液(3268,pH7.0)为流动相;流速0.8ml·min-1。结果尿囊素在14.0μg/ml-1～224.0μg·ml-1范围内线性关系良好,r=0.9997,平均回收率为101.1%,RSD为0.5%(n=6)。结论本品制备简单,疗效较好,用高效液相色谱法测定尿囊素含量结果准确可靠。     

尿囊素凝胶的制备及含量测定

目的:制备尿囊素凝胶并建立其含量测定方法。方法:以尿囊素为主药,卡波姆-940为基质制备凝胶;采用高效液相色谱法测定其中主药含量。结果:所制凝胶涂展性好;尿囊素检测浓度的线性范围为12.78～68.16μg.mL-1(r=0.9999),平均回收率为99.7%(RSD=0.36%)。结论:本制剂制备工艺简便可行,含量测定方法准确、快速,可用于该制剂的质量控制。     

HPLC法测定维生素E尿囊素乳膏中维生素E与尿囊素含量

目的采用高效液相色谱法测定维生素E尿囊素乳膏中维生素E与尿囊素的含量。方法采用高效液相色谱法。维生素E用C18柱,以甲醇为流动相,流速1.5 mL/min,检测波长284 nm;尿囊素用ZOR-BAX NH3柱,以甲醇:水=80∶20为流动相,流速1.0 mL/min,检测波长为224 nm。结果维生素E线性范围29.32~175.92μg/mL,r=0.999 99,平均回收率为98.89%,RSD=1.54%(n=9);尿囊素线性范围187.68~938.40μg/mL,r=0.999 95,平均回收率为99.90%,RSD=1.92%(n=9)。结论本品制备简单,含量测定用高效液相色谱法,测定方法专属性强,结果准确可靠,并能很好地控制制剂质量。     

便秘舒胶囊中芦荟苷含量测定方法的研究

目的:对便秘舒胶囊中指标成分芦荟苷含量测定方法进行研究。方法:采用反相高效液相色谱法,KESTON ODS2(250mm×4.6 mm,5μm)色谱柱,流动相为水-甲醇(58:42),流速1.0 mL·min~(-1),检测波长359nm。结果:本法平均回收率98.7％(n=9)。结论:建立了一种操作简便、重现性良好的高效液相色谱法测定含芦荟中药制剂中芦荟苷含量。     

HPLC对人血浆中葛根素及葛根黄酮的线性考察

目的:对葛根素及葛根黄酮进行人血浆的线性考察,据此检测葛根素、葛根黄酮及其制剂人体内的药动学行为。方法:用高效液相色谱法考察,色谱条件:流速=1mL·min~(-1);柱温:20℃;检测波长:250nm;进样量50μL;流动相:甲醇:水=25:75。结果:葛根素R=6.56,精密度试验RSD≤5.02％,平均回收率=(100.9±0.5)％,葛根素及葛根黄酮血浆测定的线性范围0.0295～0.708μg·mL~(-1)。结论:用高效液相色谱法可作为葛根素、葛根黄酮及制剂人体内药动学的检测手段,为检测葛根黄酮及制剂人体内的药动学行为提供了方法。     

HPLC法测定吡拉西坦注射液的含量

目的:建立用高效液相色谱测定吡拉西坦注射液的方法。方法:用Diamonsil C_(18)柱,以甲醇—水(10:90)为流动相,流速0.6ml·min~(-1),检测波长230nm。结果:吡拉西坦线性范围0.17～0.78mg·ml~(-1),r=0.9995。平均回收率为100.0％,RSD为0.24％(n=6)。结论:方法简便、准确、重现性好,可作为该制剂的含量测定方法。     

牛黄息炎痛胶囊中胆红素的含量测定

目的:建立牛黄息炎痛胶囊中胆红素的含量测定方法。方法:采用高效液相色谱法,Hypersil C_(18)柱(4.6mm×250mm,10μm),Nova-Pak C_(18)预柱,以二甲基亚砜-乙腈-0.5mol·L~(-1)醋酸铵缓冲液(用冰醋酸调pH=5.3)(6:6:7)为流动相,流速1.0mL·min~(-1) ,检测波长452nm。结果:胆红素在0.28～4.5μg范围内呈良好的线性关系(r=0.99999),平均回收率(n=3)分别为99.1％(RSD=1.0%);98.9%(RSD=1.3％);98.2％(RSD=1.2％)。结论:制定的含量测定方法准确,快速,有效。     

HPLC法测定日本薯蓣中尿囊素的含量

目的:建立测定日本薯蓣中尿囊素含量的方法,并比较日本薯蓣与山药中尿囊素的含量。方法:采用高效液相色谱法。色谱柱为Kromasil C18(250mm×4.6mm,5μm),流动相为甲醇-水(2:98),流速为0.8mL·min-1,检测波长为224nm,柱温为30℃。结果:尿囊素进样量在0.355～4.260μg范围内与峰面积积分值呈良好线性关系(r=0.9998);平均加样回收率为98.77%,RSD=1.49%(n=6)。日本薯蓣明显高于山药中尿囊素的含量。结论:该方法可作为日本薯蓣中尿囊素的含量测定方法。     

HPLC法测定盐酸米诺环素缓释片主药的含量

目的:建立以高效液相色谱法测定盐酸米诺环素缓释片主药含量的方法。方法:色谱柱为Thermo ODS-C_(18),流动相为0.2 mol·L~(-1)草酸铵-0.01 mol·L~(-1)乙二胺四乙酸二钠-二甲基甲酰胺-四氢呋喃(600:180:120:80),检测波长为280 nm,进样量为20μL,流速为1.5 mL·min~(-1)。结果:米诺环素检测浓度的线性范围为0.05～0.5 mg·mL~(-1)(r=0.999 8);平均回收率为99.11%,RSD=0.5%。结论:本方法准确可靠、灵敏度高、重现性好,可用于该制剂的含量测定。     

反相高效液相色谱法测定伪麻黄碱水杨酸盐血药浓度

目的:用反相高效液相色谱法测定伪麻黄碱水杨酸盐在兔血的药物浓度及药代动力学研究。方法:血清样品分别用硫酸铵沉淀蛋白,甲醇提取,用反相高效液相色谱法测定伪麻黄碱水杨酸盐。色谱柱:CLC-DOS 4.6 mm×150 mm,流动相:0.5％硫酸铵-甲醇(48:52),流速:0.8 mL·min~(-1),检测波长210 nm。结果:该方法回收率为99.95％～101.6％,RSD≤8.5％,在兔血中最低检测浓度1.14μg·mL~(-1)。回归方程为A=126.841C-127.976,r=0.999 3。结论:反相高效液相色谱可用于伪麻黄碱水杨酸盐测定。药代动力学参数符合静脉给药二室模型。     

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.