维血宁颗粒的质量标准研究

目的:提高维血宁颗粒的质量标准.方法:采用薄层色谱法 (TLC法 )对处方中虎杖、白芍、太子参进行定性鉴别;采用反相高效液相色谱法 (RP- HPLC法 )测定颗粒中大黄素的含量.结果: TLC鉴别方法专属性强、大黄素在 0.014 98～ 0. 074 90 μ g范围内进样量与峰面积积分值呈良好的线性关系, r=0.999 3,平均回收率为 99.89% (n=6),RSD=0.97%.结论:本质量标准可有效控制维血宁颗粒的质量.     

复方虎杖烧伤凝胶的制备及质量标准

目的：制备复方虎杖烧伤凝胶并建立其质量标准.方法：以卡波姆-940为基质制备凝胶,用TLC法鉴别凝胶中五倍子、阿魏酸,采用HPLC法测定其中大黄素的含量.结果：复方虎杖烧伤凝胶外观良好、易涂展,pH适宜.薄层色谱斑点清晰,阴性对照无干扰.大黄素在进样量为0.030 6～0.173 4μg范围内与峰面积呈良好的线性关系（r=0.999 6）,平均回收率为99.6%,RSD=1.55%（n=5）.结论：复方虎杖烧伤凝胶制备工艺简单、可行.五倍子和阿魏酸的薄层色谱鉴别方法可靠,大黄素含量测定方法灵敏度高、准确性高、重复性好,可作为复方虎杖烧伤凝胶的质量控制方法. 关     

反相高效液相色谱法测定烧伤涂膜中黄芩苷含量

目的建立测定烧伤涂膜中黄芩苷含量的方法。方法用薄层色谱法鉴别涂膜剂中的黄芩,用反相高效液相色谱法测定涂膜中黄芩苷含量。结果薄层色谱法鉴定结果满意;黄芩苷质量浓度在0.712～3.00 g/L范围内与峰面积线性关系良好,r=0.998 2(n=6),平均加样回收率为95.37%,RSD为1.55%(n=6)。结论定性定量方法简便、可靠、重现性好,可作为烧伤涂膜的质量控制方法。     

HPLC法测定前列达康片中虎杖苷与大黄素的含量

目的:制订前列达康片的质量标准,寻找控制产品质量方法。方法:用高效液相色谱法测定虎杖中虎杖苷和大黄素的含量:Shim-pack C_(18)柱(250 mm×4.6 mm,5μm);虎杖苷以乙腈-水(19:81)为流动相;检测波长为306 nm。大黄素以甲醇- 0.1%磷酸溶液(80:20)为流动相;检测波长为254 nm。结果:虎杖苷在0.146～0.730μg间线性关系良好,r=0.9999;回收率为97.48%,RSD 1.52%;大黄素在0.032 5～0.1625μg间线性关系良好,r=0.9999;回收率为97.29%,RSD 1.64%。结论:本方法准确可靠、重现性好,可用于该制剂的质量控制。     

创愈烧伤膏中大黄素的质量控制

目的 建立创愈烧伤膏的质量标准.方法 采用薄层色谱法对创愈烧伤膏中大黄素进行定性鉴别,采用高效液相色谱法测定创愈烧伤膏中大黄素含量.结果 大黄素的标准曲线回归方程为Y=35.362X+27.283,r2=0.9999(n=7),质量浓度线性范围为2.35 ～150 μg/mL.结论 该法专属性强、简便、准确,可作为控制创愈烧伤膏质量的方法.     

补血糖浆的质量标准

目的:制定补血糖浆的质量标准。方法:采用薄层色谱(TLC)法对处方中鸡血藤、虎杖进行定性鉴别;采用高效液相色谱法测定补血糖浆中大黄素的含量。结果:TLC鉴别方法专属性强,大黄素在4.6～46.2μg·ml~(-1)浓度范围内与峰面积线性关系良好,r=0.999 9,平均回收率为99.2%,RSD=1.2%(n=6)。结论:本质量标准可有效控制补血糖浆的质量。     

HPLC色谱法同时测定川产虎杖中白藜芦醇、白藜芦醇苷及大黄素苷的含量

目的:采用HPLC色谱法,建立同时测定虎杖中白藜芦醇、白藜芦醇苷及大黄素苷(大黄素-8-O-β-D-葡萄糖苷)含量测定方法。方法:选用十八烷基硅烷键合硅胶为填充剂(C18柱250×4.6,5μm),以甲-醇0.8%磷酸水溶液梯度洗脱,0~50 min,甲醇43%~100%,流速为1.0ml/min,检测波长为284nm。结果:白藜芦醇在0.30μg~2.50μg范围内呈良好的线性关系,平均回收率为101.68%(n=5);白藜芦醇苷在0.37μg~3.10μg范围内呈良好的线性关系,平均回收率为100.05%(n=5);大黄素苷在0.24μg~2.00μg之间呈良好的线性关系,平均回收率为99.82%(n=5)。结论:该方法操作简便,结果准确可靠,适于中药虎杖中白藜芦醇、白藜芦醇苷及大黄素苷的同时测定,为含虎杖的药品质量控制提供一定的参考价值。     

烧伤涂膜剂质量标准的拟定

目的建立烧伤涂膜剂的质量标准。方法采用薄层色谱法(TLC)对处方中黄柏、大黄进行定性鉴别;采用高效液相色谱法测定大黄酚的含量,以TechsphereC18为色谱柱,流动相为甲醇-0.1%磷酸(85∶15),检测波长为254nm。结果在TLC色谱中均能鉴别出黄柏、大黄;大黄酚在5.09~50.9μg·ml-1范围内,浓度与峰面积线性关系良好(r=0.9997),平均回收率为99.46%(n=6),RSD为2.34%。结论本法简便、结果准确,可用于烧伤涂膜剂的质量控制。     

虎柏烧伤酊质量标准的研究

目的建立虎柏烧伤酊的质量控制标准。方法采用薄层色谱法对虎柏烧伤酊中的虎杖、黄柏等进行鉴别,并采用HPLC法对制剂中的大黄素进行含量测定。流动相:甲醇-水-冰醋酸(80:20:0.5,V:V);流速:1.0 mL.mL-1;柱温:室温;检测波长:254 nm。结果鉴别项下阴性对照无干扰,专属性强;大黄素在2.575μg.mL-1~20.6μg.mL-1范围内线性关系良好(r=0.9993),平均回收率为98.95%,RSD=1.20%(n=9)。结论该方法简便、准确,可以用于该制剂的质量控制标准。     

高效液相色谱法测定虎杖膏中大黄素的含量

目的:建立虎杖膏中大黄素的含量测定方法。方法:用正交试验考察大黄素最佳提取条件;用高效液相色谱法测定含量,选用Agilent XDB-C18(150 mm×4.6 mm,5μm)色谱柱,以甲醇-0.1%冰醋酸(80∶20)为流动相,柱温30℃,流速1.0mL.min-1,检测波长254 nm。结果:大黄素在6～60 mg.L-1范围内呈良好线性关系(r=0.999 9);平均回收率为99.76%,RSD为1.18%。结论:本实验方法简便、准确,可用于虎杖膏的质量控制。     

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.     

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.     

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.