RP-HPLC测定藏药邦贝抗炎栓中的盐酸小檗碱

目的 建立测定藏药邦贝抗炎栓中盐酸小檗碱含量的方法.方法 采用RP-HPLC法,色谱柱为Kromosil C18(200mm x4.6 mm,5 μm),流动相为0.1%磷酸-乙腈(65:35),流速1 ml·min-1,检测波长346 nm.结果 盐酸小檗碱质量浓度0.34～1.68 mg·ml-1与峰面积呈良好的线性关系(r=0.9998),平均回收率为99.7%,RSD=1.25%.结论 所建方法简便、准确、重复性好,适用于藏药邦贝抗炎栓制剂中盐酸小檗碱的含量测定.     

HPLC测定脂溶性前列安栓中盐酸小檗碱的含量

目的 建立一种简便的测定脂溶性前列安栓中盐酸小檗碱含量的方法.方法 采用高效液相色谱法(HPLC)测定盐酸小檗碱的含量.色谱条件为Kromasil C18 柱( 4.6 mm × 200 mm,5 μm), 流动相为乙腈-0.1%磷酸溶液(50:50)(每100 ml中加入十二烷基硫酸钠0.1 g ),检测波长350 nm.供试品预处理采用超声溶解法.结果 盐酸小檗碱在20～200 μg·ml-1范围内有良好的线性关系(r=0.9999),平均回收率为98.9%,RSD为0.5%.结论 本方法可用于脂溶性前列安栓中盐酸小檗碱的含量测定,方法简便、快速、灵敏.     

HPLC法测定羚黄宝儿丸中盐酸小檗碱的含量

目的:建立高效液相色谱法测定羚黄宝儿丸中盐酸小檗碱的含量测定方法.方法:色谱柱:SHISEIDO C18(250mm×4.6 mm,5μm),流动相∶乙腈-0.05％磷酸二氢钾溶液(35∶65),流速:1.0 ml ·min-1,检测波长:345nm.结果:盐酸小檗碱在0.1 ～3.0 μg范围内呈良好的线性关系,r=0.999 5,平均回收率为98.26％,RSD =0.21％ (n =6).结论:该方法准确、重复性好,可用于羚黄宝儿丸中盐酸小檗碱含量测定.     

HPLC法同测定芩连片中盐酸巴马汀和盐酸小檗碱的含量

目的 建立同时测定芩连片中盐酸巴马汀和盐酸小檗碱含量的方法,用于芩连片的质量控制.方法 采用HPLC法.色谱柱为Diamonsil ODS柱(4.6 mm×200 mm,5μm),流动相为50mmol·L-1磷酸二氢钠(pH 4.6)-乙腈(体积比72:28),流速为1.0 mL·min-1,检测波长为343nm,柱温为35℃.结果 芩连片中盐酸巴马汀、盐酸小檗碱与其他成分分离良好;盐酸巴马汀的质量浓度在5.2～52.0mg·L-1(r=0.9998)内、盐酸小檗碱的质量浓度在30.4～304.0mg.L-1(r=0.9997)内与峰面积呈良好的线性关系;盐酸巴马汀、盐酸小檗碱的回收率分别为100.1%、99.9%,RSD分别为1.1%、0.80%.结论 所建立的同时测定芩连片中盐酸巴马汀和盐酸小檗碱含量的HPLC法准确、重现性好,可用于芩连片的质量控制.     

HPLC法测定止痛顺气胶囊中盐酸小檗碱的含量

目的:建立HPLC法测定止痛顺气胶囊中盐酸小檗碱含量的方法.方法:色谱柱:Phenomenex Synergi C18(250 mm×4.6mm,4 μm),流动相:乙腈-0.05 mol·L-1磷酸二氢钠溶液(用磷酸调节pH至3.0)(28:72),检测波长:265 nm,流速:1.0ml·min-1.结果:盐酸小檗碱在0.11～1.11 μg范围内线性关系良好,r＝0.9999,平均加样回收率为98.2%,RSD=1.8%(n=6).结论:该方法操作简便,结果准确可靠,可作为止痛顺气胶囊中盐酸小檗碱的含量测定方法.     

高效液相色谱法测定上清丸中盐酸小檗碱的含量

目的 建立上清丸中盐酸小檗碱的含量测定方法.方法 采用HPLC法.色谱柱为DiamonsilTM C18柱(250mm×4.6 mm,5 μm);流动相为乙腈-0.05 mol·L-1磷酸二氢钠溶液(每1 000 mL中加十二烷基磺酸钠1.7 g)(40:60);流速1.0 mL·min-1;柱温:25℃;检测波长:345 nm.结果 盐酸小檗碱进样量在0.257 5～0.600 9μg与峰面积呈良好线性关系(r=0.999 9),平均加样回收率为98.42%(RSD=1.09%,n=9).结论 该方法简便、准确、重现性好,可用于上清丸中盐酸小檗碱含量的质量控制.     

HPLC法测定前列通片中盐酸小檗碱的含量

目的 建立用高效液相色谱法测定前列通片中盐酸小檗碱的含量.方法 采用Hypersil BDS C18(4.6mm×200mm,5μm)色谱柱:以乙腈-0.1mol·L-1磷酸二氢钾溶液(35∶65)为流动相,流速1.0mL·min-1,紫外检测波长为347nm测定.结果盐酸小檗碱在0.029～3.625 μg·mL-1范围内线性关系良好(r=0.9999),平均回收率为为98.08%,RSD为1.58%(n=6).结论 本方法简便、快速,重现性好,可用于前列通片质量控制.     

HPLC法分析黄藤素及其掺杂的盐酸小檗碱

目的:建立高效液相色谱法分析黄藤素的含量及其掺杂的盐酸小檗碱.方法:采用Agilent TC-C18色谱柱(150 mm ×4.6 mm,5μm);以水(含0.4%磷酸和0.7%三乙胺)-乙腈(70:30)为流动相;流速1.0 ml·min-1 ;检测波长为345 nm;柱温:室温.结果:盐酸巴马汀和盐酸小檗碱分别在22.57~112.86 μg·ml-1和4.65~23.26μgoml-1范围内线性关系良好,盐酸小檗碱的平均回收率为98.90%,RSD为0.43%(n=6).结论:该方法操作简便,测定结果准确可靠,可有效的用于黄藤素及其掺杂的盐酸小檗碱的含量测定.     

HPLC测定三黄汤中4种成分含量

目的 建立高效液相色谱法测定三黄汤中4种重要活性成分（绿原酸、盐酸药根碱、盐酸小檗碱和盐酸巴马汀）的含量。方法 采用Agilent C18色谱柱（4.6 mm×200 mm,5 μm）,流动相为1%醋酸甲醇溶液-1%醋酸溶液梯度洗脱;检测波长：329 nm;流速：1.0 mL·min^-1。结果 绿原酸、盐酸药根碱、盐酸小檗碱和盐酸巴马汀的线性范围分别为0.5-4.0 μg·mL^-1（r=0.999 1）,0.5-4.0 μg·mL^-1（r=0.999 7）,0.5-12.0 μg·mL^-1（r=0.999 3）,0.3-4.0 μg·mL^-1（r=0.999 9）。平均回收率分别为99.0%（RSD=1.13%）,99.3%（RSD=1.20%）,99.0%（RSD=0.27%）,99.8%（RSD=0.88%）。日内、日间RSD均〈2%。结论 本方法准确、灵敏、重复性好,可同时测定三黄汤中4种重要化学成分的含量。     

高效液相色谱法测定连苏胶囊中盐酸小檗碱含量

目的 建立测定连苏胶囊中盐酸小檗碱含量的高效液相色谱法.方法 采用Waters symmetryC18色谱柱(150 mm×3.9mm,5 μm),水(每1000mL中加磷酸二氢钾3.4g,十二烷基硫酸钠1.7g)-乙腈(1∶1)为流动相,检测波长为341 nm.结果 盐酸小檗碱进样量在0.1984 ～0.992 0 μg范围内与峰面积呈良好线性关系,平均回收率为100.25％,RSD=0.88％(n=9).结论 该方法简便、灵敏、准确,适用于连苏胶囊中盐酸小檗碱的含量测定.     

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.