HPLC法测定祛斑散中盐酸小檗碱的含量

目的 建立制剂中盐酸小檗碱的含量测定方法. 方法 采用HPLC,以十八烷基硅烷键合硅胶为填充剂,乙腈-0.01 mol·L-1磷酸溶液(含0.15%十二烷基磺酸钠)(50∶50)为流动相,检测波长为350nm,测定制剂中盐酸小檗碱的含量. 结果 盐酸小檗碱在0.065～0.387μg范围内有良好的线性关系,r=1.0000,平均回收率为99.34%,RSD=1.6%(n=5). 结论 可作为该制剂控制质量的参考依据.     

RP-HPLC测定祛疣软膏中盐酸小檗碱的含量

目的测定祛疣软膏中盐酸小檗碱含量.方法采用反相高效液相色谱法,Dikma HPLC column色谱柱(4.6 mm×200 mm,5 μm),以0.033 mol·L-1磷酸二氢钾溶液-乙腈(70∶30)为流动相,流速1.0 mL·min-1,检测波长349 nm,柱温25 ℃测定.结果RP-HPLC测定的线性范围为0.041～0.41 μg,相关系数为r=0.999 8;软膏中盐酸小檗碱的平均回收率为98.6%,RSD=1.6%(n=6),精密度良好(RSD=0.51%).结论该法操作简便、快速、准确,适用于祛疣软膏中盐酸小檗碱的含量测定.     

HPLC法测定炎可宁片中盐酸小檗碱的含量

目的采用高效液相色谱法测定炎可宁片中盐酸小檗碱的含量。方法Kromasil C18色谱柱(250 mm×4.6 mm,5μm);乙腈-0.05 mol.L-1磷酸二氢钾溶液(30∶70)为流动相,流速为1.0 ml.min-1;检测波长为347 nm。结果盐酸小檗碱线性范围为20.2~181.8 mg.L-1(r=0.999 9,n=5),平均回收率为99.71%,RSD=0.32%(n=6)。结论该方法准确、简便,可用于该制剂的质量控制。     

加味左金丸中盐酸小檗碱的提取与含量测定

目的建立加味左金丸中盐酸小檗碱的提取和测定方法。方法以50%甲醇-盐酸(100∶1)为溶剂,超声提取30min作为盐酸小檗碱的提取方法。色谱柱CAPCELL PAK C18;流动相:乙腈-0.05mol/L磷酸二氢钠溶液(含0.2%的三乙胺,用磷酸调pH值为3.0)(25∶75);检测波长263nm。结果盐酸小檗碱在进样量0.06672~1.3344mg范围内线性良好r=1,平均回收率为99.27%,RSD=0.71%,(n=6)。结论该方法操作简便,准确可靠,可用于提取和测定加味左金丸中盐酸小檗碱的含量。     

RP-HPLC法测定肛安栓中盐酸小檗碱的含量

目的采用RP-HPLC法测定肛安栓中盐酸小檗碱的含量。方法色谱柱为Diamonsil C18;流动相为乙腈-0.05mol.L-1磷酸二氢钠溶液（用磷酸调节pH值至3）（30∶70）;检测波长为270nm。结果盐酸小檗碱的进样量在0.16765~0.50294μg之间与峰面积呈良好的线性关系,r=1.0000,平均加样回收率为96.62%,RSD=0.80%（n=6）。结论本方法简便、准确,可用于肛安栓中盐酸小檗碱的含量测定。     

盐酸小檗碱片含量测定方法的改进

目的改进盐酸小檗碱片含量测定的方法。方法采用Agilent Eclipse plus C18(4.6mm×150mm,5μm)色谱柱,流动相:0.05mol.L-1乙酸铵溶液(用乙酸调节pH至5.0)-甲醇(60∶40),以流动相为溶剂,超声溶解,流速为1.0mL.min-1,检测波长为263nm。结果盐酸小檗碱线性范围为8~128mg.L-1,平均加样回收率(n=9)为100.3%(RSD为1.0%)。结论该方法快速简单,结果准确可靠。     

HPLC法测定宁心安神胶囊中盐酸小檗碱的含量

目的建立宁心安神胶囊的RP-HPLC测定方法。方法采用C18柱(250mm×4.6mm,5μm),流动相为0.05mol.L-1磷酸二氢钾溶液(用KOH试液调节pH值至5.0)-乙腈(70∶30),检测波长350nm。结果盐酸小檗碱在0.03904～0.976μg范围内线性关系良好,r=0.99998,平均加样回收率为99.04%,RSD=1.4%(n=5)。结论该方法结果准确,重现性好,可用于测定宁心安神胶囊中盐酸小檗碱的含量。     

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.     

高效毛细管电泳法测定黄连中盐酸小檗碱的含量

目的建立高效毛细管电泳法(HPCE)测定黄连中盐酸小檗碱的含量。方法熔融石英毛细管柱50 cm×75μm,缓冲液为0.05 mol.L-1四硼酸钠溶液(pH=7.0)-甲醇(85∶15),分离电压14 kV,毛细管柱温20℃,UV检测波长254 nm。结果盐酸小檗碱进样浓度在0.026~0.414 mg.mL-1内线性关系良好(r=0.999 4),平均加样回收率为98.90%(RSD=2.64%,n=5)。结论本法灵敏、快速、准确,可用于黄连的质量控制。     

RP-HPLC法测定妇科清糜气雾剂中盐酸小檗碱的含量

目的：建立妇科清糜气雾剂中的盐酸小檗碱含量测定方法。方法用RP-HPLC法,分析色谱柱为十八烷基硅烷键合硅胶为填充剂（Shim-Pack VP-ODS,250 mm×4.6 mm,5μm）,柱温25℃,0.05 mol·L-1磷酸二氢钾溶液-乙腈（50：50,每1000 mL流动相含十二烷基硫酸钠1.7 g）为流动相,检测波长为265 nm。结果盐酸小檗碱与其它各组分基线分离良好,在所试浓度5.064-253.200 mg·L-1范围内与峰面积值呈良好的线性关系,回归方程为Y=111728X-14416,相关系数r=0.9999（n=6）;精密度试验 RSD 为0.70%（n =6）;重复性试验 RSD 为0.68%（n =6）;平均回收率为99.40%（n =6）,RSD 为0.45%;三批妇科清糜气雾剂中盐酸小檗碱的含量为5.78-5.82 g·L-1。结论该法样品处理简单,准确性高,精密度好,适合妇科清糜气雾剂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.

---

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.