酸碱滴定法测定复方乳酸依沙吖啶软膏中硼酸的含量

目的:建立复方乳酸依沙吖啶软膏中硼酸的含量测定方法。 方法:采用酸碱滴定法对同一批次复方乳酸依沙吖啶软膏供试品进行硼酸含量测定,对其专属性、线性范围、精密度、准确度实验结果进行数据分析,以判断方法的适用性。 结果:本实验方法专属性良好,硼酸在 5. 05~51. 60 mg 范围内线性关系良好,线性方程 Y = 0. 160 498X+0. 051 24(r = 0. 999 98);硼酸检出限为 0. 2 mg,定量限为 0. 6 mg;重复性实验相对标准差(RSD)为 0. 37%(n = 6),精密度实验 RSD 为 0. 58%(n = 12);硼酸平均加样回收率为 99. 1% ~100%(RSD<1. 0%)。 结论:该方法简单、快速,测定结果均符合《中华人民共和国药典》2020 年版四部通则9101 要求,适用于复方乳酸依沙吖啶软膏中硼酸的含量测定。     

HPLC法同时测定复方乳酸依沙吖啶溶液中两种组分的含量

目的：建立HPLC法同时测定复方乳酸依沙吖啶溶液中乳酸依沙吖啶和盐酸苯海拉明的含量。方法：色谱柱为Luna氰基柱（4.6 mm×250 mm,5μm）;流动相为乙腈-水-三乙胺（50∶50∶0.5）;流速1.0 mL·min-1;柱温30℃;检测波长230 nm;进样量20μL。结果：乳酸依沙吖啶和盐酸苯海拉明与二苯酮分离良好。乳酸依沙吖啶在0.6012~1.4030 mg·mL-1范围内线性关系良好（r=0.9994）,盐酸苯海拉明在0.1487~0.3469 mg·mL-1范围内线性关系良好（r=0.9999）,依沙吖啶和苯海拉明的平均回收率分别为99.91%、99.73%,RSD分别为1.06%（n=9）、1.10%（n=9）。结论：本方法简便准确,快速可靠,可用于复方乳酸依沙吖啶溶液的含量测定和质量控制。     

复方乳酸依沙吖啶散中乳酸依沙吖啶含量测定方法研究

目的：探讨复方乳酸依沙吖啶散中乳酸依沙吖啶含量的测定方法。方法排除影响乳酸依沙吖啶吸光度值的因素,筛选出供试液制备的最佳方法：减少取样量,采用微孔滤膜于80℃以下条件下加压过滤。采用紫外分光光度法在362 nm处测定吸光度（A）,计算乳酸依沙吖啶含量。结果乳酸依沙吖啶在5~22.5 mg/L（r=0.9997）范围内线性关系良好,高、中、低含量样品（n=5）平均测定率分别为93.132%、93.074%和93.261%。结论该方法简单、快速,测定结果符合要求,可作为复方乳酸依沙吖啶散中乳酸依沙吖啶含量的测定方法。     

复方乳酸依沙吖啶混悬液的制备与临床应用

目的制备复方乳酸依沙吖啶混悬液，建立其质量标准，并进行临床疗效观察。方法以乳酸依沙吖啶和氧化锌为主药制备复方乳酸依沙吖啶混悬液；采用分光光度法和容量法分别测定乳酸依沙吖啶和氧化锌的含量；考察该药常温下的稳定性。选择接触性皮炎患者267例，随机分为治疗组135例和对照组132例。治疗组在患处涂抹复方乳酸依沙吖啶混悬液，tid；对照组在患处涂抹炉甘石洗剂，tid。治疗7 d后观察治疗效果。结果复方乳酸依沙吖啶混悬液性质稳定，乳酸依沙吖啶和氧化锌的平均回收率分别为99.01 %和99.86 %，RSD分别为0.42 %和0.23 %。复方乳酸依沙吖啶混悬液对接触性皮炎的治愈率和有效率分别为94.0 % 和100.0 %。结论复方乳酸依沙吖啶混悬液性质稳定，质量控制方法可靠，疗效好，值得临床推广。     

HPLC法测定乳酸依沙吖啶溶液的含量

目的 应用HPLC法测定乳酸依沙吖啶溶液的含量。方法 用C18柱以甲醇-0.1mol/L醋酸铵-乙腈（50：40：10）（冰醋酸调节pH至4.5）为流动相；检测波长为270nm。结果 该方法在4.5-13.5μg/ml的浓度范围内线性关系良好（r=0.9998,n=5），平均回收率为100.0%，RSD=0.9%（n=9）。结论 方法简便，快速准确，更适用于乳酸依沙吖啶的含量测定。     

分光光度法测定依沙吖啶溶液中乳酸依沙吖啶的含量

目的建立紫外分光光度法测定依沙吖啶溶液中乳酸依沙吖啶含量的方法。方法水为溶媒,在362 nm波长处测定吸光度,测定乳酸依沙吖啶的含量。结果吸光度与其浓度具有良好的线性关系（r=0.9998）,线性范围2.5～20 μg*ml－1;平均回收率为100.28%,RSD为0.42%（n=5）。结论该方法简便,结果可靠,适用于该制剂的质量控制。     

复方利锌混悬液中乳酸依沙吖啶的含量测定

目的:建立复方利锌混悬液中乳酸依沙吖啶的含量测定方法.方法:采用化学和物理方法排除干扰,制备空白溶液和待测溶液;采用分光光度法,以362 nm为检测波长,△λ=±1 nm,测定乳酸依沙吖啶的吸收度.结果:乳酸依沙吖啶在8.28～33.12 μg/mL范围内浓度与吸收度的线性关系良好,回归方程为A=0.031 57 C-0.003 1,r=0.999 9(n=7),平均回收率为99.01%,RSD为0.419%.结论:用分光光度法测定复方利锌混悬液中乳酸依沙吖啶的含量,结果稳定、准确、可靠.     

HPLC法同时测定复方水杨酸搽剂中乳酸依沙吖啶与水杨酸的含量

目的建立同时测定复方水杨酸搽剂中乳酸依沙吖啶和水杨酸含量的HPLC法。方法采用Alltima C18色谱柱(150mm×4.6mm,5μm);以甲醇-1mL·L~(-1)磷酸(50∶50)为流动相;流速:1.0mL·min~(-1);检测波长:270nm。结果乳酸依沙吖啶和水杨酸的线性关系良好,线性相关系数(r)分别为1.000 0和0.999 0;精密度和稳定性良好,RSD值均小于1.0%;回收率良好,乳酸依沙吖啶和水杨酸的平均回收率(n=9)分别为100.8%和101.3%。结论该方法准确、简单、快速,可用于同时测定复方水杨酸搽剂中乳酸依沙吖啶和水杨酸的含量。     

HPLC法测定乳酸依沙吖啶注射液的含量

目的应用HPLC法测定乳酸依沙吖啶注射液的含量。方法高效液相色谱法。色谱柱为Kromasil C18柱（4.6 mm×250mm,5μm）;流动相为0.05%十二烷基磺酸钠-甲醇（30∶70）（磷酸调节pH3.3）;流速为1 ml·min^-1;检测波长370 nm。结果该方法在20.1～201.2 mg·L^-1的浓度范围内线性关系良好（r=0.999 9,n=6）,平均回收率为99.8%,RSD=0.9%（n=5）。结论方法快速准确,可用于乳酸依沙吖啶注射液的含量测定。     

HPLC法测定复方乳酸依沙吖啶溶液中乳酸依沙吖啶和间苯二酚的含量

目的采用HPLC法测定复方乳酸依沙吖啶溶液中乳酸依沙吖啶和间苯二酚的含量。方法色谱柱为C₁₈,流动相为甲醇-0.05 mol·mL^-1磷酸二氢钾溶液（20%H₃PO₄调pH至3.3）（48:52,V/V）,检测波长269nm,流速0.6 mL·min^-1,柱温35℃,进样量10μL。结果乳酸依沙吖啶、间苯二酚分别在1.012～20.24 mg·L^-1（r=0.999 9）和20.28～405.6 mg·L^-1（r=0.999 9）质量浓度内线性关系良好,加样回收率均>99%（RSD<1.5%）。结论本方法简便,准确性、重现性好,适用于复方乳酸依沙吖啶溶液中乳酸依沙吖啶和间苯二酚的含量测定。     

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.     

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.