乌司他丁治疗急性胰腺炎的临床疗效评价

目的 :观察乌司他丁 (UTI)治疗急性胰腺炎(AP)的临床疗效。方法 :将 86例AP患者随机分为UTI治疗组(4 6例 )和甲磺酸加贝酯对照组 (4 0例 )进行对比观察。结果 :UTI组总有效率 82 .6% ,明显优于甲磺酸加贝酯组的 65 .0 % (P <0 .0 5 )。治疗后除血糖外 ,两组患者的主要临床表现和实验室指标异常率皆比治疗前降低 (P <0 .0 5或 0 .0 1 ) ;UTI组对腹痛、腹胀、恶心呕吐、发热、上腹部压痛、反跳痛、血尿淀粉酶、白细胞和TB等的恢复明显优于甲磺酸加贝酯组(P <0 .0 5 )。结论 :UTI是针对发病机理治疗AP的一种价廉、高效、广谱及使用方便的酶抑制剂 ,无明显不良反应 ,值得临床推广应用     

甲磺酸加贝酯在五种输液中的稳定性

采用紫外分光光度法考察甲磺酸加贝酯在五种输液中的配伍稳定性。葡萄糖注射液 ( 10 % ,5% )、葡萄糖氯化钠注射液、复方氯化钠注射液、氯化钠注射液在 4℃ ,2 5℃ ,37℃下测定配伍后不同时间甲磺酸加贝酯含量 ,同时观察外观并测定 p H值。结果 :7h各配伍液外观无变化 ,p H值及甲磺酸加贝酯含量无明显变化     

国产乌司他丁治疗急性胰腺炎的疗效和安全性

目的：观察国产乌司他丁治疗急性胰腺炎的疗效及安全性。方法：本研究是一项随机对照和开发相结合的多中心临床试验。419例急性胰腺炎患者随机分为乌司他丁试验组（n=108)甲磺酸加贝酯对照组（n=103),另设乌司他丁开放组（n=208)。和法为乌司他丁静脉滴注滴注50000IU,tid,持续3d之后改qd,疗程共10d。甲磺酸加贝酯100mg,tid,持续3d后改为qd,疗程共10d结果：乌怀他丁对急性胰腺炎的治愈率为71．5％,总有效率为90．2％,对照药物磺酸加贝酯的治愈率为59．2％,总有效率78．65,整体疗效比较乌司他丁高于甲磺酸加贝酯,但无统计学差异（P＞0．05）。乌司他丁有1例（0．316）,对照药甲磺酸加贝酯也有1例（0．971％）皮疹,未见其他不良反应,结论：乌司丁是治疗急性胰腺炎的一个安全有效的药物。     

RP-HPLC法检测甲磺酸帕珠沙星注射剂中右旋体含量

目的 :建立RP HPLC法检测甲磺酸帕珠沙星注射剂中右旋体含量。方法 :采用岛津C1 8柱 (4 6mm× 2 5 0mm ,5 μm) ,流动相为甲醇 手性溶液 (30∶70 ) ,流速为 1 0mL min ,紫外检测波长为 32 0nm。 结果 :甲磺酸帕珠沙星右旋体的保留时间为 6 8min ,其浓度在 12 5 2～ 37 5 4 μg mL范围内 ,呈良好的线性关系 (r =0 9995 ,n =5 ) ,平均回收率为 99 16 % ,RSD为 0 33% (n =5 )。结论 :本法简便快速 ,精密度良好 ,可作为甲磺酸帕珠沙星制剂的质量控制方法。     

甲磺酸多沙唑嗪片剂的含量、含量均匀度和溶出度的测定

目的 :建立一种测定甲磺酸多沙唑嗪片剂的HLPC法 ,并用该方法测定甲磺酸多沙唑嗪片剂含量、含量均匀度和溶出度。方法 :色谱柱为DikmaC18(15 0mm× 4 6mm ,5 μm) ,流动相 :甲醇 -醋酸缓冲液 (5 2∶4 8,V/V) ;检测波长 2 5 0nm ;柱温 30℃。结果 :甲磺酸多沙唑嗪对照品溶液的线性方程为A =6 0 72 4c +1 94 1(n =7,r =1 0 0 0 ,线性范围 0 5～ 5 0mg·L-1) ,日内、日间RSD均 <2 % ,检测限为 2 5ng(rSN=3)。甲磺酸多沙唑嗪片剂含量在 10 1%～ 10 4 %之间 ,3批片剂 4 5min平均溶出度在 84 %～87%之间 ,含量均匀度A +1 8S <15。结论 :此法适用于甲磺酸多沙唑嗪片剂含量和溶出度测定     

甲磺酸罗哌卡因中2,6-二甲基苯胺的HPLC-电化学法测定

建立了测定甲磺酸罗哌卡因中 2 ,6 -二甲基苯胺的高效液相色谱 -电化学检测法。采用 C1 8柱 ,流动相为含乙二胺四乙酸二钠和磷酸氢四丁铵的 0 .5 mol/ L磷酸盐缓冲液 -乙腈 (6 0∶ 4 0 ) ,流速 1.0 m l/ min,电极电压为 0 .90 V。2 ,6 -二甲基苯胺在 5× 10 - 3～ 6× 10 - 2 μg/ ml的范围内线性良好 (r=0 .9980 ) ,RSD为 2 .7%。     

RP-HPLC法测定注射用甲磺酸加贝酯中有关物质的含量

目的:建立测定注射用甲磺酸加贝酯中有关物质含量的方法。方法:采用反相高效液相色谱法。色谱柱为AgilentC18,流动相为甲醇-混合缓冲盐溶液(pH5.2)-异丙醇(382∶152∶8),流速为1.0mL·min-1,柱温为30℃,采用双波长检测,已知杂质羟苯乙酯检测波长为258nm,其他未知杂质检测波长为236nm。结果:在选定的色谱条件下,主成分与有关物质能完全分离,羟苯乙酯检测浓度线性范围为0.0149～9.90μg·mL-1(r=0.9995),平均回收率为99.4%,RSD=0.5%。3批样品中羟苯乙酯含量分别为0.22%、0.21%、0.24%;其他有关物质分别为0.31%、0.20%、0.24%。结论:该方法灵敏度高、专属性强,可用于注射用甲磺酸加贝酯中有关物质的质量控制。     

高效液相色谱法测定高三尖杉酯碱氯化钠注射液含量及其有关物质的限量

目的 :建立新的高效液相色谱法 (HPLC)分离测定高三尖杉酯碱及其降解产物。方法 :采用HPLC ,AgilentExtend C1 8色谱柱 ;甲醇 pH2 .5的磷酸盐缓冲液 三乙胺 (40∶60∶0 .1 )为流动相 ;流速为 0 .5ml·min- 1 ,检测波长 :2 4 0nm。结果 :在 1 .0 4～52 .2 0 μg·ml- 1 范围内 ,溶液的浓度与峰面积呈良好的线性关系。r =0 .9999,平均回收率 99.5 % (n =6) ,RSD =1 .0 % ,高三尖杉酯碱及其降解产物得到基线分离。结论 :本方法简便、快速、准确、灵敏 ,适用于高三尖杉酯碱注射液的含量测定及其降解产物的检查     

高效液相色谱法测定甲磺酸帕珠沙星注射液中右旋体的含量

目的建立甲磺酸帕珠沙星注射液中右旋异构体含量的高效液相色谱测定方法。方法Shim pakCLC ODS柱 (15 0mm× 6 .0mm ,5 μm) ,流动相为L 异白氨酸硫酸铜溶液 (取L 异白氨酸 1.3g、硫酸铜 1.0g和水 10 0 0ml溶解用 0 .1mol/L盐酸或 0 .1mol/L氢氧化钠调pH至 3.5 ) 甲醇 (75∶2 5 ) ;检测波长 :32 0nm。结果甲磺酸帕珠沙星右旋体在 0 .5～ 10 0 μg/ml浓度范围内呈良好的线性关系 (r=0 .9993) ,平均回收率为 99.5 4 % ,RSD为 1.0 1% (n =9)。结论此法快捷、专属性及重现性好 ,可用于甲磺酸帕珠沙星和D 甲磺酸帕珠沙星杂质的含量测定。     

HPLC测定克拉霉素及其制剂的含量

目的　采用HPLC法测定克拉霉素及其制剂的含量。方法　C1 8或C8色谱柱 (4 .6mm× 2 5 0mm ,5 μm) ,流动相分别为磷酸二氢钾溶液 (0 .0 6 7mol·L- 1 ) -甲醇 (4 0 0∶6 0 0 ) (pH 4 .0 )和磷酸二氢钾溶液 (0 .0 6 7mol·L- 1 ) -乙腈 (5 5∶4 5 ) ,检测波长 2 10nm ,均采用外标法。结果　 3种方法线性范围均为 0 .0 2 5～ 2 .0mg·ml- 1 (r=0 .9999) ,平均回收率为 10 0 .2 % ,RSD =0 .4 8% (n =6 )。结论　 3种方法的分离效果均较好 ,没有明显差异 ,其中方法b较为适宜。     

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.     

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.     

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.