肾上腺色腙片溶出度测定

目的　建立肾上腺色腙片的溶出度测定方法。方法 　选用《中国药典》2 0 0 0年版二部附录溶出度测定法第三法 ,紫外分光光度法检测。结果 　肾上腺色腙的线性范围为 0 .991～ 6.93 7μg·m L- 1 ,r=0 .99999(n=6)。 结论 　本方法可用于肾上腺色腙片的溶出度测定。     

紫外分光光度法测定止血敷料中肾上腺色腙的含量

目的:建立紫外分光光度法测定止血敷料中肾上腺色腙的含量.方法:利用肾上腺色腙在354 nm处有最大吸收峰,测定止血敷料中的肾上腺色腙的含量.结果:在2～7μg·ml-1的范围内,肾上腺色腙的吸光度与其浓度呈良好的线性关系(r =0.999 9);平均回收率为101.02％,RSD为1.96％.结论:本法操作简单,快速,可以作为止血敷料中肾上腺色腙含量测定方法.     

阳离子交换固相萃取-流动注射化学发光法测定肾上腺色腙

目的:基于酸性高锰酸钾氧化肾上腺色腙产生微弱的化学发光现象,建立一种简单、灵敏、选择性高,可用于药物质量控制和体内药物分析的肾上腺色腙的化学发光新方法。方法:药物样品经阳离子交换固相萃取技术净化后,采用流动注射化学发光法分析。结果:方法测定肾上腺色腙的线性范围为7.0×10-10～1.0×10-7μg.mL-1,检出限为2.0×10-10μg.mL-1(3σ),对1.0×10-8μg.mL-1的样品连续进行11次平行测定,相对标准偏差为2.5%;用于肾上腺色腙注射剂测定的回收率为96%～98%,而用于尿样中加入肾上腺色腙1.00×10-7～5.00×10-9μg.mL-1,回收率为80.2%～98.6%。结论:该方法具有很高的灵敏度和较好的选择性,不但可以用于制剂的分析,还适用于血样、尿样等复杂的生物样品中极低浓度肾上腺色腙的分析。     

HPLC测定肾上腺色腙注射液的含量及有关物质

目的测定肾上腺色腙注射液的含量及有关物质。方法采用HPLC法,用Zorbax C18色谱柱(250 mm×4.6 mm,5μm);甲醇-0.01 mol.L-1磷酸二氢钾溶液(含0.1%三乙胺,磷酸调pH3.8)(25:75)为流动相;流速1.0 ml.min-1;检测波长355 nm;柱温30℃;进样量10μl。结果在该色谱条件下,肾上腺色腙与其相邻杂质峰能完全分离,在10~100μg.ml-1线性关系良好(r2=0.9999)。结论所建方法简便、准确、专属性好,可作为肾上腺色腙注射液中主药的测定及有关物质检查。     

肾上腺色腙片对髋关节置换术后止血消肿的效果研究

目的:探讨肾上腺色腙片对髋关节置换术后止血消肿的效果.方法:选取2020年1月至2021年1月该院收治的行髋关节置换术治疗的132例患者,按照随机数字表法分为对照组和肾上腺色腙片组,每组66例.对照组患者在髋关节置换术后使用凝血酶冻干粉干预,肾上腺色腙片组患者在髋关节置换术后使用肾上腺色腙片干预.观察两组患者失血、输血...     

肾上腺色腙片剂及注射液的有效性安全性回顾分析

目的分析评估肾上腺色腙片剂及注射液的有效性与安全性。方法查阅＂中文科技期刊数据库＂（1989～2009年）和＂中国期刊全文数据库＂（1994～2009年）有关肾上腺色腙的临床研究、不良反应报道文献,分析临床研究数据,不良反应严重性。结果肾上腺色腙的临床研究涉及片剂、注射液,所有临床研究未能做到双盲随机对照,片剂文献报道临床有效率为70%～90%,注射液的报道有效率为20%。文献报道不良反应均为注射液所致,作者均推测为其中水杨酸钠所致。结论应加强肾上腺色腙临床研究的设计,肾上腺色腙注射液处方设计合理性欠充分,其不良反应的危险性超过了临床有效性,已有安全性有效性较强的产品可以替代,建议淘汰肾上腺色腙注射液制剂。     

肾上腺色腙-止血纱布复合敷料动脉止血效果研究

目的：对肾上腺色腙-止血纱布复合物的止血效果进行评价，为止血材料的选择提供依据。方法：新西兰兔11只，每只分别用不合药止血纱布、含肾上腺色腙分别为50，100，200μg/块的载药纱布对股动脉断端止血，记录止血时间，并计算出血量。另外分别用止血纱布、明胶海绵、胶原蛋白封闭剂、含肾上腺色腙200μg/块的普通纱布和止血纱布对犬胫前动脉断端止血，记录止血时间，并计算出血量。结果：兔股动脉止血实验中，随肾上腺色腙浓度增加，止血率逐渐提高并且出血量减少，含肾上腺色腙200μg/块组止血率为100％，出血量为（0．84±0．62）g，明显低于对照组（P〈0．05）；犬胫前动脉止血实验中，含肾上腺色腙200μg/块的止血纱布组止血时间和出血量分别为3．58min和0．34g，低于其他组。结论：肾上腺色腙-止血纱布复合物止血效果显著。     

HPLC法测定．肾上腺色腙片的含量

目的用高效液相色谱法测定肾上腺色腙片的含量。方法采用HPLC法。色谱柱为Waters C18（4．6mm×150mm。5um）;流动相：乙腈-水（10：90）;检测波长：356nm;流速：1mL·min^-1;进样量：10uL。结果线性范围为40．64ug-203．2ug,平均回收率为100．3％（n=9）,RSD=0．6％。结论方法简便。重现性好,结果准确可靠,可用于肾上腺色腙片的质量控制。     

HPLC测定布南色林片的含量

目的采用HPLC测定布南色林片的含量。方法色谱柱为Cosmosil C18柱(250 mm×4.6 mm,5μm),流动相为甲醇-0.02 mol.L-1磷酸氢二钾溶液(90∶10),流速为1.0 mL.min-1,检测波长为238 nm。结果线性回归方程为:Y=2.374×105X-4.897×104(r=0.9999),线性范围为32～48μg.mL-1,平均回收率为99.06%,RSD=1.57%。结论所用方法简便、快速、灵敏度高,可用于布南色林片的含量测定。     

肾上腺色腙片的含量及含量均匀度测定方法的探讨

肾上腺色腙 (安络血 )片是临床常用的促凝血药 ,能增强毛细血管对损伤的抵抗力 ,促进毛细血管收缩 ,降低通透性 ,增进断裂毛细血管断端的回缩作用。用于因毛细血管通透性增高引发的出血 ,如鼻出血、咯血、血尿等。肾上腺色腙片收载于卫生部药品标准[1] 中 ,对含量均匀度未作规定。按《中国药典》[2 ] 每片标示量小于 10ｍｇ或主药含量小于每片重量 5 %的片剂均应检查含量均匀度的要求 ,该品种质量标准应符合药典附录的要求 ,即应增加含量均匀度检查。为此本文采用紫外分光光度法探讨了其含量均匀度的检查方法 ,结果简便、快速、准确 ,适于基…     

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.     

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.