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...     

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.     

高效液相色谱法测定卡巴克络片的含量

目的建立卡巴克络(肾上腺色腙)片的HPLC含量测定方法。方法色谱柱为Nuc leodur C18(4.6×150mm,5μm),流动相为甲醇-水(15∶85),355nm检测。结果线性范围为20~200μg.mL-1,平均回收率为100.9%(n=9),RSD=0.5%。结论方法专属性强、灵敏度高、重现性好,结果准确,适合肾上腺色腙片的质量控制。     

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。     

盐酸西替利嗪片的溶出度考察

目的　对盐酸西替利嗪片进行溶出度测定 ,以考察其质量。方法　采用紫外分光光度法测定了盐酸西替利嗪片的溶出度 ,线性范围为 2～ 4 0 mg· L-1(r =0 .9999)。结果　自制品与国外同种产品比较 ,溶出参数T50 、Td、m无显著性差异。结论　自制品溶出度较好。     

盐酸左氧氟沙星片溶出度测定方法研究

目的建立盐酸左氧氟沙星片的溶出度测定方法。方法采用紫外分光光度法测定盐酸左氧氟沙星片的溶出度,测定波长为293nm。结果盐酸左氧氟沙星质量浓度在2．0～20．0μg／mL范围内与吸收度线性关系良好,r=0．9997（n=6）,平均回收率为98．5％,RSD=0．6％（n=6）。结论该方法灵敏、可靠、重现性好,可用于盐酸左氧氟沙星片的溶出度测定。     

盐酸吡格列酮片的溶出度研究

目的　建立盐酸吡格列酮片的溶出度试验方法。方法　以 0 .1mol/L盐酸为溶出介质 ,采用桨法进行溶出度测定 ,转速为 5 0r/min ,温度为 37± 0 .5℃ ,进行累积溶出百分率测定。用紫外分光光度法在 2 6 9nm的波长处测定。结果　该方法线性关系良好 ,回归方程为A =0 .0 2 2C +0 .0 2 9,r=0 .9999(n =8) ,平均回收率为 10 0 .1% ,RSD为 0 .4 4 % (n =9) ,盐酸吡格列酮片各时间的累积溶出量和拟合后提取的参数均无显著性差异。结论　测定方法简便 ,结果准确可靠     

SOTAX自动溶出仪与普通溶出仪测定西洛他唑片溶出度比较

目的以西洛他唑片为例,利用SOTAX自动溶出仪对溶出度方法作方法学验证。方法采用中国药典西洛他唑的溶出度方法,手动稀释改为自动循环测定（1mm比色皿）。结果回收率100．1％,重复性RSD为0．4％,回归方程为A=3．7655C-0．0151,r=0．9999,并对自动溶出法和手动溶出法作了比较试验,两者无显著差异。结论自动取样溶出法可以用于西洛他唑片的溶出度检测。     

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。     

贝诺酯米溶出度与人体内血药浓度相关性的研究

目的：了解贝诺酯片溶出度与人体内血药浓度的相关性，建立溶出度测定法。方法：用1％十二烷基硫酸钠溶液为溶剂，桨法测定，45min时取样，紫外分光光度法测定贝诺酯片溶出度；贝诺酯片人体内血药浓度是以对二甲氨基苯甲醛为内标，用HPLC法分别测定血浆中扑热息痛与水杨酸的含量，数理统计贝诺酯片溶出度与人体内药代动力学参数的相关性。结果：贝诺酯片溶出度与人体内药代动力学参数AUC、Cmax相关性显著[相关系数（r)分别为0．968与0．985（n=5),查表r0.01,3=0.959]。结论：建立的贝诺酯片溶出度测定法可有效地控制药品的质量。     

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.