布替萘芬对豚鼠皮肤须发癣霉的疗效观察

目的：观察布替萘芬乳膏剂治疗豚鼠皮肤真菌病的疗效。方法：本实验共建立皮肤真菌病豚鼠感染模型４５处,分别是１％布替藉芬治疗组,１％萘替芬乳膏治疗组,１％联苯苄唑乳膏治疗组,１％克霉唑软膏治疗组和空白对照组和空白,疗程为１４天,药物治疗结束后观察复发状况。结果：布替萘芬乳膏１０天临床治愈率比联苯苄唑乳膏和萘替分乳膏高２２．３％,但无显著性差异（Ｐ〉０．０５）,与克霉唑软膏差异有显著性意义（Ｐ〈０．０５     

盐酸萘替芬溶液剂的含量测定

目的：建立紫外分光光度法测定盐酸萘替芬溶液剂含量的方法。方法：采用多台紫外分光光度仪,配制盐酸萘替芬高低两种浓度的溶液,进行盐酸萘替芬吸收系数（Ｅ１ｃｍ＾１％）测定,并建立样品的含量测定方法。结果：空白基质地测定波长处对样品测定没有干扰,盐酸萘替芬的线性范围为１．６～１６μｇ．ｍｌ＾－１,ｒ＝１．００００,日内偏差为０．２０％（ｎ＝６）,平均回收率为１００．４％,ＲＳＤ＝０．３９％（ｎ＝６）。结论：方法灵敏简便,满足了盐酸萘替芬溶液剂的含量测定的要求。     

1%布替萘芬乳膏治疗浅部真菌病疗效观察

目的：观察1％盐酸布替茶芬乳膏（嘉瑞）治疗浅部真菌病临床疗效和安全性。方法：1％盐酸布替萘芬乳膏qd连续2周和4周，分别治疗经临床和真菌学检查证实的体股癣、汗斑和手足癣（角化型除外），在第6周时全面评价临床疗效、真菌清除率和安全性。结果：1％盐酸布替萘芬乳膏治疗体股癣、汗斑、手足癣患者的临床治愈率98．13％，真菌清除率95．32％。结论：1％盐酸布替萘芬乳膏为疗效高、安全性好的抗真菌药。     

HPLC法测定镇痛复方制剂阿司匹林萘磺酸右丙氧芬片含量及对…

本文介绍了用高效液相色谱法测定阿司匹林，萘磺酸右丙氧芬片含量及其分解产物水杨酸含量的方法，采用μ－ＢｏｎｄａｐａｋＣ１８为固定相，０．０２ｍｏｌ．Ｌ＾－１磷酸二氢钾－甲醇－四氢呋喃（ＴＨＦ）（２：１：０．１）为流动相，紫外检测器于２３０ｎｍ波长处测定，方法准确可靠，对阿司匹林和萘磺酸右丙氧芬的回收率分别为９９．２５％（ＲＳＤ０．７８％），９９．７％（ＲＳＤ１．０５％），由于阿司匹林不稳定，易分解成     

反相高效液相色谱法和气相色谱法测定盐酸芬氟拉明片含量的比 …

目的：研究一种用反相高效液相色谱测定盐酸芬氟拉明（ＦＨ）片含量的方法,并与法定气相色谱法作比较研究。方法：以水为溶剂处理样品,采用Ａｌｌｔｉｍａ Ｃ１８柱为色谱柱,以０．０５ｍｏｌ．Ｌ＾－１磷酸液（用三乙胺调ｐＨ２．５）－甲醇（５０：５０）为流动相,紫外检测波长２５４ｎｍ,流速１．０ｍＬ．ｍｉｎ＾－１,柱温３０℃。结果：ＦＨ浓度在０．２０￣１．０ｍｇ．ｍＬ＾－１浓度范围内呈良好线性关系（ｒ＝０．９     

反相高效液相色谱法同时测定金马通络胶璐东茛菪碱及士的宁含量

目的：建立一种反相高效液相色谱法检测金马通络胶囊中东莨菪碱及士的宁含量。方法：用Ｃ１８ＯＤＳ柱为固定相。甲醇－水（５８：４２）（水相含０．０５ｍｏｌ．Ｌ＾－１醋酸盐缓冲液及０．００２５ｍｏｌ．Ｌ＾－１十二烷基硫酸钠）为流动相。检测波长２２６ｎｍ。结果：该方法回收率氢溴酸东莨菪碱为１００．５％，ＲＳＤ＝２．３％（ｎ＝５）；士的宁为９７．５％，ＲＳＤ＝２．４％（ｎ＝５）。结论：该方法操作简便、快捷、专     

反相高效液相色谱法测定萘普生钠血浆浓度

目的：建立用高效液相色谱法测定萘普生钠血浆浓度的方法。方法：血浆样品在酸性条件下,以１,２二氯乙烷提取,吲哚美辛为内标,采用ＬｉｃｈｒｏｓｏｒｂＣ１８（５μｍ）柱,流动相为甲醇∶醋酸醋酸铵缓冲液（ｐＨ４．５）＝７４∶２６,流速为１．０ｍｌ·ｍｉｎ－１,检测波长３１８ｎｍ,萘普生和内标的保留时间分别为３．３５和４．７１ｍｉｎ。结果：线性范围在１～９０μｇ·ｍｌ－１（ｒ＝０．９９９９,最低检测浓度为０．４μｇ·ｍｌ－１血浆,ＲＳＤ％＜３．５。结论：本方法可用于萘普生钠的药物动力学研究     

HPLC法测定盐酸布替萘芬软膏的含量

目的：用HPLC法测定盐酸布替萘芬软膏的含量，方法：采用Kromasil-C18柱，以乙腈－甲醇－0．05mol/L^-1醋酸铵缓冲液（pH=6.8,66:19:15) 为流动相，检测波长为282nm，结果：进样量在4．1－20．5μg范围内线性关系良好。平均回收率为98．17％，相对标准偏差（RSD）为0．13％，结论：该方法结果准确，方法精密度和性良好，可用于盐酸布替萘芬软膏的质量控制。     

重组人胰岛素类似物的HPLC分析

目的：探讨ＨＰＬＣ分析在重组人胰岛素类似物临别和杂质检测中的适用性。方法：采用反相然谱柱（Ｃ１８）,以硫酸钠－磷酸缓冲液（０．２ｍｏｌ．Ｌ＾－１,ｐＨ２．３）和乙腈为流动相,流速０．８或１．０ｍＬ．ｍｉｎ＾－１,柱温４０℃,检测波长２１４ｎｍ;用分子筛柱（Ｚｏｒｂａｘ ＧＦ２５０）以磷酸铵缓冲液（０．１ｍｏｌ．Ｌ＾－１,ｐＨ７．５）和乙腈为流动相,流速０．５ｍＬ．ｍｉｎ＾－１,检测波长２１４ｎｍ;     

呼吸道感染病人复方磺胺甲恶唑血药浓度监测

建立反相高效液相色谱法监测复方磺胺甲恶唑在呼吸道感染病人中的血药浓度。方法：Ｃ１８填料柱（２２０ｍｍ＊４．６ｍｍ）,流动相为水：甲醇（６６：４４）,流速１．０ｍｌ．ｍｉｎ＾－１,检测波长２２３ｎｍ。结果：磺胺甲恶唑（ＳＭＺ）与甲氧苄啶（ＴＭＰ）,线性范围各为２－２５μｇ．ｍｌ＾－１,０．５－１０μｇ．ｍｌ＾－１,平均回收率１００．３％,日内变异〈５％,８名上呼吸道感染病人口服ＳＭＺｃｏ１．０ｇ,ｂ     

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.