P—矩阵法与吸光度减法联合用于复方制剂中低含量组分的测定

目的：探索复方制剂中低含量组分的光度分析新定量方法。方法：将吸光度减法技术同Ｐ－矩阵法相结合测定了两种片剂中低含量组分ＶＢ６。结果：复方甲硝唑片和复方异烟肼片中ＶＢ６的回收率分别为１００．０％和１００．９％,相对标准差分别为１．５２％主１．８７％。结论：Ｐ－矩阵法同吸光度减联用可用于复方制剂中低含量组分的光度分析。     

反相高效液相色谱法测定胸腺肽中胸腺素α1

采用反相高效液相色谱法测定胸腺肽中胸腺素α１,色谱柱为Ｎｏｖａ－ＰａｋＣ１８柱,以乙腈－三氟乙酸－水（２０：０．０２：８０）为流动相,检测波长２０６ｎｍ。测定组分与其它组分的色谱峰达到基线分离。加样回收率平均值为９８．７％,ＲＳＤ为１．２％,为控制胸腺肽质量提供了新的测定指标和可靠的方法。     

卡尔曼滤波分光光度法同时测定替硝唑含漱液三组分含量

本文研究了卡尔曼滤波分光光度法同时测定替硝唑含漱液中三组分：替硝唑、达克罗宁、地塞米松，结果各组分平均回收率分别为１００．１％，１００．８％和９９．３％，ＲＳＤ分别为０．８３％，０．７７％和１．４７％。     

Use of cafeine as a probe for rapid determination of cytochrome P-450 CYP1A2 activity in humans

目的：建立快速测定细胞色素Ｐ４５０ＣＹＰ１Ａ２酶活性的高压液相色谱方法．方法：取３００μＬ血浆样品，用β羟乙基茶碱作内标，经５ｍＬ氯仿／异丙醇（９∶１）萃取处理后，用００５％的乙酸、乙腈和甲醇作为基本流动相，采用梯度洗脱程序在ＯＤＳ柱上分离待测组分，紫外检测波长２８２ｎｍ．结果：无内源性物质干扰测定．次黄嘌呤、内标和咖啡因快速基线分离，三者的保留时间均小于１３分钟．次黄嘌呤和咖啡因的检测下限均为０１μｍｏｌ·Ｌ－１，线性范围分别为１－１００μｍｏｌ·Ｌ－１和１－２００μｍｏｌ·Ｌ－１，相关系数分别为０９９９９和０９９８７，变异系数分别小于６％和１０％．两者的平均相对回收率为９６％－１０８％．结论：本方法快速、灵敏，可用于人群ＣＹＰ１Ａ２酶活性研究．     

反相高效液相色谱法同时测定苯巴比妥和卡马西平血药浓度

目的：建立同时测定微量血浆中苯巴比妥和卡马西平浓度的方法。方法：采用ＲＰ－ＨＰＬＣ法,以艾司唑仑为内标,同时测定微量血浆中苯芭巴比妥和卡马西平浓度。色谱柱ｓｈｉｍａｄｚｕ ｓｈｉｒｍｐａｃｋ ＣＬＣ－Ｃ１８不锈钢柱,流动相为醇－水（６０：４０）,流速０．８ｍｌ．ｍｉｎ＾－１,检测波长２５４ｎｍ。结果：苯巴比妥在４～６０μｇ．ｍｌ＾－１浓度范围内线性良好（ｒ＝０．９９９８）,卡马西平在２～１６μｇ．ｍｌ＾－１浓度范围内线性良好（ｒ＝０．９９９５）,最低检测限分别为１１．５７ｎｇ．ｍｌ＾－１和４．９２ｎｍ．ｍｌ＾－１,两者高、中、低３种浓度的平均回收率分别为９９．９２％,１０１．３０％,９７．９２％和９９．４１％,１０１．５２％,９８．２２％（ｎ＝９）,日内ＲＳＤ分别为３．１％,２．６％,３．８％和１．９％,１．６     

反相高效液相色谱法测定小儿平热静片的含量

介绍高效液相色谱法同时测定小儿平热静片中对乙酰氨基酚与盐酸异丙嗪两组分含量的方法。采用ＹＷＧ－Ｇ１８柱,以甲醇－水－磷酸（５５：４５：０．２）为流动相,在３１２ｎｍ波长处检测,实验结果表明两组分在一定浓度范围内均呈良好的线性关系,平均回收率分别为１００．４％和１００．４％,ＲＳＤ分别为０．５２％和０．７４％（ｎ＝５）。该法专属性强,操作简便,快速,结果准确。     

泄痢停片中三组分的反相离子对HPLC测定

采用反相离子对ＨＰＬＣ法,以无水吗啡为内标,ＹＷＧ－Ｃ１８为固定相,乙腈－水（３５：６５）内含４ｍｍｏｌ／Ｌ十二烷基磺酸钠及０．１％冰醋酸为流动相,同时测定泄痢停片中三组分的含量,方法简便,快速准确,ＳＭＺ,ＴＭＰ,ＰＡ的平均回收经分别为１００．５％,１００．０％和１００．１％,ＲＳＤ分别为０．７％,０．６％和０．６％。     

高效液相色谱法测定复方替加氟胶囊的含量

介绍用高效液相色谱法同时测定复方替加氟胶囊中替加氟与尿嘧啶两个组分含量的方法,采用Ｃ１８柱：以甲醇－水（１５：８５）为流动相;以烟酰胺为内标物;在２８２ｎｍ检测。结果表明在一定浓度范围内呈良好的线性关系,平均回收率分别为１００．０％和１００．１％,ＲＳＤ均为０．２９％（ｎ＝６）。     

双波长分光光度法测定新福林滴眼液中二组分的含量

目的： 测定新福林滴眼液中二组分的含量。方法： 采用双波长分光光度法。结果： 实验中分别选择λＳ１ ＝２４６ ｎｍ 　λＲ１ ＝ ２６５ ｎｍ 和λＳ２ ＝ ２６６ ｎｍ 　λＲ２ ＝ ２８２ ｎｍ 为测定新福林和尼泊金乙酯的组合波长, 其平均回收率分别为１０２－３３ ％ 和１００－５６ ％ 其ＲＳＤ 分别为０－１５ ％ 和０－３４ ％ 。结论： 回收率试验和样品测试结果满意, 符合制剂快检要求。     

新痢灵片的导数双波长及系数倍率测定

采用导数双波长法及导数系数倍率法分别测定新痢灵片中的ＴＭＰ及洗必泰的含量，测定波长分别为ＴＭＰ２４５．６、２５２．６ｎｍ，洗必泰２６４．０ｎｍ和２７３．０ｎｍ。此法不经分离，可在同一乙醇溶液中测定两种组分。在１０－３２μｇ／ｍｌ的浓度范围内线性关系良好，平均回收率及相对标准偏差分别为ＴＭＰ１００．３％，１．２３％；洗必泰９８．８％，１．３２％。     

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.