薄层扫描法测定利脑心胶囊中芍药甙的含量

应用ＴＬＣＳ法测定利脑心胶囊中芍药甙含量．样品用甲醇提取、大孔吸附树脂分离芍药甙，以硅胶Ｇ为薄层吸附剂，苯－甲醇－醋酸乙酯－氨水（１０：４：２：０．５）为展开剂，茴香醛－冰醋酸－硫酸（０．１：１０：０．２）溶液为显色剂，用ＣＳ－９３０薄层扫描仪，在λｓ＝５５５ｎｍ，λＲ＝６７０ｎｍ波长处测定含量。本法平均加样回收率为１００．５％，ＲＳＤ为３．７６％（ｎ＝５）。     

芸香甙的药代动力学研究

目的研究芸香甙在兔体内的药代动力学。方法家兔一次静注芸香甙５ｍｇ·ｋｇ－１后，利用荧光分光光度法测定不同时间的血药浓度。应用３Ｐ８７药动学软件程序对数据进行计算机处理。结果芸香甙的药时（Ｃ－Ｔ）方程为：Ｃ＝８５．９７８９ｅ－０．９０４４Ｔ＋３４．５１０５ｅ－０．０５８７Ｔ＋４．３８３８ｅ－０．００４６Ｔ。芸香甙的主要药代动力学参数如下：Ｔ１／２ａ：（０．７６０９±０．１０６６）ｍｉｎ，Ｔ１／２ｂ：（１２．５６６７±３．７１３９）ｍｉｎ，Ｔ１／２ｃ：（１６２．５６５１±５０．６０３５）ｍｉｎ，Ｋ１２：（０．５１２３±０．１３１６）ｍｉｎ－１，Ｋ２１：（０．３２９８±０．０７３７）ｍｉｎ－１，Ｋ１３：（０．０７３９±０．０１８２）ｍｉｎ－１，Ｋ３１：（０．０１００±０．００３７）ｍｉｎ－１，Ｋ１０：（０．０７７４±０．０１６０）ｍｉｎ－１，Ｖｃ：（０．０４０４±０．００４４）Ｌ·ｋｇ－１，ＡＵＣ：（１６７９．７５８３±４８０．６０４５）ｍｇ·Ｌ－１·ｍｉｎ－１，ＣＬ（ｓ）：（０．００３１±０．０００８）Ｌ·ｋｇ－１·ｍｉｎ－１。结论芸香甙在兔体内的Ｃ－Ｔ变化符合三室开放模型；芸香甙在体内的分布、消除迅速。     

高效液相色谱法测定四逆散胶囊中芍药甙和甘草酸的含量

目的：建立高效液相色谱法分别测定四逆散胶囊中芍药甙和甘草酸的含量测定方法。方法：用ＯＤｓ柱，以甲醇—水（４０：６０）为流动相，检测波长２３０ｎｍ，流量０．６ｍｌ／ｍｉｎ测定芍药甙；以甲醇—水—冰醋酸（６８：３２：１）为流动相，检测波长２４９ｎｍ，流量０．６ｍｌ／ｍｉｎ测定甘草酸。结果：芍药甙；线性范围：０．６３—０．９５μｇ／ｍｌ（ｒ＝０．９９９３），平均回收率９８．８％，ＲＳＤ为０．９％；甘草酸：线性范围：１．１２７—１．６９１μｇ／ｍｌ（ｒ＝０．９９９４），平均回收率１０２．０％，ＲＳＤ为２．７％。结论：本法简便、灵敏、准确。     

诺氟沙星治疗阿米巴肝脓肿

目的：探索新的、有效的治疗阿米巴肝脓肿的药物。方法：诺氟沙星０．３－０．４９，ｔｉｄ，ｐｏ×１５ｄ，治疗３０例（男性２２例，女性８例；年龄４５±ｓ３ａ）阿米巴肝脓肿病人。用０．５％甲硝唑１００ｍＬ静脉滴注（静滴），ｂｉｄ×（３－５）ｄ，以后改为０．４ｇ，ｔｉｄ，ｐｏ×（７－１０）ｄ治疗２９例作对照。２组合并细菌感染者均加用四环素１．０ｇ，ｑｄ，静滴５－７ｄ或用氨苄西林２．０ｇ，ｔｉｄ，ｉｖ×（５－７）ｄ。结果：诺氟沙星组在治疗有效率，体温恢复正常时间，平均住院无数与甲硝唑组相似（Ｐ＞０．０５）。但脓腔缩小时间短，肝区疼痛消失早，不良反应少（Ｐ＜０．０１或０．０５）。结论：诺氟沙星治疗阿米巴肝脓肿优于甲硝唑。     

薄层扫描法测定贝芪口服液中黄芪甲甙的含量

建立了测定贝芪口服液中黄芪甲甙含量的薄层扫描测定法。采用硅胶Ｇ－ＣＭＣＮａ薄层板，以氯仿－甲醇－水（６５：３５：１０）为展开剂、１０％硫酸乙醇为显色剂，测定波长（λ_s）与参比波长（λ_Ｒ）分别为６００、７００ｎｍ。黄芪甲甙的量在１～６μｇ与斑点面积呈线性关系，ｒ＝０．９９８８。方法平均回收率为９８．２６±２．７６％（ｎ＝６）．三批供试品中黄芪甲甙的含量为０．１２２～０．１８０ｍｇ／ｍｌ，方法精密度（ＲＳＤ）分别为３．１０％、３．７１％、３．７０（ｎ＝４）。     

高效液相色谱法测定护肝颗粒中芍药甙的含量

用ＨＰＬＣ法测定了护肝颗粒中芍药甙的含量，其分析柱为ＯＤＳ－Ｃ_(１８)，流动相为甲醇－异丙醇－醋酸（３６％）－水（２５：２：２：７１），检测波长为２３０ｎｍ，样品提取溶剂为水，提取方法和时间为超声振荡１０ｍｉｎ。芍药甙的平均回收率为９７．４４％，ＲＳＤ＝０．６１％（ｎ＝６）．线性范围０．２０８～０．８５２μｇ。方法简便、快速，精密度和稳定性良好，适于护肝颗粒生产的质量控制。     

高效毛细管电泳测定盐酸小檗碱脂质体包封率

目的：建立一个快速、简便且经济的盐酸小檗碱脂质体包封率测定方法。方法：采用高效毛细管电泳法，分析条件为，石英毛细管，７０ｃｍ×７５μｍｉｄ；温度，２０℃，运行缓冲液，１０ｍｍｏｌ／Ｌ磷酸氢二钠（０１ｍｏｌ／Ｌ氢氧化钠调至ｐＨ１０８１）；运行电压，３０ｋｖ；检测波长，２５４ｎｍ。结果：线性范围１００～５０００ｍｇ／Ｌ，ｒ＝０９９８９，平均回收率９８７％（ｎ＝５），ＲＳＤ＝３５１％，薄膜分散法的包封率（１９５±２３）％远高于乙醇注入法的包封率（８３±３７）％。结论：本法适用于盐酸小檗碱脂质体包封率测定     

17β-雌二醇对人成骨细胞株HOS TE85细胞增殖及胞内cAMP,cGMP,iNOS影响

目的观察１７β－雌二醇（Ｅ２）对ＨＯＳＴＥ８５细胞增殖及胞内ｃＡＭＰ，ｃＧＭＰ，ｉＮＯＳ影响。方法［３Ｈ］－ＴｄＲ参入，放射免疫及Ｌ－３Ｈ－精氨酸转化法。结果Ｅ２１．０ｍｍｏｌ·Ｌ－１处理４８ｈ，细胞计数为（９４．３×１０７±７．５×１０７）个·Ｌ－１，对照组为（６５．０×１０７±５．９×１０７）个·Ｌ－１，［３Ｈ］－ＴｄＲ参入量增加４５．０％；细胞ｉＮＯＳ活性为（７３．０±６．６）ｐｍｏｌ·Ｌ－１·ｇ－１·ｍｉｎ－１（比对照组增加４６１．５％），ｃＧＭＰ为（０．６９±０．０３）ｐｍｏｌ·Ｌ－１·１０－８ｃｅｌ（比对照组增加３０５．９％）；抑制ｈＰＴＨ诱导胞内ｃＡＭＰ升高。结论Ｅ２能刺激成骨细胞增殖。Ｅ２可能通过影响胞内ｃＡＭＰ，ｃＧＭＰ，ｉＮＯＳ含量和活性而发挥作用。     

降纤酶与川芎嗪治疗急性缺血性脑血管疾病的比较

目的：比较降纤酶与川芎嗪治疗急性缺血性脑血管疾病（ＡＩＣＤ）的疗效。方法：降纤酶组３２例（男性１７例，女性１５例；年龄５９±ｓ９ａ）用降纤酶１０ＩＵ加入０．９％氯化钠注射液２５０ｍＬｉｖ，ｄｒｉｐ，ｑｄ×３ｄ，ｄ４剂量减半，ｉｖ，ｄｒｉｐ，ｑｄ×３ｄ，均于１～１．５ｈ滴完。川芎嗪组３１例（男性１７例，女性１４例；年龄５７±８ａ）用川芎嗪２００ｍｇ加入０．９％氯化钠注射液２５０ｍＬ静滴×１２ｄ。结果：降纤酶组与川芎嗪组总有效率分别为９７％与８１％（Ｐ＜０．０１）；血小板聚集率、血液粘度２组均有显著下降，凝血因子Ｉ与血脂仅降纤酶组有显著下降（Ｐ＜０．０５或Ｐ＜０．０１），２组均无严重不良反应。结论：降纤酶治疗ＡＩＣＤ明显优于川芎嗪     

女性肥胖病外周血细胞胰岛素受体的结合特性

对肥胖病患胰岛素与受体结构性进行研究，采用放射受体技术对２０例女性肥胖病患和２０例对照的单个核细胞和红细胞与胰岛素结合进行测定，结果显示：１．对照组单个核细胞和红细胞与＾１２５Ｉ－胰岛素的最大特异性结合分别为０．８％±０．０６％（１．２×１０＾７细胞／ｍｌ）和１３．５％±１．１％（３×１０＾９细胞／ｍｌ）而肥胖病组是０．４２％±０．０５％和９．１％±３．０％，均显示存在显性差异，Ｐ分别〈０     

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.