HPLC法测定复方苦木消炎片中穿心莲内酯溶出度

目的：建立复方苦木消炎片中穿心莲内酯溶出度的测定方法,并对市售产品进行溶出度的测定。方法：采用高效液相色谱法测定穿心莲内酯的溶出度。用500 ml 0.2%十二烷基硫酸钠为溶出介质,使用转篮法在100 r·min-1的转速下进行溶出度的试验,于45 min取样测定。结果：穿心莲内酯的浓度在0.37-3.70μg·ml-1范围内呈良好的线性关系（r=0.999 8）,回收率为99.4%,RSD为0.22%（n=6）。在45 min取样测定,复方苦木消炎片中穿心莲内酯的溶出度不低于标示量的80%。结论：本方法简便,结果准确可靠,可用于复方苦木消炎片中穿心莲内酯的溶出度的测定。     

复方磺胺嘧啶分散片的制备与体外溶出度考察

目的建立复方磺胺嘧啶分散片制备工艺,考察磺胺嘧啶体外溶出度测定方法。方法依据《中华人民共和国药典》2010年版溶出度测定法（附录ⅩC第三法）, 以盐酸溶液（9～1 000）为溶出介质,转速50 r•min－1, 45 min内取样测定溶出度。结果磺胺嘧啶在10～90 μg•mL－1浓度范围内与峰面积呈良好的线性关系（r＝0.999 7）, 回收率99.86%（RSD＝1.5%）,3批样品在45 min平均溶出量均＞75.0%。结论该处方合理,制备工艺简单可行,体外溶出度测定方法稳定、准确,为进一步制定复方磺胺嘧啶分散片质量标准提供了依据。     

不同厂家复方黄连素片的溶出度试验

目的对复方黄连素片进行溶出度试验。方法采用溶出度测定第一法，纯化水1 000 mL为溶剂，转速120 r·min 1；高效液相色谱法(HPLC)测定盐酸小檗碱的累积溶出量。结果不同厂家复方黄连素片溶出速率差异较大，但60 min时累积溶出量基本＞70%。结论建议建立复方黄连素片的溶出度检查项目。     

复方利福平片溶出度测定方法的研究

目的 建立复方利福平片的溶出度测定方法。方法 采用溶出度测定法第二法，以水为溶剂，转速为50r／min，经45min取样，紫外分光光度法在474nm处测定利福平的溶出量，溶出限度为标示量的75％。结果利福平在10．3—36．1μg／ml范围内线性关系良好(r＝1．0000)，平均回收率99．8％。结论 本方法准确、快速、简便。通过测定复方利福平片的溶出度可有效检测其制剂工艺水平。     

基于模糊-粗糙集的移动对象k近邻预测

目的：建立复方氨酚烷胺胶囊的最佳溶出度方法。方法：采纳了《国家药品标准》第16册复方氨酚烷胺片的溶出度介质，通过转速和取样时间的选择，确定了复方氨酚烷胺胶囊的溶出度方法。同时对方法的回收率和线性进行了考察。结果：采用转篮法，以盐酸溶液（9～1000）1000mL为溶出介质，转速75r·min^-1，溶出时间为15min。取样后采用紫外可见分光光度法，在257nm波长处测定吸光度，按对乙酰氨基酚（C8H9NO2）吸收系数（E1cm^1%）715计算各粒的溶出量。结论：本方法符合溶出度方法的建立原则，可控制复方氨酚烷胺胶囊的内在质量。     

蜂胶软胶囊的体外溶出度测定

［摘要］目的测定蜂胶软胶囊中总黄酮的溶出度。方法选用转篮法,以0.1 mol•L 1盐酸溶液（9→1 000 mL） 1 000 mL为溶出介质,转速100 r•min 1,溶出时间45 min。采用紫外分光光度法测定溶液吸光度,测定波长265 nm。结果线性回归方程：Y＝0.093 1X－0.058 8,r＝0.999 5。平均加样回收率99.35%,RSD＝1.51%。同一批次样品溶出度均一性良好,溶出参数：T50＝16.41,Td＝22.98,T80＝35.6,m＝1.087 3。不同批次软胶囊的溶出量均＞80%。结论该方法可靠、准确、快速,可作为蜂胶软胶囊的溶出度测定方法。     

洛美利嗪片体外溶出度研究

目的建立洛美利嗪片体外溶出度的测定方法。方法以0.1 mol·L^-1盐酸溶液为溶出递质，采用小杯法，转速为75 r·min^-1，温度为(37.0±0.5)℃，进行累积溶出百分率测定。用紫外分光光度法在225 nm的波长处测定。结果洛美利嗪在盐酸溶液中8～20 μg·mL^-1范围内线性关系良好，平均回收率为100.4%，RSD＝0.7%(n＝5)。洛美利嗪片15 min内溶出＞90.0%，45 min时溶出度RSD＜2.0%。结论洛美利嗪片溶出速度快，溶出均一性好。     

布洛芬颗粒及混悬液的溶出度考察

目的建立布洛芬颗粒和混悬液体外溶出度试验的测定方法。方法采用浆法,以磷酸缓冲液（pH7.2）为溶出介质;溶出量采用液相色谱的方法测定。以DiamondC18柱（5μm,250mm×4.6mm）,流动相为0.1%磷酸溶液-乙腈（35：65）,流速为1ml？min-1,检测波长222nm。结果在15min内颗粒剂中布洛芬的溶出较混悬液中布洛芬溶出快;而30min内溶出度均大于80%。结论本方法可用于布洛芬颗粒剂和混悬液的溶出度测定。     

不同厂家复方氨酚烷胺胶囊的溶出度考察

目的对不同厂家的复方氨酚烷胺胶囊进行溶出度考察。方法采用桨法和紫外分光光度法进行溶出度测定。结果 4个厂家5个批号的复方氨酚烷胺胶囊于10min取样时溶出度分别为:77.8%,85.0%,67.1%,88.1%和79.2%;20min取样,对乙酰氨基酚的含量不低于标示量的80%。结论不同厂家复方氨酚烷胺胶囊的溶出度有一定差异,建议对复方氨酚烷胺胶囊进行溶出度测定。     

复方岩白菜素分散片的制备及其溶出度研究

目的：考察处方中各组分对复方岩白菜素分散片制剂的溶出的影响因素。方法：以分散均匀性和溶出度为指标进行处方筛选，对优选的处方进行溶出度试验，并与普通片进行比较。结果：按优化处方制备的复方岩白菜素分散片可在1min内完全崩解，其体外溶出度明显优于普通片。结论：将岩白菜素制备成分散片可提高其溶出度。     

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.     

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.     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

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.