高效液相色谱法测定诺甲栓中诺氟沙星和甲硝唑的含量

目的：建立高效液相色谱法测定诺甲栓中诺氟沙星和甲硝唑的含量。方法：采用Kromasil C18柱（4．6mm×250mm，5μm），0．025mol·L^-1磷酸溶液（用三乙胺调节pH至3．0）-乙腈（80：20）为流动相，梯度洗脱，流速为1．0mL·min^-1，进样量10μL，检测波长278nm。结果：诺氟沙星在20-200mg·L^-1范围内、甲硝唑在42～420mg·L^-1范围内与峰面积线性关系良好，回收率分别为99．6％，100．1％，RSD分别为0．9％，0．9%。结论：方法简便、可靠、准确。可用于同时测定诺甲栓中诺氟沙星和甲硝唑的含量。     

高效液相色谱法测定复方甲硝唑栓中甲硝唑及诺氟沙星的含量

目的建立测定复方甲硝唑栓中甲硝唑及诺氟沙星含量的高效液相色谱法.方法采用Symmetry C18色谱柱(4.6 mm×150 mm,5μm),以乙腈-0.03 mol·L-1磷酸溶液(用三乙胺调节pH 3.0)(15;85)为流动相,流速为1.0 mL·min-1,检测波长为315 nm.结果甲硝唑及诺氟沙星在浓度范围内,峰面积与其浓度线性均关系良好(甲硝唑r=0.999 9,诺氟沙星r=1.000 0),平均回收率分别为100.64%和100.29%,精密度试验RSD分别为0.1%和0.2%,重复性试验RSD分别为1.5%和0.92%.结论该方法准确,简便,快速,专属性强,灵敏度高,适用于复方甲硝唑栓中甲硝唑及诺氟沙星的含量测定.     

高效液相色谱法测定甲硝唑诺氟沙星栓的含量

建立甲硝唑诺氟沙星栓中甲硝唑、诺氟沙星含量的HPLC测定方法.色谱柱为SUNTEK Kromasil C18柱;流动相为0.025mol·L-1磷酸溶液(用三乙胺调节pH值至3.0±0.1)-乙腈(80:20),流速为1.0ml·min-1,检测波长为278nm,线性范围为甲硝唑2.5～20μg·ml-1,r=0.9999,诺氟沙星2.5～20μg·ml-1,r=0.9999,平均回收率甲硝唑为97.55%,RSD为0.6%,诺氟沙星为97.96%,RSD为0.8%.方法准确可靠,简单易行,适用于甲硝唑诺氟沙星栓中甲硝唑、诺氟沙星的含量测定.     

氟甲栓的制备及质量控制

目的:制备氟甲栓并建立其质量控制方法。方法:以聚乙二醇为基质,甲硝唑、诺氟沙星为主药制备栓剂;采用高效液相色谱法同时测定其中主药的含量;并考察该制剂室温放置12个月的稳定性。结果:所制制剂为乳白色至淡黄色的圆锥形栓,鉴别、检查均符合2005年版《中国药典》中的相关规定;甲硝唑、诺氟沙星检测浓度的线性范围分别为8.32～41.60、2.08～10.40μg·mL-(1r=0.9999),平均回收率分别为98.23%、98.69%,日内、日间平均RSD分别为0.70%、0.62%,0.76%、0.65%;制剂12个月时各项指标未见明显变化。结论:该制剂制备工艺简便可行,质量稳定可控。     

HPLC法同时测定甲硝唑含漱液中甲硝唑和羟苯乙酯含量

目的建立同时测定甲硝唑含漱液中甲硝唑和羟苯乙酯含量的方法。方法高效液相色谱法,选用phenomenex-C18（4.6×250mm,5μm）柱,以乙腈∶水（25∶75）为流动相,检测波长为255nm。结果甲硝唑和羟苯乙酯的回归方程分别为：Y=1.3892×10^4X-1.068226×10^4（r=0.9999,n=9）和Y=1.092077×10^5X-2.022870×10^4（r=0.9999,n=9）;线性范围分别为2.7-270.8μg.mL^-1和0.2-53.0μg.mL^-1;平均回收率分别为104.5%和98.3%。结论所用方法简便快速,结果准确可靠,可作为甲硝唑含漱液的质量控制方法。     

高效液相色谱法测定复方己唑乳膏中己烯雌酚、氯霉素和甲硝唑的含量

目的 建立高效液相色谱测定复方己唑乳膏中己烯雌酚、氯霉素和甲硝唑含量的方法.方法 采用高效液相色谱法,色谱柱为Diamonsil C18 column（250 mm×4.6 mm,5μm）;流动相为甲醇-乙腈-水（55：5：40）;流速：1 mL·min-1;测定波长252 nm;柱温35℃;进样20μL.结果 该方法不受处方中基质干扰.己烯雌酚、氯霉素、甲硝唑的线性范围分别为0.016 8～0.184 8μg（r=0.999 8,n=6）、1.593 6～17.529 6 μg（r=0.999 9,n=6）、1.587 2～17.459 2μg（r=0.999 8,n=6）,平均回收率分别为99.5%、99.8%、99.9%,RSD分别为0.84%、1.2%、1.1%（n=9）.结论 该方法操作简便,灵敏度高,重现性好,可用于复方己唑乳膏中己烯雌酚、氯霉素和甲硝唑的含量测定.     

复方甲硝唑泡腾栓的制备及质量控制

目的 制备复方甲硝唑泡腾栓并建立质量标准.方法 以甲硝唑、诺氟沙星、醋酸泼尼松为王药制备复万甲硝唑泡腾栓,对其进行性状、重量差异、融变时限、发泡量、卫生学检查,并采用高效液相色谱法测定甲硝唑和诺氟沙星的含量,色谱条件为:色谱柱:Kromasil C18色谱柱(250 mm×4.6 mm,5 μm);流动相:乙腈-0.03 mol·L-1磷酸溶液(用三乙胺调节pH 3.0)(15∶85),流速:1.0 mL·min-1;柱温:30℃;检测波长:278 nm.结果 所制栓剂的鉴别、检查等结果均符合中国药典2010年版二部相应规定;甲硝唑和诺氟沙星检测浓度线性范围分别为32～160μg·mL1(r=0.999 9)、16～80 μg·mL-1(r=0.999 8);平均回收率分别为97.4％ (RSD=1.4％),97.3％ (RSD=0.87％).结论 该制备工艺简单,含量测定方法操作简便,结果准确可靠,可用于复方甲硝唑泡腾栓的质量控制.     

高效液相色谱法测定双唑泰阴道泡腾片中三主药含量

目的 用高效液相色谱法（HPLC法）测定双唑泰阴道泡腾片中甲硝唑、克霉唑和醋酸氯己定的含量。方法色谱柱为C18柱，流动相为甲醇-水-三乙胺（70：30：0．3），检测波长为260nm。结果 甲硝唑、克霉唑和醋酸氯己定的线性范围分别为50～300μg／mL，40～240μg／mL和2～12μg／mL，平均回收率分别为99.41％，99.33％和99．19％，RSD分别为0．17％，0.18％和0.14％。结论 HPLC法灵敏、准确、专属性强，可作为双唑泰阴道泡腾片的质量控制方法。     

高效液相色谱法同时测定复方甲硝唑散中甲硝唑、盐酸丁卡因及醋酸地塞米松的含量

目的:建立以高效液相色谱法同时测定复方甲硝唑散中甲硝唑、盐酸丁卡因及醋酸地塞米松含量的方法。方法:色谱柱为C18,流动相为甲醇-水-三乙胺(65∶35∶0.36),检测波长甲硝唑、盐酸丁卡因为310nm,醋酸地塞米松为240nm,流速为1ml/min,柱温为25℃。结果:甲硝唑、盐酸丁卡因、醋酸地塞米松进样量分别在0.412μg~2.06μg(r=0.9999)、0.191μg~0.956μg(r=0.9999)、0.121μg~0.604μg(r=0.9998)范围内线性关系良好;平均回收率分别为100.69%(RSD=1.28%)、101.37%(RSD=0.23%)、102.40%(RSD=0.89%)。结论:本方法简便、准确,重现性好,可用于复方甲硝唑散的质量控制。     

高效液相色谱法同时测定复方甲硝唑搽剂中甲硝唑和氯霉素含量

目的建立同时测定复方甲硝唑搽剂中甲硝唑和氯霉素含量的高效液相色谱法。方法采用高效液相色谱仪,色谱柱为AgilentZorbax Eclipse XDB-C18柱(250 mm×4.6 mm,5μm),以甲醇-水-冰醋酸(45∶55∶0.1)为流动相,检测波长为277 nm,流速为1.0 mL/min,柱温为30℃。结果甲硝唑和氯霉素的进样量线性范围分别为214.10～2 141.00μg(r=0.999 9)和55.96～559.60μg(r=0.999 9),平均回收率分别为98.09%(RSD=0.73%)和98.48%(RSD=0.87%)。结论该方法两种成分分离效果好,可同时测定,方法简便快速,结果准确可靠,可作为复方甲硝唑搽剂的质量控制方法。     

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.

     

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.     

Glycofection: The Ubiquitous Roles of Sugar Bound on Glycoplexes

Glycofection (transfection by using sugar-substituted polylysine) was assessed in order to provide an alternative to viral vectors for the transfer of genes into vascular smooth muscle cells. A rabbit vascular smooth muscle cell line (Rb-1 cells) was selectively transfected by using glycoplexes (glycosylated polylysine/pSV2LUC complexes) in the presence of 10 mu M of the fusogenic peptide GALA. A sugar-specific transfection was obtained when the glycofection was conducted for 1 h with glycoplexes containing either alpha Gal, alpha -Glc, alpha -GalNAc, beta -GlcNAc, or beta -GalNAc residues. The gene expression was high after transfection, with glycoplexes bearing alpha Gal, alpha -GalNAc, or beta -GalNAc residues that were weakly internalized, and low with glycoplexes carrying Lact or Rha residues that were well taken up by cells. These results suggest that 1) glycofection can be a good approach for a selective transfer of genes intovascular smooth muscle cells, 2) an efficient uptake of the glycoplexes is not the unique limiting step for an efficient transfection, and 3) the sugar-dependent trafficking of the glycoplexes inside the cells may account for the transfection efficiency.     

直肠癌下切缘病理组织学分析

目的探讨直肠癌逆向浸润与下切缘的安全距离的关系。方法对36例直肠癌Miles手术和Dixon手术后标本的肿瘤下缘1.0cm、2.0cm、3.0cm的肠壁及对应的系膜病理组织学检查,观察直肠癌逆向浸润或转移的距离。结果36例直肠癌标本距癌肿下缘1.0 cm、2.0cm、3.0cm的肠壁及对应的系膜病理组织学检查均为阴性,结论直肠癌远恻逆向浸润或转移未见超过1.0cm,因此认为保肛手术时切除肿瘤远侧肠管(包括系膜)2.0cm是安全的。