芳伯胺类药物的恒电流库仑法测定

用恒电流库仑法测定芳伯胺类药物含量.在中性介质中电解NaNO3溶液,使Pt阴极电生出NO2-,然后在盐酸存在下以NO2-滴定芳伯胺类药物,以永停终点法确定终点.方法相对误差为0.20%～0.24%,RSD为0.029%～0.033%.     

盐酸阿米替林零电流示波电位和双电位滴定的研究

本文首次以涂有PVC膜的铂片作为指示电极,以四苯硼钠为滴定剂,对盐酸阿米替林进行零电流示波电位滴定和零电流示波双电位滴定,方法准确、简便、直观,还可用于其它药物的测定。     

Gran电位滴定法测定甲氰咪胍的含量

目的:测定甲氰咪胍片的含量.方法:用电位滴定法,以0.2 mol*L-1 KCl溶液作离子强度调节剂,用NaOH标准溶液滴定.滴定剂分步等体积加入,测定其pH值.以强碱滴定弱酸计量点后之Gran函数对滴定剂体积作图,直线外推求滴定终点.结果:平均回收率为99.85%,RSD为0.35%.结论:该法准确性高,精密度好,操作简便,快速.     

电位滴定法测定克林霉素磷酸酯氯化钠注射液中氯化钠含量

目的建立一种用电位滴定法测定克林霉素磷酸酯氯化钠注射液(商品名:恒新,以下简称恒新注射液)中氯化钠含量的方法.方法采用银电极为指示电极,以0.1 mol·L-1硝酸银为滴定剂,有电位滴定仪在常温下进行测定.结果该方法测定线性范围为9～90 mg,r=0.999 9,加样平均回收率为99.7%,精密度RSD为0.08%.结论该法快速准确,无干扰,可用于恒新注射液质量控制.     

甘草苷的电化学伏安行为及其应用

目的:研究了甘草苷(LQ)在碳糊电极(CPE)上的电化学行为及电化学动力学性质,据此建立了LQ的方波伏安法的新测定方法。方法:采用循环伏安法(CV)、控制电位电解库仑法(BE)、计时库仑法(CC)、计时电流法(CA)及方波伏安法(SWV)等电化学方法。结果:LQ在CPE上的电化学过程是一不可逆电化学氧化过程,氧化峰电位(Ep)为0.882 V。在扫描速度10～800 mV.s-1范围内其氧化峰电流与扫描速度平方根(υ1/2)呈良好的线性关系,表明LQ在CPE上的伏安行为是一受扩散控制的电极过程。用SWV法测定LQ的氧化峰电流与其浓度在1.8×10-7～1.6×10-3 mol.L-1(r=0.9964)范围内呈良好的线性关系,检出限8.0×10-8 mol.L-1,RSD 2.8%～3.2%,加样回收率98.0%～102.0%。结论:该方法简便快捷,用于中成药及模拟尿样中LQ含量测定,结果令人满意。     

库仑滴定法测定苯酚滴耳液中苯酚含量

目的探讨测定苯酚滴耳液中苯酚含量的简便方法。方法采用库仑滴定法，以双铂电极电流法确定库仑滴定的终点。结果苯酚的平均回收率为100．24％，RSD为2．80％（n=5）。结论库仑滴定法简便易行，易于推广，可用于苯酚滴耳液的含量测定。     

黄酮类化合物库伦滴定法 大豆甙元的库伦滴定

本文根据黄酮化合物所具有苯酚性质,利用含有溴化钾的醋酸溶液电解产生溴对大豆甙元的库伦滴定进行了研究。通过实验,确定了滴定条件,测定了大豆甙元溴取代反应电子数(n=8),并建立了库伦滴定法;即以1M溴化钾和冰醋酸(1:1)作电解液,选择适当电流,电解发生过量的溴与样品反应后,加入一定量的亚砷溶液,然后再发生溴,滴定过剩的亚砷,用死停法确定终点。     

动态库仑法测定药物中抗坏血酸含量

目的：建立动态库仑法测定药物中抗坏血酸含量的新方法，用于维生素C的质量控制。方法：通过在0．05％KI-0．04％HAc电解液中，动态电流电解I3^-氧化滴定抗坏血酸，由电解I3^-所消耗的电量计算维生素C含量。结果：该法测量范围0．02～3．0mg·L^-1，检出限可达0．01mg·L^-1，与2，6-二氯靛酚法对照用于对片剂、针剂中维生素C测定，二者结果吻合，相对误差小于2％。结论：该法制样简单、试样用量少，操作简便、快速，灵敏度高、重现性好，不受试样颜色和浊度的影响，可用于临床向液和尿液中维牛素C的微量分析。     

测定复方磺胺甲蘸唑片剂含量的简易方法

根据复方磺胺甲噁唑片磺胺甲噁唑(SMZ)分子结构中磺酰胺基-SO2NH-的酸性,我们参考了文献:多数酸性较强的磺胺类药物可用标准碱液直接滴定以测定含量的原理,采用酸量法不经分离测定SMZ含量;用简便分离法以单光束分光光度计测定TMP含量,可在2h内完成复方磺胺甲噁唑片剂的含量测定.较药典法配制对照品精称干燥恒重步骤简捷,同样准确,现介绍如下.     

聚氨基苯甲酸修饰电极的制备及其在阿卡波糖含量测定中的应用

目的:建立测定阿卡波糖含量的新方法。方法:采用电化学分析法。先通过循环伏安法将氨基苯甲酸电聚合在电极表面形成聚氨基苯甲酸,再利用铁氰化钾作为探针分子,以其在修饰电极上产生的氧化峰电流,采用方波伏安法进行阿卡波糖的含量测定,电位窗口为-0.1～+0.6V。结果:阿卡波糖检测浓度线性范围为0.10020～2.5050μg·mL-(1r=0.9998),平均回收率为96.33%,RSD=2.1%(n=4)。结论:该方法快速、简便,可用于片剂中阿卡波糖的含量测定。     

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.     

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.

     

Lung disease and PKCs

The lung offers a rich opportunity for development of therapeutic strategies focused on isozymes of protein kinase C (PKCs). PKCs are important in many cellular responses in the lung, and existing therapies for pulmonary disorders are inadequate. The lung poses unique challenges as it interfaces with air and blood, contains a pulmonary and systemic circulation, and consists of many cell types. Key structures are bronchial and pulmonary vessels, branching airways, and distal air sacs defined by alveolar walls containing capillaries and interstitial space. The cellular composition of each vessel, airway, and alveolar wall is heterogeneous. Injurious environmental stimuli signal through PKCs and cause a variety of disorders. Edema formation and pulmonary hypertension (PHTN) result from derangements in endothelial, smooth muscle (SM), and/or adventitial fibroblast cell phenotype. Asthma, chronic obstructive pulmonary disease (COPD), and lung cancer are characterized by distinctive pathological changes in airway epithelial, SM, and mucous-generating cells. Acute and chronic pneumonitis and fibrosis occur in the alveolar space and interstitium with type 2 pneumocytes and interstitial fibroblasts/myofibroblasts playing a prominent role. At each site, inflammatory, immune, and vascular progenitor cells contribute to the injury and repair process. Many strategies have been used to investigate PKCs in lung injury. Isolated organ preparations and whole animal studies are powerful approaches especially when genetically engineered mice are used. More analysis of PKC isozymes in normal and diseased human lung tissue and cells is needed to complement this work. Since opposing or counter-regulatory effects of selected PKCs in the same cell or tissue have been found, it may be desirable to target more than one PKC isozyme and potentially in different directions. Because multiple signaling pathways contribute to the key cellular responses important in lung biology, therapeutic strategies targeting PKCs may be more effective if combined with inhibitors of other pathways for additive or synergistic effect. Mechanisms that regulate PKC activity, including phosphorylation and interaction with isozyme-specific binding proteins, are also potential therapeutic targets. Key isotypes of PKC involved in lung pathophysiology are summarized and current and evolving therapeutic approaches to target them are identified.     

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.     

Gender-related symptoms and correlates of alcohol dependence among men and women with a lifetime diagnosis of alcohol use disorders

This study explored gender-related symptoms and correlates of alcohol dependence in a crosssectional study of 150 men and 150 women with a lifetime diagnosis of alcohol use disorders (AUD). Participants were recruited in equal numbers from treatment settings, correctional centres and the general community. Standardized measures were used to determine participants' use of substances, history of psychiatric disorders and psychosocial stress, their sensation seeking and family history of substance use and mental health disorders. Multivariate analyses were used to detect patterns of variables associated with gender and the lifetime severity of AUD. Men had a longer history of severe AUD than women. Women had similar levels of alcohol dependence and medical and psychological sequelae as men, despite 6 fewer years of AUD. More women than men had a history of severe psychosocial stress, severe dependence on other substances and antecedent mental health problems, especially mood and anxiety disorders. There were differences in family history of alcohol-related problems approximating same-gender aggregation. The severity of a lifetime AUD was predicted by its earlier age at onset and the occurrence of other disorders, especially anxiety, among both men and women. The limitations in the generalizability of these findings due to sample idiosyncrasies are discussed.     

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.