高效液相色谱法测定醋酸氯己定痔疮栓的含量

目的建立测定醋酸氯己定痔疮栓中酸酸氯己定含量的高效液相色谱（HPLC）法。方法色谱柱为C18柱（150mm×4.6mm,5μm）,流动相为0.8%三乙胺（冰醋酸调pH至4.9）-甲醇（40：60）,流速1.0mL/min,检测波长259nm。结果醋酸氯己定质量浓度在16～120μg/mL范围内与峰面积线性关系良好（r=0.9999,n=5）,平均回收率为98.67%,RSD=1.36%（n=6）。结论所用方法简单、准确、重现性好,可用于醋酸氯己定痔疮栓的含量测定。     

醋酸氯己定栓剂中醋酸氯己定的含量测定

目的建立醋酸氯己定栓剂中醋酸氯己定的含量测定方法。方法采用紫外分光光度法测定醋酸氯己定的含量。结果醋酸氯己定在2～10μg/mL浓度范围内线性关系良好,其回归方程为:C=13.35A+0.06273(r=0.9997),平均回收率99.6%,RSD=0.83%(n=9)。结论此含量测定方法简便,准确可靠。     

高效液相色谱法测定复方甲硝唑嗽口液中两组分的含量

目的：测定复方甲硝唑嗽口液中甲硝唑和醋酸氯己定的含量。方法：采用高效液相色谱法，色谱柱为Shim-Pack CLC-ODS；流动相为0.3%庚烷磺酸钠甲醇液－水（5:2)，用冰醋酸调节pH至3.2；流速为1.0ml/min；检测波长为260nm。结果：甲硝唑和醋酸氯己定的回收率分别为99.7%,RSD=0.51%;99.5%,RSD=0.59%。结论：方法简便，准确，可作为该制剂的质控标准。     

高效液相色谱法测定复方替硝唑氯己定含漱液中醋酸氯己定含量

目的 建立测定复方替硝唑含漱液中醋酸氯己定含量的高效液相色谱法.方法 采用美国Agilent 1260型高效液相色谱仪,流动相为三乙胺缓冲液(0.05 mol/L,用磷酸调pH至3.5)-乙腈-甲醇(42:13:45),流速为1.0 mL/min,检测波长为259 nnl.结果 醋酸氯己定在该条件下实现基线分离,质量浓度线性范围为10.4～82.9μg/mL(r=0.999 9),平均回收率为103.25%,RSD=0.32%(n=6).结论 所用方法简便快速、结果准确可靠,可作为复方替硝唑氯已定含漱液的质量控制方法.     

RP-HPLC法测定导便栓中醋酸氯己定的含量

目的:建立以反相高效液相色谱法测定导便栓中醋酸氯己定含量的方法。方法:色谱柱为Diamond C_(18),流动相为乙腈-水-三乙胺(30:70:0.5,用磷酸调pH至3.0),检测波长为260 nm,流速为1.0 mL·min~(-1),进样量为20μL,柱温为30℃。结果:醋酸氯己定检测浓度的线性范围为1.092～13.10μg·mL~(-1)(r=0.999 9);平均回收率为98.29%(RSD=2.16%,n=9)。结论:本方法操作简便、准确、灵敏,可用于该制剂的含量测定。     

RP-HPLC同时测定复方替硝唑溶液中替硝唑和醋酸氯己定的含量

目的建立同时测定复方替硝唑溶液中替硝唑和醋酸氯己定含量的反相高效液相色谱方法 (RP-HPLc)。方法采用高效液相色谱法,C18色谱柱(4.6 mm×250 mm,5μm);流动相以甲醇为流动相A,甲醇-0.05 mol/L磷酸二氢钾溶液(p H 3.5)(20∶80)为流动相B,采用梯度洗脱方法 ;检测波长为280 nm。结果替硝唑和醋酸氯己定的含量分别在80.2~280.7μg/ml、80.28~280.98μg/ml的范围内线性关系良好,平均回收率分别为100.08%和100.33%(n=6)。结论该方法操作简便,结果可靠,可以用于同时测定复方替硝唑溶液中替硝唑和醋酸氯己定的含量,以控制该制剂的质量。     

双波长反相高效液相色谱法测定口腔溃疡油中3组分含量

目的建立测定口腔溃疡油中盐酸达克罗宁、醋酸泼尼松龙和醋酸氯己定含量的反相高效液相色谱法。方法色谱柱为Waters C18柱(150 mm×4.6 mm,5μm),流动相为0.02 mol/L磷酸二氢钾(含0.4%三乙胺,pH=2.5)-甲醇(60∶40),流速1.2 mL/min,检测波长243 nm和259 nm,柱温25℃。结果 259 nm波长处,盐酸达克罗宁质量浓度线性范围是80～240μg/mL(r=0.999 9),平均回收率为100.78%,RSD=0.72%;243 nm波长处,醋酸泼尼松龙质量浓度线性范围是8.56～25.68μg/mL(r=0.999 9),平均回收率为101.66%,RSD=0.15%,醋酸氯己定质量浓度线性范围是8.46～25.44μg/mL(r=0.999 4),平均回收率为101.24%,RSD=0.46%。结论所用方法简便、准确、重现性好,可用于口腔溃疡油的质量控制。     

高效液相色谱法测定施美乐涂膜中醋酸氯己定含量

目的建立测定施美乐涂膜中醋酸氯己定含量的高效液相色谱法。方法采用ODS C18柱(250 mm×4.6 mm,5μm),以水相(取三乙胺5 mL,磷酸二氢钠7.8 g,加水450 mL,用85%磷酸调pH至2.5,再加水至500 mL)-甲醇-乙腈(40∶40∶20)流动相,检测波长为258 nm。结果醋酸氯己定进样量在0.212～1.060μg范围内与峰面积呈良好线性关系(r=0.999 9),平均回收率为100.28%,RSD为1.74%(n=6)。结论该方法操作简便,重现性好,结果准确可靠,适用于该制剂的质量控制。     

反相高效液相色谱法测定双唑泰栓中甲硝唑、克霉唑和醋酸氯己定的含量

目的:建立双唑泰栓中甲硝唑、克霉唑和醋酸氯己定含量的测定方法。方法:采用反相高效液相色谱法,以十八烷基键合硅胶柱(Kromasil C_(18))为分析柱,甲醇-水相(庚烷磺酸钠3g,三乙胺2.5 mL,加水至1000 mL,冰醋酸调pH2.5)(65:35)为流动相,流速:1.0 mL·min~(-1),UV250～350nm范围扫描,检测波长甲硝唑为315nm、克霉唑和醋酸氯己定为260nm;采用外标法室温检测。结果:甲硝唑、克霉唑和醋酸氯己定线性范围分别为125～625,100～500,5～25μg·mL~(-1),r=0.999 9;平均回收率分别为99.2％,99.7％,100.5％(n=6)。结论:该法快速、方便,分离度好,辅料无干扰,适用于该复方制剂中3种成分的同时测定。     

梯度洗脱高效液相色谱法测定宁肤露中3 组分的含量

目的 :建立梯度洗脱反相高效液相色谱法测定宁肤露中水杨酸、醋酸氯己定、醋酸地塞米松含量的方法。方法 :ODS2色谱柱 ;流动相 :乙腈 0 .0 1mol·L-1 磷酸氢二钠溶液 (用磷酸调 pH3.6 )梯度洗脱 ,检测波长 2 4 0nm。结果 :水杨酸、醋酸氯己定、醋酸地塞米松的平均回收率分别为 99.4 5 %,RSD为 1 .1 %(n =9) ;99.33%,RSD为 1 .4 %(n =9) ;1 0 0 .1 %,RSD为1 .1 %(n =9)。结论 :用HPLC同时测定宁肤露中水杨酸、醋酸氯己定、醋酸地塞米松含量 ,操作简便 ,结果准确。     

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.