高效液相色谱法测定消银片含量

目的：用高效液相色谱法测定消银片含量；方法：ODS柱，以乙腈：0．1％磷酸溶液(40：60)为流动相，于220nm波长处检测，流速1．0ml／min；结果：该方法在50μg／ml～460μg／ml范围内，峰面积与浓度呈良好的线性关系(r=0．9998)，重复性试验RSD=1．21％(n=6)；结论：方法简便快速、重现性好。     

HPLC法测定苦参药材中苦参碱的含量

目的：建立测定苦参药材中苦参碱含量的高效液相色谱法。方法：采用Alltech Alltima C18（250mm×4．6mm，5μm）色谱柱，柱温25℃；流动相为0．02mol·L^-1三乙胺（醋酸调节pH9．5）-乙腈（60：40），流速1．0mL·min^-1；检测波长为220nm。结果：线性范围为0．01～2．0mg·mL^-1；稳定性试验RSD为0．57％（n=5）；平均回收率为99．42％（n=6）；重复性试验RSD为1．78％（n=6）。结论：本方法快速简便、准确，重复性好。     

高效液相色谱法测定苯妥英钠凝胶剂的含量

目的：建立了高效液相色谱法测定苯妥英钠凝胶剂的含量。方法：采用Hypersil ODS-2C18色谱柱（250mm×4．6mm，5μm）；流动相为0．05mol·L-1磷酸二氢钾（pH3．5）-甲醇（53：47）；流速1．0mL·min；检测波长220nm；柱温：35℃。结果：苯妥英钠在1—20μg·mL-1浓度范围内线性关系良好（r=0．9998）；平均回收率为100．1％（n=9）。结论：本方法简单，灵敏，重现性好，可用于苯妥英钠凝胶剂的含量测定。     

HPLC法测定复方甘草口服溶液中吗啡的含量

目的：应用HPLC法测定复方甘草口服溶液中吗啡的含量。方法：采用硅胶柱，以水-乙腈-甲酸（85：15：0．05）为流动相；流速0．8ml／min，检测波长220nm。结果：吗啡在1．98-29．72μg/ml浓度范围内线性关系良好，平均加样回收率为99．4％，RSD=1．90％。结论：本方法简便、准确、重现性好，可用于复方甘草口服溶液的质量控制。     

HPLC法测定橘红化痰丸中吗啡的含量

目的：建立HPLC法测定橘红化痰丸中吗啡含量。方法：预处理应用固相萃取技术；液相色谱采用Shim—pack C18色谱柱（150mm×6．0mm，5μm），流动相为乙腈-0．05mol·L^-1磷酸二氢钾-0．005mol·L^-1庚烷磺酸钠（10：45：45），流速：1mL·min^-1．柱温：25℃，检测波长：220nm。结果：吗啡进样量在0．027～2．668μg范围内线性关系良好（r=0．9999）。低、中、高3个加入量的回收率（n=3）分别为99．96％，101．0％，98．63％；RSD分别为1．7％，0．7％，1．0％。结论：方法简便、准确，重复性好。     

HPLC法测定龙血竭胶囊中血竭素的含量

建立龙血竭胶囊中血竭素的含量测定方法。方法：采用HPLC法，色谱柱为YWC-C18；柱温40℃；流动相为乙腈-0．05mol／L磷酸二氢钠(35：65)；pH约3.0左右；流速1、0ml／min；检测波长440mm。结果：线性范围0．26-2．60μg／ml，平均回收率为97．9％，RSD=1．21％。结论：该方法重现性好，结果准确，可作为龙血竭胶囊的质量控制方法。     

HPLC法测定乌丹降脂颗粒中大黄素的含量

目的：建立HPLC法测定鸟丹降脂颗粒中大黄素的含量。方法：固定相为C18ODS柱；流动相为甲醇-0．1％磷酸溶液；检测波长254nm。结果：大黄素标准对照品线性关系好，r=0．9999，样品平均回收率为97．55％，RSD=1．48％。结论：本法简便、准确、灵敏度高、重复性好，可用于该产品的含量测定。     

HPIC法测定天麻素氯化钠注射液中天麻素的含量

目的：建立HPLC测定天麻素氯化钠注射液中天麻素的含量。方法：用HypersilBDS（5um，4．6mm＊250mm）C18柱；以甲醇-0．01mol／L磷酸二氢钠（8：92，磷酸调节PH至4．0±0．1）为流动相；流速0．8ml／min；检测波长220hm；进样量2μl。结果：天麻素在2．5μg／ml～25μg／ml范围内，天麻素浓度与峰面积的线性关系良好（r=0．9998），检测限为1．15ng（S／N=3）。回收率为98．9％，R5D=0．08％（n=9）。结论：方法简便，结果准确，重复性好。     

HPLC法测定天益颗粒中天麻素的含量

目的测定中药天益颗粒中天麻素的含量。方法用十八烷基键合硅胶柱分离天麻素，流动相：乙腈-0．05％磷酸（4：96）；检测波长：220nm。结果天麻素在0．4—2μg之间呈良好的线形关系，r=0．9998；平均回收率为98．41％，RSD=1．72％（n=5）。结论方法简便，快速，准确，专属性强，可作为样品的检验方法。     

离子对HPLC法测定N-乙酰-D-葡萄糖胺的含量

目的：建立离子对HPLC法测定N-乙酰-D-葡萄糖胺及其制剂含量的方法。方法：采用Alltima ODS色谱柱（5μm，250mm×4．6mm）；流动相为含10mmol·L^-1四丁基硫酸氢铵的磷酸氢二钾（0．1mol·L^-1）溶液，用磷酸调pH至6．5±0．1；流速0．8mL·min^-1；柱温：室温；波长：220nm。结果：在0．4～8×g的范围内N-乙酰-D-葡萄糖胺峰面积与进样量呈良好的线性关系，r=0．9999；最低检出限为1．3ng；最低定量限为4ng；高、中、低3种浓度的回收率分别为99．9％，100．1％，100．2％；RSD分别为0．46％，0．32％，0．28％。结论：该方法简单、灵敏、准确、专属性好。     

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.