高效液相色谱法测定二羟丙茶碱的含量

目的:采用高效液相色谱法测定二羟丙茶碱的含量。方法:色谱柱(Welchrom)C18柱(250mm×4.6mm,5μm);以甲醇:水(25:75)为流动相;流速为:1.0ml/min,检测波长为273nm。结果:二羟丙茶碱在25～125μg/ml范围内线性关系良好,r=1.0000;平均回收率为99.4%(n=6),含量测定RSD=0.36%。结论:本方法测定二羟丙茶碱含量简便、灵敏、快速,结果准确可靠。     

HPLC法同时测定复方阿托伐他汀钙分散片中2组分含量

目的:建立同时测定复方阿托伐他汀钙分散片中氨氯地平、阿托伐他汀含量的方法。方法:采用高效液相色谱法。色谱柱为Waters XTerra RP18;流动相为乙腈-0.03moL·L-1磷酸二氢钾溶液=58:42,流速为1.0mL·min-1;检测波长为240nm;柱温为30℃。结果:氨氯地平、阿托伐他汀检测浓度线性范围分别为3.86～61.83(r=0.9999,n=5)、9.28～148.56(r=0.9999,n=5)μg·mL-1;平均回收率分别为100.7%(RSD=0.94%,n=6)、100.6%(RSD=0.85%,n=6)。结论:所建立的方法简便、灵敏、准确,可用于复方阿托伐他汀钙分散片的含量测定。     

高效液相色谱法测定盐酸氟西汀胶囊含量

目的:建立反相高效液相色谱法测定盐酸氟西汀胶囊的含量.方法:采用kromasil C18色谱柱(5μm,4.5mm×15mm)为分离柱;流动相为甲醇:0.05mol/L磷酸二氢钾缓冲液(55:45);流速:1mL/min;检测波长:230nm;柱温:室温.结果:盐酸氟西汀在52.5mg/L～315mg/L浓度范围内线性良好(r=0.9994);方法平均回收率为99.66%(RSD=0.98%,n=5);5次测定的精密度0.16%～0.35%.结论:本方法操作简便、快速、准确、灵敏,适用于盐酸氟西汀胶囊的含量测定.     

HPLC法测定藿香正气胶囊中厚朴酚与和厚朴酚的含量

目的测定藿香正气胶囊中厚朴酚与和厚朴酚的含量.方法采用HPLC法.色谱柱:采用Thermo 1254133T色谱柱(250×4.6mm,5μm);流动相:甲醇-水(75∶25);流速:1.0mL·min-1;检测波长:294nm.结果厚朴酚平均回收率为99.81%,RSD=0.3%(n=5);和厚朴酚平均回收率为100.14%,RSD=0.8%(n=5).结论方法简单易行,结果准确,可靠,适用于本品的含量测定.     

HPLC同时测定益精丸中梓醇和阿魏酸的含量

目的建立测定益精丸中梓醇和阿魏酸含量的HPLC方法。方法色谱条件:色谱柱:Atlantis T3 C18色谱柱(4.6 mm×250 mm,5μm);混合流动相:乙腈(A)-0.1%磷酸(B)梯度洗脱;流速:0.8 ml/min;检测波长:210 nm;柱温:32℃。结果梓醇和阿魏酸分别在6.24~124.80μg/ml(r=0.9997,n=6),4.96~99.20μg/ml(r=1.0000,n=6)范围内线性关系良好,平均回收率分别为95.2%、95.3%,RSD分别为1.3%和1.8%。结论该方法简单、快速、准确可靠,可用于测定益精丸中梓醇和阿魏酸含量。     

反相高效液相色谱-柱前衍生化法测定大青叶中氨基酸的含量

目的:建立以反相高效液相色谱法测定大青叶中精氨酸和脯氨酸含量的方法。方法:采用2,4—二硝基氟苯柱前衍生化,将氨基酸在碱性条件下衍生后直接进样测定;色谱柱为KromasilC18,流动相为醋酸钠缓冲溶液(pH=6.4)-乙腈(850∶150),检测波长为360nm,外标法计算含量。结果:精氨酸和脯氨酸进样量分别在0.627μg～5.016μg(r=0.9996)、0.874μg～7.000μg(r=0.9995)范围内线性关系良好;平均回收率均为98.2%(RSD=2.3%、2.2%)。结论:本法简便、准确、可靠,适用于大青叶中氨基酸的含量测定。     

高效液相色谱法测定联苯苄唑凝胶的含量

目的建立联苯苄唑凝胶质量标准的分析方法。方法采用高效液相色谱法(RP-HPLC)测定联苯苄唑凝胶中联苯苄唑的含量,色谱柱:Hypersil C18柱(4.6 mm×250 mm,5μm);流动相:甲醇-水-乙腈(80∶15∶5);流速1 mL.m in-1;柱温:40℃;检测波长:254 nm。结果联苯苄唑在12.56~125.60μg.mL-1的浓度范围内线性关系良好(r=0.999 9)。联苯苄唑平均回收率(n=3)分别为99.0%(RSD=0.74%),100.5%(RSD=0.96%),98.7%(RSD=0.55%)。结论该方法可以用于测定联苯苄唑凝胶中联苯苄唑的含量。     

龙胆泻肝丸中龙胆苦苷含量的检测方法

目的建立龙胆泻肝丸中龙胆苦苷含量测定的方法。方法色谱柱:VP-ODS柱(150mm×4.6mm,5μm);流动相:A组分:乙腈:0.1%磷酸溶液(10∶90);检测波长270nm;流速:1.0mL/min;柱温:25℃。结果龙胆苦苷的线性范围是0.3554～5.331μg,r=0.9998,平均回收率是100.04%,RSD=1.80%。结论该法可同时测定龙胆泻肝丸中龙胆苦苷和栀子苷的含量。     

RP-HPLC法测定槐角丸中柚皮苷的含量

目的建立RP-HPLC法同时测定槐角丸中柚皮苷含量的方法。方法色谱柱:ZORBAX SB-C18柱,流动相:甲醇-1%冰醋酸(37.5∶62.5);检测波长283nm;柱温:35℃。结果柚皮苷进样量在0.1012～0.7591μg(r=0.99999)范围内线性关系良好;平均回收率为97.0%,RSD为0.62%。结论该方法简便、快速、准确,适用于槐角丸中柚皮苷的含量测定。     

高效液相色谱法测定丹参药材中丹参素的含量

目的:建立丹参药材中丹参素含量测定的方法.方法:色谱条件:色谱柱为C18柱,流动相为甲醇-0.5%冰醋酸水溶液(15:85),检测波长为280 nm.结果:其回归方程为Y=714 525.615 4X-274 34.826 6,r=0.999 9,丹参素在0.343～2.058μg范围内线性关系良好;重现性RSD为0.76%(n=5);平均回收率为97.95%,RSD为0.38%(n=5).结论:本方法灵敏、简便、准确可靠,可作为丹参药材中丹参素的含量测定标准.     

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.

     

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.     

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.     

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.     

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.