高效液相色谱法测定醋酸曲安奈德含量

目的:建立高效液相色谱法测定强力皮炎灵中醋酸曲安奈德的含量.方法:以C18反相键合硅胶为固定相,甲醇-水(80:20)为流动相,流速1.0 mL·min-1,醋酸地塞米松为内标,检测波长为240 nm.结果:醋酸曲安奈德在3.0～60.0 mg·L-1浓度范围内呈良好线性关系,r=0.999 9,方法平均回收率为99.7%,RSD为0.4%(n=6).结论:该方法测定醋酸曲安奈德的含量简便快捷,适于医院制剂的含量测定.     

反相高效液相色谱法测定复方醋酸曲安奈德溶液中醋酸曲安奈德和氯霉素含量

目的 :建立同时测定复方醋酸曲安奈德溶液中醋酸曲安奈德和氯霉素的方法。方法 :采用反相高效液相色谱法 ,以Shim packvp ODS(5 μm ,4.6mm× 15 0mm)为色谱柱 ,甲醇 水 乙醚 (6 2∶38∶4)为流动相 ,检测波长 2 40nm ,峰面积外标法定量。结果 :平均回收率 :醋酸曲安奈德为 99.5 % ,RSD 0 .8% (n =7) ;氯霉素为 99.2 % ,RSD 0 .7% (n =7)。结论 :方法简便 ,快速 ,准确可靠 ,适于该制剂的含量测定。     

高效液相色谱法测定复方醋酸曲安奈德软膏中2组分的含量

目的:建立用高效液相色谱法测定复方醋酸曲安奈德软膏含量的方法.方法:采用高效液相色谱法.色谱柱为ODS-C18,流动相为甲醇-水-乙醚(50∶50∶2),流速为1.0 mL·min-1,检测波长为240 nm.结果:可同时测定2组分的含量.醋酸曲安奈德在0.002 5～0.125 g·L-1、氯霉素在0.05～2.5 g·L-1范围内峰面积与其浓度呈良好线性关系,平均回收率依次为99.8%(RSD=0.8%)、99.4%(RSD=0.8%).结论:高效液相色谱法可简便、快速、准确地同时测定复方醋酸曲安奈德软膏中2组分的含量.     

高效液相色谱法测定醋酸曲安奈德注射液中醋酸曲安奈德含量

目的建立醋酸曲安奈德注射液中醋酸曲安奈德含量测定的方法。方法采用高效液相色谱法,流动相为甲醇-水（70：30）,流动速度为1.0ml/min,检测波长为240nm。结果醋酸曲安奈德的线性范围为0.0064～0.128mg/ml,线性方程：y=1.8683×10^-6＋5.3174x（r=0.999976,n=7）,回收率99.9%,RSD为0.36%（n=9）。结论采用高效液相色谱法测定醋酸曲安奈德注射液中醋酸曲安奈德含量的方法具有简便、准确、重现性好等优点,可作为该制剂的质量控制方法。     

高效毛细管电泳法测定复方氯霉素洗剂中醋酸曲安奈德和氯霉素的含量

目的建立同时测定复方氯霉素洗剂中醋酸曲安奈德和氯霉素的方法.方法采用高效毛细管电泳法,以100 mmol/L硼砂溶液(用稀磷酸溶液调节至pH 7.0)为运行缓冲液.运行缓冲液的溶媒为水-甲醇(7∶3).稀释样品的缓冲液为0.5% 硼砂的醇(7∶3)溶液.分离电压为23 kV;检测波长为254 nm;工作温度为25℃;高气压进样4秒.测定氯霉素时以头孢拉定作为内标物,测定醋酸曲安奈德时以已知含量的氯霉素作为内标物.未涂渍毛细管47 cm×75 μm i.d.,有效长度为40 cm.结果平均回收率醋酸曲安奈德为99.4%,RSD 1.2%(n=6);氯霉素为99.7%,RSD 1.5%(n=6).结论本法分离效率高,结果比较准确,与高效液相色谱法相比结果无显著性差异.为同时测定醋酸曲安奈德和氯霉素含量的又一种方法.     

RP-HPLC法同时测定复方曲安奈德乳膏中醋酸曲安奈德和盐酸苯海拉明的含量

目的:建立同时测定复方曲安奈德乳膏中醋酸曲安奈德和盐酸苯海拉明含量的方法。方法:采用反相高效液相色谱法。色谱柱为SunFireC18,流动相为甲醇-水(含三乙胺,磷酸调pH为7.2)(70:30,V/V),流速为1.0ml/min,检测波长为230nm,柱温为30℃。结果:醋酸曲安奈德和盐酸苯海拉明检测质量浓度线性范围分别为0.008～0.048mg/m(lr=0.9990)、0.0484～0.2904mg/m(lr=0.9999);平均回收率分别为99.0%(RSD=1.1%,n=9)、98.8%(RSD=1.6%,n=9)。结论:该方法简便、快速、准确,可用于复方曲安奈德乳膏的质量控制。     

高效液相色谱法测定复方醋酸曲安奈德溶液中醋酸曲安奈德含量

目的建立测定复方醋酸曲安奈德溶液中醋酸曲安奈德含量的高效液相色谱法。方法采用DiamonsilTM C18柱（200mm×4.6mm,5μm）,流动相为乙腈-水（60：40）,检测波长240nm,流速1.0mL/min,柱温30℃,进样量10μL。结果醋酸曲安奈德进样量在5.88～15.68μg范围内与峰面积线性关系良好,r=0.9999（n=6）,平均回收率为100.43%,RSD为0.28%（n=9）。结论高效液相色谱法测定复方醋酸曲安奈德溶液中醋酸曲安奈德含量简便、准确、重现性好,能满足医院制剂质量标准的要求。     

HPLC法测定醋酸曲安奈德尿素乳膏中醋酸曲安奈德的含量

目的:建立高效液相色谱法测定醋酸曲安奈德尿素乳膏中醋酸曲安奈德的含量。方法:采用 Shim-pack C_(18)色谱柱(4.6mm×250mm,5μm);以甲醇-水(75:25)为流动相;流速1.0mL·min~(-1);检测波长为240nm;柱温:室温。结果:醋酸曲安奈德线性范围为15.23～35.55μg·mL~(-1)(r=0.9999),平均回收率为99.8%,RSD 为0.77%(n=6)。结论:本方法简便、灵敏、准确,能有效地控制醋酸曲安奈德尿素乳膏的质量。     

高效液相色谱法测定复方醋酸曲安奈德乳膏中醋酸曲安奈德和氯霉素的含量

目的建立HPLC法同时测定复方醋酸曲安奈德乳膏中醋酸曲安奈德和氯霉素的含量。方法用Hypersil CN(200mm×4.6mm,5μm)色谱柱,以水-甲醇-四氢呋喃(60∶28∶12)为流动相,检测波长为240nm。结果醋酸曲安奈德和氯霉素的平均回收率分别为101.0%(RSD为1.23%)和100.1%(RSD为1.40%);其浓度分别在5.02~100.40μg/mL(r=0.9999,n=5)及99.73~1994.50μg/mL(r=0.9998,n=5)范围内线性关系良好。结论该方法准确可靠,可用于复方醋酸曲安奈德乳膏中醋酸曲安奈德和氯霉素的含量测定。     

HPLC法测定乳膏中联苯苄唑和醋酸曲安奈德的含量

目的:建立高效液相色谱法同时测定乳膏中联苯苄唑和醋酸曲安奈德的含量。方法:采用BDSC18色谱柱(200 mm×4.6 mm,5μm),以pH 7.4值磷酸盐缓冲液-乙腈-甲醇(25∶15∶60)为流动相,酮康唑为内标,检测波长为240 nm。结果:醋酸曲安奈德的线性范围是0.976~7.808μg.mL-1,r=0.9998,加样回收率为99.6%,RSD为0.71%(n=9);联苯芐唑的线性范围是10.08~80.64μg.mL-1,r=0.9999,加样加收率为99.9%,RSD为0.69%(n=9)。结论:本法简便、准确,可用于联苯苄唑醋酸曲安奈德乳膏的含量测定。     

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.

---

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.