医院制剂感冒颗粒质量标准研究

目的 建立医院制剂感冒颗粒的质量标准。方法 采用薄层色谱法（TLC）对黄芩、黄柏、柴胡进行薄层鉴别;采用高效液相色谱法（HPLC）测定黄芩苷的含量,色谱柱为Agilent HC-C₁₈（250 mm×4.6 mm,5 μm）,流动相为甲醇-0.2%磷酸（43：57）,流速为1.0 ml/min,柱温30℃,检测波长为280 nm。结果 黄芩、黄柏、柴胡的薄层色谱图均斑点清晰,阴性无干扰;黄芩苷在1.81~72.40 μg/ml范围内浓度与峰面积线性关系良好（r=0.999 9）,平均回收率为98.55%,RSD为1.91%（n=9）。结论 本研究建立的鉴别方法重现性更好,确定了黄芩苷的含量测定方法,增强了该制剂质量的可控性。     

健脾补肾颗粒的质量标准研究

目的 建立健脾补肾颗粒的质量标准。方法 采用薄层色谱法（TLC）鉴别制剂中黄芪、丹参、党参、陈皮和白芍五味药材。用高效液相色谱法（HPLC）测定白芍中芍药苷的含量：色谱柱：Agilent Eclipse Plus C₁₈柱（4.6 mm×250 mm,5 μm）;流动相：乙腈-0.1%磷酸水溶液梯度洗脱;流速：1.0 ml/min;柱温：25℃;检测波长：230 nm。结果 5种药材的TLC图谱斑点清晰,无阴性对照干扰;芍药苷在8.676~277.632 μg/ml范围内线性关系良好,（r=0.999 9）。结论 该法操作简单、重复性好,能够有效控制健脾补肾颗粒的质量。     

复方黑参颗粒质量标准研究

目的 建立复方黑参颗粒的质量标准。方法 采用TLC法对复方黑参颗粒中玄参和射干进行定性鉴别,应用HPLC法同时测定肉桂酸、射干苷和次野鸢尾黄素的含量,色谱柱为Kromasil C₁₈柱（150 mm×4.6 mm,5 μm）,流动相为乙腈（A）-0.1%磷酸（B）水溶液,进行梯度洗脱;柱温30℃,检测波长270 nm;流速1.0 ml/min。结果 采用TLC法对玄参和射干进行定性鉴别具有良好的专属性,阴性对照无干扰。肉桂酸、射干苷、次野鸢尾黄素分别在16.22~113.57 μg/ml（r=0.999 8）、48.19~337.34 μg/ml（r=0.999 8）、16.40~114.80 μg/ml（r=0.999 9）范围内与峰面积呈良好的线性关系,平均加样回收率分别为99.23%、98.82%、99.17%。结论 本实验建立的方法快速、简便、重复性好,可用于复方黑参颗粒的质量标准控制。     

复方生化颗粒的定性鉴别和含量测定研究

目的 提高复方生化颗粒的质量标准。方法 采用薄层色谱（TLC）法对处方中的甘草、丹参进行定性鉴别;采用高效液相色谱（HPLC）法鉴别苦杏仁苷;采用HPLC法测定处方中的丹酚酸B含量,色谱柱为Agilent HC-C₁₈（4.6 mm×250 mm,5 μm）,流动相为乙腈-0.1%磷酸（23：77）,流速为1.0 ml/min,检测波长为286 nm,柱温为30 ℃。结果 TLC斑点清晰,分离度较好,专属性强,阴性对照无干扰;HPLC法定性鉴别更加准确、可靠与客观;丹酚酸B在1.56~49.92 μg/ml范围内浓度与峰面积呈良好的线性关系（r=0.999 9）,平均回收率为100.07%,RSD为1.61%（n=9）。结论 建立的方法准确、可靠,重复性好,可用于复方生化颗粒的质量控制。     

乌金胶囊的质量标准研究

目的 建立乌金胶囊的质量控制方法。方法 采用薄层色谱（TLC）法对乌金胶囊中的臣药郁金和使药山楂进行定性鉴别;采用高效液相色谱-蒸发光散射检测（HPLC-ELSD）法测定乌金胶囊中通关藤苷H的含量,色谱柱：Waters Xbridge C₁₈柱（100 mm×3.0 mm,3.5 μm）,柱温：35 ℃,流动相为水-乙腈（50：50）,等度洗脱;流速为0.8 ml/min;采用ELSD检测器进行检测,蒸发器温度：35 ℃,雾化器温度：60 ℃,氮气流速：1.50 L/min,运行时间：5 min。结果 TLC法鉴别郁金、山楂,色谱斑点清晰,阴性样品无干扰;通关藤苷H出峰时间为2.98 min,且在11.60~580.00 μg/ml范围内线性关系良好（r=0.999 0）,加样回收率为101.54%。结论 本实验建立的TLC法鉴别郁金、山楂,操作步骤简单;建立的HPLC-ELSD联用方法专属性强,灵敏度高,重复性好,可作为乌金胶囊质量控制的方法。     

虎杖饮片指纹图谱的研究及其耐用性考察

目的 为用数据识别虎杖饮片的真伪及评价其质量提供技术支持。方法 采用高效液相色谱(HPLC)法分析虎杖饮片提取物的指纹图谱,色谱柱:Agilent ZORBAX SB-C₁₈柱(4.6 mm×250 mm,5μm);流动相:0.1%甲酸水溶液-乙腈(A-B);梯度洗脱;检测波长306 nm;流速1ml/min;柱温30℃;进样量20μl。结果 成功分离出虎杖饮片提取液中的虎杖苷、白藜芦醇、大黄素、大黄素甲醚等有效成分。结论 该方法稳定有效,具有良好的耐用性,对虎杖饮片的数据识别具有指导意义。     

桃红通脉颗粒质量标准提高研究

目的 提高桃红通脉颗粒的质量标准。方法 采用薄层色谱（TLC）法对赤芍、地黄、甘草进行薄层鉴别,以及采用高效液相色谱法对主药桃仁的有效成分苦杏仁苷进行鉴别;采用高效液相色谱法测定芍药苷的含量,色谱柱为Agilent HC-C₁₈柱（250 mm×4.6 mm,5 μm）,流动相为乙腈-水（13：87）,流速为1.0 ml/min,柱温为30℃,检测波长为230 nm。结果 赤芍、地黄、甘草的TLC图均斑点清晰,阴性无干扰;芍药苷在1.79~57.28 μg/ml范围内浓度与峰面积线性关系良好（r=0.999 9）,平均回收率为99.99%,RSD为2.05%（n=9）。结论 提高桃红通脉颗粒质量标准后,鉴别方法重现性更好,优化了芍药苷的含量测定方法,增强了成品质量的可控性。     

高效液相色谱法测定鼻炎灵胶囊中黄芩苷含量

目的 建立高效液相色谱法测定鼻炎灵胶囊中黄芩苷的含量。方法 色谱柱为Waters XBridge C₁₈柱（4.6 mm×250 mm,5 μm）,流动相为乙腈-0.8%甲酸（25：75）,检测波长276 nm,流速1.0 ml/min,柱温30℃,进样量10 μl。结果 黄芩苷在1.25~40 μg/ml范围内（r=0.999 9）呈良好的线性关系,精密度实验中RSD均小于2%,加样回收率在95%~100%之间。结论 该测定方法简便、准确,分离效果好,可用于鼻炎灵胶囊的质量控制。     

益视明目颗粒质量标准研究

目的 建立益视明目颗粒的质量标准。方法 用薄层色谱法（TLC）鉴别制剂中的枸杞子、丹参;用高效液相色谱法（HPLC）定量测定丹参素钠的含量。色谱柱：Kromasil C₁₈柱（4.6 mm×150 mm,5 μm）;流速：0.4 ml/min;检测波长：280 nm;柱温：30 ℃;进样量：10 μl;流动相：甲醇-0.5%醋酸水溶液（10∶90）。结果 薄层色谱斑点清晰可见、阴性干扰小,可用于鉴别益视明目颗粒中的枸杞、丹参;丹参素钠在2.00~60.00 μg/ml范围内线性关系良好,r=0.999 7（n=6）,平均加样回收率105.6%,RSD=1.60%。结论 建立的方法简便、准确、可靠性高、重现性好,可作为控制益视明目颗粒质量的有效方法。     

三藤口服液的质量标准研究

目的 建立三藤口服液的质量标准。方法 采用薄层色谱法鉴别处方中的大血藤和鸡血藤,采用HPLC法测定绿原酸的含量,色谱柱为Agilent Zorbax SB-C₁₈柱（4.6 mm×250 mm,5 μm）;流动相为乙腈-水（0.1%甲酸）（9∶91,v/v）等度洗脱;流速：1.0 ml/min;柱温：30 ℃;检测波长：330 nm;进样量：20 μl。结果 薄层鉴别色谱中特征斑点明显,专属性强。绿原酸在2.70~202.50 μg/ml浓度范围内线性关系良好,其回归方程为Y = 60.14X－6.37（r>0.999 9）。结论 该法简便、稳定可靠、重复性好,能够较好地控制三藤口服液的质量。     

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.     

Nachweis einiger Heilmittel in der Kniegelenksynovialflüssigkeit

Zusammenfassung Mittels Gaschromatographie und Dünschichtchromatographie wiesen die Autoren 11 Substanzen nach, welche durch Injektion oder nach Verabreichung per os in die Kniegelenksynovialflüssigkeit eindrangen. In ihrer Aufstellung konnten sie eine direkte Beziehung zwischen Struktur sowie chemischphysikalischen Eigenschaften der Substanz und ihrer Fähigkeit, aus dem Blut in die Kniegelenksynovialflüssigkeit einzudringen, nicht nachweisen, außer der Tatsache, daß Substanzen mit starker Affinität zu Eiweißstoffen erst in höheren Dosen nachweisbar waren.     

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.     

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.     

Biochemical and molecular characterisation of cubozoan protein toxins

Class Cubozoa includes several species of box jellyfish that are harmful to humans. The venoms of box jellyfish are stored and discharged by nematocysts and contain a variety of bioactive proteins that are cytolytic, cytotoxic, inflammatory or lethal. Although cubozoan venoms generally share similar biological activities, the diverse range and severity of effects caused by different species indicate that their venoms vary in protein composition, activity and potency. To date, few individual venom proteins have been thoroughly characterised, however, accumulating evidence suggests that cubozoan jellyfish produce at least one group of homologous bioactive proteins that are labile, basic, haemolytic and similar in molecular mass (42-46 kDa). The novel box jellyfish toxins are also potentially lethal and the cause of cutaneous pain, inflammation and necrosis, similar to that observed in envenomed humans. Secondary structure analysis and remote protein homology predictions suggest that the box jellyfish toxins may act as α-pore-forming toxins. However, more research is required to elucidate their structures and investigate their mechanism(s) of action. The biological, biochemical and molecular characteristics of cubozoan venoms and their bioactive protein components are reviewed, with particular focus on cubozoan cytolysins and the newly emerging family of box jellyfish toxins.     

Dose tolerability of chronically inhaled voriconazole solution in rodents

Invasive pulmonary aspergillosis (IPA) is a fungal disease of the lung associated with high mortality rates in immunosuppressed patients despite treatment. Targeted drug delivery of aqueous voriconazole solutions has been shown in previous studies to produce high tissue and plasma drug concentrations as well as improved survival in a murine model of IPA. In the present study, rats were exposed to 20 min nebulizations of normal saline (control group) or aerosolized aqueous solutions of voriconazole at 15.625 mg (low dose group) or 31.25 mg (high dose group). Peak voriconazole concentrations in rat lung tissue and plasma after 3 days of twice daily dosing in the high dose group were 0.85 ± 0.63 μg/g wet lung weight and 0.58 ± 0.30 μg/mL, with low dose group lung and plasma concentrations of 0.38 ± 0.01 μg/g wet lung weight and 0.09 ± 0.06 μg/mL, respectively. Trough plasma concentrations were low but demonstrated some drug accumulation over 21 days of inhaled voriconazole administered twice daily. Following multiple inhaled doses, statistically significant but clinically irrelevant abnormalities in laboratory values were observed. Histopathology also revealed an increase in the number of alveolar macrophages but without inflammation or ulceration of the airway, interstitial changes, or edema. Inhaled voriconazole was well tolerated in a rat model of drug inhalation.