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。     

复方颠茄合剂质量标准研究

目的 提高复方颠茄合剂的质量控制标准。方法 采用薄层色谱法（TLC）对复方颠茄合剂中的吗啡进行定性鉴别;采用高效液相色谱法（HPLC）测定复方颠茄合剂中吗啡的含量。以WondaSil C₁₈（4.6 mm×150 mm,5 μm）为色谱柱;A相：0.01 mol/L磷酸二氢钾溶液-0.002 5 mol/L庚烷磺酸钠溶液（含0.1%三乙胺,磷酸调pH至2.5）,B相：乙腈,A∶B=90∶10为流动相;流速：1.0 ml/min;检测波长：220 nm;柱温：30 ℃。结果 在TLC图谱中可检出吗啡的特征斑点。吗啡在0.525~10.5 μg/ml范围内与其峰面积线性关系良好（r=0.999 9）,平均回收率为99.44%,RSD= 0.23%（n=9）。结论 本方法简便准确,专属性强,能够用于复方颠茄合剂的含量测定和质量控制。     

康咳灵合剂质量标准研究

目的 建立康咳灵合剂的质量标准。方法 采用薄层色谱法（TLC）对矮地茶、百部进行定性鉴别;采用高效液相色谱法（HPLC）测定岩白菜素的含量。色谱柱为Lichrospher C₁₈柱（4.6 mm×250 mm,5 μm）;流动相：甲醇-水（20：80）;检测波长：275 nm;柱温：30℃;流速：1 ml/min。结果 TLC法能准确鉴别矮地茶和百部,斑点清晰;岩白菜素在0.064 8~0.648 μg（r=0.9998）范围内线性关系良好,平均回收率100.24%（RSD为1.9%,n=6）。结论 本实验建立的方法简便、专属性高、重复性好,结果准确可靠,可用于康咳灵合剂的质量控制。     

SPE-HPLC测定风湿骨痛片中6种生物碱类物质的含量

目的 建立SPE-HPLC同时检测风湿骨痛片中6种生物碱类物质含量的方法。方法 采用Welch XB-C₁₈（4.6 mm×250 mm,5 μm）色谱柱,以含乙腈-四氢呋喃（25：15）溶液为流动相A,以0.05%醋酸铵溶液为流动相B进行梯度洗脱,流速为1.0 mL·min^-1,检测波长为235 nm,柱温为30℃,进样量为10 μL。结果 6种生物碱在优化条件下均可有效分离,苯甲酰新乌头原碱、苯甲酰乌头原碱、苯甲酰次乌头原碱、新乌头碱、次乌头碱和乌头碱分别在162.4~8 121 ng（r=1.000 0）、24.96~1 248 ng（r=1.000 0）、58.03~2 902 ng（r=1.000 0）、17.26~863.0 ng（r=1.000 0）、20.16~1 008 ng（r=1.000 0）和19.90~995.0 ng（r=1.000 0）内有良好的线性关系,平均回收率为88%~98%,RSD为1.8%~2.4%。结论 该方法准确、可靠,适用于风湿骨痛片中生物碱类物质含量的分析。     

藏药六味木香丸的定性定量检测方法研究

目的： 建立藏药六味木香丸的定性定量检测方法,为质量标准修订提供参考。方法：采用TLC法对藏药六味木香丸中木香、石榴子、余甘子和荜茇进行定性鉴别;采用HPLC法测定藏药六味木香丸中木香烃内酯和去氢木香烃内酯的含量,使用C18（4.6 mm×250 mm,5 μm）色谱柱,以乙腈-水（65∶35）为流动相,流速1.0 mL·min^-1,检测波长225 nm,柱温25℃。结果：薄层色谱斑点清晰,分离度良好,阴性样品无干扰。木香烃内酯质量浓度在12~60 μg·mL^-1范围内线性关系良好（r=0.9997）,平均回收率（n=6）为98.8%,RSD=1.6%;去氢木香烃内酯质量浓度在17~85 μg·mL^-1范围内线性关系良好（r=0.9996）,平均回收率（n=6）为99.8%,RSD=1.4%。结论：所建立的方法准确、可靠,专属性强,可用于六味木香丸的质量控制。     

气相色谱法测定清肠栓中樟脑残留量和冰片含量

目的 建立清肠栓中樟脑残留物和冰片含量的气相测定方法。方法 采用气相色谱法,色谱柱为Agilent毛细管柱（30 m×0.25 mm×0.25 μm）,柱温为140 ℃,进样口温度250 ℃,检测器（FID）温度为250 ℃。结果 樟脑、龙脑和异龙脑在0.0299~1.497μg（r=1.000）、0.0205~1.025μg（r=1.000）、0.0097~0.4830 μg（r=1.000）范围内呈现良好的线性关系。精密度、稳定性、重复性试验结果的RSD均小于2%,平均加样回收率分别为99.7%、101.0%、102.5%。结论 该方法准确、可靠、简便快速,可用于清肠栓中龙脑含量的测定。     

芥辛化痰通窍巴布剂的质量标准研究

目的 建立芥辛化痰通窍巴布剂的质量标准。方法 对芥辛化痰通窍巴布剂中白芥子、延胡索、甘遂和细辛采用TLC定性鉴别;采用HPLC对芥子碱硫氰酸盐、延胡索乙素和细辛脂素进行定量测定。结果 薄层色谱法鉴别斑点清晰,分离度好,阴性无干扰;芥子碱硫氰酸盐在20.2~202.0 μg·mL^-1（r=0.999 4）、延胡索乙素在1.312~20.992 μg·mL^-1（r=0.999 7）和细辛脂素在1.925~38.500 μg·mL^-1（r=0.999 4）内与峰面积的线性关系良好;芥子碱硫氰酸盐的平均回收率为99.06%,RSD=2.20%;延胡索乙素的平均回收率为98.66%,RSD=2.35%;细辛脂素的平均回收率为99.75%,RSD=1.74%。结论 该法简便、准确、重复性好,可用于芥辛化痰通窍巴布剂的质量控制。     

芪黄扶正颗粒的质量控制方法研究

目的 建立芪黄扶正颗粒的质量控制方法。方法 采用TLC法对方中黄芪、熟地黄、山茱萸、当归、川芎、赤芍、牡丹皮、麦门冬进行定性鉴别;采用HPLC法对臣药山茱萸中马钱苷进行含量测定。结果 建立了主要药味的TLC鉴别方法,斑点清晰,阴性无干扰;马钱苷在4.02~80.40 μg/ml范围内线性关系良好（r=0.999 9）,平均加样回收率为99.02%,RSD为0.64%（n=9）。结论 本研究建立的质量控制方法准确、可靠、专属性强,为芪黄扶正颗粒的质量控制奠定了基础。     

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。     

乌芪舒筋通络片质量标准的研究

目的 建立乌芪舒筋通络片的质量控制方法。方法 用薄层色谱法鉴定方中续断、黄芪、防已、牛膝,用高效液相色谱法测定方中细辛的细辛脂素含量。结果 续断、黄芪、防已、牛膝的薄层色谱法鉴别专属性强,阴性无干扰;细辛脂素在46.05~460.5 ng（r=1.000）内呈良好的线性关系,平均加样回收率为100.4%（n=9）,RSD为1.86%。结论 本方法简便,专属性强,重复性好,可作为乌芪舒筋通络片的质量标准。     

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.     

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.