石淋通片喷雾干燥工艺研究

目的优选石淋通片喷雾干燥的最佳工艺条件。方法应用正交试验法，以浸膏粉的含水量为评价指标，考察影响石淋通片喷雾干燥过程的因素。结果影响喷雾干燥过程中的4个因素中，进风温度影响最大，出风温度次之，药液相对密度影响较小。结论石淋通片的最佳喷雾干燥工艺为进风温度220℃、进料泵流量900r／min、出风温度100℃、药液相对密度1．15。     

正交试验法优选鲜益母草提取工艺

目的 优选鲜益母草的提取工艺。 方法采用正交试验法，考察提取过程中真空浓缩后药液相对密度、循环水加热温度及喷雾干燥器进风温度等3个因素对鲜益母草提取工艺的影响。结果最佳提取工艺为鲜益母草榨汁、过滤、滤液真空浓缩，浓缩后药液相对密度为1.04，加热温度为60 ℃，进行喷雾干燥，进风温度为175 ℃，得喷干粉。结论该优选工艺稳定可行。     

安神胶囊喷雾干燥工艺的研究

目的优选安神胶囊提取液的喷雾干燥的最佳工艺参数.方法以喷雾干燥成品的水分作为指标,对进风温度、排风温度以及药液的相对密度进行考察.结果正交实验法设计的三个因素中,进风温度与浸膏的相对密度对成品的水分影响较显著.结论综合成品的收率与水分,最佳的喷雾干燥工艺为:进风温度160℃,排风温度75℃,浸膏的相对密度1.10 g/ml(60℃热测),其成品的收率为96.2%,水分为3.46%.     

黄芪多糖喷雾干燥工艺研究

目的 优选黄芪多糖喷雾干燥的最佳工艺条件。方法 应用正交试验法，以每小时药粉产量为考察指标，对影响黄芪多糖喷雾干燥过程的因素进行考察。结果 正交试验法设计的4个因素中，清膏的相对密度影响显著，进风温度和出风温度的影响较显著，进风压力影响较小。结论 最佳工艺条件为清膏相对密度1．10、进风温度140℃、出风温度70℃、进风压力40MPa。     

喷雾干燥与沸腾造粒法制备热咳停颗粒

目的研究热咳停颗粒剂的喷雾干燥条件与成型工艺。方法通过考察影响干燥与成型的单个因素，包括物料相对密度、入塔风压、进出风温度、辅料种类与用量、制粒工艺等，确定最佳喷雾干燥条件及成型工艺。结果喷雾干燥工艺参数为60 ℃下药液相对密度为1.10，入塔风压为－1 700 Pa，进风温度为160～170 ℃，出风温度为70～80 ℃，干浸膏粉与糊精比例为8∶3，浸膏相对密度为1.10(60 ℃)，沸腾制粒浸膏与喷雾干燥浸膏比例为1∶2；沸腾造粒参数为进液速度50～55 mL·min^-1，喷雾压力0.37 MPa，物料温度为55～60 ℃，进风温度78～88 ℃，出风温度40～45 ℃，室内温度20 ℃，相对湿度50%时成型最好。结论该喷雾干燥条件与成型工艺合理、可行，可用于热咳停颗粒剂的制备。     

盐酸二甲双胍流化床制粒工艺的影响因素研究

摘 要 目的：研究流化床制粒工艺参数对盐酸二甲双胍颗粒物理性质的影响。方法: 以盐酸二甲双胍颗粒物理性质作为评价指标,采用单因素试验法分别考察了流化床制粒过程中的设备因素（喷枪高度、喷枪孔径）和工艺参数（黏合剂用量、进风温度、进风速度、进液速度、雾化压力）对其产生的影响。结果: 设备因素中喷枪高度、喷枪孔径对颗粒物理性质影响较小,工艺参数中黏合剂用量、进风温度、进风速度、进液速度、雾化压力对颗粒物理性质影响均较大。结论: 流化床制粒工艺中黏合剂用量、进风温度、进风速度、进液速度、雾化压力对盐酸二甲双胍颗粒会产生较大影响,可按照颗粒性质要求进行控制。     

流化床喷雾制粒在枫蓼肠胃康无糖颗粒制备中的应用

目的研究流化床制粒设备在中药无糖颗粒制备中的应用.方法采用正交试验法,选定进风温度、喷入浸膏的相对密度、喷浆速度、进风量为考察因素,每个因素取3个水平,筛选枫蓼肠胃康无糖颗粒流化床制粒的最佳工艺.结果最佳工艺条件为浸膏的相对密度1.25,进风温度80℃,喷入速度40 mL·min-1,进风量为1 400 m3·h-1.结论本方法生产工艺简单,自动化程度更高,是中药制剂现代化生产的一条良好途径.     

苦参提取纯化浓缩液喷雾干燥工艺优化

摘 要 目的： 优选苦参水提纯化浓缩液喷雾干燥最佳工艺参数。方法: 采用L9(34)正交设计试验法,以浸膏粉重量及苦参碱和氧化苦参碱两者含量之和为评价指标,通过考察药液浓缩密度、进风温度、泵药速度等对苦参提取纯化浓缩液喷雾干燥工艺条件的影响。结果: 最佳喷雾干燥工艺条件为：药液密度1.07,进风温度120℃,泵药速度4 r·min^-1。结论: 该优选工艺科学、合理、稳定、可行,可为苦参提取纯化浓缩液的喷雾干燥工业化生产提供试验依据。     

清热感冒颗粒流化床制粒工艺研究

目的 探索研究清热感冒颗粒流化床制粒的最佳工艺.方法 采用正交试验法,以制粒收得率和颗粒水分为指标,探索清热感冒颗粒流化床制粒的最佳工艺条件.结果 清热感冒颗粒流化床制粒的最佳工艺条件为:进风量2000m3/h,进风温度78℃、进液速度20rpm.结论 本试验为清热感冒颗粒的工艺改进提供了依据.     

正交试验法优选胃乐舒颗粒喷雾干燥工艺

目的：研究胃乐舒颗粒最佳喷雾干燥工艺,为其质量稳定提供保证.方法：以延胡索乙素含量、干粉收率、含水率为考察指标,采用正交试验方法主要考察进风温度、浸膏比重、供液速度三个因素对干燥效果影响.结果：优选的最佳干燥工艺条件为进风温度145℃、浸膏比重1.10、供液速度25 ml·rmin-.结论：优选的最佳工艺条件合理、重复性好、稳定可靠,可做为胃乐舒颗粒的干燥条件,为其制剂的干燥工艺改进提供依据.     

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.