芪山无糖颗粒剂的提取工艺优化

摘 要 目的：研究芪山无糖颗粒的最佳提取工艺。方法: 应用L9（34）正交设计法对水提取工艺进行优选,以总黄酮、黄芩苷、盐酸小檗碱含量为指标,考察煎煮时间、煎煮次数、加水倍数对提取工艺的影响。结果: 最佳工艺条件为：加水量为10倍药材量,煎煮2次,每次1 h。结论: 优选出芪山无糖颗粒剂的最佳提取工艺,该工艺稳定可行,有效成分含量高。     

正交试验法优选三仁通便合剂提取工艺

摘 要 目的：优选三仁通便合剂的最佳提取工艺。方法: 以加水量、煎煮时间、煎煮次数为考察因素,以苦杏仁苷含量及出膏率为指标,采用L₉(3⁴)正交试验法,优选三仁通便合剂的最佳提取工艺。结果: 确定三仁通便合剂最佳提取工艺为：加水煎煮2次,每次8倍量水煎煮1.5 h。结论:本试验为三仁通便合剂的提取工艺提供了科学的试验数据支持,并通过验证性试验论证了该优选工艺的稳定可行。     

正交试验法优选芪葛颗粒的提取工艺

摘 要 目的：优化芪葛颗粒的提取工艺。方法: 建立芪葛颗粒中黄芪甲苷、葛根素2 种成分测定的HPLC 方法。采用 L9(34)正交设计,以黄芪甲苷、葛根素 2 种成分含量综合评分法进行数据分析,对芪葛颗粒的加水量、提取时间和提取次数3个因素进行优化。结果: 最佳提取工艺为：加入 12倍水,提取3次,每次 30 min。结论: 优选芪葛颗粒提取工艺能较好地保证制剂的质量。     

赤丹肝纤颗粒的醇提工艺研究

摘 要 目的： 优选赤丹肝纤颗粒的醇提最佳工艺。方法: 以虎杖苷含量为考察指标,先优选出最佳乙醇浓度,再采用L₉(3⁴)正交试验法,考察提取次数、提取时间及乙醇用量对提取效果的影响。结果: 最佳醇提工艺条件为以70%乙醇为溶媒回流提取2次,每次2 h,每次溶媒量为药材量的5倍。结论: 优选的工艺合理可行、重复性良好、提取效率高,适合于工业化生产。     

正交试验优化止咳平喘颗粒处方药材的乙醇提取工艺

目的 优选止咳平喘颗粒处方药材的提取工艺。方法 以麻黄碱、连翘酯苷A提取率为指标,以乙醇体积分数、乙醇倍量、提取时间、提取次数为因素,采用L₉(3⁴)正交试验对提取工艺进行优选。结果 最佳提取工艺条件为65%乙醇,回流提取2次,每次8倍量,每次1 h。结论 优选的止咳平喘颗粒处方药材提取工艺条件合理、可行。     

糖肝煎浓缩丸水提部分的提取工艺研究

摘 要 目的：优选糖肝煎浓缩丸水提部分的提取工艺参数。方法: 以芍药苷含量和浸膏得率作为评价指标, 芍药苷含量采用高效液相色谱法,色谱条件：色谱柱:WondaSil C₁₈柱(250 mm×4.6 mm,5 μm);流动相：乙腈-0.15%磷酸溶液(16∶84);流速：1.0 ml·min^-1;柱温:30℃;检测波长：230 nm。以加水量、煎煮时间和煎煮次数作为考察因素,采用正交设计法进行方差分析优选水提取工艺参数。 结果: 优选的提取工艺为加12倍量水,提取3次,每次1 h。结论:优选的提取工艺合理、稳定、可行,为糖肝煎浓缩丸提取工艺提供了试验依据。     

多指标综合评分法优选芩黄凝胶剂提取工艺

目的 优选芩黄凝胶剂的提取工艺。方法 以黄芩苷、芦荟大黄素、大黄酸、大黄素、大黄酚、大黄素甲醚的转移率为评价指标,采用L9（3⁴）正交法优选芩黄凝胶剂的水提取与醇提取工艺。结果 最佳水提取工艺为加6倍量水,浸泡0.5 h,回流提取2次,每次提取1.5 h;最佳醇提取工艺为加8倍量40%乙醇,回流提取3次,每次提取1.0 h。结论 采用多指标综合评分法优选的芩黄凝胶剂提取工艺合理、可行。     

升阳益胃颗粒的制备工艺研究

目的 优选升阳益胃颗粒的提取及成型工艺。方法 以甘草苷和芍药苷含量为指标,优选升阳益胃颗粒水提工艺并进行3次验证;以颗粒成品率和制粒可操作性为指标,优选润湿性和赋型剂,以160倍处方量投料中试生产3批产品。结果 升阳益胃颗粒提取工艺为水提3次,每次加8倍量水,煎煮30分钟;赋型剂为糖粉、糊精和可溶性淀粉,以低浓度乙醇制粒,颗粒剂成品率,甘草苷和芍药苷含量稳定。结论 优选的升阳益胃颗粒工艺稳定,可行。     

镇癫开窍颗粒提取工艺研究

目的 确定镇癫开窍颗粒的最佳提取工艺。方法 应用HPLC同时测定龙胆苦苷、芍药苷、黄芩苷的含量,并以含量测定的综合评分为考察指标,采用正交试验法L₉（3⁴）优选提取工艺条件。结果 对提取工艺的影响因素从大到小依次为提取次数、提取时间、乙醇浓度、加入溶媒量,最适工艺条件为8倍量的80%乙醇,浸泡30 min,提取3次,每次60 min。结论 该工艺稳定、可行。     

经舒宁颗粒提取纯化工艺优选

摘 要 目的:优选经舒宁颗粒的提取纯化工艺。方法: 以芍药苷的转移率和浸膏得率作为评价指标,采用正交试验对水提条件进行优选,以醇沉前后芍药苷的转移率和干膏量对醇沉条件进行考察。结果:优选出最佳的工艺条件是8倍量的水,提取3次,每次2.5 h,醇沉浓度为70%。结论:优选出的工艺稳定,可行,适合该制剂的批量生产。     

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.