阿霉素聚乳酸微球的含量测定

阿霉素（ADM）的含量测定方法国内已报道有很多种,如荧光分光光度法测定明胶磁性微球中阿霉素的含量,紫外分光光度法测定阿霉素磁性明胶微球的含量,反相高效液相色谱一荧光检测法测定阿霉素磁性豪微球等啊。本实验用溶解法将聚乳酸的网状结构破坏后,再采用紫外一可见分光光度法测定聚乳酸微球中阿霉素的含量。该方法快速、准确、结果满意。     

氨甲喋呤铁磁性微球的制备及物理性质测定

目的：制备氨甲喋呤铁磁性微球，探讨工艺条件对成球的影响，并测定微球的粒径，磁性物质和药物的含量以及药物释放度等主要物理性质。方法；以人血白蛋白作载体，磁铁粉作磁响应物质用加热固化法制备抗肿瘤药物ＭＴＸ的磁性微球，显微镜下观察微球形态大小，计算粒径分布，重量法测定磁性物质的含量，紫外分光光度法测定ＭＴＸ含量及体外释放度。     

磁性靶向紫杉醇微球制备的初步研究

目的：制备磁性靶向紫杉醇微球.方法：以紫杉醇和纳米Fe3O4为材料制备出磁性靶向紫杉醇微球,并利用高分辨透射电子显微镜（HRTEM）观察微球的形貌,同时采用紫外可见分光光度法测定微球的载药量和包封率.结果：磁性靶向紫杉醇微球的载药量为3.013%,包封率为35.26%.结论：通过实验研究制备了磁性紫杉醇微球,具有靶向定位功能,形成一种磁靶向给药系统.     

复方阿霉素磁性白蛋白微球的制备及含量测定

目的：将阿霉素与维拉帕米（ＶＰＭ）制成复方磁性微球制剂以抑制阿霉素耐药性的产生和降低其不良反应。方法：实验采用加热固化制备复方磁性白蛋白微球,用充体法蛊磁粉以紫外和双波长分光光度法分别测定维拉帕米和阿霉素的含量。结果：微球粒径较均匀,收率为７８％,制剂中阿素ＶＰＭ含量分别为０．１５％,１５％。结论：微球的制备及呈测定方法均简单可行。     

紫外分光光度法测定胰岛素注射液的含量

胰岛素是治疗糖尿病的重要药物,胰岛素制剂的含量测定一直都采用生物测定法。近年来又发展了高效液相色谱法、放射免疫法和酶免疫法等。但这些方法往往受到某些条件的限制。紫外分光光度法是药物制剂含量测定中常用的方法之一,Shan-Yang Lin曾用紫外分光光度法在波长220nm处测定了胰岛素——聚乳酸微球和乙基纤维素微球中胰岛素的含量。本试验探索了用紫外分光光度法来测定胰岛素及其注射液含量的方法。     

多柔比星磁性葡聚糖微球的制备及特性检测

目的:制备多柔比星磁性葡聚糖微球并检测其特性。方法:采用吸附法制备多柔比星磁性葡聚糖微球。高倍显微镜观察微球粒径大小及形态,紫外分光光度法检测微球中多柔比星的含量,测定微球磁吸附率,计算求和值 S,确定最佳投料比(药物:载体),绘制药物微球体外释放曲线。结果:制备的多柔比星磁性葡聚糖微球最佳投料比为1:15,磁吸附率为100%。微球外形圆整,分散性好。多柔比星30 min 释放28%;60min 释放45%;6h 释放65%。结论:制备的多柔比星磁性葡聚糖微球缓释性好,磁响应性强,可作为一种治疗顽固性疼痛的靶向神经损毁剂。     

亚甲蓝磁性明胶微球的制备及特性试验

目的：制备亚甲蓝磁性明胶微球并检测其特性。方法：采用乳化-交联法制备亚甲蓝磁性明胶微球，高倍镜观察微球粒径大小及形态，紫外-可见分光光度法检测微球中亚甲蓝的含量及其体外释放规律。结果：亚甲蓝磁性明胶微球粒径38—50μm，在4000GS的磁场下动作距离为70—80mm，载药量为9．8％，180min体外累积释放量为90％。结论：亚甲蓝磁性明胶微球是一种新剂型，制备工艺简便，具有较好的磁响应性和一定缓释性。     

庆大霉素聚氰基丙烯酸丁酯毫微球冻干注射剂的制备及其特性

用乳化聚合法制备庆大霉素聚氰基丙烯酸丁酯毫微球，经冷冻干燥制成冻干型注射剂。用一阶导数分光光度法测定药物的结合率和载药量；以浊度作为评价冻干毫微球重分散性能的指标，筛选配方和工艺；用透射电镜测定了冻干前后粒度分布的变化；对体外释药进行了考察；还对毫微球的其他理化特性进行了测定。     

莪术油明较微球剂的含量测定

目的：研究莪术油明胶微球的含量测定方法。方法：莪术油明胶微球用胰酶-超声法消解,硫酸－香草醛显色后,用可见－分光光度法进行测定,结果：胰酶的用量,超声时间,消解时间,对测定均有影响。结论：所建立的方法准确,可靠,适用于莪术油明磁微球剂的含量测定。     

喷雾干燥牛血清白蛋白微球中地塞米松磷酸钠和5-氟尿嘧啶的含量测定

用等吸收双波长紫外分光光度法测定了喷雾干燥牛血清白蛋白微球中地塞米松磷酸钠和 ５氟尿嘧啶的含量。回收率及重现性均好。方法快捷、准确。     

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.