南极海茸多糖果冻的润肠通便功能研究

目的 制备南极海茸多糖果冻,研究其对便秘小鼠的润肠通便作用。方法 以南极海茸多糖为原料,制备一款酸甜可口的果冻。采用PMP柱前衍生-HPLC法测定果冻中南极海茸多糖的含量。探索了南极海茸多糖果冻对便秘小鼠润肠通便作用：将昆明小鼠随机分为空白组、模型组、阳性对照组、果冻低剂量组和高剂量组。果冻低剂量组和高剂量组小鼠按0.2 mL/10g剂量分别灌胃给予添加量为5%南极海茸多糖果冻溶液;阳性对照组按0.2 mL/10 g剂量灌胃给予乳果糖口服液;空白组和模型组小鼠给予相同剂量的果冻基质,连续灌胃7d。采用盐酸洛哌丁胺小鼠便秘模型,观察各组小鼠的首粒排黑便时间、5h内排便粒数、排便重量以及小肠墨汁推进率。结果 采用PMP柱前衍生-HPLC法,以岩藻糖表征南极海茸多糖含量为5.06%,测定值与实际添加量相符。实验结果表明,与模型组相比,南极海茸多糖果冻可显著提高小肠墨汁推进率(P＜0.05),明显增加便秘小鼠的排便粒数和排便重量(P＜0.05),显著缩短便秘小鼠的首粒排黑便时间(P＜0.01)。结论：成功制备了南极海茸多糖果冻,PMP柱前衍生-HPLC法检测果冻中岩藻糖含量结果准确,专属性好,可用于南极海茸多糖果冻的质量控制。南极海茸多糖果冻具有良好的润肠通便作用。     

苗药热淋清咀嚼片的质量研究

目的：研究热淋清咀嚼片,确定合理质量检测方法。方法：对热淋清咀嚼片的没食子酸含量检测进行方法学研究。结果：确定了热淋清咀嚼片中没食子酸含量在4.9～196.0μg/mL浓度范围之间具有良好的线性关系（r=0.99995）,平均回收率为99.68%,RSD为0.48％。结论：热淋清咀嚼片含量检测方法可行,质量可控,稳定。     

灰树花多糖咀嚼片中多糖含量测定

目的：建立简单易行的多糖含量测定方法,测定灰树花多糖咀嚼片中多糖的含量。方法：采用硫酸-蒽酮法,618nm测定,葡萄糖作对照。结果：线性关系为Y=0.1259X＋0.1248（R2=0.9991）,线性范围为0.0232~0.1392mg/ml,回收率99.6%,制剂中多糖含量73.0%。结论：该方法简单易行,能用于灰树花多糖咀嚼片中多糖的含量测定。     

正交试验法优选复方淫羊藿咀嚼片的提取工艺

目的:优选复方淫羊藿咀嚼片的提取工艺。方法:以淫羊藿苷提取率、粗多糖含量和浸膏得率为综合指标,采用正交试验法考察加水倍量、提取时间、提取次数对提取效果的影响,优化提取工艺并进行验证试验。结果:最优提取工艺为药材加6倍量水提取3次,每次提取2 h。验证试验显示,淫羊藿苷提取率均值为(83.80±0.02)%,粗多糖含量均值为(29.28±0.55)mg/g,浸膏得率均值为(28.47±0.29)%,RSD均≤0.55%(n=3)。结论:优选的工艺稳定,可用于复方淫羊藿咀嚼片的提取。     

HPLC法测定海藻药材质量标志物岩藻糖的含量

目的 建立中药海藻药材岩藻糖含量的HPLC测定方法。方法 水提得海藻粗多糖,继而经2 mol/L三氟乙酸降解、1-苯基-3-甲基-5-吡唑啉酮衍生后,采用HPLC测定岩藻糖含量,并进行方法学考察。结果 岩藻糖在6.44 ~ 824.52 μg/mL 浓度范围内具有良好的线性关系,y = 15.074 x - 52.068,r = 0.9998;最低检测限0.80 μg/mL,最低定量限1.61 μg/mL;供试品溶液在40 h内稳定性良好,RSD 0.04%;精密度、重复性良好,RSD分别为0.51%、1.15%;平均加样回收率为99.28 %,RSD 2.15 %(n = 9)。结论 建立的方法简便准确、精密度高、重复性好,可用于海藻药材的质量控制。     

HPLC法测定小儿消食咀嚼片中橙皮苷的含量

目的 采用HPLC法测定小儿消食咀嚼片中橙皮苷的含量.方法 HPLC法,VP-ODS柱(4.6 mm×250 mm,5 μm),流动相:乙腈-0.4%磷酸溶液(22∶78),检测波长:283 nm,流速:1.0 ml·min-1.结果 橙皮苷含量测定线性范围1.31～13.11 μg,相关系数r=0.9999,平均回收率为100.26%,RSD=1.53%(n=5).结论 该方法分离度高,重现性好,简便,准确,可用于小儿消食咀嚼片的质量控制.     

硝苯地平咀嚼片的制备工艺研究

目的:制备硝苯地平咀嚼片。方法:采用单因素试验对硝苯地平咀嚼片的填充剂、矫味剂、润滑剂、崩解剂及黏合剂进行优选;以外观、口感、片重差异、脆碎度、硬度和崩解时限为评价指标,采用正交试验优化咀嚼片的填充剂(甘露醇-蔗糖)、矫味剂(阿斯巴甜)、崩解剂(交联聚维酮)和润滑剂(硬脂酸镁)的用量,并进行中试验证工艺。结果:硝苯地平咀嚼片的最佳制备工艺处方(1 000片)为:硝苯地平5.0 g、甘露醇106.7 g、蔗糖53.3 g、预胶化淀粉26 g、阿斯巴甜2.0 g、聚乙烯吡咯烷酮水溶液2%、柑桔香精0.3%、交联聚维酮3.0%、硬脂酸镁1.0%;制得片剂的外观、口感、片重差异、脆碎度、硬度和崩解时限等质量指标均符合2010年版《中国药典》的有关规定。结论:硝苯地平咀嚼片制备工艺合理、可行。     

孟鲁司特钠咀嚼片含量测定及初步稳定性研究

目的为实现对孟鲁司特钠咀嚼片质量的关键指标的控制和制剂稳定性研究。方法建立一种专属性好,灵敏度高,快速,准确的HPLC分析方法,测定3批次孟鲁司特钠咀嚼片中孟鲁司特钠含量;并通过高温、高湿度、强光照射试验和加速试验及长期稳定性试验,进行制剂的初步稳定性试验。结果建立的方法经验证,孟鲁司特钠的线性范围为0.5～16.0μg/mL,检测限为0.12μg/mL,定量限为0.39μg/mL,平均加样回收率分别是99.7%、101.2%和99.8%,精密度试验RSD值为1.04%、1.23%和1.27%,初步稳定性试验中含量变化的RSD值均为1.22%、1.67%和1.45%。结论该方法分析时间短、专属性好、准确度高,可用于孟鲁司特钠咀嚼片中孟鲁司特钠含量测定。孟鲁司特钠咀嚼片质量稳定,符合要求。     

高效液相色谱法测定健胃咀嚼片中橙皮苷的含量

目的：建立高效液相色谱法测定健胃咀嚼片中主要的功效成分陈皮中橙皮苷的含量。方法：WatersC18柱（XBridgeTMC18;5μm;4.6mm×250mm）;以甲醇∶冰醋酸∶水（34∶4∶62）为流动相;检测波长283nm。结果：橙皮苷在48.45～339.51ng范围内呈良好的线性关系,r=0.9998,平均加样回收率为105.11%,RSD为1.9%（n=9）。结论：本方法操作简便,结果准确,重现性好,可用于健胃咀嚼片的质量控制。     

火焰原子吸收分光光度法测定牡蛎碳酸钙咀嚼片中钙的含量

目的建立火焰原子吸收分光光度法测定牡蛎碳酸钙咀嚼片中钙的含量。方法采用钙空心阴极灯。检测波长：422．7nm,狭缝宽：0．7nm,灯电流：10mA,火焰类型：Air-C2H2,燃气流量：2．0L/min,助燃气流量：15．0L／min。结果钙元素浓度在2.4496-7.3488μg/mL范围内与吸收度呈良好的线性关系（r=0．9996,n=5）,高、中、低3种浓度的平均加样回收率为98．S％,RSD值为0．85％（n=9）。结论该方法操作简便、快速,结果准确,可以用于牡蛎碳酸钙咀嚼片的质量控制。     

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.