荔大前合剂质量标准的研究

采用聚酰胺薄膜色谱法鉴别荔大前合剂中荔枝草,展开剂为甲醇-乙酸-水(65:15:20)。用高效液相色谱法测定,以ODS(250mm×4.6mm,5μm)为分析柱,甲醇-磷酸盐缓冲液(45:55)为流动相;检测波长为335nm柱温45℃,用面积外标法。结果表明,根据聚酰胺薄膜色谱图可鉴定制剂中荔枝草。当高车前苷在3.36×10~(-3)～0.215μg范围内呈线性。平均回收率为98.8％,RSD为2.14％。     

高效液相色谱法测定复方荔枝草颗粒剂中高车前苷含量

目的 :建立测定复方荔枝草颗粒剂中高车前苷含量的高效液相色谱法。方法 :以KF -C18(2 5 0mm× 4 6mm ,10 μm)为分析柱 ,流动相为甲醇 -水 -pH 3 5的 1 0mol·L-1磷酸盐缓冲液 (4 0∶5 5∶5 ) ;柱温为 45℃ ;检测波长为 335nm ;流速为 1 0mL·min-1,采用面积外标法。结果 :线性范围 3 12× 10 -3 ～ 0 2 0 μg ,平均回收率为 96 96 %～ 10 1 5 % ,RSD <0 6 9% (n =3)。结论 :本法简便、灵敏、重现性好 ,可用于测定该颗粒剂高车前苷的含量和质量标准的控制。     

利福平滴眼液的高效液相色谱法鉴别

目的　建立高效液相色谱法鉴别利福平滴眼液。方法　采用Spherisorb CN色谱柱(4.6mm×250mm,5μm) ;流动相:甲醇-乙腈-0.075mol·L^-1磷酸二氢钾溶液 (80∶80∶65);流量 1ml·min^-1;检测波长254nm;进样体积为20μl。结果　具有良好的重复性。结论　本法专属性强。     

高效液相色谱法测定苯磺酸氨氯地平分散片的含量

目的 用高效液相色谱法测定苯磺酸氨氯地平分散片的含量。方法 采用ODS色谱柱(4.6mm×250 mm,5μm,phnomenex),甲醇-0.03 mol·L^-1磷酸二氢钾溶液(65∶35)为流动相,检测波长为237 nm。结果 苯磺酸氨氯地平在49.34μg·ml^-1～91.62μg·ml^-1浓度范围内,峰面积与浓度呈良好的相关性,相关系数为0.9996,平均回收率为99.91%,RSD为0.76%,平均含量为101.6%,RSD为0.56%(n=6)。     

HPLC法测定头孢呋辛酯及其片剂的含量

建立头孢呋辛酯及其片剂的含量测定方法。以岛津Shim-Pack C₁₈(4.6 mm×150 mm,5μ)色谱柱,以0.2 mol/L磷酸二氢铵溶液-甲醇(62:38)为流动相,以278 nm为检测波长。线性范围为0.05～2 mg/ml,回归方程为Y=2.69×10⁶X-1.87×10⁵,r=0.9999,平均回收率为99.4％(RSD=0.9％,n=9)。     

高效液相色谱法测定复方荔枝草颗粒剂中桃叶珊瑚苷的含量

目的建立测定复方荔枝草颗粒剂中桃叶珊瑚苷含量的高效液相色谱法.方法色谱柱为KF-C18柱(250mm×4.6mm,10tμm),流动相为甲醇-水-磷酸(30969.50.5);柱温为35℃;检测波长为203nm;流速为1.0mL@min1.结果线性范围0.05～0.80μg,平均回收率为84.46%,RSD为1.37%(n=9).结论本法简便、灵敏、重现性好,可作为该制剂的质量控制标准.     

HPLC法测定布洛伪麻缓释片的释放量

摘 要 目的:建立高效液相色谱法测定布洛伪麻缓释片释放量的方法。方法: 色谱柱为迪马 C₁₈（250 mm×4.6 mm,5 μm）,流动相为甲醇-三乙胺-0.04 mol·L^-1 磷酸二氢钠溶液 (60∶0.02∶40),流速为1.0 ml·min^-1,检测波长为215 nm,柱温为35℃,进样量为20 μl。结果:布洛芬的线性范围为40～2 000 μg·mL^-1（r＝1.000 0）,平均加样回收率为99.2％,RSD＝0.8％(n=9),最低定量浓度为0.04μg· mL^-1;盐酸伪麻黄碱的线性范围为6～300 μg·mL^-1（r＝1.000 0）,平均加样回收率为98.5％,RSD＝0.6％(n=9),最低定量浓度为0.06μg· mL^-1。结论: 该方法简便快速、准确灵敏,可用于布洛伪麻缓释片释放量的测定。     

曲安奈德新霉素贴膏中麝香草酚含量测定方法的建立

目的：建立曲安奈德新霉素贴膏处方中麝香草酚的含量测定方法。方法：首先,通过正己烷溶解膏剂,90%乙醇萃取的方法提取贴膏剂中的麝香草酚,然后建立高效液相色谱法测定其含量,色谱条件为： Kromasil C18色谱柱(250 mm×4.6 mm,5 μm),柱温：30℃,流动相：甲醇-0.2 %乙酸(45:55),流速：1.0 ml.min^-1,进样量：20μl,检测波长：276 nm。     

高效液相色谱法测定人血清盐酸劳卡尼浓度

介绍了一种测定人血清盐酸劳卡尼(lorcainide hydrochloride)浓度的高效液相色谱法(HPLC)。不锈钢分析柱(200mm×5mmID)固定相为YWG C₁₈H₃₇,5μm颗粒。流动相为甲醇-水-0.625mol·L^-1醋酸铵(86:13:1v/v),用浓氨水调至pH8.0。流速1ml·min^-1。取地尔硫(diltiazem)为内标物。紫外检测波长226nm。低、中、高3种浓度方法回收率分别为95.85%,100.63%,100.09%,由低至高四种浓度日内、日间RSD小于7%。血清最低检测浓度为5μg·L^-1。在20～800μg·L^-1浓度范围内线性良好,r=0.9996。     

双嘧达莫片中有关物质测定法方法的研究

目的：建立双嘧达莫片中有关物质的方法。方法：采用高效液相色谱法,色谱柱为Agilent XDB-C₁₈(4.6mm×250mm,5μm),流动相为0.1%磷酸氢二钠溶液(用磷酸调节pH值至4.6)-甲醇(25:75),检测波长为288nm,流速1.0mL.min^_-1。结果:双嘧达莫与其降解产物在该色谱条件下能够有效分离。结论:所建方法简便,专属性强,可以用于双嘧达莫片中有关物质的测定。     

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.