茵虎黄片中大黄素和大黄酚的含量测定

目的：测定茵虎黄片中大黄素和大黄酚的含量.方法：采用高效液相色谱法,在以Nova Pak C18(3.9 mm×150.0 mm)为色谱柱,甲醇 0.1%磷酸溶液(9∶1)为流动相,流速1 mL•min 1,检测波长428 nm,柱温40℃的色谱条件下对该制剂提取物进行了分析.结果：大黄素的平均回收率97.57%,大黄酚的平均回收率97.38%,符合分析要求.重复性试验的RSD分别为：大黄素1.93%,大黄酚2.10%.结论：高效液相色谱法可以用于该制剂中大黄素和大黄酚的含量测定.     

RP HPLC测定家兔血浆中银杏叶提取物浓度方法研究

目的:建立用反相高效液相色谱(RP HPLC)测定家兔血浆中银杏叶提取物(extract ginkgo biloba, EGB)浓度的方法,对银杏叶提取物在家兔体内的药物动力学进行研究.方法:采用ODS Hypersil色谱柱(100 mm×2.1 mm,5 μm)柱温22℃,甲醇 水 磷酸为流动相(32∶67.6∶0.4),流速1.0 mL•min 1,紫外检测波长368 nm等条件下进行分析测定.结果:最低检测浓度1.25 μg•mL 1,方法平均回收率分别为98.82%和101.06%精密度为107.80%,相对标准差(RSD)＜4%(n＝3),线性范围2.50～5.00 μg•mL 1(r＝0.997 2,n＝5)和6.25～15.00 μg•mL 1(r＝0.995 7,n＝5).结论:该法具有操作简单、干扰小、准确灵敏等优点.为临床应用EGB提供实验依据.     

当归注射液中阿魏酸的含量测定

目的:以反相高效液相色谱(RP HPLC)法测定当归静脉注射液中阿魏酸的含量.方法:采用CLC ODS色谱柱(5 μm,150 mm×6 mm),流动相:甲醇 水 冰醋酸(70∶30∶1),流速:0.8 mL•min 1,检测波长:323 nm.结果:阿魏酸在4.4～26.4 μg• mL 1范围内线性关系良好,r＝0.999 1,平均回收率98.96%(RDS＝1.96%).结论:该法简便、易行,可用于当归静脉注射液中阿魏酸的含量测定.     

人血浆中盐酸氨溴索的HPLC测定及其在药动学研究中的应用

［摘要］　目的：建立人血浆中盐酸氨溴索浓度HPFC测定法。方法：采用液-液萃取高效液相色谱紫外检测法，以盐酸尼卡地平为内标，色谱柱为Diamonsil C18柱（150 mm×4.6 mm，5 μm），流动相为甲醇-乙腈-0.01 mol•L-1磷酸盐缓冲液（45∶27∶28），流速为1 mL•min-1，检测波长245 nm。结果：盐酸氨溴索血浆浓度测定方法线性范围为10~480 ng•mL-1，r=0.999 9，定量下限为10 ng•mL-1，方法回收率＞94%。日内和日间RSD＜5%。结论：本试验所建立起来的人血浆中盐酸氨溴索浓度测定法灵敏、准确，可靠，适用于盐酸氨溴索的人体药动学研究。     

气相色谱法测定搏心通原料药中亚油酸含量

目的 建立搏心通原料药中亚油酸含量测定的方法 . 方法 采用气相色谱法, 色谱柱为：HP-INNOWAX(30 m×0.53 mm, 1 μ m), 程序升温法：120 ℃保持2 min, 以10 ℃•min-1升到180 ℃, 保持2 min, 以2 ℃•min-1升到184 ℃, 以1 ℃•min-1升到190 ℃; 采用甲酯化法对样品进行衍生化处理, 并对该衍生方法进行方法学考察. 结果亚油酸含量为8.16%, RSD为1.66%. 精密度RSD为2.08%,加样回收率为97%～103%. 结论该方法操作简便, 结果准确可靠.     

高效液相色谱法测定双嘧达莫的含量

目的:用高效液相色谱法(HPLC)测定双嘧达莫的含量.方法:十八烷基硅烷键合硅胶色谱柱,甲醇－0.1%磷酸二氢钠溶液(用1%的氢氧化钠调至pH 4.6)以3∶1为流动相,检测波长为283 nm.结果:线性范围9.94～49.7 μg&;#8226;mL 1,r＝0.999 9,平均回收率为101.82%,RSD为1.87%(n＝5).     

高效液相色谱法同时检测替泰洗液中替硝唑和氯霉素的含量

目的 采用高效液相色谱法同时测定替泰洗液中替硝唑和氯霉素的含量. 方法 色谱条件：Hypersil BDS C18色谱柱(4.6 mm ×250 mm ,5 μm),流动相为0.1%庚烷磺酸钠的溶液(0.1%庚烷磺酸钠溶液:二甲基甲酰胺:冰醋酸为100：1：0.1)-乙腈(75：25),检测波长278 nm. 结果替硝唑和氯霉素的线性范围分别为：100～1 250 μg•mL^-1, 4～50 μg•mL^-1; 替硝唑和氯霉素的平均回收率(n＝9)分别为100.70 %和102.72 %, RSD分别为0.86%和0.91%. 结论该法同时测定替泰洗液中替硝唑和氯霉素含量,方法 简单可靠,准确灵敏.     

高效液相色谱法测定大鼠脑组织中腺苷与肌苷的含量

目的 建立大鼠脑组织中腺苷与肌苷的高效液相色谱检测方法 . 方法 脑组织用提取液(含0.1 mol&#8226;L 1 高氯酸溶液和0.2 mmol&#8226;L 1 乙二胺四醋酸二钠溶液)匀浆提取后进样. 色谱柱用Agilent HC C18(4.6 mm×250 mm); 流动相为甲醇 水(含磷酸二氢钠50 mmol&#8226;L 1、磷酸氢二钠4 mmol&#8226;L 1, pH值 5.8)(12：88), 流速：1.0 mL&#8226;min 1; 检测波长： 254 nm, 柱温40 ℃. 结果腺苷与肌苷的标准曲线在一定浓度内线性关系良好, 方法 加样回收完全, 日内及日间测定RSD<3.87%. 结论该方法 简便、快速、准确, 可用于脑组织中腺苷与肌苷测定.     

高效液相色谱法测定三叶委陵菜中β-谷甾醇含量

目的 建立测定三叶委陵菜中β-谷甾醇含量的方法 .方法 采用高效液相色谱(HPLC)法,Agilent TC C18柱(250 mm×4.6 mm,5 μm);流动相：甲醇 水(96：4);流速：1.2 mL&#8226;min-1;检测波长：210 nm;柱温：30 ℃.结果 β-谷甾醇在40.48～202.4 μg&#8226;mL-1范围内线性关系良好,r=0.999 8,平均回收率为98.11%,RSD为1.36%;β-谷甾醇在三叶委陵菜中平均含量为1.83 mg&#8226;g-1.结论 该方法 简便,准确,可控,可作为该产品的质量控制方法 .     

高效液相色谱法测定泮托拉唑钠肠溶微丸胶囊的含量

目的 建立高效液相色谱(HPLC)法测定泮托拉唑钠肠溶微丸胶囊的含量. 方法 采用HPLC法, 色谱柱为Symetry C18柱(4.6 mm×150 mm, 5 μm), 流动相：0.025 mol&#8226;L-1磷酸二氢钾缓冲液 乙腈(70：30), 柱温35 ℃, 流速1.0 mL&#8226;min-1, 检测波长：288 nm. 结果所选定的条件下样品峰分离良好, 泮托拉唑钠在36～84 mg&#8226;L-1范围内线性关系良好, 线性回归方程为Y＝13 130C+155 709(r＝0.999 7), 精密度、回收率RSD均<3%, 平均回收率100.40%, RSD＝1.23%. 3批泮托拉唑钠肠溶微丸胶囊的标示含量平均值为99.53%. 结论该法简便快速, 灵敏准确, 可用于测定泮托拉唑钠肠溶微丸胶囊的含量.     

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.     

Nachweis einiger Heilmittel in der Kniegelenksynovialflüssigkeit

Zusammenfassung Mittels Gaschromatographie und Dünschichtchromatographie wiesen die Autoren 11 Substanzen nach, welche durch Injektion oder nach Verabreichung per os in die Kniegelenksynovialflüssigkeit eindrangen. In ihrer Aufstellung konnten sie eine direkte Beziehung zwischen Struktur sowie chemischphysikalischen Eigenschaften der Substanz und ihrer Fähigkeit, aus dem Blut in die Kniegelenksynovialflüssigkeit einzudringen, nicht nachweisen, außer der Tatsache, daß Substanzen mit starker Affinität zu Eiweißstoffen erst in höheren Dosen nachweisbar waren.     

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.