木香顺气丸鉴别与含量测定

的研究木香顺气丸的质量标准。方法采用薄层色谱法（TLC）对香附、木香、苍术、陈皮、青皮进行定性鉴别;采用高效液相色谱法（HPLC）测定橙皮苷含量,色谱柱为Diamonsil C18柱,流动相为甲醇 水 醋酸（40：60：0.3）,流速为1.0 mL•min－1,检测波长283 nm,柱温25 ℃。结果采用TLC可鉴别出香附、木香、苍术、陈皮、青皮对应的斑点;采用HPLC测定橙皮苷的含量,橙皮苷在0.180 2～1.802 0 μg范围内有良好的线性关系（r＝0.999 4）,平均回收率为99.0%,RSD为2.3%（n＝9）。结论所建立的质量标准简便可行、重复性好,可用来评价木香顺气丸质量。     

HPLC测定木香顺气丸中的4种有效成分

目的采用HPLC法同时测定木香顺气丸中木香烃内酯、去氢木香烃内酯、厚朴酚和厚朴酚的含量。方法采用Kro-masil C18色谱柱(250 mm×4.6 mm,5.0μm),流动相为乙腈-甲醇-水(50:8:42);检测波长210 nm;流速1.0 m.lmin-1。结果木香顺气丸中4种指标成分的线性关系良好,r为0.9996~0.9999;回收率为97.49%~100.80%,RSD为0.88%~1.77%。结论所建方法专属性强、重复性好,可用于木香顺气丸的质量控制。     

HPLC测定木香顺气丸中的木香烃内酯

目的 测定不同批次木香顺气丸中的木香烃内酯的含量.方法 采用HPLC法,色谱柱为Kromasil C18 (250 mm ×4.6mm,5μm),流动相为甲醇-水(60∶40),检测波长225 nm,流速1.0 mL· min-1,柱温30℃,进样体积10 μL.结果 木香烃内酯1.033 ～ 20.67 μg·mL-1与峰面积呈良好的线性关系(r =0.9999),平均加样回收率为98.95％,RSD=1.2％ (n =9);5批次木香顺气丸中的木香烃内酯的含量为0.08％.结论 所用方法简单、稳定,可作为木香顺气丸的品质评价依据之一.     

薄层扫描法测定木香顺气丸中橙皮苷的含量

采用双波长薄层扫描法测定木香顺气丸中橙皮苷的含量。乙酸乙酯-甲醇-水（10：2：1．3）为展开剂,橙皮苷Rf=0．47。锯齿反射扫描,λs=275nm,λR一37Onm,Sx=3,回收率为100.75％,RSD=2．57％。     

木香顺气丸甲醇提取物的高效液相特征图谱

目的:建立木香顺气丸(陈皮、厚朴、苍术等)甲醇提取物特征图谱的HPLC特征图谱分析条件,为木香顺气丸的内在质量评价积累数据,为优化及评价中药复方特征图谱提供一种方法。方法:采用HPLC-UV检测,ZORBAX EclipseXDB-C18(4.6 mm×150 mm,5μm)色谱柱,乙腈-水为流动相,在35℃柱温下采用梯度洗脱,流速1 mL.min-1;检测波长280 nm,225 nm(木香);进样量5μL;实验比较了7个厂家和自制木香顺气丸的高效液相特征图谱,并考察了单味药材的高效液相特征图谱。结果:该方法在104～520μg.mL-1范围内线性关系良好,Y=70 580 X+1.187 5,r=0.999 7(和厚朴酚);木香顺气丸甲醇提取物各组分分离较佳,精密度、稳定性、重复性好,相对保留时间RSD小于0.5%。结论:表明HPLC特征图谱方法重复性好,稳定性可靠,可用于木香顺气丸的质量控制方法,不同厂家木香顺气丸质量有差异,而药材是影响木香顺气丸质量的因素之一。     

温中止泻丸质量标准研究

目的建立温中止泻丸的质量标准。方法采用薄层色谱法对处方中丁香、木香进行定性鉴别;用HPLC法测定橙皮苷含量。结果在TLC定性鉴别中丁香酚、去氢木香内酯分离度好,专属性强;橙皮苷0.00592~7.40μg范围内,线性关系良好,相关系数r=0.9999(n=5);平均加样回收率为97.70%,RSD为1.59%(n=9)。结论该方法简便、准确,重复性好,可作为温中止泻丸的质量控制方法。     

HPLC同时测定羌药川木香顺气丸中木香烃内酯和去氢木香内酯的含量

目的:采用HPLC法同时测定羌药川木香顺气丸中木香烃内酯和去氢木香内酯的含量。方法:色谱柱为Ultimate XB-C18色谱柱(4.6×250 mm,5μm),流动相为乙腈-0.2%甲酸水溶液(80:20,v/v),流速为1 ml.min-1,检测波长为225 nm,柱温为30℃。结果:木香烃内酯、去氢木香内酯分别在1.47~47.12、3.26~104.24μg.m L-1范围内呈良好的线性关系,川木香顺气丸中木香烃内酯、去氢木香内酯平均总含量为3.35mg/g。结论:实验所建立的HPLC方法可用于羌药川木香顺气丸中木香烃内酯和去氢木香内酯的含量测定。     

木香顺气丸制备工艺研究

目的优选并确定木香顺气丸的制备工艺。方法采用均匀设计法以水分百分数、崩解时限和成丸难易为指标,筛选木香顺气丸的辅料,考察辅料的用量,确定木香顺气丸的制备工艺。结果实验结果表明,以低取代羟丙基纤维素(L-HPC)和羧甲基淀粉钠(CMS-Na)为辅料,其比例为3∶1时制备木香顺气丸崩解时限较低,丸的水分约为8%。结论优选的木香顺气丸处方合理,方法简单,易于控制。     

HPLC测定木香顺气丸中柚皮苷的含量

目的采用HPLC法测定木香顺气丸中柚皮苷的含量。方法HPLC法,Hypersil C18柱(5μm,4.6mm×250mm),流动相:乙腈-水(19:81),检测波长:284nm,流速:1.0ml·min-1;结果柚皮苷在10.07μg～50.36μg范围内有良好的线性关系,R=0.9999,平均回收率为97.95%,RSD=1.99(n=5)。结论该方法简便,准确,重现性好,可用于木香顺气丸的质量控制。     

平安丸的质量标准研究

目的:建立平安丸的质量标准。方法:采用薄层色谱(TLC)法对平安丸中的青皮、陈皮、枳实、肉豆蔻、木香、延胡索进行定性鉴别;采用高效液相色谱法测定处方中橙皮苷的含量。结果:TLC斑点清晰、分离度好;橙皮苷进样量在0.1～1.1μg(r=0.9999)范围内与峰面积积分值呈良好线性关系,平均回收率为99.48%,RSD=0.62%(n=6)。结论:所建标准可用于平安丸的质量控制。     

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.     

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.     

Emerging drugs for epilepsy

Epilepsy affects ≤ 1% of the world's population. Antiepileptic drugs (AEDs) are the mainstay of treatment, although more than a third of patients are not rendered seizure free with existing medications. Uncontrolled epilepsy is associated with increased mortality and physical injuries, and a range of psychosocial morbidities, posing a substantial economic burden on individuals and society. Limitations of the present AEDs include suboptimal efficacy and their association with a host of adverse reactions. Continued efforts are being made in drug development to overcome these shortcomings employing a range of strategies, including modification of the structure of existing drugs, targeting novel molecular substrates and non-mechanism-based drug screening of compounds in traditional and newer animal models. This article reviews the need for new treatments and discusses some of the emerging compounds that have entered clinical development. The ultimate goal is to develop novel agents that can prevent the occurrence of seizures and the progression of epilepsy in at risk individuals.     

盐酸达泊西汀中甲磺酸甲酯、甲磺酸乙酯及甲磺酸异丙酯的顶空毛细管GC-ECD法测定

建立了衍生化顶空毛细管气相色谱-电子捕获检测器(ECD)法测定盐酸达泊西汀中的甲磺酸甲酯(MMS)、甲磺酸乙酯(EMS)和甲磺酸异丙酯(IMS).应用碘化钠衍生技术,使用PW-5毛细管柱,载气为氮气,ECD检测,程序升温.MMS、EMS和IMS分别在0.03～0.30、0.05～0.50和0.05～0.50 μg/ml浓度范围内线性关系良好,平均回收率分别为63.5％、100.3％和96.2％,最低检测限分别为0.30、0.50和0.50 ng/ml.     

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.