正交试验优选微乳超声提取灵芝中灵芝多糖工艺

目的 探讨优选微乳超声法提取灵芝中灵芝多糖工艺.方法 以超声功率、提取时间和药材与溶媒比作为考察因素,以灵芝多糖得率为考察指标,采用正交试验优选微乳超声提取灵芝中灵芝多糖工艺条件,并进行验证性试验.结果 最佳条件为超声功率500W、超声提取时间50min、药材与溶媒比1∶20时,是微乳超声提取灵芝中灵芝多糖工艺最佳条件.结论 应用微乳超声法提取灵芝中基础物质,可同时提取脂溶性和水溶性成分的特性,并具有省时环保和操作简便的优点,可为灵芝基础物质的研究提供科学依据.     

冬虫夏草多糖脂质体口服液制备工艺优选

目的:优选冬虫夏草多糖脂质体口服液的制备工艺.方法:采用正交试验法考察提取时间、次数、加水体积和超声乳化时间4个因素,以冬虫夏草多糖含量和包封率为评价指标.结果:最佳制备工艺为A3B3C3D2,即加药材8倍量的水提取3次,每次3 h,超声乳化时间为15 min.结论:制剂稳定,测定方法重现性好.     

正交试验法优选“艾辛止痛膏”提取工艺的研究

目的“艾辛止痛膏”有效成分的提取工艺条件。方法以总浸膏得率、复方提取物中桂枝主要成分桂皮酸和桂皮醛的总吸收度A(权重系数分别为0.7和0.3)为综合考察指标,采用正交实验法对提取工艺的溶媒用量、提取时间、提取次数、溶媒浓度4个因素进行考察,优选出"艾辛止痛膏"的最佳提取工艺条件。结果影响提取的主次因素为:溶媒浓度>提取次数>提取时间>溶媒用量;最佳提取工艺条件是:A3B2C3D3,即乙醇用量10倍,提取2次,时间为60m in,55%乙醇。结论优选得到的提取工艺稳定可行。     

正交试验提取虫草素的工艺研究

目的 研究蛹虫草中虫草素最佳提取工艺。方法 以虫草素得率为指标，采用正交试验方法考查溶媒浓度、提取次数、提取时间以及料液比等因素对虫草素提取得率的影响。结果 虫草素的最佳提取工艺为：A2、B2、C2、D2。结论 加入药材20倍量的79%乙醇超声提取三次，每次40min是虫草素的最佳提取条件。     

星点设计-响应面法优选鹿药总黄酮提取工艺

目的利用响应面法优选鹿药总黄酮的提取工艺条件。方法以乙醇体积分数、溶媒用量、提取时间为主要影响因素,以总黄酮提取率为评价指标,用响应面法选择提取工艺的最佳条件。结果响应面法筛选的最佳提取工艺为:82.6%乙醇,溶媒用量11.4倍量,提取时间1.91h,理论提取率为2.31%,实际测得值为2.26%。结论星点设计-响应面法优选鹿药中总黄酮提取工艺,方法简单,结果可靠。     

超声提取延胡索总生物碱的研究

目的考察超声对延胡索的干燥粉末中总生物碱提取的影响,探讨、改进延胡索总碱的提取工艺。方法以活性成分延胡索乙素、原阿片碱二者的含量为指标,采用单因素轮换试验法,考察超声时间、温度、功率以及提取溶媒的酸度、用量、体积分数等因素对提取的影响。结果实验确定延胡索总生物碱提取条件为超声时间60min,提取温度40℃,超声功率350W,提取溶媒用量30倍,乙醇体积分数70%,醋酸调pH3.5。结论此提取方法的提取率高,温度低,时间短,提取工艺简便,在工业化生产中可以降低能耗,提高经济效益。     

正交试验优选竹节参多糖提取工艺

目的:优选竹节参多糖的提取工艺。方法:采用正交试验法,以总多糖的提取率为考察指标,以溶媒用量、提取时间、提取次数为考察因素优选提取工艺。结果:最佳提取工艺为溶媒用量10倍,每次提取时间2.0h,提取3次。结论:优选的工艺提取率高、稳定、可行。     

正交试验优化云南松松针中莽草酸的提取工艺

目的:优化云南松松针中莽草酸提取的最佳工艺。方法:采用L9(34)正交试验,以提取溶剂的浓度、溶媒用量、提取时间、提取次数为因素,HPLC法测定莽草酸含量并作为考察指标。结果:最佳提取工艺为80%乙醇为溶媒,12倍量的溶媒,回流2次,每次1.5 h。结论:优化后的提取工艺简单、稳定、提取率高。     

泽泻中泽泻醇B－23乙酸酯两种提取工艺的比较与优化

目的优选泽泻中泽泻醇B-23乙酸酯的提取工艺。方法比较超声提取和热回流提取两种提取工艺。应用正交设计法优选泽泻醇B－23乙酸酯的提取工艺,采用高效液相色谱法测定该成分提取率。结果影响提取的主次因素为D〉C〉B〉A（A为提取时间,B为溶媒倍量,C为溶媒浓度,D为生药目数）。优选提取工艺为60目泽泻粗粉。20倍量95％乙醇,超声提取30分钟。结论优选所得工艺简单,合理,可行。     

丹参提取工艺研究

目的：优选丹参最佳提取工艺条件。方法：以丹参酮ⅡA和丹酚酸B的提取率为指标,采用正交设计法对影响提取的因素进行优化。结果：影响浸出的主要因素为乙醇浓度、溶媒用量和提取时间,最佳提取工艺为12倍量70％乙醇,80℃,回流提取150min（第一次90min,第二次60min）。结论：该工艺合理,稳定可行,适合于生产。     

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.     

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.     

血管内皮生长因子的异常与子(癎)前期发病的关系

目的:研究血浆可溶性细胞间黏附分子-1(sICAM-1)浓度和胎盘组织血管内皮生长因子(VEGF)、胎盘生长因子(PLGF)及其血管内皮生长因子受体1(VEGFR1,Flt-1)、可溶性血管内皮生长因子受体1(sVEGFR1,sFlt-1)mRNA的表达与子前期的关系.方法:采用酶联免疫吸附测定法(ELISA)检测45例子前期患者和45例健康产妇血清sICAM-1的浓度,逆转录-聚合酶链反应(RT-PCR)方法检测胎盘组织中VEGF、PLGF、Flt-1、sFlt-1 mRNA的表达.结果:(1)子前期组sICAM-1水平为(218.45±29.93) μg/L,显著高于对照组的(168.84±19.39) μg/L(P < 0.01).(2)子前期患者胎盘组织VEGF、PLGF、Flt-1、sFlt-1 mRNA的相对表达量显著高于对照组(均P < 0.01).(3)血清sICAM-1浓度与胎盘组织中sFlt-1mRNA的相对表达量呈正相关(r = 0.90,P < 0.01).结论:子前期患者血清sICAM-1浓度升高,其胎盘组织VEGF、PLGF、Flt-1、sFlt-1 mRNA的相对表达量也升高.胎盘组织sFlt-1mRNA的高表达与子前期内皮损伤等有密切关系.     

Antiparasitic protozoan vaccines

Parasitic infections caused by pathogenic protozoa affect over 1 billion people worldwide and impose a substantial health and economic burden, particularly on inter-tropical less-developed countries where they are more prevalent. Despite encouraging progress in vaccine development, chemotherapy remains the single most effective, efficient and inexpensive means to control most parasitic infections [1]. However, day to day parasites are becoming increasingly resistant to drugs currently in use, such as Plasmodium towards chloroquine, lending to the start of a promising future for vaccines. Patent applications regarding vaccines for the prevention, control and diagnosis of parasitic protozoan infections are reviewed for the period December 1996 - October 2000. However, vaccines for some of the protozoan infections do not appear in the literature in the period reviewed; only, vaccines against malaria, leishmaniasis, trypanosomiasis, cryptosporidiosis, pneumocystosis, eimeriosis, toxoplasmosis and neosporosis, as well as Babesia microti infections have been found.     

Binding affinity in drug design: experimental and computational techniques

ABSTRACT

Introduction: In pharmaceutical design where future drugs are developed by targeting a specific chosen protein, the evaluation of ligand affinity is crucial. For this very purpose are a multitude of diverse methods which are continuously being improved, which, in turn, makes it difficult to choose which techniques to use in practice.

Areas covered: In this review, the authors discuss both experimental and computational approaches for affinity evaluation. Basic principles, general limitations and advantages, as well as main areas of application in drug discovery, are overviewed for some of the most popular ligand binding assays. The authors further provide a guide to affinity predictions, collectively covering several techniques that are used in the first stages of rational drug design.

Expert opinion: All affinity estimation methods have limitations and advantages that partially overlap and complement one another. Some of the suggested best practices include cross-verification of data using at least two different techniques and careful data interpretation.