应用紫外分光光度法测定苦参总碱的含量

用岛津UV-210紫外分光光度计对苦参膏中苦参总硷的含量进行了测定。结果表明，苦参总硷的光谱图在200nm处有最大吸收，并且吸收值与苦参总硷的含量间存在着良好的线性关系。并对苦参总硷在水溶液中的稳定性和实验方法的精密度进行了考察，认为此方法适合于作含量测试分析，其平均回收率为103.2%。     

滴定法与高效液相色谱法测定苦参提取液中苦参总碱含量比较研究

目的筛选苦参提取工艺研究中苦参总碱含量的测定方法。方法用滴定法和高效液相色谱(HPLC)法对苦参原药材、苦参醇提取液及酸水提取液中苦参总碱的含量测定进行对比研究。结果在测定苦参原药材、苦参醇提取液及酸水提取液中苦参总碱的含量时,滳定法所得的相对标准偏差(RSD)较HPLC法低(0.92%vs.6.30%、0.72%vs.8.85%、1.53%vs.4.00%)。结论在进行含苦参原药材的提取工艺研究时,宜采用滴定法对苦参总碱进行含量测定。     

阳离子交换树脂酸水洗脱法纯化苦参总碱的工艺优选

目的优选阳离子交换树脂不同浓度盐酸溶液洗脱纯化苦参总碱的最佳工艺条件。方法以苦参碱、氧化苦参碱和总生物碱的洗脱率为考察指标,以盐酸溶液作为洗脱剂,优选阳离子交换树脂纯化苦参总碱的最佳工艺和参数条件。结果苦参总碱阳离子交换树脂纯化洗脱条件为:以5%盐酸溶液作为洗脱剂,以6 BV.h-1的流速洗脱,苦参碱和氧化苦参碱、苦参总碱洗脱率均可达85%。结论采用阳离子交换树脂酸水洗脱法纯化苦参总碱效率高,工艺简便,可用于苦参总碱的提取纯化。     

复方苦参洗剂中小檗碱的含量测定

目的: 建立三元络合物比色法测定复方苦参洗剂中小檗碱的含量,为制剂质量控制提供依据.方法: 小檗碱在pH6.7的溶液中, 与溴酚蓝、奎宁形成三元络合物比色, 经氯仿提取, 在610 nm波长处测定吸收度.结果: 回归方程为A=0.182C-0.004(r=0.999 9),小檗碱在0.8～4 mg·L-1浓度范围内线性关系良好(r=0.999 9),平均回收率为98.65%,RSD为1.12%.结论: 本方法准确,灵敏度好,可用于复方苦参洗剂中小檗碱的含量测定.     

注射用苦参总碱(冻干)中苦参总碱的提取工艺实验研究

本次研究通过控制注射用苦参总碱(冻干)中苦参总碱的质量指标和药效学的比较研究确定了最佳的提取工艺为工艺Ⅲ,并对质量标准进行合理的改进和提高,以期获得符合临床制剂质量标准要求的苦参总碱,从而使注射用苦参总碱(冻干)更加安全、有效和质量可控。     

酸性染料比色法测定醋酸洗必泰溶液的含量

本文采用溴甲酚绿酸性染料比色法测定醋酸洗必泰溶液的含量.在波长420nm 处测定,其浓度在0.05～0.3mg/ml 范围内与吸收度呈线性关系,平均回收率为99.51%.变异系数小于0.90%本法具有操作简便、快迅、灵敏、准确度和精密度均可满足制剂分析的要求,适用于医院制剂分析。     

HPLC-DAD法测定自采苦参根茎和根中5个生物碱的含量

目的:测定自采苦参根茎和根中苦参碱、氧化苦参碱、槐果碱、氧化槐果碱、槐定碱的含量,以便了解采自同一株植物的苦参根茎和根中苦参碱和氧化苦参碱的总量。方法:采用Welch Materials XtimateTMC18(4.6 mm×150 mm,5μm)色谱柱,流动相A为10 mmol.L-1醋酸铵水溶液(0.1%氨水调至pH 9.2),流动相B为乙腈,梯度洗脱,流速1 mL.min-1,检测波长220nm。结果:自采苦参根茎中苦参碱和氧化苦参碱的总量为四川资阳2.17%、北京怀柔2.53%、山西原平3.21%,根中二者总量为四川资阳2.86%、北京怀柔2.26%、山西原平3.34%。结论:采自不同产地或同一株植物的苦参根茎和根中,苦参碱和氧化苦参碱的总量各有高低。     

苦参总碱片抗心血管系统疾病的药理作用

苦参总碱片是由豆科植物苦参的干燥根经渗漉法提取，精制而得的苦参总碱浸膏，再加入适宜的辅料制剂而成。苦参总碱中含多种生物碱，主要为苦参碱和氧化苦参碱；另外还含有羟基苦参碱、去氧苦参碱、安那吉碱、N-甲基金雀花碱等及多种黄酮类。苦参总碱具有抗心率失常，增加冠脉流量，保护心肌缺血、增加心肌收缩力、降血脂、抗肝炎、抗肿瘤、防止白细胞减少、抗辐射、抗过敏、镇痛平喘、祛痰等作用。本文就苦参总碱片的抗心血管疾病方面的作用予以综述。     

HPLC法同时测定人血浆中苦参4种生物碱的含量

目的:建立同时测定人血浆中苦参4种生物碱含量的方法。方法:采用高效液相色谱(HPLC)法。色谱柱为Agilent ZORBAX NH2(150 mm×4.6 mm,5μm),流动相为乙腈-无水乙醇-3%磷酸溶液(81∶10∶9,V/V/V),流速为1 ml/min,检测波长为210 nm,柱温为室温。结果:槐定碱、槐果碱、苦参碱、氧化苦参碱的进样量分别在0.034 72⁰.258 60、0.012 840.258 60、0.012 84⁰.113 65、0.023 770.113 65、0.023 77⁰.240 93、0.452 480.240 93、0.452 48⁴.520 63μg范围内与待测物峰面积积分值呈良好线性关系(r≥0.999 3);槐定碱、槐果碱、苦参碱、氧化苦参碱精密度试验的RSD均小于2.0%;短期、长期、循环稳定性的RSD均小于3.20%;重复性试验的RSD均小于3.0%;提取回收率分别为1.14%4.520 63μg范围内与待测物峰面积积分值呈良好线性关系(r≥0.999 3);槐定碱、槐果碱、苦参碱、氧化苦参碱精密度试验的RSD均小于2.0%;短期、长期、循环稳定性的RSD均小于3.20%;重复性试验的RSD均小于3.0%;提取回收率分别为1.14%².35%、1.45%2.35%、1.45%².32%、1.29%2.32%、1.29%².51%、1.62%2.51%、1.62%².47%。结论:该方法灵敏度高、精密度好,可用于苦参中4种生物碱的药动学研究。     

双波长等吸收紫外法同时测定复方阴道泡腾片中酮康唑与替硝唑含量

目的 建立同时测定酮康唑和替硝唑含量的双波长等吸收紫外分光光度法.方法 建立双波长法测定酮康唑和替硝唑含量的标准曲线,并考察检测方法的精密度和回收率.结果 选择317nm作为替硝唑的测定波长,221nm作为酮康唑的含量测定波长,并以352nm作为参比波长.二者标准曲线方程为:A=0.029C+0.0168;A=0.456C-0.0742,高、中、低浓度的平均回收率分别为(100.2±0.70)%;(99.4±0.92)%,测定的日内精密度RSD分别为0.62%,1.03%;日间精密度RSD为1.13%,1.42%.结论 双波长等吸收紫外光度法同时测定酮康唑和替硝唑含量的方法学特异性好,精密度和回收率符合测定要求,测定结果可靠.     

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.