加味酸枣仁合剂的薄层色谱鉴别研究

目的 建立和完善加味酸枣仁合剂的质量标准,保障其临床疗效。方法 采用薄层色谱法对处方中的知母、茯苓、川芎、甘草进行定性鉴别。结果 薄层色谱可以鉴别知母、茯苓、川芎、甘草,且斑点清晰,阴性对照无干扰。结论 该方法简便、可靠,重复性好,可作为加味酸枣仁合剂的质量控制方法。     

酸枣仁颗粒薄层鉴别方法研究

目的:建立酸枣仁颗粒的薄层色谱(TLC)鉴别方法,为控制其产品质量提供依据.方法:采用薄层色谱对方中的酸枣仁、知母、甘草进行定性鉴别.结果:在TLC色谱中均能检测出酸枣仁、知母、甘草.结论:定性方法准确可行,重复性好,该方法可作为该品种的质量标准.     

酸枣仁合剂的薄层鉴别及酸枣仁皂苷A的含量测定

目的:建立酸枣仁合剂的鉴别和含量测定方法.方法:采用TLC法和HPLC法.结果:TLC法鉴别酸枣仁合剂中知母、茯苓和川芎等药材;HPLC测定酸枣仁皂苷A的含量,酸枣仁皂苷A在0.55～1.1 mg/mL范围内线形关系良好(r=0.9997),平均加样回收率为100.45%,RSD为1.30%.结论:鉴别重复性好、专属性强,含量测定方法简便,准确.     

独活寄生合剂的薄层色谱鉴别

目的对独活寄生合剂中当归、川芎、茯苓、熟地黄的定性鉴别方法进行研究。方法采用薄层色谱法鉴别。结果薄层斑点清晰、结果可靠。结论薄层色谱法可用于独活寄生合刺的定性鉴别。     

眼明丸的鉴别研究

目的建立眼明丸质量控制的方法。方法显微鉴别茯苓、红花、甘草；采用薄层色谱(TLC)鉴别制剂中当归、川芎、黄连及陈皮。结果各种药材定性鉴别特征明显，易于区别。结论该鉴别方法准确可靠，可用于该制剂的质量控制。     

康宁Ⅰ号浓煎剂中酸枣仁的薄层色谱鉴别

本院研制的康宁Ⅰ号浓煎剂，系由酸枣仁、茯苓、知母、五味子、玄参、清甘草等多味中药制成的纯中药制剂。该品具有养血安神、清热除烦之功效，用于夜眠多梦、心悸盗汗、头晕目眩、咽干口煤。笔者应用薄层色谱法对该品中的酸枣仁进行鉴别，以利监控质量。1实验材料康宁Ⅰ号浓煎剂由宁波市康宁医院制剂室提供，批号970715；标准品酸枣仁皂甙A购自中国药品生物制品检定所，批号0734－9404；酸枣仁药材产于河北，由浙江省鄞县医药公司提供；硅胶G为青岛海洋化工厂产品；所用试剂均为分析纯。2实验方法与结果2．1供试品溶液的制备：取该品40ml…     

小酸枣汤对小鼠自主活动及睡眠时间影响的拆方研究

目的:考察小酸枣汤对小鼠自主活动及睡眠时间的影响,并进行拆方研究。方法:将小酸枣汤组方中7味药材(酸枣仁、茯苓、川芎、知母、甘草、生姜、桂心)作为实验因素,每个因素选取有或无2个水平,按L_8(2~7)正交表安排试验。采用直观分析法和方差分析法比较小酸枣汤组方和方中各单味药对小鼠2 min内自主活动及阈上剂量戊巴比妥钠致小鼠睡眠时间的影响。结果:小酸枣汤组方中对小鼠自主活动具有明显影响作用的是酸枣仁和知母;对阈上剂量戊巴比妥钠所致小鼠睡眠时间有明显影响的是酸枣仁。结论:小酸枣汤具有抑制小鼠自主活动及延长阈上剂量戊巴比妥钠致小鼠睡眠时间的作用,方中酸枣仁作用最强。     

乌苓苁蓉合剂的薄层色谱鉴别研究

目的:建立乌苓苁蓉合剂中制首乌、茯苓和菟丝子的薄层鉴别方法。方法:采用薄层色谱法,考察供试液展开条件、色谱检视方法、耐用性等因素,对制首乌、茯苓和菟丝子进行定性鉴别。结果:制首乌、茯苓和菟丝子薄层鉴别斑点清晰,阴性对照无干扰,专属性强。结论:该方法操作简单,重现性好,准确可靠,可用于乌苓苁蓉合剂的质量控制。     

壮腰止痛合剂的薄层色谱鉴别

目的鉴别壮腰止痛合剂中的当归、川芎,防风。方法采用薄层色谱（TLC）鉴别制剂中的当归,川芎,防风。结果薄层色谱法鉴别制剂中的当归,川芎,防风,专属性强,分离度好,色谱斑点清晰。结论本方法简便灵敏,结果准确可靠,为本品的质量控制提供了简便的方法。     

八珍袋泡茶的薄层色谱鉴别

目的建立八珍袋泡茶中主要药味的薄层色谱鉴别方法。方法采用薄层色谱法分别对八珍袋泡茶中的党参、当归、川芎、白术、茯苓进行鉴别。结果在薄层色谱图中可检出党参、当归、川芎、白术、茯苓的特征斑点。结论该方法操作简便,重复性及专属性均符合要求,可用于建立八珍袋泡茶的定性质量标准。     

手性药物研发进展与相关指导原则介绍

随着对手性药物认识的不断深入,不对称合成技术、拆分技术的飞速发展以及手性药物监管政策的日益完善,手性药物已成为新化学实体研发的重要方向。从手性药物的发展情况、手性药物的药理,毒理学特点,各国药品监管部门针对手性药物开发所颁布的指导原则的进展情况与我国手性药物安全性评价的现状几个方面进行综述总结,为手性药物的开发及其毒理学评价提供参考。     

手性药物的开发、审评与评价

目的:介绍几种手性药物的制备方法,讨论国内外药政部门对手性药物审评的差别,并评价我国手性药物的发展趋势.方法:查找文献并综述.结果和结论:手性药物的开发是当前药物研究的一个热点.我们应该充分利用手性科学研究取得的重大进展,推动我国手性科学的发展.     

Chiral inversion of drugs: coincidence or principle?

2-arylpropionic acid derivatives are probably the most frequently cited drugs exhibiting the phenomenon that is best known as chiral inversion. One enantiomer of drug is converted into its antipode either in the presence of a solvent or more often in inner environment of an organism. Mechanistic studies of the metabolic chiral inversion were carried out for several drugs from NSAIDs, and a model of this inversion was suggested and subsequently confirmed. The chiral inversion of NSAIDs has been intensively studied in the context of the pharmacological and toxicological consequences. However, the group of NSAIDs is not the sole group of drugs in which the inversion phenomenon can be observed. There exist several other drugs that also display chiral inversion of one or even both of their enantiomers. These drugs belong to different pharmacotherapeutic groups as monoamine oxidase inhibitors, antiepileptic drugs, drugs used in the treatment of hyperlipoproteinemia or drugs that are effective in the treatment of leprosy. Moreover, some chiral or prochiral drugs are metabolized to give chiral metabolites that undergo chiral inversion too, which can have direct impact on pharmacological properties or toxicity of the drug. As the process of chiral inversion is affected by several factors, so the intensity of chiral inversion of individual substances and at different conditions can differ considerably. Interspecies differences and types of tissue are reported to be the main factors that were recognized to play the key role in the process of chiral inversion. Some of more recent studies have revealed that several other factors, such as the route of administration or interaction with other xenobiotics, can influence the enantiomeric conversion, too. Chiral inversion does not seem to be a phenomenon connected with only several drugs from some unique group of 2-arylpropionic acid derivatives: it is also observed in drugs with rather different chemical structures and is much more frequent than it can be realized.     

手性药物的生物效应

本文对手性药物的不同生物效应进行述评,为手性药物的进一步研究与手性药物的临床合理使用及手性药物的开发生产提供参考。     

聚合物固载试剂在手性药物合成中应用的研究进展

当前手性药物合成的研究已成为国际药学研究领域的热点之一,近几年发展起来的在聚合物固载试剂条件下进行的不对称合成由于其各种优点,引起了药学界广泛的关注.无论从经济角度还是从“绿色化学”角度考虑,聚合物固载试剂的巨大潜力势必会推动手性药物合成技术的迅速发展.从抗肿瘤类、抗生素类、天然产物类和生物化学类活性物质对近几年来聚合物固载试剂在手性药物合成方面的应用进行简述,并对其前景进行展望.     

Selected fundamental aspects of chiral electromigration techniques and their application to pharmaceutical and biomedical analysis.

While capillary electrophoresis has been established as a major enantioseparation technique within the last decade, the potential of capillary electrochromatography is still studied extensively. This review summarizes recent applications of electromigration techniques with regard to the enantioseparation of chiral drugs. The first part discusses the general aspects of migration models and the enantiomer migration order. The application of capillary electrophoresis to chiral pharmaceutical analysis considers recent literature on: (1) chiral resolutions of non-racemic mixtures of enantiomers for the development of assays and the determination of the stereochemical purity of the drugs, (2) chiral separations of compounds in pharmaceutical formulations and products, and (3) enantioseparations of drugs in biological samples. A shorter section devoted to chiral electrochromatography discusses some fundamental aspects as well as the application to the chiral analysis of drugs including bioanalysis.     

手性药物对映体在药效学与药代动力学的相互作用

当手性药物以外消旋体供药用时，其对映体间就可能发生药效学和药代动力学的相互作用。本文综述了手性药物对映体间的药效学和药代动力学相互作用及其对手性药物药效学和药代动力学立体选择性的影响。     

手性药物高效毛细管电泳拆分方法的研究进展

高效毛细管电泳法（high performance capillary electrophoresis,HPCE）在手性药物拆分领域得到了广泛的应用。目前,手性离子液体用于毛细管电泳拆分手性药物时,常与环糊精（CD）类手性选择剂构成二元体系产生协同作用,增强了手性离子液体潜在的手性拆分能力。依据对映体拆分的手性选择剂的种类及浓度、缓冲液的浓度和pH、电泳工作电压和温度,选出手性拆分的最佳条件。综述手性药物的发展以及应用HPCE拆分手性药物的文献资料,并对其研究的新进展作了分析。     

Enantioselective quantification of chiral drugs in human plasma with LC-MS/MS

Today, approximately 60% of synthetic drugs are chiral and 88% of these chiral synthetic drugs are used therapeutically as racemates. However, for many racemic drugs, their stereospecific plasma pharmacokinetics in humans are not known due to the limitations of the analytical methods. Nowadays, liquid chromatography (LC)-tandem mass spectrometry (MS/MS) methods based on various chiral stationary phases (CSPs), with a high degree of specificity and sensitivity, have been widely used in enantioselective determination of chiral drugs and/or their metabolites in human plasma. The technologies and issues when coupling chiral chromatography with MS/MS detection in bioanalytical methods will be reviewed herein. The introduction and applications of various CPSs, including polysaccharide-, macrocyclic glycopeptide-, protein- and cyclodextrin-based phases, are described here. This review also includes a discussion of interface and matrix effects in enantioselective LC-MS/MS methods.     

手性药物的色谱分离方法

综述了手性药物常用的色谱分离方法，如气相色谱、高效液相色普、高效毛细管电泳色谱及超临界流体色谱等在手性药物扩分研究中的应用及近年来的研究进展。