固定pH滴定法测定弱酸弱碱性药物

报道一种水溶液吕测定弱酸弱碱性药物的新型滴定分析方法－固定ｐＨ滴定法，其理论基础是弱酸弱碱在水溶液中各种存在形式的分布系数在ｐＨ值固定时为常数，对甲硝唑，盐酸美西律等离散常数在１０＾－８至１０＾－１１范围内的７种弱酸弱碱性药物进行测定。结果与药典法吻合，回收率在９９．４％～１００．６％，方法简便，快速，准确，制剂中的赋形剂及色物不影响测定。     

极弱酸碱的pH滴定法研究

ｐＨ滴定法是指酸碱滴定至某一指定ｐＨ值时，即可根据滴定剂浓度，用量及有关公式，计算被测物浓度或含量的方法。本文深入讨论了测定原理，方法和应用，对１０种不同极弱酸碱进行了大量测定，测定结果相对误差一般在０．２％左右，相对标准偏差在０．３％左右，达到化不。ｐＨ滴定法具有简便，价廉，快速和通用的优点，为直接滴定极弱酸碱和化学分析仪化开辟了新的途径。     

两维pH滴定法同时测定混合极弱酸碱

两维ｐＨ滴定法同时测定混合极弱酸碱朱仲良，李通化，鲁准军（同济大学化学系，上海，２０００９２）关键词两维ｐＨ滴定，极弱酸碱，同时测定，主成分回归法传统的酸碱滴定法必须根据滴定过程中的ｐＨ突跃确定等当点，因此当弱酸（或弱碱）的浓度和离解常数之积ＣＫ＜１...     

固定pH跨度法滴定弱酸（碱）混合体系

１引言为了克服固定ｐＨ法在酸、碱干扰组分存在时，无法扣除空白的问题，我们提出了固定ｐＨ跨度法。当溶液的温度、离子强度及滴定剂浓度不变，滴定极弱酸（碱）至ｐＨ为Ａ时，消耗滴定剂体积ＶＡ与极弱酸（碱）的含量。之间存在如下关系：当滴至ｐＨ为Ｂ时（设此时反应还未完全），（２）－（１）得：αＡ、αＢ只与极弱酸（碱）的性质和ｐＨ值有关。故对于某一极弱酸（碱），当ｐＨ跨度一定时，△α为一常数，可通过滴定纯品测得。由于只取不完全质子化（失质子化）反应时由某一固定ｐＨ跨度而无须先加入强酸（碱）使待测组分完全质子化…     

新西佛碱3.5—二溴水杨醛缩氨基硫脲的合成及其在荧光滴定中的应用

本文研究了新西佛碱３．５－二溴水杨醛缩氨基硫脲（简称３．５－ＤＢＳＴＳ）的合成，及基为一种新荧光滴定指示剂，应用于有色溶液中酸碱滴定的条件，建立了一种简便，准确，快速测定有色溶液中酸碱浓度的新方法，用于有色饮料中酸含量的测定，结果满意，指示剂发光的ｐＨ突跃范围为７．４８－９．７２，λｅｘ＝５００ｎｍ。     

5－Br－PADAP作指示剂络合滴定法连续测定矿石中的锌和铜

本文在ｐＨ５．５的乙酸－乙酸钠介质中，对以５－Ｂｒ－ＰＡＤＡＰ作指示剂络合滴定法连续测定锌和铜进行了研究，对滴定的ｐＨ值及指示剂用量进行了选择，试验了锌、铜不同配比的滴定结果，研究了共存离子的干扰。实验表明，用５－Ｂｒ－ＰＡＤＡＰ作指示剂、ＥＤＴＡ作滴定剂连续测定锌和铜，滴定终点颜色变化敏锐，准确度高，锌和铜均在０～２０ｍｇ范围内与ＥＤＴＡ用量成正比，锌、铜比例在１：１０～１０：１范围内相互无影响，方法用于标样及金矿中锌、铜的连续测定，结果满意。     

5—Br—PADAP作指示剂络合滴定法连续测定矿石中的锌和铜

本文在ｐＨ５．５的乙酸－乙酸钠介质中，对以５－Ｂｒ－ＰＡＤＡＰ作指示络合滴定法连续测定锌和铜进行了研究，对滴定的ｐＨ值及指示剂用进行了选择，试验了锌，铜不同配比的滴定结果，研究了共存离子的干扰。实验表明，用５－Ｂｒ－ＰＡＤＡＰ作指示剂，ＥＤＴＡ作滴定剂连续和铜，滴定点颜色变化敏锐，准确度高，锌和铜均在０－２０ｍｇ范围内与ＥＤＴＡ用量成正比，锌，铜比例在１：１０－１０：１范围内相互无影响。方法用于标     

新西佛碱3．5－二溴水杨醛缩氨基硫脲的合成及其在荧光滴定中的应用

本文研究了新西佛碱３．５－二溴水杨醛缩氨基硫脲（简称３．５－ＤＢＳＴＳ）的合成，及其作为一种新型荧光滴定指示剂，应用于有色溶液中酸碱滴定的条件，建立了一种简便、准确、快速测定有色溶液中酸碱浓度的新方法，用于有色饮料中殴含量的测定，结果满意，指示剂发荧光的ｐＨ突跃范围为７．４８～９．７２，λ＿（ｅｘ）＝３８５ｎｍ，λ＿（ｅｍ）＝５００ｎｍ。     

一元弱酸(弱碱)准确滴定界限的简易推导

１　引言　　在酸碱滴定分析中,一般常用指示剂颜色的变化来目测终点,判断强碱（或强酸）能否准确滴定一元弱酸（或弱碱）的界限为［１,２］：ｃａｋａ≥１０－８或ｃｂｋｂ≥１０－８。对于这个滴定界限的提出,少数教材及教学参考书进行了简要的推导［３,４］。王毓芳等［５］采用多步近似法对滴定界限作了理论上的求证,但推导过程太繁琐,且近似处理欠严密。本文提出另一种方法,从缓冲容量的定义出发,通过引入滴定分数和敏锐指数,导出了弱酸（弱碱）能否被直接滴定的界限。２　滴定界限的推证　　首先引入缓冲容量β,教材［１］…     

1—（5—溴—2—吡啶偶氮）—2—萘酚—6—磺酸作指示剂络合滴定连续测定铜和锌

对５－Ｂｒ－ＰＡＮ－Ｓ作指示剂络合滴定连续测定铜和锌进行了研究，在ｐＨ６．０的乙酸乙酸的钠介质中，以５－Ｂｒ－ＰＡＮ－Ｓ作指示剂，ＥＤＴＡ为滴定剂连续测定铜和锌，滴定终点颜色变化敏锐，准确度高，铜和锌量各在０～２０ｍｇ范围内与ＥＤＴＡ用量成正比，铜，锌比例在１：１０～１０：１范围内相互无影响，方法用于合金中铜，锌的连续测定，结果满意。     

Pharmaceutical Applications of Ionic Liquids: A Personal Account

Ionic liquids (ILs) have been extensively used in drug formulation and delivery as designer solvents and other components because of their inherent tunability and useful physicochemical and biopharmaceutical properties. ILs can be used to manage some of the operational and functional challenges of drug delivery, including drug solubility, permeability, formulation instability, and in vivo systemic toxicity, that are associated with conventional organic solvents/agents. Furthermore, ILs have been recognized as potential solvents to address the polymorphism, limited solubility, poor permeability, instability, and low bioavailability of crystalline drugs. In this account, we discuss the technological progress and strategies toward designing biocompatible ILs and explore potential biomedical applications, namely the solubilization of small and macromolecular drugs, the creation of active pharmaceutical ingredients, and the delivery of pharmaceuticals.     

Insight into the Inhibition of Drug‐Resistant Mutants of the Receptor Tyrosine Kinase EGFR

Targeting acquired drug resistance represents the major challenge in the treatment of EGFR‐driven non‐small‐cell lung cancer (NSCLC). Herein, we describe the structure‐based design, synthesis, and biological evaluation of a novel class of covalent EGFR inhibitors that exhibit excellent inhibition of EGFR‐mutant drug‐resistant cells. Protein X‐ray crystallography combined with detailed kinetic studies led to a deeper understanding of the mode of inhibition of EGFR‐T790M and provided insight into the key principles for effective inhibition of the recently discovered tertiary mutation at EGFR‐C797S.     

Hybrid Drugs—A Strategy for Overcoming Anticancer Drug Resistance?

Despite enormous progress in the treatment of many malignancies, the development of cancer resistance is still an important reason for cancer chemotherapy failure. Increasing knowledge of cancers’ molecular complexity and mechanisms of their resistance to anticancer drugs, as well as extensive clinical experience, indicate that an effective fight against cancer requires a multidimensional approach. Multi-target chemotherapy may be achieved using drugs combination, co-delivery of medicines, or designing hybrid drugs. Hybrid drugs simultaneously targeting many points of signaling networks and various structures within a cancer cell have been extensively explored in recent years. The single hybrid agent can modulate multiple targets involved in cancer cell proliferation, possesses a simpler pharmacokinetic profile to reduce the possibility of drug interactions occurrence, and facilitates the process of drug development. Moreover, a single medication is expected to enhance patient compliance due to a less complicated treatment regimen, as well as a diminished number of adverse reactions and toxicity in comparison to a combination of drugs. As a consequence, many efforts have been made to design hybrid molecules of different chemical structures and functions as a means to circumvent drug resistance. The enormous number of studies in this field encouraged us to review the available literature and present selected research results highlighting the possible role of hybrid drugs in overcoming cancer drug resistance.     

Surface-modulated and thermoresponsive polyphosphoesternanoparticles for enhanced intracellular drug delivery

The chemical structure of end groups influenced the phase transition temperature of thermoresponsive polymers. We demonstrated a strategy for the preparation of the pH/thermo-responsive polymeric nanoparticles via subtle modification of end groups of thermoresponsive polymer segments with a carboxyl group and revealed its potential application for enhanced intracellular drug delivery. By developing a polymeric nanoparticle composed of poly(aliphatic ester) as the inner core and thermoresponsive polyphosphoester as the outer shell, we showed that end groups of thermoresponsive polyphosphoester segments modified by carboxyl groups exhibited a pH/thermo-responsive behavior due to the hydrophilic to hydrophobic transitions of the end groups in response to the pH. Moreover, by encapsulating doxorubicin into the hydrophobic core of such pH/thermo-responsive polymer nanoparticles, their intracellular delivery and cytotoxicity to wild-type and drug-resistant tumor cells were significantly enhanced through the phase-transition-dependent drug release that was triggered by endosomal/lysosomal pH. This novel strategy and the multi-responsive polymer nanoparticles achieved by the subtle chain-terminal modification of thermoresponsive polymers provide a smart platform for biomedical applications.     

Recent Aspects of Pharmaceutical Application of Cyclodextrins

Because of the multi-functional characteristics and bioadaptability, cyclodextrin (CyD) is capable of alleviating the undesirable properties of drug molecules through the formation of inclusion complexes. This paper outlines the current application of natural and chemically modified CyDs in the various pharmaceutical formulations including peptide and protein drugs. Furthermore, potential use of CyD/drug conjugates in site-specific drug delivery is discussed.     

胆汁酸为载体的肝靶向一氧化氮释放药物的设计与合成

新型肝靶向一氧化氮释放药物对许多肝脏疾病具有较好的治疗作用. 以胆酸和熊去氧胆酸作为药物的载体, 以氨基酸作为联接子, 以氨基酸的α羧基模拟胆酸或熊去氧胆酸分子24位羧基的负电性, 最大限度地保持胆酸或熊去氧胆酸的结构特征, 通过酰胺键将载体与一氧化氮供体硝酸酯偶联, 设计并合成了一系列新型肝靶向一氧化氮释放偶合物, 其结构经元素分析, IR, 1H NMR和MS光谱分析确证. 利用四氯化碳及对乙酰氨基酚所致小鼠急性肝损伤模型研究化合物对小鼠急性肝损伤的修复作用.     

Four‐fold Channel‐Nicked Human Ferritin Nanocages for Active Drug Loading and pH‐Responsive Drug Release

Human ferritins are emerging platforms for non‐toxic protein‐based drug delivery, owing to their intrinsic or acquirable targeting abilities to cancer cells and hollow cage structures for drug loading. However, reliable strategies for high‐level drug encapsulation within ferritin cavities and prompt cellular drug release are still lacking. Ferritin nanocages were developed with partially opened hydrophobic channels, which provide stable routes for spontaneous and highly accumulated loading of Fe^II‐conjugated drugs as well as pH‐responsive rapid drug release at endoplasmic pH. Multiple cancer‐related compounds, such as doxorubicin, curcumin, and quercetin, were actively and heavily loaded onto the prepared nicked ferritin. Drugs on these minimally modified ferritins were effectively delivered inside cancer cells with high toxicity.     

Proteomics and Its Application in Biomarker Discovery and Drug Development

Proteomics is a research field aiming to characterize molecular and cellular dynamics in protein expression and function on a global level. The introduction of proteomics has been greatly broadening our view and accelerating our path in various medical researches. The most significant advantage of proteomics is its ability to examine a whole proteome or sub-proteome in a single experiment so that the protein alterations corresponding to a pathological or biochemical condition at a given time c…     

空心纳米磷酸钙载药体系的制备与表征

非离子表面活性剂Tween 80和PEG 6000在水溶液中以一定的比例混合可形成稳定的类磷脂囊泡结构,这些囊泡可以作为模板来合成磷酸钙纳米空球颗粒。所制备的磷酸钙材料的结构和形貌通过TEM,SEM,FTIR,XRD进行了表征,是尺寸为100～150 nm左右的无定形磷酸钙空心颗粒。磷酸钙具有良好的生物相容性,因此这些具有空心结构特征的磷酸钙可发展为理想的载药体系。我们以牛血清蛋白(BSA)为模型体系研究了材料的载药和释放性能,发现所获得的空心纳米磷酸钙不仅具有良好的蛋白质负载量而且还具有优异的可释放性,明显优于传统的羟基磷灰石体系。