非离子表面活性剂囊泡对头孢菌素药物的缓释作用

用超声法制备了Span系列非离子表面活性剂囊泡,研究了它们对几种水溶性头孢菌素药物的包封作用及影响包封率的因素,通过透射电镜对囊泡的形态和大小进行了鉴定.实验表明,制得的囊泡多为球形单室囊泡,且包封后的药物在模拟肠液和模拟胃液中均有缓释作用.     

类脂囊泡作为头孢噻肟钠药物载体的研究

用司盘(Span)系列非离子表面活性剂和胆固醇(CHOL)通过真空旋转一超声波法制备了头孢噻肟钠囊泡,研究了包封条件对包封率的影响及包封后的药物在体外的模拟释放,考察了头孢噻肟钠囊泡的形态和构造。实验表明:Span20与CHOL摩尔比为2∶1,50°C超声30m in,对1.00g/L的注射用头孢噻肟钠的包封率可达55%以上,而且在模拟肠流体和模拟胃流体中均有缓释作用。     

类脂囊泡包封药物顺铂的研究

用司盘(Span)系列非离子表面活性剂和胆固醇(CHOL)为主要膜材,通过薄膜-超声波法制备了顺铂囊泡,研究了影响包封率的主要因素,考察了顺铂囊泡在体外的释放性能.实验表明:在50℃超声50 m in的条件下,由Span20与CHOL(摩尔比为5∶3)制备的囊泡对0.60 g.L-1注射用顺铂包封率可达65%以上,且包封后的药物在模拟肠流体和模拟胃流体中均有缓释作用.     

类脂囊泡作为5-氟尿嘧啶药物载体的研究

采用薄膜分散法,以司盘类非离子表面活性剂和胆固醇为主要原料,制备抗肿瘤药物5-氟尿嘧啶(5-FU)类脂囊泡.以包封率为考察指标,对可能影响包封的各种实验条件进行优化.实验表明:药物浓度为1.0 g/L,Span 20与胆固醇比例为4∶3,50℃超声30min,所制得的5-FU类脂囊泡的包封率可达40%以上.透射电镜照片显示所制得的类脂囊泡为球形单室结构,测得平均粒径为393nm,且分布较均匀,表明制得的囊泡粒径符合注射给药的要求.     

失水山梨醇脂肪酸酯-聚乙二醇嫁接的聚乙烯醇化磁性药物载体的制备及应用

通过丁二酸酐将失水山梨醇脂肪酸酯(Span80)和聚乙二醇(PEG400)联接在一起,合成了一种新的非离子表面活性剂.然后将其嫁接在聚乙烯醇(PVA)化的Fe3O4磁性粒子上,合成了一种新型靶向药物载体.这种载体兼备了Span80/PEG400类脂囊泡和磁性材料的特点,具有良好的稳定性和靶向作用.将这种新型载体用于两性霉素的包封,包封率可达96.6%,且方法简便.实验过程中采用了FTIR, NMR, XRD和TEM等多种手段进行表征.     

盐引发阴离子/非离子表面活性剂复配体系中囊泡自发形成

在无盐时, 阴离子表面活性剂十二烷基苯磺酸钠(SDBS)与非离子表面活性剂壬基酚聚氧乙烯(10)醚(TX-100)的复配体系中只有混合胶束存在, 而盐的加入即可以引发体系中囊泡的自发形成, 这使得囊泡的形成变得更加简单. 引发机理可以归因于盐对离子表面活性剂的极性头双电层的压缩作用, 减少了极性头的面积, 加上非离子表面活性剂的参与使得堆积参数P增加, 导致了半径更大的聚集体的形成. 制作了SDBS/TX-100/盐水拟三元相图, 通过目测和表面张力的变化确定了囊泡形成的带状区域, 并用负染色电镜(TEM)对囊泡进行了表征, 同时测定了盐度以及相同盐度下表面活性剂浓度对囊泡粒径的影响, 发现囊泡的粒径随着盐度的增加而增加, 而在同一盐度下, 囊泡的粒径基本不受表面活性剂浓度的影响.     

最大泡压法测定吐温-80的表面参数及亲水基分子截面积

运用溶液表面吸附原理,以升级后的最大泡压装置测定了25℃下非离子表面活性剂吐温-80的表面吸附等温线,通过近似处理得到吐温-80的临界胶束浓度(CMC),进一步求得吐温-80的亲水基截面积,分析了图解法处理数据的不足和实验开展的优势。该实验对学生学习和解析复杂的表面吸附等温线具有重要的指导意义。     

吐温表面活性剂囊泡对姜黄素的包载作用

本文研究了烷基链不饱和度对吐温表面活性剂囊泡包载姜黄素的影响。相比吐温-80囊泡,吐温-60囊泡的包载使姜黄素表现出更大的紫外吸收和荧光发射强度、缔合常数和DPPH自由基清除能力。核磁共振氢谱结果表明姜黄素缔合于吐温-60囊泡双分子层中的亲水头基附近,而且姜黄素的酚羟基与吐温-60的酯基产生氢键作用。在吐温-80囊泡中,双键会使吐温-80烷基链产生弯曲或折叠,导致双分子层排列更加松散、极性更高。因此,姜黄素除了与吐温-80的酯基产生氢键作用外,还能与吐温-80烷基链尾部和中部的亚甲基发生作用。     

肽类药物口服剂型材料及控制释放性能研究：Ⅰ.壳聚糖—海藻酸盐？…

应用壳聚糖－海藻酸盐微囊技术制备了一系列胰岛素微型,并研究了不同反应条件如海藻酸钠浓度,壳聚糖浓度,壳聚糖分子量及壳聚糖溶液ｐＨ值对生囊的胰岛素包封率及其释放性能的影响。结果表明,海藻酸钠浓度越高,微囊对胰岛素的包封率越高,在模拟小肠液中释放速度越低;壳聚糖浓度越大,微囊的胰岛素包封率及其在模拟胃液中释放率越高,在模拟肠液中释放达最大值所需时间越长;而随壳聚糖分子量减小,微囊在胃液中释放率增高;壳     

季铵盐型Gemini表面活性剂诱导囊泡结构改变机理研究

用动态光散射技术以及荧光探针方法, 研究了不同连接基长度的季铵盐型Gemini表面活性剂对卵磷脂囊泡结构改变的影响, 并借助理论模型和临界堆积参数理论探索了Gemini表面活性剂诱导囊泡结构改变的机理. 实验结果表明, 表面活性剂诱导囊泡结构改变的主要原因是表面活性剂嵌入到囊泡的双分子层中, 从而改变了囊泡的表面电荷强度以及嵌入后的表面活性剂在囊泡双分子层中分布的不均匀性. 此外, 表面活性剂分子的结构也会对其产生影响, 不同连接基长度的季铵盐型Gemini表面活性剂对囊泡结构改变的影响不完全相同, 但会呈现出一定的规律性.     

二氧化碳和丙烯直接合成甲基丙烯酸的NiPMo/TiO2催化剂的研究

用溶胶-凝胶法以磷钼酸(MPA)的镍盐溶液水解钛酸四丁酯制备了NiPMo/TiO2催化剂.使用ICP、 XRD、 TG-DTA、 IR、 TPD-MS和微反应技术研究了催化剂的化学组成、热稳定性、化学吸附性质和催化反应性能.杂多钼酸盐与TiO2通过O2-在TiO2表面发生了键合.在623 K下,杂多阴离子仍保持原有的Keggin结构.CO2在Lewis酸位Ni(Ⅱ)和Lewis碱位Ni-O-Mo的桥氧协同作用下生成CO2卧式吸附态Ni(Ⅱ)←O-(CO)←(O--Ni).丙烯有多种吸附态在催化剂上吸附.在563 K、 1 MPa和空速1500 h-1的反应条件下,丙烯的摩尔转化率为3.2%,产物MAA选择性为95%.     

Synthesis of 1-benzyloxypyrazin-2(1H)-one derivatives

Different approaches for the synthesis of 1-benzyloxypyrazin-2(1H)-one derivatives from simple amino acids have been investigated. A library of 33 precursors for the preparation of N-hydroxy pyrazinones was obtained in moderate to good yields.     

Toward new camptothecins. Part 6: Synthesis of crucial ketones and their use in Friedländer reaction

In the context of the preparation of camptothecin and luotonin A analogs, the synthesis of some key keto-precursors and their use in Friedländer condensation are described. This paper also focuses on the stability of these keto intermediates and emphasizes the major differences between indolizinones and pyrroloquinazolinones series. Noteworthy is also the report of some original structures isolated as by-products of some experiments.     

CoFe2O4自形成磁性液体场致结构化对磁化的影响

The Langevin paramagnetic theory can’t describe the relation between magnetization of ferrofluids and applied magnetic field. The structuralization of ferrofluids, which is considered the main influence factor of the magnetization, is regarded. The part of magnetization works is deposited when the structure is forming. This action influences the magnetization of ferrofluids directly or indirectly. On the base of the “compressing” model, the Langevin function that usually describes the magnetization of ferrofluid is modified, and a well-fitted curve is obtained. An equation of the relation between the equivalent volume fraction after being “compressed” and the intensity of magnetic field is discovered, which approximately describes the process of magnetization. The relation between the approximate initial susceptibility and the volume fraction can be obtained from modified formula.     

Highly regioselective Buchwald–Hartwig amination at C-2 of 2,4-dichloropyridine enabling a novel approach to 2,4-bisanilinopyridine (BAPyd) libraries

The highly regioselective Buchwald–Hartwig amination at C-2 of the cheap and readily accessible reagent, 2,4-dichloropyridine with a range of anilines and heterocyclic amines is described. This new methodology is robust and provides a facile access to 4-chloro-N-phenylpyridin-2-amines on 0.25 mol scale. These intermediates undergo a further Buchwald–Hartwig amination at higher temperature to enable rapid exploration of the chemical space at C-4 and to provide a library of 2,4-bisaminopyridines.     

KMnO4-mediated oxidative CN bond cleavage of tertiary amines: Synthesis of amides and sulfonamides

KMnO₄-mediated oxidative CN bond cleavage of tertiary amines producing secondary amine was introduced, which was trapped by electrophiles (acyl chloride and sulfonyl chloride) to form amides and sulfonamides. The reaction could take place at mild condition, tolerating a wide range of function groups and affording products in moderate to excellent yields.     

Chemistry of heterocyclic compounds at the A. E. Favorsky Irkutsk Institute of Chemistry, Siberian Branch of the Russian Academy of Sciences, over 50 years (Review)

The review contains a concise historical account and information on the most significant researches undertaken by the staff at the A. E. Favorsky Irkutsk Institute of Chemistry, Siberian Branch of the Russian Academy of Sciences on the Chemistry of Heterocyclic Compounds. Dedicated to Academician of the Russian Academy of Sciences B. A. Trofimov on his 70th jubilee. Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 10, pp. 1443–1502, October, 2008.     

A general and convenient synthesis of 4-(tosylmethyl)semicarbazones and their use in amidoalkylation of hydrogen,heteroatom, and carbon nucleophiles

A general synthesis of previously unknown semicarbazone-based α-amidoalkylating reagents, 4-(tosylmethyl)semicarbazones, has been developed. The synthesis involved three-component condensation of semicarbazones of aliphatic or aromatic aldehydes with the same or other aldehydes and p-toluenesulfinic acid. The scope and limitations of this reaction were investigated. The compounds obtained were demonstrated to be an efficient α-(4-semicarbazono)alkylating agents. They were reacted with H- (sodium borohydride), O- (sodium methylate), S- (sodium phenylthiolate), N- (pyrrolidine, sodium succinimide), P- (trialkyl phosphites), and C-nucleophiles (sodium diethyl malonate) to give the corresponding products of the tosyl group substitution, 4-substituted semicarbazones, including analogues of nitrofurazone. Among the prepared compounds tested in vitro for antibacterial and antifungal activity, three nitrofuryl-containing semicarbazones exhibited high biological activities with minimum inhibitory concentration (MIC) values of 8–32 μg/mL.     

Sulfur-directed metal-free and regiospecific methyl C(sp3)–H imidation of thioanisoles

Regiospecific and direct imidation of the methyl C(sp³)–H bond of thioanisoles is realized under mild and metal-free conditions with N-fluorobis(benzenesulfonyl)imide as an oxidant and nitrogen source. Proposed mechanism suggests that thionium ion intermediates and a Pummerer-type reaction are involved. The imidation has advantages such as high step-economy, excellent functionality tolerance, and regiospecificity, giving structurally diverse imidation products.     

Synthesis of novel chiral bidentate hydroxyalkyl-N-heterocyclic carbene ligands and their application in palladium-catalyzed Mizoroki–Heck couplings and asymmetric addition of diethylzinc to benzaldehyde

A small library of new chiral bidentate hydroxyalkyl-imidazolium salts 1 is conveniently synthesized on multi-gram scale from inexpensive and commercially available chiral pool amino acids. The corresponding carbenes, generated by deprotonation of imidazolium salts 1, in combination with palladium(II) chloride were tested in the Mizoroki–Heck coupling reaction. The most significant results in terms of yields and reactivities were achieved with low catalyst loading. The catalytic activities of these imidazolium salts were also investigated in the asymmetric addition of diethylzinc to benzaldehyde. The use of MgO nanoparticles as an additive in conjunction with these ligands played a crucial role in increasing the efficiency of these reactions.