单甲氧聚乙二醇化学修饰药物酶的研究进展

用单甲氧基聚乙二醉(1)化学修饰药物酶是生化药物研究开发的重要手段之一。本文综述了1化学修饰药物酶的一般方法及修饰后酶在生物和理化性质方面的变化，同时对1研究前景进行展望，并指出了尚待解决的问题。     

线性变温法研究硫酸链霉素粉针剂的稳定性

用线性变温法对硫酸链霉素粉针的稳定性进行了测定,得出25℃时的降解反应速度常数 k_(25)为1.744×10~(-6)h~(-1)、化学反应的表观活化能为107.9kJ/mol,25℃时贮存的 t_(0.9)为6.9年。     

免疫抑制剂SIIA9268A的研究.Ⅰ.发酵、分离及理化性质

在用含ｒａｐａｍｙｃｉｎ结合蛋白基因（ＲＢＰ）的啤酒酵母ＲＳ１８８Ｎ及其变株ＲＳ１８８Ｎ△ｒｂｐ：：：ＬＥＵ筛选免疫抑制剂的过程中，得到活性菌株Ｎｏ．ＳＩＩＡ９２６８（鉴定为吸水链霉菌东湖变种）。应用硅胶柱层析和制备ＴＬＣ等方法从其发酵液中分离出活性化合物ＳＩＡ９２６８Ａ。经理化性质鉴定与ｒａｐａｍｙｃｉｎ同质。     

流态化化学气相淀积制备Al2O3—SnO2复合粒子的研究

利用流态化化学气相淀积（ＣＶＤ）制备Ａｌ＿２Ｏ＿３－ＳｎＯ＿２复合粒子。探讨了ＳｎＯ＿２在Ａｌ＿２Ｏ＿３超细颗粒上的包敷状态，考察了反应温度、反应物进料浓度比、反应时间等对反应结果的影响。结果表明，ＳｎＯ＿２在复合粒子团聚体体相中呈均匀分布，形成Ａｌ＿２Ｏ＿３－ＳｎＯ＿２复合粒子，ＳｎＯ＿２均匀淀积在Ａｌ＿２Ｏ＿３超细颗粒原生粒子表面，流态化ＣＶＤ包敷效果优于非流化过程；随反应时间的延长，产物中ＳｎＯ＿２含量线性递增；而当反应温度高于３００℃，反应物Ｈ＿２Ｏ和ＳｎＣｌ＿４配比大于４：１时，ＳｎＯ＿２含量基本保持不变。     

Z-3-(2-羟基丁烯基)苯酞的合成研究

研究目的探讨苯酞类天然产物的合成方法及其生物活性。研究方法以邻苯二甲酐为底物，首先引入丁烯基，再进行烯丙位氧化，制得目标化合物。结果通过丁基锂反应，得到了具有药物活性的丁烯基苯酞，然后利用SeO2烯丙位氧化，首次合成了Z－3－（2－羟基丁烯基）苯酞。结论此合成方法原料易得，方法简便，为苯酞类化合物的合成研究提供了一个新的途径。     

鱼腥草的有效成分、药理作用及临床应用的研究进展

鱼腥草中含有癸酰乙醛、癸醛、月桂醛及甲壬酮等成分，其中癸酰乙醛具有抗病原微生物活性．药理研究证明鱼腥草具有抗菌、抗病毒、增强机体免疫、抗炎等作用，故在呼吸科、五官科及消化科疾病中都有广泛的应用．     

亮氨酸脑啡肽的电子结构及构效关系研究

对亮氨酸脑啡肽进行了量子化学(INDO)计算,研究其电子结构特征,讨论其活性部位、作用机理及构效关系。同吗啡和R31833进行了活性部位的电子结构与空间结构比较,推断它们的活性药效结构具有共同特点,与阿片受体相互作用时作用方式相同,作用部位有对应关系,因而具有相同的药理性质。     

Cardiovascular malformations, work attendance, and occupational exposures during pregnancy in Finland

To explore for associations between occupational factors and cardiovascular malformations, information on the parents of 160 infants with cardiovascular malformations and 160 control parents was studied. The case infants had been reported consecutively to the Finnish Register of Congenital Malformations. All mothers were interviewed identically after delivery, using both open and pro forma questions about detailed work tasks, exposures, and leisure activities during pregnancy. The interview information was evaluated blindly. Neither parental occupational titles nor maternal working per se gave new clues to the teratogenic risk; nor did shift working, wearing of personal protective equipment, or the mother's own opinion on exposures during pregnancy. Identified occupational exposures, as categorized by an industrial hygienist, showed no remarkable associations to cardiovascular malformations. Few mothers were exposed substantially to specific occupational hazards. Comparing mothers who used medications in the first trimester with those who did not showed an odds ratio of 2.2 (95% confidence interval 1.3-3.9) when adjusted for potential confounding by multivariate logistic methods.     

羧基化多壁碳纳米管修饰电极伏安法测定多巴胺

目的 :研究用羧基化多壁碳纳米管修饰电极伏安法测定痕量多巴胺 (DA)的效果。方法 :采用涂布法制成羧基化多壁碳纳米管修饰电极 ;在pH =5 .4的KH2 PO4 Na2 HPO4缓冲溶液中 ,采用该修饰电极伏安法测定DA。结果 :该修饰电极对DA有着显著的电催化作用 ,与裸玻碳电极相比较 ,其灵敏度大大提高 ,在2 .0× 10 -7～ 6 .0× 10 -4mol/L浓度范围内 ,DA的氧化峰电流与浓度成良好的线性关系 ,检测限为 5 .0× 10 -8mol/L。将该修饰电极用于盐酸多巴胺针剂的测定 ,相对平均偏差为 1.4 % ,平均回收率为 99.2 %。结论 :该修饰电极响应快 ,灵敏度高 ,稳定性好 ,寿命长 ,适合于具有电活性生物分子的测定     

Oral Controlled Release Technology for Peptides: Status and Future Prospects

In spite of significant efforts in academic and commercial laboratories, major breakthroughs in oral peptide and protein formulation have not been achieved. The major barriers to developing oral formulations for peptides and proteins include poor intrinsic permeability, lumenal and cellular enzymatic degradation, rapid clearance, and chemical and conformational stability. Pharmaceutical approaches to address these barriers, which have been successful with traditional, small, organic drug molecules, have not readily translated into effective peptide and protein formulations. The success achieved by Sandoz with cyclosporin formulations remains one clear example of what can be achieved, although it is likely that effective oral formulations for peptides and proteins will remain highly compound specific. Although the challenges are significant, the potential therapeutic benefit remains high, particularly with the increasing identification of potential peptide and protein drug candidates emerging from the biotechnology arena. Successful formulations will most likely require a systematic and careful merger of formulation and design delivery systems which maximize the potential for absorption across the epithelial cell layer.