甲苯咪唑微丸质量标准的研究

目的：建立对甲苯咪唑微丸进行定性鉴别和含量测定的方法。方法：采用薄层层析法进行定性鉴别,用紫外分光光度法进行含量测定。结果：含量测定方法平均回收率为１００．６％ , Ｒ Ｓ Ｄ＝ １．７２％ 。结论：所用方法简便可靠,可控制甲苯咪唑微丸的质量。     

中国健康中青年女性全血比粘度参考值与海拔高度的关系

目的：为制定中国健康中青年女性全血比粘度参考值的统一标准提供科学依据。方法：收集了中国各地用毛细管法测定的健康中青年女性全血比粘度参考值,并对其与海拔高度的关系进行了研究。结果：发现随着海拔高度的逐渐增大,健康中青年女性全血比粘度参考值也在逐渐增大,相关性很显著。用一元回归分析的方法推导出一个回归方程。结论：如果知道了中国某地的海拔高度,就可以用回归方程估算这个地区的健康中青年女性全血比粘度参考值。     

霍乱弧菌O139菌毛微球疫苗制备初探

为寻求Ｏ１３９型霍乱弧菌菌毛疫苗研制的新途径,用高分子聚乳酸－聚乙二醇共聚物（ＤＬ－ＰＬＧ）包裹毒素共调菌毛（ＴＣＰ）抗的,进行免疫学研究,结果表明微轩比游离疫苗诱导的抗体水平高,其中小鼠血清ＩｇＧ以皮下ＭＳ－ＴＣＰ组最高,唾液中的ｓＩｇＡ以口服ＭＳ－ＴＣＰ组最高,口服组主要诱导粘膜免疫,皮下组主要导全身性免疫,ＴＣＰ是霍乱弧菌的共同抗原之一,可作为霍乱疫苗的候选抗原。     

猪背驮式原位肝移植的动物模型

为建立猪背驮式原位肝移植（ＰＢＯＬＴ）模型,共施行ＰＢＯＬＴ１２次。结果表明：１２次ＰＢＯＬＴ术后成活１０头,手术成功率８３３％;平均手术时间７±１ｈ,平均无肝期３４±１２ｍｉｎ,平均失血量１２００±２００ｍｌ。术后各时期病理学检查示移植肝形态结构正常。提示建立猪ＰＢＯＬＴ模型具可行性。缩短无肝期对手术成功有重要意义。     

十二指肠腔内置管引流减压在毕-Ⅱ式胃大部切除术中应用疗效的观察

目的探讨防止毕-Ⅱ式胃大部切除术后十二指肠残端破裂发生的方法;方法对毕-Ⅱ式胃大部切除术中出现十二指肠残端水肿或血运差的病例,采取预防性十二指肠腔内置管引流减压的方法,收集临床资料、观察治疗效果;结果采取十二指肠腔内置管引流减压后,十二指肠残端破裂发生率明显下降;结论十二指肠腔内置管引流减压,可以预防十二指肠残端破裂的发生,并可拓宽溃疡穿孔病例采用胃大部切除术的适应证。     

Design and synthesis of modified quinolones as antitumoral acridones.

The bacterial topoisomerase II (DNA gyrase) and the mammalian topoisomerase II represent the cellular targets for quinolone antibacterials and a wide variety of anticancer drugs, respectively. In view of the mechanistic similarities and sequence homologies exhibited by the two enzymes, tentative efforts to selectively shift from an antibacterial to an antitumoral activity was made by synthesizing a series of modified tricyclic quinolones, in which the essential 3-carboxylic function is surrogated by phenolic OH and the classic C-6 fluorine atom is replaced by a NH2 group. The resulting 7-amino-9-acridone derivatives were assayed for their antibacterial as well as cytotoxic activities. No antibacterial activity was found. On the other hand, many derivatives showed significant cytotoxic activity against both HL-60 and P388 leukemias and a wide panel of human and rodent solid tumor cells, derivatives 25 and 26 displaying the best overall antiproliferative activity. Against the LoVo cell line, derivative 25 exhibited higher cytotoxic effects than etoposide.     

Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones

Dihydropyrimidinones such as compound 12 exhibited high binding affinity and subtype selectivity for the cloned human alpha(1a) receptor. Systematic modifications of 12 led to identification of highly potent and subtype-selective compounds such as (+)-30 and (+)-103, with high binding affinity (K(i) = 0.2 nM) for alpha(1a) receptor and greater than 1500-fold selectivity over alpha(1b) and alpha(1d) adrenoceptors. The compounds were found to be functional antagonists in human, rat, and dog prostate tissues. Compound (+)-103 exhibited excellent selectively to inhibit intraurethral pressure (IUP) as compared to lowering diastolic blood pressure (DBP) in mongrel dogs (K(b)(DBP)/K(b)(IUP) = 40) suggesting uroselectivity for alpha(1a)-selective compounds.     

微细药物表面包覆技术在制剂中的应用

新型药物开发制备过程中，需要对药物颗粒进行粒子设计，通过多层微胶囊化而得到复合包覆药物颗粒。药物包覆、微胶囊制备方法很多，可分为化学法、物理化学法、物理法。本文着重介绍了制备复合多层包覆药物颗粒的几种物理机械方法：复合杂化系统，高速椭圆转子混合法、喷流床包覆法。简要分析了该技术用于中药现代化加工的可能性。     

胃癌患者术后NDV-ATV治疗对机体免疫功能的影响

目的 探讨新城鸡瘟病毒修饰的自体肿瘤疫苗(NDV—ATV)治疗胃病术后患者机体免疫功能的影响。方法 采用流式细胞术分析36例胃病术后(术后2、3、4、5周)NDV—ATV治疗患者外周静脉血T淋巴细胞亚群及NK细胞的变化情况，并以15例术后未接受NDV—ATV治疗的胃癌患者作对照。结果 对照组术后CD3^ 、CD4^ 、NK细胞所占百分比和CD4^ /CD8^ 逐渐升高，以术后3周内升高最为明显。NDV—ATV治疗组，术后CD3^ 、CD4^ 、NK细胞所占百分比和CD4^ /CD8^ 上升速度更快，持续时间更长。治疗结束后与治疗前比较，有非常显著性差异(P＜0．01)；且明显高于未接受NDV—ATV治疗的对照组患者(P＜0．05)。第1次治疗后和治疗结束后相比较有显著性差异(P＜0．05)。结论 NDV—ATV可同时视为1种免疫调节剂，能明显改善胃癌患者术后机体的免疫功能，提高机体抗肿瘤能力。     

大枣多糖的分离、纯化及分子量的测定

大枣果肉用乙醇回流脱脂,80～100℃热水浸提,提取液经减压浓缩,乙醇分级沉淀,三氯乙酸脱蛋白,透析,透析内液再经减压浓缩、醇沉得到三个粗多糖ZJ-A’,ZJ-B’,ZJ-C’,ZJ-B’经DEAE-Cellulose柱、Sephacryl S-300柱反复纯化,得大枣多糖ZJ-1、ZJ-2,高效凝胶渗透色谱(HPGPC)和常压凝胶柱色谱分析表明,ZJ-1、ZJ-2为均一多糖,HPGPC法测定分子量(MW)分别为9848、8991,紫外吸收光谱表明,ZJ-1、ZJ-2无核酸和蛋白质的特征吸收峰。