2-甲氧基雌二醇脂质体的质量评价

目的:对2-甲氧基雌二醇(2-ME)脂质体进行质量评价. 方法:用乙醚注入法制备2-ME脂质体,与原料药相比,体外释药情况的考察. 并从粒径包封率两个方面进行稳定性考察. 结果:体外释药试验表明,与原料药相比,脂质体无突释现象且持续释药, 4℃存放两周稳定性较好. 结论:用乙醚注入法制备的2-ME脂质体质量稳定,可为2-ME的临床应用提供一种新剂型.     

2-甲氧基雌二醇的研究进展

目的 讨论2-甲氧基雌二醇(2-ME)在抗肿瘤作用中的研究进展.方法 通过试验及CNKI期刊全文数据库检索系统,以2-ME、抗癌活性和结构改造为关键词,检索2003-2010年2-ME抗肿瘤作用方面的相关文献.结果 2-甲氧基雌二醇是体内分泌的一种雌性激素,对雌激素受体的亲和力较低,而对多种肿瘤细胞具有抑制作用.结论 ...     

2-甲氧基雌二醇对小鼠急性毒性研究

目的:观察2-甲氧基雌二醇(2-methoxyestradiol,2-ME)灌胃给药的小鼠急性毒性反应。方法:经预试确定按最大给药量法设计试验,小鼠40只,♀♂各半,随机分为给药组和阴性对照组,给药组以2-ME2 000 mg.kg-1为最大给药剂量,40mL.kg-1为最大给药容量,在24 h内一次灌胃,阴性对照组以等容积的纯化水一次灌胃,给药后自由饮食饮水,连续2周观察小鼠体质量、行为活动以及死亡情况。结果:给药组小鼠观察期间内体质量及行为活动异常无变化,未见死亡。结论:2-ME灌胃给药对小鼠急性毒性甚低,提示该药为低毒化学物。     

2-甲氧基雌二醇对CEM细胞增殖的影响及其机制研究

目的研究2-甲氧基雌二醇(2-ME2)对人白血病细胞系CEM细胞的作用及其分子机制。方法采用MTT法检测不同浓度2-ME2处理CEM细胞48 h后细胞的增殖活性;2μmol.L-1 2-ME2处理CEM细胞0、24、48和72 h,采用RT-PCR法检测VEGF和hTERT mRNA的表达情况,Westernblot法检测Akt和p-Akt蛋白表达变化。结果不同浓度2-ME2能够有效抑制CEM细胞增殖,并呈量效关系,2μmol.L-1 2-ME2处理CEM细胞24、48和72 h可降低CEM细胞中的VEGF和hTERT mRNA表达,并降低Akt蛋白磷酸化水平,而总Akt蛋白表达无变化。结论 2-ME2能够有效抑制CEM细胞增殖,其可能作用机制与下调hTERT和部分通过下调VEGF mRNA表达,阻断PI3K/Akt信号通路转导有关。     

2-甲氧基雌二醇大鼠血浆蛋白结合率的测定

目的建立测定2-甲氧基雌二醇大鼠血浆蛋白结合率的方法。方法采用平衡透析法对2-甲氧基雌二醇大鼠血浆蛋白结合率进行HPLC测定。结果高、中、低3个浓度(2、4、8 mg.L-1)的2-甲氧基雌二醇血浆蛋白结合率分别为(85.2±3.4)%、(82.1±5.3)%、(83.0±5.2)%。结论该方法灵敏度高,重现性好,操作简单,能满足生物样品分析要求。2-甲氧基雌二醇大鼠血浆蛋白结合率不具有浓度依赖性,使其临床用药具备较好的安全性。     

2-甲氧基雌二醇抑制骨髓增生异常综合征SKM-1细胞增殖和诱导细胞凋亡

目的 探讨2-甲氧基雌二醇(2-ME)对骨髓增生异常综合征SKM-1细胞增殖和细胞凋亡的影响.方法 常规培养的SKM-1细胞分为2-ME处理组与非处理对照组,SKM-1细胞分别与不同浓度2-ME(1、2、4和8 μmol/L)和对照组共同培养,MTT法检测2-ME对SKM-1细胞增殖抑制作用;光学显微镜观察瑞氏-姬姆萨染色后的细胞形态;流式细胞术分析细胞周期和凋亡;荧光探针JC-1检测细胞线粒体膜电位(△Ψm).结果 2-ME对SKM-1细胞的生长抑制作用具有浓度和时间依赖性;光学显微镜下可见典型的凋亡细胞形态特征;SKM-1细胞被阻滞于G2/M期,表现为Go/G期细胞和S期细胞逐渐减少,G2/M期细胞逐渐增多(P＜0.05＝;2-ME降低细胞△Ψm具有时间依赖性(P＜0.05＝.结论 2-ME对人骨髓增生异常综合征SKM-1细胞的增殖具有显著的抑制作用并可诱导细胞凋亡.其机制可能与细胞G2/M期阻滞和△Ψm下调有关.     

人参皂苷C-K静脉乳剂的制备及理化性质考察

目的研究人参皂苷C K静脉乳剂的处方及制备工艺 ,并对其理化性质进行考察。方法以人参皂苷C K为原料 ,以精制豆磷脂为乳化剂 ,加入适量的辅助乳化剂、稳定剂 ,用正交实验法优化乳剂的处方及工艺 ;用加速实验法考察乳剂的理化性质。结果制备的乳剂符合《中华人民共和国药典》对静脉乳剂的要求 ,经过影响因素试验确定了乳剂的储存条件。结论制备的乳剂性质稳定 ,为乳剂的进一步开发奠定了基础     

HPLC法测定2-甲氧基雌二醇原料药中主药和有关物质的含量

目的:建立测定2-甲氧基雌二醇原料药中主药及有关物质含量的方法。方法:采用高效液相色谱法。色谱柱为AgilentEclipse XDB-C18;流动相为甲醇-水(65∶35),流速为1.0 mL·min-1;柱温为30℃;检测波长为285 nm。结果:2-甲氧基雌二醇与杂质分离度良好,其检测浓度线性范围为45.96～229.8μg·mL-1(r=0.999 8,n=5),检测限和定量限分别为2、10 ng;3批样品的有关物质含量均低于2.0%。结论:该方法准确、快速、分离度好、灵敏度高,可用于2-甲氧基雌二醇原料药的质量控制。     

注射用硫酸头孢匹罗安全性实验研究

［摘要］目的评价注射用硫酸头孢匹罗的安全性。方法采用变态反应实验、静脉血管刺激实验、肌肉刺激实验、溶血实验进行毒理学研究。结果注射用硫酸头孢匹罗对动物无变态反应、无溶血现象，对静脉血管、肌肉无刺激性反应。结论注射用硫酸头孢匹罗在该实验条件下用于注射是安全的。     

1-［1-(6-甲氧基-2-萘基)乙基］-2-(4-硝基苄基)-6,7-二甲氧基-1,2,3,4-四氢异喹啉氢溴酸盐的光降解产物研究

研究1-［1-(6-甲氧基-2-萘基)乙基］-2-(4-硝基苄基)-6,7-二甲氧基-1,2,3,4-四氢异喹啉氢溴酸盐(编号P91024)遇光后颜色变暗的光降解产物。采用HPLC-MS及波谱分析鉴定光降解产物的化学结构，并经有机反应合成对照验证。P91024光降解的3个主要产物分别为溴化N-(4-硝基苄基)-6,7-二甲氧基-3,4-二氢异喹啉、1-［1-(6-甲氧基-2-萘基)乙基］-6,7-二甲氧基-1,2,3,4-四氢异喹啉和2-异丙基-6-甲氧基萘。     

Rational use of intravenous fat emulsions

The composition, effect on blood components, relative value compared with intravenous dextrose, clinical applications as a caloric and fatty acid source, adverse reactions, limitations, and administration of intravenous fat emulsions are reviewed. Fat emulsions provide essential fatty acids and calories and are primarily used to supplement of parenteral nutrition regimens. Their use as a major source of calories remains limited because of cost. However, the trend toward aligning intravenous nutrition to that of the normal diet and the increased demand for peripherally administered parenteral nutrition have increased demand for use. The advantages and disadvantages presented may be used by clinicians to assist in establishing the role of intravenous fat therapy in nutritional support services.     

Bacterial and fungal growth in intravenous fat emulsions

Growth of bacterial and fungal organisms in i.v. fat emulsions was studied. A total of 81 isolates of 15 bacterial and fungal strains were used to inoculate (in test tubes) 10% soybean oil emulsion (Intralipid, Cutter Laboratories), 10% safflower oil emulsion (Liposyn, Abbott Laboratories), trypticase soya broth, and 0.9% sodium chloride at about 2500 organisms/ml. Duplicate samples and negative controls were prepared. Samples were handled under two procedures after inoculation: (1) initially refrigerated overnight, then stored at room temperature for 24 hours, and (2) stored only at room temperature for 24 hours. Samples were taken at 3, 7, and 24 hours after the samples were placed at room temperature, and colony counts were performed. Most organisms grew equally well in the fat emulsions and trypticase soya broth. Fungal strains grew more slowly than bacterial strains but reached equal numbers by 24 hours. Organisms grew quite slowly in sodium chloride, and negative controls showed no growth. These i.v. fat emulsions supported bacterial and fungal growth at the same level as trypticase soya broth.     

儿童静脉输液安全问题的调查与干预模式探讨

目的:探讨药师与临床合作,参与静脉输液安全的管理的模式。方法:采用WHO推荐的监测-培训-计划(monitoring-training-planning,MTP)模式,设计调查问卷,了解临床医生、护士对静脉输液安全用药相关知识认知现况和需求;药师针对调查反馈的信息,对临床医护人员开展相应的培训、编写《静脉输液手册》和搭建静脉输液信息共享平台。结果:通过MTP循环,临床医护人员对静脉输液安全用药相关知识的认知有了显著的提高,药师亦更多地参与静脉输液安全的管理。结论:药师在静脉输液安全管理中可发挥重要的作用。     

药用静脉注射乳剂的研究进展

目的:介绍药用静脉注射乳剂的种类和主要作用,重点介绍药物的种类、作用特点及开发动态。方法:以国内外相关文献为基础进行分析和归纳。结果:药用静脉注射乳剂提高了药物的靶向性和缓释作用,增加了脂肪乳剂的应用范围。结论:药用静脉注射乳剂具有重要的实用价值和应用前景。     

Effect of phospholipid emulsifiers on physicochemical properties of intravenous fat emulsions and/or drug carrier emulsions

The physicochemical properties of soy bean oil emulsions stabilized with purified egg lecithins (phosphatides) of various concentrations have been examined. The zeta potential of the emulsion droplets and the mean particle size of oil droplets in 10% (w/w) o/w-type emulsion decreased with increasing emulsifier concentration and then levelled off at more than 1.2% (w/w). In rheological measurements, at the initial stage, the viscosity of 10% (w/w) o/w-type emulsion gradually increased with increasing purified egg lecithin concentration, at the next stage, a plateau was reached at about 1.0-1.4% (w/w), and at the final stage, the viscosity curve showed a dramatic increase. These results indicate that emulsions stabilized by purified egg lecithin at more than 1.2% (w/w) are likely to be sufficiently stable.     

对静脉注射脂肪乳剂质量影响因素的探讨

通过查阅国内外相关文献,对近几年静脉注射脂肪乳制剂学方面的研究进行分析综合,为静脉注射脂肪乳的工艺研究提供参考.结果表明静脉注射脂肪乳是一些水溶性差的药物的良好载体,用不同处方和方法制备而成的乳剂在制剂质量上有较大差别.影响其制剂质量的因素主要有处方组成和制备方法.     

Investigation of drug-containing multiple phase emulsions

We studied the efficiency of the formation of w/o/w emulsions as a function of composition and mixing time. We found that the concentration of emulsifier 1, the concentration and HLB of emulsifier 2, the viscosity of the oil phase and the external water phase as well as the mixing time in second step of preparing the emulsion characteristically influence the "efficiency" of emulsification and the stability of the emulsions.     

Formulation of intravenous carbamazepine emulsions by SolEmuls technology.

Oil in water (O/W) emulsions for parenteral nutrition can be employed as intravenous (i.v.) carriers for drugs that are poorly soluble in water and in oil by localising the drug in the interfacial lecithin layer, e.g. Amphotericin B emulsions. By now, the emulsion production required organic solvents. SolEmuls technology localises the drug in the interfacial layer by a solvent-free high-pressure homogenisation process. SolEmuls was applied to produce Carbamazepine emulsions at increasing drug concentrations from 0.5 to 10mg/ml. Drug powder and Lipofundin emulsion were mixed and homogenised at 1500bar. Characterisation of emulsions and short-term stability were performed by photon correlation spectroscopy (PCS) and laser diffractometry. Drug incorporation (absence of non-dissolved drug crystals) was investigated by light microscopy and a centrifugation test. The emulsions were physically stable and complete drug dissolution is possible up to 3mg/ml. Up to 10mg/ml drug hybrid dispersions of emulsion droplets and ultrafine nanocrystals were obtained. Both, emulsions and hybrid dispersions are suitable as i.v. injectables regarding size and stability.     

Compatibility of intravenous fat emulsions with prodrug amino acids

Three prodrugs, N-alpha-acetyl-L-arginine, N-alpha-acetyl-L-histidine and N-alpha-acetyl-L-lysine have been examined to see if they could induce significant changes in the stability of an intravenous fat emulsion, the stability being evaluated in terms of physicochemical measurements such as particle size distribution, surface tension, pH and zeta potential. The acetyl amino acids had an excellent stabilizing effect on the emulsion compared with amino acids without acetyl groups.