双氯芬酸钠微乳的家兔体内药代动力学考察

目的 :考察双氯芬酸钠微乳在家兔体内的药代动力学过程。方法 :家兔单次口服双氯芬酸钠微乳和双氯芬酸钠混悬液后 ,用 HPL C法测定血中双氯芬酸钠浓度。 结果 :双氯芬酸钠微乳和混悬液的 AU C0 -∞ 分别为 13.45 6和 10 .5 84μg· h· m l- 1 ,cmax 1 为 2 .85 2和 3.145 μg/m l,tmax1 为 1.438和 0 .75 0 h。 结论 :双氯芬酸钠微乳在家兔体内吸收过程较为平缓 ,可在较长时间内维持一定的血药浓度。     

Facile Production of Polypyrrole Nanofibers Using a Freeze‐Drying Method

Conjugated polymer nanofibers with lengths of tens of micrometers and diameters of hundreds of nanometers are prepared via the assembly of polypyrrole (PPy) nanoparticles in water using a freeze‐drying method. The structure and uniformity of the PPy nanofibers are critically affected by the processing conditions, such as the freezing temperature and the concentration of the latex dispersion. These nanofibers are subsequently applied as vapor sensors for efficient detection of organic explosive chemicals.

     

毛细管微乳电动色谱法的研究进展

目的 介绍近年来毛细管微乳电动色谱法的研究和应用进展,为该技术在药物分析中的应用提供参考。方法 通过检索阅读毛细管微乳电动色谱的文献报道,对微乳电动色谱在正辛醇-水分配系数（logP）测定、天然产物和手性化合物分离等方面的应用进行总结。结果 毛细管微乳电动色谱对于难溶性物质和复杂混合物的分离具显著优势,同时是目前报道的测定logP值最为简便快速准确的色谱方法。微乳液的微观结构分析尚需进一步深入研究。结论 毛细管微乳电动色谱兼具色谱和电泳分离的特点,应用范围较广,可以同时分离水溶性、脂溶性、酸性、碱性及中性物质。但毛细管微乳电动色谱分析的稳定性和重复性还有待提高。     

Holographic Characterization of Protein Aggregates in the Presence of Silicone Oil and Surfactants

Characterizing protein aggregates in the presence of silicone oil is a long standing challenge for the pharmaceutical industry. Silicone oil is often used as a lubricant in devices that deliver and store therapeutic protein products and has been linked to protein aggregation, which can compromise a drug’s effectiveness or cause autoimmune responses in patients. Most traditional technologies cannot quantitatively distinguish protein aggregates and silicone oil in their native formulations for sizes less than 5 μm. We use holographic video microscopy to study protein aggregation to demonstrate its capability to quantitatively distinguish protein aggregates and silicone oil in the presence of varying amounts of the surfactants SDS and polysorbate 80 in the size range of 0.5-10 μm without the need for dilution or special sample preparation. We show that SDS denatures proteins and stabilizes silicone oil. We also show that polysorbate 80 may limit protein aggregate formation if it is added to an IgG solution before introducing silicone oil.     

Synthesis of Hyperbranched Polymers via Metal‐Free ATRP in Solution and Microemulsion

Atom transfer radical polymerization (ATRP), as one of the most successful controlled radical polymerization techniques, has been broadly used by polymer chemists and nonspecialists for synthesis of various functional materials, although the use of copper as traditional catalyst often results in undesired color or properties. The first homopolymerization of an initiable monomer, that is, inimer, is reported via metal‐free ATRP using 10‐phenylphenothiazine (Ph‐PTH) as photocatalyst in both solution and microemulsion media. Although polymerizations of inimers in both media can be carried out, only the microemulsion polymerization of methacrylate‐based inimer 1 effectively confines the random bimolecular reaction within each segregated latex and produces hyperbranched polymers with high molecular weight and low polydispersity. Several experimental parameters in the microemulsion polymerization of inimer 1 are subsequently studied, including the Ph‐PTH amount, the solids content of microemulsion, and the light source of irradiation. The results not only provide an effective method to tune the structure and molecular weights of hyperbranched polymers in confined‐space polymerization, but also expand the toolbox of using metal‐free ATRP method for synthesizing highly branched polymers in controlled manner.     

微乳液多重PCR基因芯片法在早孕期无创性胎儿性别诊断中的应用

目的 探讨微乳液多重PCR基因芯片法在早孕期无创性胎儿性别诊断中的应用价值。方法 收集138例4—12孕周孕妇的外周血液样品，提取血浆DNA。选取胎儿DNAY染色体上的6个特异性序列SRY1、SRY2、SRY3、DYS1、DYS14和DYZ3基因作为男性胎儿标志物，采用微乳液PCR进行扩增，同时标记荧光，以β-globin基因作为阳性内对照。扩增产物与固定在基因芯片上的探针分子杂交，采用ScanArray 5000扫描仪扫描芯片。检测结果与胎儿出生性别进行比较。结果 最早的检出样品来自孕31d的孕妇，在78份男性胎儿孕育者血样中，有76份样本6个Y染色体特异序列均为阳性；60份女性胎儿孕育者血样中没有一个Y染色体特异序列阳性。微乳液多重PCR基因芯片法对男性胎儿早孕期检测的灵敏度达到97．4％，特异度达到100％。结论 微乳液多重PCR基因芯片法检测孕妇外周血中男性胎儿DNA的方法具有较高的灵敏度和特异度，能够早期鉴定胎儿性别，对性连锁遗传病的筛选具有潜在的应用价值。     

Lipid Microemulsions for Improving Drug Dissolution and Oral Absorption: Physical and Biopharmaceutical Aspects

Purpose. This review highlights the state-of-the-art in pharmaceutical microemulsions with emphasis on self-emulsifying systems, from both a physical and biopharmaceutical perspective. Although these systems have several pharmaceutical applications, this review is primarily focused on their potential for oral drug delivery and intestinal absorption improvement. Methods. Physicochemical characteristics and formulation design based on drug solubility and membrane permeability are discussed. Results. Case studies in which lipid microemulsions have successfully been used to improve drug solubilization/dissolution and/or intestinal absorption of poorly absorbed drugs/peptides are presented. Conclusions. Drug development issues such as commercial viability, mechanisms involved, range of applicability, safety, scale-up and manufacture are outlined, and future research and development efforts to address these issues are discussed.     

Retinoids: new use by innovative drug-delivery systems

Background: Retinoids represent an old class of bioactives used in the treatment of different skin pathologies (such as acne and psoriasis) and in the treatment of many tumors. Unfortunately, they present several side effects, i.e., burning of skin and general malaise after systemic administration and they are very unstable after exposition to light. Methods: One of the most promising new approaches for reducing the side effects of retinoids while improving their pharmacological effect is the use of drug-delivery devices. This review explains the current status of retinoid drug transport, which has been developing over the last few years, explaining the modification of their biopharmaceutical properties in detail after encapsulation/inclusion in vesicular and polymeric systems. Results/conclusion: Different colloidal and micellar systems containing retinoid drugs have been realized furnishing important potential advancements in traditional therapy.     

反相微乳制备的影响因素考察及处方优化

目的:考察油相、乳化剂和药物对反相微乳形成的影响。方法:采用伪三元相图法,考察乳化剂为司盘-80/吐温-80,模型药为胸腺五肽,油相为长链甘油酯、中链甘油酯、非甘油酯等各因素不同组成对反相微乳形成的影响,筛选最优处方。结果:以中链甘油酯为油相制得的反相微乳具有最大的W/O区域面积;确定最终处方为蒸馏水/司盘-80/吐温-80/辛癸酸三甘油酯(2∶3∶6∶9),胸腺五肽溶于水相中较宜。结论:乳化剂及油相组成、药物均对反相微乳的形成有影响,实际制备中应对各因素水平进行优化。     

复方藁本内酯微乳的制备和含量测定

目的:制备复方藁本内酯微乳并测定其主要成分藁本内酯和桂皮醛的含量.方法:制备复方藁本内酯微乳,HPLC法测定其主要成分含量.色谱柱为Inertsil ODS-3 (250 mm×4.6 mm,5μm).测定藁本内酯时流动相为乙腈∶甲醇∶水(10∶60∶30),柱温为5℃,检测波长为280 nm;测定桂皮醛时流动相为甲醇∶水(60∶ 40),柱温为25℃;检测波长为290 nm.流速均为1.0 ml·min-1.结果:藁本内酯在0.50 ～50.00 μg·ml-1(r =0.999 9),桂皮醛在1.30 ～130.18 μg· ml-1(r =0.999 8)范围内线性良好,藁本内酯的回收率为99.65％,RSD为0.97％(n=9);桂皮醛的回收率为99.81％,RSD为0.62％(n=9).结论:复方藁本内酯微乳制备简单,以HPLC方法测定其主成分含量快速,准确,可靠.