Long-term sustained-released in situ gels of a water-insoluble drug amphotericin B for mycotic arthritis intra-articular administration: preparation,in vitro and in vivo evaluation

Amphotericin B (AMB) was often used in intra-articular injection administration for fungal arthritis, because it could often bring a satisfactory therapeutic efficacy and a minimum systemic toxic side effect. However, because of the multiple operations and the frequent injections, the compliance of the patients was bad. Therefore, to develop a long-term sustained-released preparation of AMB for mycotic arthritis intra-articular administration is of great significance. The purpose of present study was to develop a long-term sustained-released in situ gel of a water-insoluble drug AMB for mycotic arthritis intra-articular administration. Based on the evaluations of the in vitro properties of the formulations, the formulation containing 10% (w/w) ethanol, 15% (w/w) PG, 0.75% (w/w) HA, 5% (w/w) purified soybean oil, 0.03% (w/w) α-tocopherol, 15% (w/w) water and 55% (w/w) glyceryl monooleate was selected as a suitable intra-articular injectable in situ gel drug delivery system for water-insoluble drug AMB. Furthermore, the results of the in vivo study on rabbits showed that the selected formulation was a safe and effective long-term sustained-released intra-articular injectable AMB preparation. Therefore, the presented in situ AMB gel could reduce the frequency of the administration in the AMB treatment of fungal arthritis, and then would get a good patient compliance.     

回收PET共混物的非等温结晶和熔融行为

采用双螺杆挤出机制备了聚丙烯(PP)/回收聚对苯二甲酸乙二酯(r-PET)、r-PET/马来酸酐接枝PP(PP-g-MAH)和r-PET/甲基丙烯酸缩水甘油酯接枝PP(PP-g-GMA)共混物,并研究了共混物组成、熔融温度与时间以及降温速率对共混物非等温结晶与熔融行为的影响.结果表明,r-PET与PP共混,结晶温度均提高,这与组分间起到异相成核诱导结晶作用有关.r-PET结晶温度随PP-g-MAH用量增加而降低,但受PP-g-GMA用量影响较小;r-PET可提高PP-g-MAH结晶温度,但降低PP-g-GMA结晶温度.熔融温度提高,共混物中PP结晶温度和熔点均降低,r-PET熔融峰形和熔点取决于共混物的熔融温度及界面相互作用.     

Fabrication of novel GMO/Eudragit E100 nanostructures for enhancing oral bioavailability of carvedilol

In the present work, novel nanostructures comprising of glyceryl monooleate (GMO) and Eudragit E100 were prepared using high intensity ultrasonic homogenization. 3² Factorial design approach was used for optimization of nanostructures. Results of regression analysis revealed that the amount of GMO and Eudragit E100 had a drastic effect on particle size and percent entrapment efficiency. Optimized carvedilol-loaded nanostructures (Car-NS) were characterized by FTIR, TEM, DSC, in vitro drug release study. Pharmacokinetic parameters such as C_max, T_max, Ke, Ka, V_d and AUC were estimated for Car-NS upon its oral administration in Sprague-Dawley rats. Particle size of Car-NS was found to be 183?±?2.43?nm with an entrapment efficiency of 81.4?±?0.512%. FTIR studies revealed loading and chemical compatibility of carvedilol with the components of nanostructures. DSC thermograms did not show endothermic peak for melting of carvedilol which could be attributed to solubilization of carvedilol in molten GMO during DSC run. The prepared Car-NS released carvedilol in sustained manner over a period of 10 h as suggested by in vitro drug release study. The pharmacokinetic study of Car-NS showed significant improvement in C_max (two fold, p?p?相似文献   

水溶性阿魏酸甘油酯的合成研究进展

含有甘油基的水溶性阿魏酸衍生物具有与阿魏酸相似的生理功能,其水溶性较阿魏酸大.主要对目前含有甘油基的水溶性阿魏酸衍生物的合成方法进行了总结,并对它们的生理功能进行了简单概述,为水溶性阿魏酸甘油酯的应用奠定了理论基础.     

Use of ultra-thin cross-linked polymer films for preparation of stable mono-dispersed carbon nanotubes

We report on the use of ultra-thin cross-linked polymer films to coat carbon nanotubes (CNTs). When n-dodecyl glyceryl itaconate, an amphiphilic monomer, and N,N'-methylenebis(acrylamide), a cross-linker, were mixed with CNTs, an ultra-thin cross-linked DGI polymer film formed on the surface of the individual CNTs by self-assembly polymerization. The CNTs modified with the cross-linked DGI polymer film are highly soluble in water with a multi-walled CNT concentration of up to 1 wt.%, providing an attractive approach for preparing stable, mono-dispersed CNT solutions.     

不同结构的非离子型乳化剂对冷冻面团及其面包品质的变化

该研究将三类共八种极性（HLB值）不同的非离子型乳化剂添加到冷冻面团中,通过核磁共振测定冷冻面团的水分状态及变化,用流变仪测定冷冻面团的流变学特性,质构仪和扫描仪分析面包的结构与品质,研究乳化剂的结构对冷冻面团及其面包品质的影响。结果表明：8种乳化剂对冷冻面团及其面包的品质均有改善,司盘类乳化剂改善效果最好。冷冻过程中,面团中的结合水分T21均降低,自由水T23增加;对照组冷冻面团的结合水比例由14.60%降至11.73%,结构差异使添加三类乳化剂的面团中的水分分布和状态变化各异,司盘类面团中结合水分降至13.25%、13.35%和13.15%。同时,与对照组损耗角正切值（tanδ）由0.39增至0.46相比,含司盘60、司盘65和司盘80冷冻面团的tanδ,分别由0.36、0.37和0.37增至0.40。研究结果表明添加该三种司盘的冷冻面团品质更加稳定,它们的面包比容更大,质地更柔软,面包的组织纹理结构更好,为冷冻面团产品的研究和工业化生产提供理论依据。     

Ether lipids based on the glyceryl ether skeleton: Present state,future potential

Lipids from natural sources consist mainly of saponifiable substances, such as glycerides, along with some unsaponifiable lipids, some of which are ether lipids. Typical ether lipids are monoalkyl ethers of glycerin, also called alkyl/alkenyl glyceryl ethers. Alkyl/alkenyl glyceryl ethers have also been reported in marine organisms and in human feces. Several chemical syntheses of such ether lipids have been reported. Typical examples are alkyl glyceryl ether formation by the addition reaction of alkyl glycidyl ether and the telomerization reaction of butadiene with glycerin and a transition metal catalyst. Characteristic chemical structures, such as terpene alkyl glyceryl ethers, archaebacterial macrocyclic ether lipids, and glyceryl ethers of condensed cyclic planar molecules, have been obtained as well. Over the past few decades, industry has shown much interest in the chemistry and application of highly branched fatty acids. For example, isostearyl glyceryl ether (GE-IS) with methyl branching in the middle chain was already known, but it is now prepared at an industrial scale by proprietary alkyl glycidyl ether methods. The characteristic behavior of GE-IS toward water, such as formation of water-in-oil emulsions containing large amounts of water and of liquid crystals, has made it applicable for use in hair and skin-care cosmetics. Based on these studies and considerations, glyceryl ether lipids, which are rarely investigated, may become one of the most important and useful lipids in the industry.     

多元醇对白炭黑填充NR胶料性能的影响

研究了多元醇品种及其用量对白炭黑填充NR硫化胶性能的影响。试验结果表明,多元醇能促进白炭黑填充NR胶料硫化,二甘醇的活性最高,硫化速度最快,物理性能最优,其次分别为三乙醇胺、乙二醇、聚乙二醇、丙三醇、每种多元醇都存在各自的最佳用量,二甘醇、乙二醇、聚乙二醇、丙三醇和三乙醇胺的最佳用量分别为：2.0,2.0～3.0,2.2,1.8～2.2和3.0～3.2份。     

高性能欠平衡泡沫钻井液体系的研究

针对欠平衡泡沫钻井时可能遇到的高温、高浓度地层盐水和油类物质污染问题,研究出了高性能泡沫钻井液体系,并评价了该体系的泡沫性能以及抗高温、耐盐和油类物质污染性能。该体系是以抗高温、耐盐和起泡能力强的烷基甘油基醚磺酸盐类表面活性剂AGS-8、AGS-10和茶皂素按质量比为4∶6∶5复配得到的AGSS起泡剂体系为基础,进一步加入2%的黏土和0.3?367-Ⅱ而得。实验结果表明,高性能泡沫钻井液体系具有起泡能力强、泡沫稳定的性能,并表现出良好的抗高温、耐盐和抗柴油污染能力强的特点,可有效阻止欠平衡泡沫钻井时因事故停泵而引起钻屑沉降卡钻等事故。