注射用丹参（冻干）粉针对大鼠脑微循环的影响研究

目的：观察注射用丹参（冻干）粉针对犬鼠脑微循环的影响，扩大注射用丹参的适应证。方法：将大鼠随机分为4组（高、中、低剂量组与对照组）。给予注射用丹参14d后开颅窗，利用高分子葡聚糖造成大鼠实验性微循环障碍模型，观察各组给药后1，8，25，50min时血流量以及各组全血粘度的变化。结果：注射用丹参高剂量和中剂量增加血流量效果明显；与对照组相比，注射用丹参（冻干）粉针3个剂量组均能明显降低血粘度（P〈0．05）。结论：注射用丹参（冻干）粉针对改善大鼠脑微循环和降低血液粘度有重要的意义。     

A Biodegradable Injectable Implant Sustains Systemic and Ocular Delivery of an Aldose Reductase Inhibitor and Ameliorates Biochemical Changes in a Galactose-Fed Rat Model for Diabetic Complications

Purpose. To fabricate and characterize in vitro and in vivo performance of a sustained release biodegradable implant for N-4-(benzoylaminophenylsulfonyl glycine) (BAPSG), a novel aldose reductase inhibitor. Methods. The ability of BAPSG to inhibit aldose reductase activity and glucose-induced vascular endothelial growth factor (VEGF) expression was assessed in a retinal pigment epithelial cell line (ARPE-19). A poly (DL-lactic-co-glycolic acid) implant containing 50% w/w BAPSG was fabricated and characterized for drug loading, in vitro drug release, and the thermal behavior of the drug and the polymer. Implants were injected subcutaneously into a galactose-fed diabetic rat model and cataract scores, plasma and tissue drug levels, galactitol levels in the lens and the retina, glutathione levels in the plasma, lens, cornea and retina and VEGF expression in the retina were determined on or until 18 days. Results. BAPSG inhibited aldose reductase activity and reduced VEGF expression in ARPE-19 cells. Implants (1 × 4 mm), with a loading efficiency of 106 7% for BAPSG, were fabricated. Upon implant fabrication, while the glass transition temperature of the polymer decreased, the melting point of the drug was not affected. In vivo drug release correlated well with in vitro release, with 44% drug release occurring in vivo by the end of 18 days. The implant reduced galactitol accumulation, glutathione depletion, cataract scores, and VEGF expression in galactose-fed rats. Conclusions. An injectable biodegradable implant of BAPSG sustained drug release in vitro and in vivo, and reduced galactitol accumulation, glutathione depletion, cataract scores, and VEGF expression in galactose-fed rats.     

多肽蛋白类药物的长效注射微球突释控制技术研究进展

综述了多肽蛋白类药物长效注射微球突释控制技术的研究进展。探讨了药物结构修饰、载体材料性质、添加剂、制备工艺、微球粒径及载药量等方法对微球突释的影响。     

Delivery of Soluble Tumor Necrosis Factor Receptor from In-Situ Forming PLGA Implants: In-Vivo

Pharmaceutical Research -     

Adverse Reactions to Injectable Soft Tissue Permanent Fillers

Background

Synthetic injectable facial fillers with a permanent effect are widely atoxic and nonimmunogenic, but they differ with respect to composition and in chemical and biologic characteristics. Yet, they all act as foreign bodies in the tissues eliciting a host response that try to remove the gel. Inflammatory nodules may develop at the sites of injection-for some fillers, many years later, for others, not. Why is that?

Methods

Biopsies were contributed by various plastic surgeons from Europe and Australia after requests were made at international congresses and workshops. The study was based on (a) 5 biopsies from unreactive tissue obtained at different times after injection of polyacrylamide hydrogel (Aquamid); (b) 28 biopsies from intermediate or late inflammatory nodules after injection of polyacrylamide hydrogel (Aquamid) (20 cases), a hyaluronic acid-polyhydroxyethylmethacrylate/ethylmethacrylate gel (Dermalive) (2 cases), and a gel consisting of polylactic acid in mannitol/carbomethoxycellulose (New-Fill) (6 cases); and (c) a review of the literature on adverse reactions after injection with permanent fillers.

Results

Clinically unreactive tissues after injection with Aquamid showed modest or no host reaction. Inflammatory nodules showed an increased foreign body reaction and a bacterial infection after injection with Aquamid, and a combination of moderate foreign body reaction, fibrosis, and in some cases also bacterial infection after injection with Dermalive and New-Fill. According to the literature, inflammatory nodules occur no later than 1 year after injection with polyacrylamide hydrogel, but up to 6 years after injection of combination gels (Artecol), and up to 28 years after injection of silicone gel.

Conclusions

Inflammatory nodules are likely to be caused by a low-grade infection maintained within a biogfilm surrounding the hydrophobic silicone gel and the combination gels. Aquamid gel may prevent formation of a biofilm through its high water-binding capacity, explaining why late inflammatory nodules are not seen after injection of this polyacrylamide hydrogel product.     

复合型可注射型骨替代材料在骨缺损临床应用的研究进展

摘要： 目的：总结了各种复合型可注射骨替代材料的特点及其临床应用 资料来源：综述相关文献主要来源于Pubmed 数据库，重庆维普数据库和清华同方数据库 资料选择：选择可注射型骨替代材料的特点和在临床中应用的最新相关文献，排除陈旧及重复实验的相关文献 结局评价指标：以最新的实验结果和研究热点为本综述的结局评价指标 结果：根据最新的相关文献，介绍各种复合型可注射骨替代材料的优缺点和治疗骨缺损的临床疗效 结论：复合型可注射骨替代材料在临床上治疗骨缺损有广阔的应用前景     

注射用利培酮微球的作用机制及临床应用

注射用利培酮微球是第一个非典型抗精神病药长效剂型,于2006年进入我国市场。它采用先进的Med isorb(微球体)专利技术,减少了首过效应,提高了生物利用度,减少了吸收和生物代谢的个体差异;其在体内缓慢均匀释放的特性,使患者能保持稳定的稳态血浆药物浓度,即便长期治疗中漏掉1次注射,体内药物也不会突然中断;该药物临床疗效好、不良反应少、安全性高,使患者有较好的依从性,且具有最佳的成本-疗效效益。文中综述了注射用利培酮微球的药动学、药效学、临床疗效、安全性及药物经济学效益的最新研究进展。     

In vitro and in vivo evaluation of DU6859a,a new fluoroquinolone,among injectable antibacterials tested against clinical isolates

DU6859a was evaluated for its in vitro and in vivo antibacterial activities in comparison with those of imipenem, meropenem, cefpirome, vancomycin, gentamicin, ciprofloxacin and levofloxacin. DU6859a had activity comparable to that of imipenem against methicillin-susceptible staphylococci and penicillin-susceptible and-resistantStreptococcus pneumoniae, with MICs at which 90% of strains tested are inhibited (MIC₉₀)≤0.063μg/mL. Against methicillin-resistant staphylococci and enterococci, DU6859a was as active as vancomycin and more active than other drugs tested, with MIC₉₀s ranging from 1 to 4 μg/mL. DU6859a was as active as ciprofloxacin and more active than other drugs tested against imipenem-resistantPseudomonas aeruginosa. Differences in activity between DU6859a and reference drugs against ciprofloxacin-resistant and gentamicin-resistantP. aeruginosa were particularly striking. The in vivo efficacy of subcutaneous injections of DU6859a against experimental septicemia, respiratory and pyelonephritic infections caused by gram-positive and-negative bacteria, including methicillin-resistantStaphylococcus aureus and imipenem-resistantP. aeruginosa, reflected its potent in vitro activity.     

Development and characterization of novel agar and gelatin injectable hydrogel as filler for peripheral nerve guidance channels

Injectable hydrogels are becoming of increasing interest in the field of tissue engineering thanks to their versatile properties and to the possibility of being injected into tissues or devices during surgery. In peripheral nerve tissue engineering, injectable hydrogels having shear‐thinning properties are advantageous as filler of nerve guidance channels (NGCs) to improve the regeneration process. In the present work, gelatin‐based hydrogels were developed and specifically designed for the insertion into the lumen of hollow NGCs through a syringe during surgery. Injectable hydrogels were obtained using an agar–gelatin 20:80 weight ratio, (wt/wt) blend crosslinked by the addition of genipin (A/GL_GP). The physicochemical properties of the A/GL_GP hydrogels were analysed, including their injectability, rheological, swelling and dissolution behaviour, and their mechanical properties under compression. The hydrogel developed showed shear‐thinning properties and was applied as filler of NGCs. The A/GL_GP hydrogel was tested in vitro using different cell lines, among them Schwann cells which have been used because they have an important role in peripheral nerve regeneration. Viability assays demonstrated the lack of cytotoxicity. In vitro experiments showed that the hydrogel is able to promote cell adhesion and proliferation. Two‐ and three‐dimensional migration assays confirmed the capability of the cells to migrate both on the surface and within the internal framework of the hydrogel. These data show that A/GL_GP hydrogel has characteristics that make it a promising scaffold material for tissue engineering and nerve regeneration. Copyright © 2014 John Wiley & Sons, Ltd.     

注射用微乳的研究进展

微乳是由表面活性剂、辅助表面活性剂、油和水在适当比例下自发形成的透明或半透明分散体系.作为一种新型药物输送载体,除了具有乳剂的一般特征外,微乳还具有粒径小、可过滤灭菌、热力学稳定、黏度低、注射时刺激性小及制备简单等优点,是很多疏水性药物注射给药时的良好载体.本文主要从制备注射用微乳时考虑的各因素、微乳的评价指标,及微乳存在的一些不足等方面对注射用微乳的研究进展做一概括.