The preparation and the in-vitro pharmacodynamics study of the intracapsular sustained-release preparations for the prevention of posterior capsule opacification

Docetaxel-loaded sustained-release preparation based on 2-Hydroxyethyl methacrylate(HEMA)and Methyl methacrylate(MMA)cross-linked copolymer(P(HEMA-co-MMA))was prepared to examine the potential use for preventing posterior capsule opacification(PCO).The preparations were prepared by polymerizing the mixture of HEMA,MMA,cross-linking agent(EGDMA),initiator(AIBN)and docetaxel.The influence factors and mechanism of drug release were studied in the experiments.FT-IR,X-RD and SEM methods were used to characterize the polymer(P(HEMA-co-MMA))and docetaxel-loaded sustained-release preparations.Biocompatibility of P(HEMA-co-MMA)and in-vitro effect of docetaxel-loaded sustained-release preparations were also evaluated.The results showed that docetaxel could release sustainedly from these preparations prepared by cross-linking polymerization.And the release rate could be accelerated by increasing the MMA ratio or EGDMA ratio of the polymer.Release mechanism of docetaxel fitted the Higuchi model well.The results of IR and X-RD showed that only a hydrogen bond was formed between docetaxel and P(HEMA-co-MMA).Docetaxel dispersed in P(HEMA-co-MMA)in amorphous form.The elution test showed that P(HEMA-co-MMA)had good biocompatibility and the in-vitro pharmacodynamics study proved that docetaxel could release stably from the preparations and inhibit HLECs’proliferation.The docetaxel-loaded sustained-release preparations proved to be a promising therapy for preventing PCO.These results also lay a theoretical and experimental foundation for the future.

Preparation and Characterization of Potassium Monopersulfate/Ethyl Cellulose Microcapsules and Their Sustained Release Performance

Environmental cleaning is an important aspect of bacteria control.Ethyl cellulose microcapsules containing potassium monopersulfate(PMCM)were prepared by emulsified solvent diffusion method.The chemical structure and microstructure of the obtained PMCM was characterized by methods of Fourier transform infrared spectroscopy(FT-IR),optical microscopy,scanning electron microscopy and X-ACT energy dispersive X-ray spectroscopy.The SEM micrographs of the PMCM containing 21.6%of C,46.8%of O,10.7%of S and 19.4%of K was relatively smooth.Thermal stability,sustained release performance,and antimicrobial activity of PMCM were investigated.The results showed that the drug loading and encapsulation efficiency of PMCM were 30.3%and 42.6%respectively.Potassium monopersulfate was fully released after 8 h,following a Fickian diffusion mechanism.Results showed that the microcapsules prepared with a high concentration of potassium monopersulfate solution showed a good antimicrobial effect.The microcapsule wall of the resulting PMCM increased with increasing ethyl cellulose content and had high thermal stability from the data of 69%residue rate.The excellent thermal stability and high sustained release performance of PMCM showed high application value.

Evaluation of Control Effects against Sugarcane Pests：A New Sustained-release and Long-lasting Pesticide and Convenient and Efficient Pesticide Application Technology

[Objective]The paper was to screen a new ideal sustained-release,long-lasting and low-toxic pesticide and convenient and efficient pesticide application technology for controlling Ceratovacuna lanigera and Baliathrips serratus. [Method]2% Imidacloprid GR were selected and applied in the soil for field efficacy trial. [Result] The optimum dosage of 2% imidacloprid GR was 30 kg/hm^2（ active ingredient 600 g）,which can be mixed with fertilizer（ 30 kg pesticide and 40-80 kg fertilizer per hm^2） once combined with sugarcane planting management or big ridging during February and June. The control effects against C. lanigera and B. serratus could be more than 98. 2% and 81. 1%,respectively. The actual yield and sugar content in various pesticide treatments were increased by 33 390 kg/hm^2 and 6. 6% respectively compared to blank control. [Conclusion]2% imidacloprid GR has good control effects on C. lanigera and B. serratus. It is a new pesticide with ideal sustained-release,long-lasting and low-toxin effects against C. lanigera and B. serratus. Therefore,it could be used alternatively with other pesticides,to delay production and development of drug resistance.

Implementation of a Simulation Model of the Controlled Release of Molecular Species from Halloysite Nanotubes

In this work a three-dimensional, time-quantified Monte Carlo model that efficiently describes diffusion through and from nanotubes is implemented. Controlled delivery from Halloysite Nano-tubes (HNT) is modeled based on interactions between the HNT’s inner wall and the nanoparticles (NPs) and among NPs themselves. The model was validated using published experimental data. The validated model is then used to study the effect of multiples parameter like HNT diameter and length, particle charge, and ambient temperature on the release of encapsulated NPs. The results show that release profiles depend on the size distribution of the HNT batch used for the experiment, as delivery is sensitive to HNT lumen and length. A very good agreement with the experiment is observed when a weighted average release profile is compared to the experimental profile. Although the NP dynamics is temperature-dependent, the effect is minimum within the range of temperatures relevant to biomedical applications, but will be relevant for other applications at temperatures significantly different from room temperature. This model can be used to predict the best conditions for a particular delivery need.

PEGylated PLGA Nanoparticles as Tumor Ecrosis Factor-α Receptor Blocking Peptide Carriers:Preparation,Characterization and Release in vitro

To assess the merits of PEGylated poly （lactic-co-glycolic acid） （PEG-PLGA） nanoparticles as drug carriers for tumor necrosis factor-α receptor blocking peptide （TNFR-BP）, PEG-PLGA copolymer, which could be used to prepare the stealth nanoparticles, was synthesized with methoxypolyethyleneglycol, DL-lactide and glycolide. The structure of PEG-PLGA was confirmed with ^1H-NMR and FT-IR spectroscopy, and the molecular weight （MW） was determined by gel permeation chromatography. Fluorescent FITC-TNFR- BP was chosen as model protein and encapsulated within PEG-PLGA nanoparticles using the double emulsion method. Atomic force microscopy and photon correlation spectroscopy were employed to characterize the stealth nanoparticles fabricated for morphology, size with polydispersity index and zeta potential. Encapsulation efficiency （EE） and the release of FITC-TNFR-BP in nanopartieles in vitro were measured by the fluorescence measurement. The stealth nanoparticles were found to have the mean diameter less than 270 nm and zeta potential less than -20 mV. In all nanoparticle formulations, more than 45% of EE were obtained. FITC-TNFR-BP release from the PEG-PLGA nanoparticles exhibited a biphasic pattern, initial burst release and consequently sustained release. The experimental results show that PEG-PLGA nanoparticles possess the potential to develop as drug carriers for controlled release applications of TNFR-BP.

缓控释肥硅基膜材的制备与表征

以钙镁磷肥、硅丙树脂为主要原料,加入甲基硅酸钠作粘结剂,制备了缓控释肥硅基膜材,并采用撒粉离心包衣、底喷式流化床工艺制备了密封型硅钙镁磷肥、粘结型硅钙镁磷肥、改性硅丙树脂3种包膜尿素,通过静水试验研究了此3种包膜尿素的释放特征。结果表明,3种包膜尿素的释放周期分别为60、79、96 d,在水中均能保持完整球形,耐水性较好。通过扫描电镜、红外光谱、X-射线衍射法对膜材形貌特征和结构进行表征,发现钙镁磷肥和硅丙树脂为成膜材料;甲基硅酸钠作为密封剂和防水剂参与了成膜反应,有效增加了膜材的塑性和韧性,此复合材料可用作缓控释肥的胶结剂和包膜剂。

In situ-prepared homogeneous supramolecular organic framework drug delivery systems(sof-DDSs)：Overcoming cancer multidrug resistance and controlled release

Water-soluble three-dimensional porous supramolecular organic frameworks（SOFs） have been demonstrated as a new generation of homogeneous polycationic platforms for anti-cancer drug delivery.The new SOF drug delivery systems（sof-DDSs） can adsorb dianionic pemetrexed（PMX）,a clinically used chemotherapeutic agent instantaneously upon dissolving in water,which is driven by both electrostatic attraction and hydrophobicity.The in situ-prepared PMX@SOFs are highly stable and can avoid important release of the drug during plasm circulation and overcome the multidrug resistance of human breast MCF-7/Adr cancer cells to enter the cancer cells.Acidic microenvironment of cancer cells promotes the release of the drug in cancer cells.Both in vitro and in vivo studies have revealed that sofDDSs considerably improve the treatment efficacy of PMX,leading to 6-12-fold reduction of the IC50 values,as compared with that of PMX alone.The new drug delivery strategy omits the loading process required by most of reported nanoparticle-based delivery systems and thus holds promise for future development of low-cost drug delivery systems

抗晕动病药物及其缓控释制剂的研究进展

晕动病是指机体在异常运动下受到刺激而引起的一系列生理反应,常见症状有头晕、呕吐等。目前,抗晕动病药物主要有抗组胺药、抗胆碱药、钙拮抗药、拟交感神经药、胃动力药,且多数为普通制剂,而缓控释制剂的研发及应用较少。本文对晕动病的发病机制、治疗药物分类以及抗晕动病药物缓控释制剂,如透皮制剂、鼻用制剂和口服制剂的研究进展进行综述,分析目前晕动病防治研究过程中存在的问题,为抗晕动病药物新剂型的研发提供新思路。

白屈菜总生物碱缓释片制备工艺研究

目的:以羟丙基甲基纤维素为缓释材料制备白屈菜总生物碱缓释薄膜衣片解决白屈菜有效成分药物浓度不稳定的缺点,并建立可靠的含量测定方法。方法:采用单因素实验对白屈菜总碱缓释薄膜衣片制备工艺进行筛选,以释放度为依据;采用高效液相色谱法(HPLC)建立了白屈菜总碱缓释薄膜衣片中血根碱的含量测定方法。结果:优化的缓释片工艺处方:30%白屈菜总碱提取物、30%HPMC、20%可压性淀粉、10%乳糖、10%微晶纤维素,挤压制粒,加1%硬脂酸镁,压片,即得。结论:该工艺制得白屈菜总碱缓释片释药曲线平缓,缓释效果良好,方法简单易行,所得薄膜衣片外观和可压性良好。

马铃薯淀粉膜制备工艺优化及活性包装中百里香酚释放动力学

为提高食品包装中抑菌剂百里香酚(thymol,THY)的生物利用率以延长食品的货架期,该研究采用介孔二氧化硅(mobil composition of matter No. 41,MCM-41)作为THY的控释载体(THY-MCM-41),以马铃薯淀粉为原料制备马铃薯淀粉活性包装膜。利用L_(9)(3^(4))正交试验探究马铃薯淀粉、甘油、氯化钙和THY-MCM-41质量浓度对包装膜机械、物理以及水蒸气阻隔性能的交互影响,优化马铃薯淀粉活性包装膜最佳制备工艺参数,并在不同储存环境下对最优组合活性包装膜中百里香酚的释放动力学进行研究,构建百里香酚释放预测模型。结果表明,当马铃薯淀粉质量浓度为0.04 g/mL,甘油质量浓度为0.015 g/mL,氯化钙质量浓度为0.005 g/mL,THY-MCM-41质量浓度为0.005 g/mL时,制备的包装膜A综合性能最优,其抗拉强度、溶胀度、水蒸气透过率、透氧性和不透明度分别为7.16 MPa、89.23%、1.42×10^(-10)g/(m·s·Pa)、1.02×10^(-15)cm^(2)/(s·Pa)和1.16 mm^(-1)。电子扫描电镜和傅里叶红外光谱分析均证实了THY-MCM-41均匀地分散在马铃薯淀粉膜中,与马铃薯淀粉之间具有良好的相容性。马铃薯淀粉活性包装膜可控制百里香酚的释放速率,将百里香酚的有效作用时间延长到10 d。其中,百里香酚的释放规律符合一级释放模型(R^(2)> 0.980),其释放行为遵循菲克扩散定律。该研究为智能活性包装膜中活性物质的精准控释提供了理论基础。

多杀霉素/羧甲基壳聚糖缓释悬浮剂的制备

基于羧甲基壳聚糖在等电点附近溶解度低的特性,采用pH调节法制备多杀霉素/羧甲基壳聚糖缓释悬浮剂,并初步探究其对小菜蛾幼虫的防治效果。结果表明:缓释悬浮剂适宜的制备条件为羧甲基壳聚糖盐酸溶液质量分数1.0%,多杀霉素甲醇溶液质量分数1.5%,羧甲基壳聚糖与多杀霉素的质量比2∶1,15000 r/min下剪切乳化3 min。缓释悬浮剂呈乳白色,载药量、包封率和中位粒径分别约为25%、74%和48μm,稀释施用时粒径降为约3μm。红外光谱分析表明,羧甲基壳聚糖成功包封多杀霉素,其相互间作用力主要为物理吸附。相对传统悬浮剂,多杀霉素/羧甲基壳聚缓释悬浮剂在防治小菜蛾方面具有优异的速效性和更长的持效期,在多杀霉素减施增效方面具有一定的应用潜力。

大黄素甲醚微囊缓释剂的制备及表征

制备一种大黄素甲醚微囊缓释剂,将大黄素甲醚制成微乳液,提高其溶解度,进一步采用原位聚合法,以密胺树脂作为囊壁,将大黄素甲醚微乳液微囊化。微乳液中大黄素甲醚的溶解度约为5 g/L,明显高于在其他溶剂中溶解度。当囊芯为微乳液(含水量30%),密胺树脂为囊壁,芯壁比(质量比)为3∶1时,所制大黄素甲醚微囊缓释剂的载药量和包封率最高,在水中14 d累积释放率为72.0%,土壤中35 d累积释放率为51.9%。该微囊缓释剂分布均匀、载药量高、释药缓慢持久,用于病害防控可减少给药次数,具有重要的实际应用价值。

葡萄膜炎的缓释治疗给药研究进展

葡萄膜炎病因繁多,发生机制复杂,感染、自身免疫及各种理化和机械损伤因素等均可引起,治疗较为棘手,未得到及时有效治疗常可导致失明。随着人们对葡萄膜炎及其相关机制认识的加深,各种新型的葡萄膜炎缓释治疗给药系统被研究,但是,由于眼部各种解剖学和生理学屏障的存在,使得葡萄膜炎的缓释治疗存在多重阻碍。本文综述了该领域近年来的主要研究成果,讨论了各新型缓释给药系统的创新点和局限性,以期能为未来葡萄膜炎的缓释给药治疗提供新思路。这些新型缓释给药系统有助于在未来彻底改变葡萄膜炎治疗副作用大、依从性差的传统治疗模式,带来更长时间的靶向缓释和更少的毒性反应。

中药缓控释制剂研究进展

目的归纳中药缓控释制剂研究进展,为了解中药缓控释制剂制备工艺、处方和质量评价提供参考。方法通过文献检索,对不同缓控释制剂新类型的优缺点,中药缓控释制剂制备工艺、质量评价体系进行分析。结果缓控释制剂新类型涉及固体脂质纳米粒缓控释制剂、口服渗透泵缓控释制剂、胃滞留给药缓控释制剂、生物黏附微球、固体分散体,制备工艺采用多种筛选方法得出最佳工艺,中药缓控释制剂的质量评价方法包括体外释放度研究、体内释药和体内外相关性研究等。结论中药缓控释制剂研究主要集中在中药单体成分、中药提取物或有效部位、中药多个单体成分组合开发的中药制剂,质量评价体系主要有体内释放度、体外释放度和体内外相关性研究,可为中药缓控释制剂发展提供参考。

口服液体缓控释制剂技术的研究进展

目的针对各类口服液体缓控释技术的释药机理、应用特点及局限性进行综述,为此类制剂的开发提供参考。方法查阅国内外相关文献,对口服液体缓控释技术进行整理归纳。结果目前已有基于离子交换树脂和微囊技术的口服液体缓控释制剂上市,此外,微球、固体脂质纳米粒、原位凝胶等技术也应用于口服液体缓控释制剂领域。结论口服液体缓控释给药系统相比于传统固体缓控释制剂,因其口服可接受性良好,剂量调整灵活,给药依从性优势明显,具有良好的开发应用前景。

外加电压对原位缓释碳源释碳效果影响的研究

为改善城市污水处理厂外加碳源成本高、产泥量大等问题,利用废弃纸屑与纤维素降解菌为原料制备投加型缓释碳源,并通过控制外加电压调控碳源释放速率。研究结果表明,在0.4 V的电压下,释碳微生物的响应效果最为显著。高通量测序结果显示,外加电压能够显著抑制产酸菌活性,而促进电活性菌丰度增加,证明外加电源的方法可通过调控功能微生物的群落结构及活性来控制碳源释放情况,可为进一步优化污水处理工艺自动化控制及碳源投加方式的选择提供理论依据与技术支撑。

甜橙香精微胶囊的制备及缓释性能研究

为了改善香精微胶囊的缓释性能、提高香精利用率,以甜橙香精为芯材、六亚甲基二异氰酸酯(HDI)三聚体为合成壁材的单体、聚乙二醇(PEG)和石墨烯(GR)作为温控材料,利用界面聚合法制备温控香精微胶囊(egHDI-O),考察芯壁比、剪切乳化机的转速、温控组分对甜橙香精微胶囊形貌、组成、芯材含量和缓释性能的影响。结果表明:在甜橙香精微胶囊芯壁比为1∶2,转速为8000 r/min,乳化剂为吐温80,PEG和GR用量分别为200 g/L和5 g/L工艺条件下制备的egHDI-O具有良好的形貌和均匀的粒径,其芯材含量(质量分数)可达74%;相比于未添加PEG和GR的微胶囊,egHDI-O具有优良的温控性能。研究为开发新型温控缓释赋香材料提供了新思路。

可注射奥沙利铂缓释微粒制备及其理化性质研究

目的:开发可注射奥沙利铂缓释微粒,并对其制备工艺和理化性质进行研究。方法:采用热熔挤出-冷冻研磨工艺制备可注射奥沙利铂缓释微粒,使用扫描电镜、粒度分析仪了解微粒形貌及粒径分布,采用液相色谱系统测量缓释微粒中奥沙利铂含量和微粒体外释放度。结果:可注射奥沙利铂缓释微粒粒度分布曲线稳定,微粒中奥沙利铂包封率为46.8%,包封率高;体外释放结果显示,奥沙利铂缓释微粒释放周期为144 h,最终释放度在80.0%以上,具有缓释性能;缓释微粒注射剂pH值在6.18~6.45的范围内,不会对注射部位造成损伤。结论:通过热熔挤出-冷冻研磨工艺制备的可注射奥沙利铂缓释微粒粒径分布均匀、药物包封率高,并且具有优异的缓控释特性以及稳定的理化性质。

眼用微片的研究进展

微片是一种新型的微型固体片剂,具有刺激性小、患者依从性高、作用时间长、生物利用度高等优点。眼用微片作为微片的一类,既可避免频繁给药,又可提高患者舒适度。微片制剂是目前研究的热点,眼用微片更是具有广阔的研究前景。本文主要阐述了眼用微片的特点和近年来国内外眼用微片的相关研究,并从多角度对眼用微片的影响因素及研究前景等进行总结叙述。

微球制剂的研究进展

近年来,因生物可降解高分子材料制备的载药微球制剂可以进行缓控释放给药而备受关注,是当前高端新型药物制剂的研究热点。制备微球制剂的关键因素在于选择合适的高分子材料和生产工艺技术。然而,微球的制备工艺繁杂、质量控制困难,至今只在少数产品上应用,现在越来越多的口服难吸收的生物药物开始产品化,缓释微球在提高患者依从性方面备受瞩目。通过文献研究,对目前较为经典的微球制备技术和一些制备微球的新技术进行了综述分析,并总结了微球制剂的形态、大小及颗粒分布,载药量和包封率,释放度等质量评价相关成果,以期为微球制剂的研究提供一定的参考价值。