Fe_3O_4/羧甲基壳聚糖磁性载药微球的制备及释药性能

通过乳化交联法制备了负载有抗癌药物5-氟尿嘧啶的Fe3O4/羧甲基壳聚糖磁性载药微球。利用红外光谱(IR)和扫描电镜(SEM)对载药微球的结构与形貌进行了表征,研究了影响载药微球载药和释药性能的因素。IR测试显示载药微球中含有磁性Fe3O4;SEM照片显示载药微球尺寸均一,表面光滑。确定制备磁性载药微球的最佳条件为:5-氟尿嘧啶0.5g、磁性Fe3O40.2g、戊二醛8mL;磁性载药微球在温度为35~40℃、pH值为5.2的缓冲溶液中释药量达到峰值,适用于人体十二指肠肿瘤的治疗。     

丝素-羟丙基壳聚糖微球的结构和释药性能

以胰岛素为目标药物,以丝素(SF)和羟丙基壳聚糖(HPCS)为包药材料,复凝聚法制备SF-HPCS载药微球。采用红外光谱(FTIR)、扫描电镜(SEM)、X射线衍射(XRD)、热重分析(TGA)等对载药微球的结构、外部形貌及热性能等进行了表征。结果表明,所制备的载药微球表面密实,平均粒径22.4μm,呈正态分布;载药微球对胰岛素的包埋率达73.6%,大于HPCS载药微球(64.3%)及壳聚糖(CS)载药微球(57.1%);SF-HPCS载药微球在人工胃液中4h内累计释药率为21.3%,在人工肠液中24h内累计释药率达81.2%,48h累计释药率为92.2%,释放过程平稳、缓慢。     

羟基磷灰石空心微球的制备及其释药性能

以直径200～500 μm的帕拉胶微球(Paraffin micro-spheres)为模板,采用浸渍法制备了羟基磷灰石(hydroxyapatite,HA)空心微球,观察了HA空心微球的形貌特征,并研究了其药物释放性能.结果表明:HA呈良好的空心球结构,外径300～600 μm,壁厚32～81 μm,有较大的内腔,且表面有大量1～8 μm的微孔;样品对药物阿莫西林的装载量为104 mg/g时,在模拟体液中的释药时间持续可达400 h,说明HA空心微球具有药物缓释作用.     

蒙脱石微球的可控制备及其载药性能

针对口服给药体系如何保护药物分子免受人体内环境影响这一挑战,采用乳化凝胶法设计合成了一种pH值敏感性的海藻酸钠(SA)–蒙脱石(MMT)复合微球MMT/SA,用以负载抗癌药物盐酸阿霉素(DOX),在保护药物分子的同时克服了胃肠道的生物化学屏障。探索了MMT处理工艺和合成配比的不同对微球形貌的影响,最终控制微球尺寸在20μm以内,且分布均一。复合载药微球DOX/MMT/SA的载药率为14.7%,在模拟人工胃液和人工肠液环境中表现出不同的药物缓释效果,在模拟人工肠液中的累计释放率(31.7%)明显高于在人工胃液中的释放率(15.8%),且对人结肠癌细胞有明显的杀伤效果。     

魔芋接枝丙烯酸-丙烯酰胺/高岭土复合材料的制备及其释药性能

采用溶液聚合法制备魔芋接枝丙烯酸-丙烯酰胺/高岭土复合材料.正交试验分析表明,当高岭土质量为丙烯酸质量的20％、聚合温度为80℃、丙烯酸中和度为70％、聚合时间为90 main、丙烯酰胺与丙烯酸质量比为1∶2时,制备得到的魔芋接枝丙烯酸-丙烯酰胺/高岭土复合材料的吸蒸馏水倍率最高,为506.2 g/g.以布洛芬为模型药...     

替米考星β-CDP载药微球的制备及释药性能研究

采用共沉淀法制备了替米考星β-CDP载药微球,讨论了投药比、反应时间、反应温度对替米考星β-CDP载药微球的影响,并探讨了其体外释药情况,运用红外光谱仪、电镜、粒度分析仪对产物进行了表征。结果表明,在β-CDP微球质量为3g、替米考星质量为0．25g、反应温度为50℃、反应时间为1．0h、搅拌速度为400r·min^-1的条件下制得的载药微球的产率为81．60％、包封率为66．05％。替米考星β-CDP载药微球粒径分布均匀,外观圆整,在pH值为7．4的PBS中释药效果较好。载药微球释药与Korsmeyer—Peppas方程有较好拟合。     

阿司匹林-壳聚糖缓释微球的制备和释药性能研究

采用乳化交联法制备阿司匹林-壳聚糖缓释凝胶微球,通过透析实验检测微球的体外释放特性。应用正交实验设计,考察了壳聚糖浓度,搅拌速度,阿司匹林/壳聚糖质量比,交联时间对微球制备的影响。体外释放实验表明,壳聚糖微球前5个小时的释放符合SRP的释药行为。以5个小时的体外释放总量为指标进行直观分析,交联时间对5小时的体外释放总量影响最大。     

壳聚糖／羧甲基纤维素钠多层复合载药微囊的制备及其体外释药性能初探

文章以戊二醛为交联剂制备得到以利福平（PEP）为核,壳层材料次序为CS和CMCNa交替的多层复合载药微囊,并考察了微囊的释药机制和囊材层数对体外释药的影响。结果表明,制备的多层复合微囊球形规整,表面光滑,平均粒径约为8．44±454μm。药物被很好地包埋在多层微囊囊芯中,释药方式主要以扩散作用进行,囊材层数增加,药物的缓释性能明显。     

壳聚糖烷基化改性及其纳米微球负载扑热息痛的研究

将低分子量壳聚糖经长链烷基在碱性条件下改性制得烷基化壳聚糖衍生物 ,红外光谱研究表明取代反应主要发生在壳聚糖的氨基上 ,透射电镜研究表明该衍生物在水中可自动形成粒径分布在 1 0 0nm左右的纳米微粒。以扑热息痛为模型药物 ,对烷基壳聚糖纳米微球在磷酸缓冲液 (pH =7 4)中体外释放的研究表明 ,在取代度接近的情况下 ,随着烷基链的增长 ,扑热息痛在磷酸缓冲液中的缓释作用得到改善 ,累积达到平衡时的浓度降低。     

载阿霉素聚乳酸多孔微球的表征及释药性能

以阿霉素（DOX）为小分子化学药物模型,采用吸附法对聚乳酸（poly-L-lactide,PLLA）多孔微球进行载药,采用场发射扫描电子显微镜（FE-SEM）、傅里叶变换红外光谱（FTIR）、X射线衍射（XRPD）及差示扫描量热（DSC）对DOX-PLLA复合微球的形貌粒径及空气动力学性能、药物及材料的理化性能、载药性能进行表征,并且研究了其载药量、包封率和体外释放性能。结果表明,不同载药量之间的PLLA多孔微球粒径并无显著差异,均具有良好的空气动力学性能,适合肺部可吸入给药的条件;化学组成未见明显改变,物理结构由结晶态变为无定形态;随载药量的增加（2.9%,4.0%,4.6%）,包封率逐渐降低（56%,51%,44%）;药物的体外释放与原料药相比具有一定的缓释效果,最长释放时间可达5天,表明DOX-PLLA复合微球有望作为缓释制剂用于肺部给药。     

Preparation and in Vivo Evaluation of a Dutasteride-Loaded Solid-Supersaturatable Self-Microemulsifying Drug Delivery System

The purpose of this study was to prepare a dutasteride-loaded solid-supersaturatable self-microemulsifying drug delivery system (SMEDDS) using hydrophilic additives with high oral bioavailability, and to determine if there was a correlation between the in vitro dissolution data and the in vivo pharmacokinetic parameters of this delivery system in rats. A dutasteride-loaded solid-supersaturatable SMEDDS was generated by adsorption of liquid SMEDDS onto Aerosil 200 colloidal silica using a spray drying process. The dissolution and oral absorption of dutasteride from solid SMEDDS significantly increased after the addition of hydroxypropylmethyl cellulose (HPMC) or Soluplus. Solid SMEDDS/Aerosil 200/Soluplus microparticles had higher oral bioavailability with 6.8- and 5.0-fold higher peak plasma concentration (C_max) and area under the concentration-time curve (AUC) values, respectively, than that of the equivalent physical mixture. A linear correlation between in vitro dissolution efficiency and in vivo pharmacokinetic parameters was demonstrated for both AUC and C_max values. Therefore, the preparation of a solid-supersaturatable SMEDDS with HPMC or Soluplus could be a promising formulation strategy to develop novel solid dosage forms of dutasteride.     

微/纳米药物给药系统的研究进展

在过去的几十年中,探索高效的微/纳米给药系统一直是药剂学领域的研究热点。不同的微/纳米颗粒已被用于药物输送的研究,以期实现有效靶向给药,最大限度地减少副作用,从而提高治疗效果。本文主要综述了微/纳米药物输送给药系统及在药物制剂领域应用。     

壳聚糖-琼胶复合微球的制备及其药物释放性能

采用小分子离子交联法制备了pH值敏感的壳聚糖-琼胶复合微球,对壳聚糖-琼胶复合微球的粒径、形貌、pH值敏感性等进行了表征.以茶碱为模型药物研究了壳聚糖-琼胶复合微球的药物释放性能,结果发现一定量琼胶的引入有助于改善壳聚糖微球的药物缓释性能.     

聚乳酸载药系统的研究进展

聚乳酸及其共聚物由于其生物相容性和生物可降解性,被广泛应用于医药和生物学领域。文章就国内外对聚乳酸及其共聚物作为新型载药系统的研究,进行了归纳总结。旨在说明聚乳酸作为药物载体的优势和发展前景。     

基质型经皮给药缓释贴片的体外释放研究

研究了基质中雌二醇 (E2 )的质量分数wE 对透皮贴片的释放影响。实验结果表明E2 的释放度在wE 为 1 5 %～ 3%是相近的 ,不受wE 的影响 ;wE 提高 1倍 ,累计释药量平均提高 80 %。动力学研究表明 ,前 12h内 ,释放度满足Higuchi公式 ,即与t1/2 成线性关系 ;12h后与t0 .7成线性关系 ,为非Fick扩散     

Sweet Potato Starch Microparticles as Controlled Drug Release Carriers: Preparation and In Vitro Drug Release

The aim of this study was to investigate the in vitro drug release behavior of sweet potato starch (SPS) microparticles intended for controlled drug delivery applications. Diclofenac sodium (DS) was used as a model drug candidate in the present study. SPS microparticles were prepared using a spray-drying technique by varying the polymer concentration and drug loading. The mean particles size of drug-loaded spray-dried SPS microparticles was between 10.3 and 13.1 µm. The mean particle size increased slightly with increase in the concentration of SPS. The mean particle size of spray-dried SPS microparticles increased from 10.3 to 13.1 µm when the concentration of SPS increased from 2 to 4% w/v. Under the current spray-drying conditions, the percentage yield of spray-dried SPS microparticles did not vary much among the various formulations and it was between 65.2 and 70.1%. The encapsulation efficiencies of SPS microparticles formulations was between 95.1–98.2%, suggesting good encapsulating ability of the SPS polymer by spary drying. Drug release from all the formulations of spray-dried SPS microparticles was controlled over period of 6 h. The cumulative amount of drug release from the spray-dried SPS microparticles decreased with an increase in the concentration of SPS, while it increases as the drug loading is increased. Release of the drug from spray-dried SPS microparticles followed Fick's law of diffusion since a good correlation coefficient (R²) was observed with the Higuchi plots (R² = 0.9928 to 0.9979).     

药物控释体系的研究与控释技术进展

介绍了药物控释体系的种类、作用机理及控释技术最近进展 ,指出发展控释技术意义重大     

Hydrogels Based on 2-Hydroxyethylmethacrylate and Chitosan: Preparation,Swelling Behavior,and Drug Delivery

The authors report preparation of chitosan by deacetylation of chitin extracted from shrimp shells. The quality of chitosan depended on the chemical extraction process, the concentration of chemicals used, soaking time, sequence of deproteination, decalcification, and deacetylation. Hydrogels composed of hydroxyethylmethacrylate and chitosan were subsequently prepared and their swelling and ibuprofen delivery kinetics at various chitosan concentrations were studied. The swelling properties of the network varied with the chitosan concentration. Furthermore, the swelling process followed second-order kinetics, while ibuprofen diffusion into the hydrogel showed Fickian behavior.     

智能水凝胶的制备以及在药物缓释方面的研究进展

介绍了温度、pH、电场、磁场、光,葡萄糖敏感型智能水凝胶的制备方法以及智能水凝胶在药物缓释控释领域的应用研究进展,并对未来智能水凝胶的发展方向做了展望。