果胶及果胶钙在结肠靶向给药系统中的应用

结肠近端容易产牛病变，如便秘、克罗黑氏病、溃疡性结肠炎和结肠癌等。常规制剂口服后，药物在到达结肠前就会被吸收进入体循环，无法特异性地作用于病变部位。口服结肠靶向给药系统口服后药物在上消化道不释放，到回肓部或结肠才开始崩解或溶蚀释放出来，发挥局部或全身治疗作用。     

结肠靶向给药系统研究概况

本文对结肠靶向给药系统的特点、当前制剂学手段进行介绍与分析，认为结肠靶向给药对便秘、结肠炎、大肠癌等肠道疾病的治疗以及蛋白多肽药物的口服给药都具有重要意义，是一个极具前景的新药研究领域。     

口服结肠靶向给药系统的研究现状

通过查阅献资料，综述了近几年来国内外口服结肠靶向药给系统的研究情况，介绍了口服结肠靶向给药的概念及其优点和结肠靶向给药系统的几种类型：pH依赖型，时滞释药型，菌群触发型及其使用的材料。     

结肠靶向给药系统

本文介绍结肠的特殊生理结构和功能．综述3种结肠靶向给药系统的制备方法及其所用的材料。阐明药物在结肠的吸收和作用机理。     

中药结肠靶向给药系统研究进展

目的对结肠靶向给药(CTDD)系统的相关进展全面综述,探讨其今后的发展方向,为研究人员提供参考与依据。方法查阅国内外19种期刊25篇相关文献,并进行分析、归纳。结果中药CTDD系统包括pH依赖型、时间依赖型、微生物酶解型、生物黏附型、压力依赖型、脉冲型和联合应用型。结论中药CTDD具有广阔的应用前景,但中药指标成分、体内评价等方面的研究还需加强。     

新型结肠靶向给药系统

结肠靶向给药系统已取得一定进展，主要包括：前体药物、pH依赖型、时滞型及菌群触发型等。恰当的结肠给药系统要求释药机制只与结肠的特定生理因素相关。随着研究深入，近年来研发出一些新的结肠给药系统，它们设计原理独特、靶向性强、适合于工业化生产。本文将在回顾以往给药系统的基础上，对这些新的给药系统的制备及其体内外评价进行详细描述。     

结肠吸收及结肠靶向给药

目的：对目前结肠吸收及其靶向给药方面的研究进行综述。方法：讨论药物结肠吸收特点和结肠靶向给药方法。结果：结肠是多肽药物口服的最佳吸收部位和缓控释制度口服持续吸收的重要部位。结肠靶向制剂可用于结肠局部病患的治疗和多肽药物的口服给药。结论：结肠吸收及其靶向给药是有意义而又有许多有待研究的领域。     

口服结肠靶向给药系统的研究概况

口服结肠靶向给药系统具有很多优点,尤其对肠病的治疗。本文综述了口服结肠靶向蛤药系统的机制、类型的研究概况。     

结肠靶向给药系统的研究

２０年前 ,人们对用于溃疡性结肠炎的药物吡柳磺胺 (Ｓｕｌｆ＿ａｓａｌａｚｉｎｅ)的作用方式已经有了充分的了解 ,并且发现口服轻泻剂只有到达大肠后才发挥作用。因此 ,人们对结肠靶向给药产生了兴趣 ,并且不断地开发各种结肠靶向给药系统［１］。升结肠和大部分横结肠只有口服途径能接触到 ,直肠给药很少能把药物运送到结肠 ,所以发展口服结肠靶向给药系统具有重要意义。口服结肠靶向给药系统中的药物在上消化道中不释放 ,只有当药物到达人体回盲部后 ,才能使给药系统把药物释放出来 ,并且在结肠部发挥局部或全身治疗作用。１结肠靶向给…     

结肠靶向给药系统研究进展

通过查阅国内外文献综述近年来国内外结肠靶向给药的研究动态,结肠靶向给药系统的几种类型：ｐＨ依赖型,时滞释药型和菌群触发型及其所使用的材料。介绍了结肠的特殊生理结构和功能,阐明药物在结肠的吸收和作用机理。     

Pectin-based oral drug delivery to the colon

This review presents an overview of studies concerning oral formulations intended for site-specific drug delivery to the colon with pectin as the main excipient. The biological aspects covered include gastrointestinal transit and the enzymatic degradation of pectin. Scintigraphic methods demonstrating the functionality of pectin formulations are discussed. The main focus is on the various formulations reported, including matrix tablets, multiparticulate formulations as pellets and hydrogel beads, and pectin-based coatings. Also included is an evaluation of common excipients employed to improve colon specificity by crosslinking or increasing the hydrophobicity. Finally, properties of the pectin molecules that are important for successful formulations are examined. The conclusion is that the studies found in the literature provide an excellent platform for the development of pectin-based colon delivery systems.     

Pectin-based oral drug delivery to the colon

This review presents an overview of studies concerning oral formulations intended for site-specific drug delivery to the colon with pectin as the main excipient. The biological aspects covered include gastrointestinal transit and the enzymatic degradation of pectin. Scintigraphic methods demonstrating the functionality of pectin formulations are discussed. The main focus is on the various formulations reported, including matrix tablets, multiparticulate formulations as pellets and hydrogel beads, and pectin-based coatings. Also included is an evaluation of common excipients employed to improve colon specificity by crosslinking or increasing the hydrophobicity. Finally, properties of the pectin molecules that are important for successful formulations are examined. The conclusion is that the studies found in the literature provide an excellent platform for the development of pectin-based colon delivery systems.     

纳米药物和纳米载体系统

阐明了纳米技术在药剂学领域中的现状，综述了国内外纳米药物和纳米载体的发展，介绍了纳米药物与纳米载体的尺寸范围、主要类型及其应用、制备技术、载药方法、表面修饰的意义及其在促进药物溶解、改善吸收、提高靶向性等方面的作用和机制，指出了纳米载体在生物大分子药物传输中的潜在应用前景。     

Thermo-responsive systems for controlled drug delivery

Controlled drug delivery systems represent advanced systems that can be tightly modulated by stimuli in order to treat diseases in which sustained drug release is undesirable. Among the many different stimuli-sensitive delivery systems, temperature-sensitive drug delivery systems offer great potential over their counterparts due to their versatility in design, tunability of phase transition temperatures, passive targeting ability and in situ phase transitions. Thus, thermosensitive drug delivery systems can overcome many of the hurdles of conventional drug delivery systems in order to increase drug efficacies, drug targeting and decrease drug toxicities. In an effort to further control existing temperature-responsive systems, current innovative applications have combined temperature with other stimuli such as pH and light. The result has been the development of highly sophisticated systems, which demonstrate exquisite control over drug release and represent huge advances in biomedical research.     

Thermo-responsive systems for controlled drug delivery

Controlled drug delivery systems represent advanced systems that can be tightly modulated by stimuli in order to treat diseases in which sustained drug release is undesirable. Among the many different stimuli-sensitive delivery systems, temperature-sensitive drug delivery systems offer great potential over their counterparts due to their versatility in design, tunability of phase transition temperatures, passive targeting ability and in situ phase transitions. Thus, thermosensitive drug delivery systems can overcome many of the hurdles of conventional drug delivery systems in order to increase drug efficacies, drug targeting and decrease drug toxicities. In an effort to further control existing temperature-responsive systems, current innovative applications have combined temperature with other stimuli such as pH and light. The result has been the development of highly sophisticated systems, which demonstrate exquisite control over drug release and represent huge advances in biomedical research.     

Pharmaceutical plasticizers for drug delivery systems

In the field of pharmaceutical science and drug development, there are important and particular challenges related to the selection of suitable and compatible ingredients as well as the design of successful formulations. As plasticization is a phenomenon widely exploited in all formulation fields, plasticizers should be recognized as a critical aspect for drug delivery. The choice of an appropriate plasticizer requires a wide background of information. This is because they are incorporated into drug delivery systems containing an assortment of ingredients which may have different reactions to the presence of plasticizers. Concurrently, there are numerous pharmaceutical plasticizers and various environmental issues dictating favored solutions. To address these encumbrances, an extensive information concerning plasticizers; their types, properties, pharmaceutical roles, etc. is discussed. Additionally, the specific objective of this review is to substantiate the safety and performance of newly discovered plasticizers.     

胞内酶敏感肿瘤靶向递药体系的合成及应用

目的利用对乳腺癌肿瘤细胞MDA-MB-435内特有酶豆蛋白酶(legumain)敏感的多肽(AANL)连接阿霉素(DOX)构建具有胞内特异性释药功能的纳米递药系统,并对AANL在含有legumain环境下的断裂效率进行研究。方法将DOX用AANL修饰得到AANL-DOX(AD),再将AD连接至4-arm PEG上,最后将细胞穿膜肽(TAT)连接至4-arm PEG-AD上,制备出TAT-PEG-AD并自组装形成纳米粒(TPAD)。核磁表征TAT-PEG-AANL-DOX;粒度分析仪和透射电镜测定纳米粒的粒径及外观形貌;模拟体内、肿瘤微环境和胞内环境通过动态透析法研究legumain对AANL的断裂效率并模拟DOX的药物控释效率;细胞毒性研究TPAD对MDA-MB-435细胞的毒性作用。结果核磁共振氢谱证实TAT-PEG-AANL-DOX合成成功;测定TPAD的粒径为126.3 nm;透射电镜(TEM)观察纳米粒结构圆整,粒径为80 nm;24 h的累积释药量为82.2%;体外细胞毒性研究表明,TPAD对MDA-MB-435细胞有较好的杀伤作用,其效果接近游离DOX的细胞毒性。结论利用legumain敏感多肽连接DOX制备具有胞内特异性释药功能的纳米粒,能够有效实现肿瘤细胞内晚期内涵体和溶酶体精准释药,提高抗肿瘤药物的生物利用度,值得进一步研究。     

口腔黏膜给药系统研究进展

口腔黏膜给药使药物通过颈内静脉直接进入全身循环,避免胃肠道中的酸水解及肝脏首过效应,具有生物利用度高、患者依从性良好的优点。口腔黏膜给药的主要特点是利用生物粘附现象,即生物膜表面与天然或合成聚合物之间的界面分子粘合力现象,延长制剂在生物黏膜表面上的停留时间,以获得更高、更稳定的药物吸收。对口腔黏膜的结构特征、黏膜生物粘附机制、影响黏膜粘附的因素、口腔黏膜剂型设计以及口腔黏膜给药系统的研究进展进行了介绍。