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。     

口服结肠给药系统的研究进展

口服结肠靶向给药系统(oral colon targetting drug deliv-ery system,OCTDDS))将治疗结肠疾病的药物靶向输送至结肠,不仅降低常规的口服或直肠给药的毒副作用,且能将药物输送至病灶处,减少给药剂量,提高患者的顺应性;还能提高多肽、蛋白等类药物口服给药的生物利用度。笔者将近年有关口服结肠给药系统的研究综述如下。1口服结肠释药系统的应用1.1时控给药根据时辰药理学原理,应用药剂手段使药物在一定的时滞后释放,使之与人的生理周期相匹配,可用于治疗哮喘、高血压、心绞痛、消化道溃疡及风湿性关节炎等具有节律性的疾病。结肠靶向给药…     

口服结肠靶向给药系统的研究进展

口服结肠靶向给药系统在药物转运和治疗结肠局部疾病方面具有重要作用。本文总结了口服结肠靶向给药系统近年来的研究概况,并对结肠靶向药物制剂的体内、外评价方法作一介绍。     

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…     

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。     

口服结肠释药系统的研究进展

目的:综述近年来口服结肠释药系统临床和药学研究动态,为今后在此领域的研究和临床应用提供参考。方法:通过对国内外相关文献资料的整理,对比和分析,总结口服结肠释药系统制剂进展和临床应用的发展方向。结果结论:口服结肠释药系统是通过口服给药,在结肠处定位释放药物的靶向制剂。此类制剂以其靶向释药方式和独特的临床使用价值,越来越广泛地引起了临床医生的关注,同时也成为药学研究领域的一大热点。     

口服结肠定位给药系统的研究进展

口服结肠定位给药系统（oral colon—specific drug delivery system，OCDDS）是通过多种制剂技术使药物口服后，在胃及小肠内不释放，只有到达回盲部或结肠部位才定位释放药物的一种新型药物控释系统。利用结肠定位给药系统可将治疗结肠疾病的药物靶向输送至结肠，不仅降低了常规的口服或直肠给药的毒副作用，且能将药物输送至病灶处，可减少给药剂量，提高疗效，从而提高患者的顺应性；同时结肠靶向给药可以避免药物在胃肠道上端被胃肠道酶所降解，提高了多肽、蛋白、疫苗类药物的口服给药的生物利用度。     

结肠靶向给药系统研究进展

结肠靶向给药系统是近年来发展迅速的新型释药技术,它可按时间节律释药．提高药物的生物利用度,降低不良作用。本文对近年来国内外结肠靶向给药系统的几种类型及其所使用的材料．介绍并结肠的特殊结构和功能．阐明药物在结肠的吸收和作用机理作一综述。1口服结肠定位释药系统近十年来受到药学研究者的广泛重视,它不但可用于治疗结肠炎、结肠癌等局部性肠道疾病,还可通过延迟释药方法用于生理节律疾病的治疗．而且在蛋白、多肽类药物的口服吸收上有广阔的前景。短短几年来中,即形成了多种给药类型．并开发了多种靶向性材料。这一给药系统的迅速发展主要基于下列原因：     

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。     

口服结肠靶向释药系统的制备及应用

目的由于在治疗肠道或某些全身性疾病中具有特殊的优点,口服结肠靶向给药系统受到更多的关注。但消化道的复杂性导致影响药物在结肠靶向释药的因素较多,重现性不好。本文对经口服药物结肠靶向释药的生理因素、目前已有的制备技术及应用进行综述。     

Polysaccharides: a targeting strategy for colonic drug delivery

INTRODUCTION: Colon targeting has gained increasing importance for the topical treatment of diseases of the colon, such as Crohn's disease, ulcerative colitis, colorectal cancer and amebiasis. Various strategies used for targeting drugs to the colon include formation of a prodrug, coating with time or pH-dependent polymers, use of colon-specific biodegradable polymers, osmotic systems and pressure-controlled drug delivery systems. Among the different approaches used, polysaccharides that are precisely activated by the physiological conditions of the colon hold great promise, as they provide improved site specificity and meet the desired therapeutic needs. AREAS COVERED: This review aims to summarize the natural and modified properties of polysaccharides that are responsible for their colon targeting abilities. Emphasis is placed on describing formulation approaches that use polysaccharides as a strategy for targeting drugs to the colon. EXPERT OPINION: Polysaccharide-based colon-targeted drug delivery systems are effective when they are precisely activated by the physiological conditions of the colon. Absence of enzymes during colonic disorders might hinder the activation of the delivery system. To guarantee delivery of the drug to the colon, it is preferable to combine polysaccharides with enteric or cellulose polymers.     

Drug targeting to the colon with lectins and neoglycoconjugates

Targeting of drugs to specific sites of action provides several advantages over non-targeted drugs. These include the prevention of side effects of drugs on healthy tissues and enhancement of drug uptake by targeted cells. This review will cover traditional approaches of colon drug targeting as well as the use of lectins and neoglycoconjugates for the targeted delivery. Direct and reverse targeting strategies, potential molecular targets and targeting moieties for colon drug delivery, targeted drug delivery systems (DDS) for colon delivery, anticancer DDS targeted to colon cancer are examined. Directions of future development are discussed.     

Polysaccharides: a targeting strategy for colonic drug delivery

Introduction: Colon targeting has gained increasing importance for the topical treatment of diseases of the colon, such as Crohn's disease, ulcerative colitis, colorectal cancer and amebiasis. Various strategies used for targeting drugs to the colon include formation of a prodrug, coating with time or pH-dependent polymers, use of colon-specific biodegradable polymers, osmotic systems and pressure-controlled drug delivery systems. Among the different approaches used, polysaccharides that are precisely activated by the physiological conditions of the colon hold great promise, as they provide improved site specificity and meet the desired therapeutic needs.

Areas covered: This review aims to summarize the natural and modified properties of polysaccharides that are responsible for their colon targeting abilities. Emphasis is placed on describing formulation approaches that use polysaccharides as a strategy for targeting drugs to the colon.

Expert opinion: Polysaccharide-based colon-targeted drug delivery systems are effective when they are precisely activated by the physiological conditions of the colon. Absence of enzymes during colonic disorders might hinder the activation of the delivery system. To guarantee delivery of the drug to the colon, it is preferable to combine polysaccharides with enteric or cellulose polymers.     

5-氨基水杨酸结肠定位给药酶控释小丸的制备与体外释放

目的：用水分散体包衣技术制备5-氨基水杨酸(5-ASA)结肠定位释放小丸给药系统。方法：乙基纤维素水分散体(Surlease)和直链淀粉(Amylosf)为控释包衣材料，邻苯二甲酸二乙酯为增塑剂，使用流化床包衣设备，制备酶控释的结肠定位释放小丸，研究小丸在模拟人体胃肠道环境中的释放度，并观察游离包衣膜的消化性。结果：此种小丸在模拟胃肠道上部的介质中不释药，在模拟结肠介质条件下3h释药80％以上，10h内释药完全，具有脉冲释药特征。药物的释放时滞由衣膜厚度和衣膜处方组成控制。增加衣膜厚度以及处方中SurleaseE的用量，可延长释药时滞。膜的消化性试验表明，释放机制是衣膜中Amylose被结肠菌酶特异性降解而使衣膜破裂释药。结论：包衣液中加入被结肠酶特异性降解的Amylose可以使小丸具有结肠定位释放的特性。     

Azo chemistry and its potential for colonic delivery

Improved delivery systems are needed for drugs currently in use to treat localized diseases of the colon. One promising approach is to deliver the drugs specifically to the colon, an approach that has gained importance recently in the treatment of these diseases. The advantages of targeting drugs specifically to the diseased colon include fewer systemic side effects, a need for lower doses of drugs, and maintenance of the drug in its intact form close to the target site. The potential for colon-specific delivery of therapeutic proteins and peptides is also of interest. To achieve colon-specific drug delivery following oral administration, the drug needs to be protected from absorption by the upper gastrointestinal tract and from degradation by the upper gastrointestinal tract environment, allowing the drug to be abruptly released into the proximal colon. One strategy for targeting orally administered drugs to the colon exploits carriers that are degraded specifically by colonic bacteria and utilizes microbially degradable polymers/drugs, especially azo-cross-linked polymers/drugs. Prodrugs utilizing azo linkages are sulfasalazine, ipsalazine, balsalazine, and olsalazine. These were developed for delivery of 5-amino salicylic acid to the colon for localized chemotherapy of inflammatory bowl disease. The azo-conjugation approach utilizes the ability of the colonic environment to cleave these conjugates and protects the drug from absorption or degradation in the upper gastrointestinal tract. It is believed that flavin mediators present in the colon and azo-reductase enzymes released from colonic bacteria are responsible for the degradation of azo-aromatic compounds for site-specific delivery of the drug to the colon.     

双分子靶向药物联用的药学监护与分析

摘 要临床药师对晚期结肠癌患者在联用西妥昔单抗和阿帕替尼治疗过程中出现重度皮疹的原因进行分析,开展药学监护,通过查阅相关指南、文献探讨联合使用分别以表皮生长因子受体和血管内皮生长因子受体为靶点的分子靶向药物治疗晚期结肠癌患者的用药安全性,提出合理用药建议,为此类分子靶向药物在临床的合理应用提供参考。     

5-氨基水杨酸结肠定位释药包衣片在狗体内的靶向性研究

目的 考察自制的口服5-氨基水杨酸结肠定位释药包衣片在体内的结肠靶向性。方法 用γ射线显影法考察结肠定位释放包衣片在狗体内的释药部位与释药时间。结果 5-氨基水杨酸结肠定位释药片剂在狗的升结肠崩解释药。结论 5-氨基水杨酸结肠定位释药片具有结肠靶向性。