口服结肠定位给药系统中载体材料和剂型的选择

Selection of the Support Material and Dosage Forms in the Oral ColonSpecific Drug Delivery System

口服结肠定位给药系统(Oral colon-specific drug delivery system,OCDDS)是指通过制剂学手段,使药物口服后在胃肠道上段不释放,而到达回盲肠后,由结肠部位某种生理因素触发,药物开始突释或缓释,用于局部或全身治疗的一种给药系统。与传统口服给药系统相比,OCDDS具有靶向性、控制药物释放、实现结肠局部疾病的治疗以及避开肝脏首过效应等优势。OCDDS按作用机制主要分为pH值依赖型、时间依赖型、压力控制型和酶解型等4种给药系统。目前能实现口服结肠定位的剂型主要有微丸、片剂、胶囊、水凝胶和微球等。文章对OCDDS的触发机制、常用载体材料作了简单探讨,并对这些常见剂型在OCDDS中的应用进行综述,以期为新型OCDDS的研究和开发提供新的思路。

The colon-specific drug delivery system( OCDDS) is defined as a drug delivery system that could make the orally administered drug not release in the gastrointestinal tract segment,but in the cecum in response to some physiological factors in the colon.Novel OCDDS has the advantages of the targeted,controlled-release,realizating the treatment of colorectal localized disease and avoiding hepatic first-pass effect. OCDDS can be divided into four categories,including the pH-dependent,the time-dependent,the pressure-controlled and the enzymatic-type,base on the mechanism. At present,those formulations are able to realize oral colon-specific delivery mainly including pellets,tablets,capsules,hydrogels and microspheres. In this review,the mechanisms for colon-specific drug delivery and the commonly used support materials for colon-specific delivery were addressed. Besides,the main formulations for colon-specific drug delivery were fully discussed in detail with an expectation to contribute to the clinical research and development of OCDDS.