新型口服给药技术的研发进展  

Recent Advances in Novel Oral Drug Delivery Technologies

作　　者：朱春柳 俞淼荣 甘勇 ZHU Chunliu;YU Miaorong;GAN Yong(Shanghai Institute of Materia Medica,Chinese Academy of Sciences,State Key Lab.of Drug Research,Shanghai 201203;NMPA Key Lab.for Quality Research and Evaluation of Pharmaceutical Excipients,National Institute for Food and Drug Control,Beijing 100050)

机构地区：[1]中国科学院上海药物研究所,新药研究国家重点实验室,上海201203 [2]中国食品药品检定研究院,国家药品监督管理局药用辅料质量研究与评价重点实验室,北京100050

出　　处：《中国医药工业杂志》2021年第4期429-439,共11页Chinese Journal of Pharmaceuticals

基　　金：国家自然科学基金项目(82003678);国家药典委员会资助项目(2021Y25)。

摘　　要：口服是目前临床最常用的给药途径。但是,受限于药物分子本身的理化性质、药代特征以及人体复杂的生理环境,单纯依靠普通的制剂技术往往难以充分发挥药物分子的临床治疗效果。近年来,随着制药领域新技术的发展,运用纳米晶、脂质制剂、过饱和固体分散体等给药技术,可改善难溶性小分子药物的溶解性,提高其口服吸收;采用吸收促进剂、酶抑制剂等促吸收技术,可有效提高生物大分子药物的胃肠道稳定性和渗透性,从而提高口服生物利用度;对于慢性病治疗药物或治疗窗狭窄药物,缓控释给药技术则可改善其药代动力学特征,实现药物治疗的减毒增效;3D打印、数字化芯片、肠溶微针等新型给药技术的发展,则可更好地满足患者的个性化治疗需求。本文围绕口服促吸收、缓控释及个性化给药技术等方向,综述了新型口服给药技术及其制剂产品的研发进展。At present,oral drug delivery is the most common route for drug administration in clinic.However,due to the intrinsic physicochemical and metabolic properties of drug molecules and the complex physiological barriers in human body,it is difficult to ensure full clinical therapeutic effect just by using traditional formulation techniques.In recent years,with the development of novel pharmaceutical technologies,improved solubility and subsequent increased oral absorption of small molecules are realized by employing nanocrystal,lipid-based formulation,and supersaturated solid dispersion technologies.The strategies for promoting oral absorption,such as absorption enhancers and enzyme inhibitors can efficiently enhance the gastrointestinal stability and permeability of macromolecular drugs,contributing to elevated oral bioavailability.The sustained-and controlled-release drug delivery systems can ameliorate the pharmacokinetic characteristics of chronic disease medications and drugs with a narrow therapeutic window,resulting in reduced toxicity and enhanced efficacy.In addition,the innovative delivery techniques,including 3D printing,digital chips and enteric microneedles can better meet the growing demand for individualized therapy.In this paper,the research and development progress of oral drug delivery technologies and corresponding pharmaceutical preparation products are reviewed with focusing on the pharmaceutical technologies of oral absorption promotion,sustained-and controlled-release,and personalized delivery techniques.

关 键 词：口服给药技术 促吸收技术 缓控释给药技术 个性化治疗 

分 类 号：R944.9[医药卫生—药剂学]