药学学报, 2016, 51(10): 1540-1550
引用本文:
李自强, 何新, 刘昌孝. 基于胃肠道生理驱动的药物溶出/透过特征同步评价技术研究进展[J]. 药学学报, 2016, 51(10): 1540-1550.
LI Zi-qiang, HE Xin, LIU Chang-xiao. Recent advances in drug dissolution/permeation synchronous evaluation technologies based on physiological characteristics of gastrointestinal tract[J]. Acta Pharmaceutica Sinica, 2016, 51(10): 1540-1550.

基于胃肠道生理驱动的药物溶出/透过特征同步评价技术研究进展
李自强1,2, 何新1, 刘昌孝1,3
1. 天津中医药大学中药学院, 天津 300193;
2. 天津中医药大学第二附属医院, 天津 300150;
3. 天津药物研究院, 释药技术与药代动力学国家重点实验室, 天津 300193
摘要:
口服药物制剂在胃肠道的溶出和吸收过程,是一个连续、动态、同步进行的动力学过程,影响着体内生物利用度。药物溶出/透过同步评价技术将体外溶出模型和跨膜透过模型有机结合,连续、动态、同步地解析药物在体内的溶出和跨膜渗透过程,符合“关键路径计划”优先发展领域“开发更好的评价工具”的要求。溶出/透过同步评价技术的研究和应用在逐年增多,但是系统地概述该类技术理论基础及研究近况的相关报道尚不多见。基于此,本文将系统地阐述基于胃肠道多元医学信息驱动的药物溶出/吸收同步评价技术的理论基础、国内外相关模型特点及适用范围等。每个同步评价模型各有特点,研究者应该根据研究目的,选择合适的评价模型。
关键词:    口服药物制剂      溶出      跨膜透过      胃肠道      生物利用度      药代动力学     
Recent advances in drug dissolution/permeation synchronous evaluation technologies based on physiological characteristics of gastrointestinal tract
LI Zi-qiang1,2, HE Xin1, LIU Chang-xiao1,3
1. School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China;
2. Second Affiliated Hospital of Tianjin University of Traditional Chinese Medicine, Tianjin 300150, China;
3. State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China
Abstract:
Pharmacokinetic behavior of orally administrated formulations involves dissolution and absorption in the gastrointestinal tract (GIT), which is required for the systemic effects of a drug. The dissolution and subsequent penetration through the intestinal epithelia is a vital step toward in vivo bioavailability. A lot of effort has been devoted to the study of physiological characteristics of GIT by means of in vitro dissolution methods or in vitro permeation methods. Moreover, drug dissolution/permeation synchronous evaluation technology could be employed to predict the process of drug dissolution and absorption by the combination of dissolution apparatus and permeation apparatus. Better prediction tools are priority in the critical path initiative of US Food and Drug Administration. The studies and applications of the drug dissolution/permeation synchronous evaluation technology are attracting more and more attention each year. However, there is no systematic review on the theoretical basis and the recent development. Therefore, in this review, we will give an overview on the physiological basis and theoretical basis of the drug dissolution/permeation synchronous evaluation technology, as well as their recent advances of this kind of equipments at home and abroad. Moreover, we have also compared their advantages and disadvantages, and the applicable scopes. With hope that the critical path study will promote the development of innovative drug research and development, and improve the druggability.
Key words:    orally administrated formulation    dissolution    permeation    gastrointestinal tract    bioavailability    pharmacokinetic   
收稿日期: 2016-05-04
DOI: 10.16438/j.0513-4870.2016-0427
基金项目: 国家自然科学基金资助项目(81303141);天津市科技支撑重点项目(16YFZCSY00440);教育部创新团队发展计划资助项目(IRT_14R41).
通讯作者: 何新
Email: hexintn@163.com
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