[关键词]
[摘要]
口服给药作为目前中药最普遍的给药方式,具有安全性高、毒副作用低、经济便捷等特点,然而中药成分在口服给药过程中存在吸收差、生物利用度低的问题。为阐明体内-体外药物生物利用度的相关性,生物药剂学分类系统(BCS)根据药物溶解度和透膜性将其分为4类,其中除BCSI类可以有效且稳定吸收外,其余3类皆存在不同程度的低口服生物利用度的情况。现有理论对中药成分生物利用度较低的解释尚不明确,基于此,从叠加作用、协同作用、肠道菌群作用、遗传协同致死及肠道转运体等方面对口服难吸收中药成分的起效机制进行简要综述,以揭示中药有效成分体内起效机制,为诠释中药药效本质提供新思路。
[Key word]
[Abstract]
Oral administration, as the most common way of administration of Chinese materia medica (CMM), has the characteristics of high safety, low toxicity, economical convenience and so on. However, the problem of poor absorption and low bioavailability exists in the process of oral administration of CMM ingredients. In order to elucidate the correlation between in vivo and in vitro drug bioavailability, drugs are classified into four categories according to their solubility and membrane permeability by the biopharmaceutics classification system (BCS). Except for BCSI, which can be effectively and stably absorbed, the other three types have different degrees of low oral bioavailability. The current theory about the low bioavailability of CMM ingredients is not clear. What causes the bioavailability of active ingredients of CMM to be unsatisfactory? How does the effective absorption of CMM ingredients work? Based on the above problems, this paper briefly reviews the mechanism of the poorly absorbable oral CMM from the aspects of superposition, synergy, intestinal flora, genetic synergistic death and intestinal transporter to reveal the effectiveness of CMM ingredients. The mechanism provides new ideas for interpreting the essence of the efficacy of CMM.
[中图分类号]
R285
[基金项目]
国家自然科学基金资助项目(81903933);天津市教委科研计划项目(2018KJ002);天津市第三批人才发展特殊支持计划项目