中药汤剂微粒体系对有效成分吸收的影响及机制研究

汤剂是中医治疗疾病的主要药物剂型之一，很多理论上口服难以吸收的中药活性成分以汤剂形式给药往往生物利用度较好。口服微粒给药系统可以显著提高药物的吸收已经得到了广泛的证实，然而汤剂在煎煮过程中形成的固体微粒体系对中药有效成分在胃肠道的吸收与转运是否存在作用以及作用机制均不明确。本课题分别选择以水溶性差或生物稳定性差的黄芪甲苷、小檗碱与绿原酸为主要药物活性成分的药材黄芪、黄连与金银花为研究对象，经常规手段水煎煮后除净药渣，对水煎液中具有不同理化性质（粒径、表面电荷、亲疏水性等）的微粒进行系统分离，经体外Caco-2单层细胞膜、离体翻转肠囊、原位肠循环灌注、原位肠袢等实验手段评价水煎液中微粒体系理化性质对活性成分吸收与转运的调节作用，并分析其机制。本课题的实施将有助于阐明中药煎煮过程中微粒形成特点及其对中药有效成分吸收的影响与机制，为诠释中药汤剂的科学内涵与开发中药新剂型提供有益的理论及应用基础。

Decoction of traditional Chinese medicine is one of the main formulations in traditional Chinese medicine treatments. Although many kinds of active ingredients of Chinese medicine can theoretically not be absorbed by the means of oral administration, the bioavailability are often very good through the decoction form. It is well documented that the drug absorption, especially the macromolecular drug absorption, can be significantly enhanced by oral particles drug delivery system. The effect and mechanism of particle systems in decoction of traditional Chinese medicine on active ingredients absorption are still not clear. This project will respectively decoct the traditional Chinese medicine of Astragulus, Coptis chinensis, and Honeysuckle, which contained active ingredients with characteristics of water-insolubility or bad biological stability, in a conventional manner, filter the leaves, systematically separate the particles by a series of technological means, according to the physicochemical properties of particle size, surface charge, surface wettability, etc., evaluate the regulating action of particle physicochemical properties on active ingredients absorption by Caco-2 monolayer cell membrane and everted gut sac in vitro, in situ intestinal perfusion and loops, and analysis the regulating mechanism. This project will contribute to clarify the characteristics of particles in decoction of traditional Chinese medicine, and its effect and mechanism on active ingredients absorption, and will provide theoretic and applied bases to explain the scientific implications of decoction and to develop the new dosage-form.