Abstract

The 2,3,5,4’-tetrahydroxy-stilbene-2-O-β-D-glucoside (THSG) is a main active ingredient of Polygoni Multiflori Radix (PMR). In this study, THSG was found to be a differential chemical composition between PMR and its compatible herb pairs through chemometrics techniques. The effects of the herb pairs Codonopsis Radix-PMR, Astragali Radix-PMR, and Ophiopogonis Radix (OR)-PMR on the stability and absorption behavior of THSG were investigated by simulating the digestive environment in vitro and using an everted gut sac model. The results indicated that the compatible pairs were able to significantly increase the stability of THSG in the gastrointestinal tract and delay the absorption of THSG in the small intestine. OR had the most obvious influence on THSG as the t_0.9 values of THSG increased by 14.74- and 6.68-fold in simulated gastric juice and small intestinal fluid, and the apparent permeability coefficient of THSG were 2.07- and 1.97-fold lower for OR-PMR in the ileum and duodenum, respectively. Thus, the compatibility could potentially be used to change the biopharmaceutical properties of THSG. Moreover, the present study established a research method for describing the compatibilities of traditional Chinese medicine based on stability-intestinal absorption, which may provide important reference values for the compatibilities of traditional Chinese medicine.

摘要

2,3,5,4'-四羟基芪-2- O -β-D-葡萄糖苷（THSG）是何首乌（PMR）的主要活性成分。在这项研究中，通过化学计量学技术发现 THSG 是PMR与其相容的草药对之间的差异化学成分。通过体外模拟 消化 环境 , 研究 了党参- PMR ,黄芪- PMR和麦冬( OR ) - PMR对 THSG 稳定性和吸收行为的影响。并使用外翻肠囊模型。结果表明，配伍对能够显着提高THSG在胃肠道的稳定性，延缓THSG在小肠的吸收。OR对 THSG 的影响最为明显，模拟胃液和小肠液中THSG 的 t _{0.9值分别增加了 14.74 倍和 6.68 倍，而}OR -的 THSG 表观渗透系数分别降低了 2.07 倍和 1.97 倍。 PMR分别在回肠和十二指肠。因此，这种相容性可能会用于改变 THSG 的生物制药特性。此外，本研究建立了基于稳定性-肠道吸收的中药配伍描述研究方法，可为中药配伍提供重要的参考价值。