目的 采用大鼠在体单向肠灌流与Caco-2细胞模型系统探究金振口服液中黄芩苷、甘草酸、芦荟大黄素、汉黄芩素、大黄素、大黄酚6种成分的肠吸收特性。方法 体外实验借助Caco-2单层细胞模型，通过表观渗透系数（apparent permeability coefficient，P_app）初步评价6种成分的吸收能力；体内实验借助大鼠在体肠灌流，通过吸收速率常数（K_a）和有效渗透系数（effective permeability coefficient，P_eff）进一步验证6种成分在大鼠肠段（十二指肠、空肠、回肠以及结肠）的吸收情况；对比分析体内外吸收规律并解析金振口服液中6种成分吸收规律。结果 体内外实验结果呈现较好的一致性。在低、中、高3种浓度灌流条件下，6种成分在大鼠的各个肠段均具有可吸收性。其中P_eff值在十二指肠、空肠、结肠中均大于1.2×10⁻³ cm/min，表明6种成分在该3肠段均吸收良好；在回肠段，黄芩苷、甘草酸、汉黄芩素P_eff值为1.8×10⁻⁴～1.2×10⁻³ cm/min，表明该3种成分在回肠段吸收情况适中；芦荟大黄素、大黄素、大黄酚P_eff值大于1.2×10⁻³ cm/min，表明该3种成分在回肠肠段吸收良好。另外，该6种成分的吸收机制存在差异，且多数成分存在主动转运、促进扩散等需载体参与的吸收特征（部分呈浓度相关性或饱和性），同时也有成分以被动扩散为主或主动与被动转运共同参与。结论 体内外肠吸收实验揭示了金振口服液中6种主要成分的肠段特异性吸收规律，其整体吸收情况良好，符合口服制剂的要求。

Objective To systematically investigate the intestinal absorption characteristics of baicalin, glycyrrhizic acid, aloe-emodin, wogonin, emodin and chrysophanol in Jinzhen Oral Liquid (金振口服液) using the rat in situ single-pass intestinal perfusion model and Caco-2 cell model. Methods In vitro experiments were conducted using Caco-2 monolayer cell model to preliminarily evaluate the absorption capacity of the six components through apparent permeability coefficient (P_app). In situ experiments were conducted using rats in situ intestinal perfusion to further verify the absorption of the six components in rat intestinal segments (duodenum, jejunum, ileum, and colon) through the absorption rate constant (K_a) and effective permeability coefficient (P_eff). The in vitro and in situ absorption rules were compared and analyzed to clarify their absorption mechanisms. Results The in vitro and in situ experimental results showed good consistency. Under low-, medium-, and high-concentration perfusion conditions, all six components were absorbable in various intestinal segments of rats. Among them, the P_eff values in the duodenum, jejunum, and colon were all greater than 1.2 × 10⁻³ cm/min, indicating that the six components were well absorbed in these three intestinal segments. In the ileum segment, the P_eff values of baicalin, glycyrrhizic acid and wogonin were 1.8 × 10⁻⁴—1.2 × 10⁻³ cm/min, indicating moderate absorption of these three components in the ileum. The P_eff values of aloe-emodin, emodin and chrysophanol were greater than 1.2 × 10⁻³ cm/min, indicating good absorption of these three components in the ileum. In addition, there were differences in the absorption mechanisms of these six components, and most of them exhibited absorption characteristics that required carrier involvement, such as active transport and diffusion promotion (some of which were concentration dependent or saturated). At the same time, there were also components that mainly participate in passive diffusion or both active and passive transport. Conclusion In situ and in vitro intestinal absorption experiments reveal the segment-specific absorption patterns of six major components in Jinzhen Oral Liquid, with good overall absorption that meets the requirements for oral preparations.

R285.5

国家工信部项目（TC2308068）；国家中医药管理局高水平建设学科（zyyzdxk-2023272）