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目的:建立基于肠吸收技术快速发现龙胆中吸收成分群的方法,为龙胆质量控制指标的选择提供依据。方法:采用大鼠外翻肠囊模型,分别收集3个质量浓度龙胆提取物给药后不同时间点的肠囊液样品,并以龙胆苦苷、马钱苷酸、当药苦苷、当药苷为代表成分,采用HPLC对4种成分进行检测,分别计算其累计吸收量。结果:龙胆中6种主要成分可进入肠囊,在90 min后均能检测到;不同质量浓度的龙胆提取物中龙胆苦苷、马钱苷酸、当药苦苷、当药苷在各肠段均为线性吸收,R2均大于0.9,符合零级吸收;龙胆苦苷和当药苦苷在空肠中的吸收速率常数(Ka)随着剂量增加而增加(P<0.05),符合被动吸收,而在回肠中大、中剂量的Ka无显著差异,且均高于小剂量,符合主动吸收;当药苷在空、回肠中大、中剂量的Ka无显著差异,且均高于小剂量,符合主动吸收;马钱苷酸在回肠与空肠中的Ka随着剂量增加而增加(P<0.05),符合被动吸收。结论:基于肠吸收的质量评价指标选择方法可以用于龙胆吸收成分群的研究,药物在不同肠段中的吸收具有选择性。
OBJECTIVE: To establish a method for rapid detection of absorbed components in gentian based on intestinal absorption technology, and to provide evidence for the selection of gentian quality control indexes. Methods: The rat gut sac model was used to collect the gut fluid samples of three gentian extract at different time points after administration. The gentiopicroside, gentianin, When the glycoside is the representative component, the four components were detected by HPLC and the cumulative absorption was calculated respectively. Results: The main components of gentian can enter the gut, which can be detected after 90 min. Different concentrations of gentian extract, gentiopicroside, (P <0.05). The absorption rate constant (Ka) of gentiopicroside and drosoglucan in jejunum increased with the increase of dose (P <0.05) Which is in line with passive absorption. However, there is no significant difference between the large and medium doses of Ka in the ileum, both of which are higher than the lower dose, which is in line with the active absorption. When the glycosides are in the empty and ileum, there is no significant difference between the medium and medium doses of Ka, At low doses, it was in line with active absorption. The Ka in the ileum and jejunum increased with dose (P <0.05), which accorded with passive absorption. Conclusion: The method of quality evaluation based on intestine absorption can be used to study the absorption of gentian components. The absorption of drugs in different intestinal segments is selective.