[Intestinal absorption components and absorption characteristics of Wuwei Qingzhuo San by everted intestinal sac models].

This study investigated the absorption profile of Wuwei Qingzhuo San in different intestinal segments and the absorption characteristics of its alkaloids(piperine, piperanine, piperlonguminine, and dihydropiperlonguminine). The everted gut sac model was established, and the chemical components of Wuwei Qingzhuo San in different intestinal segments were detected by UPLC-Q-TOF-MS. The content of piperine, piperanine, piperlonguminine, and dihydropiperlonguminine in intestinal absorption fluid was determined by UPLC-Q-TRAP-MS and the absorption parameters were calculated. The absorption characteristics in different intestinal segments at different time were analyzed. As a result, 27, 27, 8, and 6 absorbent components from Wuwei Qingzhuo San were detected in the intestinal cyst fluid of jejunum, ileum, duodenum, and colon by UPLC-Q-TOF-MS technology, respectively. It was also found that piperine, piperanine, piperlonguminine, and dihydropiperlonguminine from Wuwei Qingzhuo San showed linear absorption in various intestinal segments, with r values exceeding 0.9. In terms of absorption content, the components were ranked as piperine>piperanine>dihydropiperlonguminine>piperlonguminine in various intestinal segments, but the absorption rate and mechanism of each component varied. The results demonstrate that the absorption of the components of Wuwei Qingzhuo San in different intestinal segments is selective and is not a simple semi-permeable membrane permeation process.

[Intestinal absorption characteristics of root tuber of Cynanchum auriculatum extract in normal and functional dyspepsia model rats via everted intestine sac model].

The study investigated the difference of intestinal absorption characteristics of root tuber of Cynanchum auriculatum extract between normal and functional dyspepsia(FD) model rats with everted intestine sac model.The content of syringic acid, scopoletin, caudatin, baishouwu benzophenone, qingyangshengenin and deacyhmetaplexigenin in the C.auriculatum extract in different intestinal segments was detected by UPLC-MS/MS.The cumulative absorption amount(Q) and absorption rate constant(K_a) of the six chemical constituents were calculated.The results showed that the six components could be absorbed into the intestinal sac and were unsaturated, which indicated that the absorption mechanism of scopoletin was active transport in the intestine, while that of the other five components were passive diffusion.For normal group, the syringic acid and baishouwu benzophenone in ileum, qingyangshengenin and deacyhmetaplexigenin in ileum and duodenum, and caudatin in colon were well absorbed and scopoletin at low, medium and high concentrations was found excellent absorption in jejunum, ileum, and colon, respectively.Whereas the best absorption site of each component was ileum in model group.The absorption characteristics of each component between normal group and model group were complex at different concentrations, showing inconsistent tendency of absorption, which suggested that the components of root tuber of C.auriculatum extract were selectively absorbed in small intestine, and the absorption characteristics of the six components could be changed under FD status.This study provided theoretical basis for the clinical drug application and development of root tuber of C.auriculatum.

[Intestinal absorption characteristics of Polygonum orientale extract in normal and isoproterenol-induced myocardial ischemia model rats via everted intestinal sac models].

The present study is to investigate the absorption characteristics of the main components in Polygonum orientale extract in normal and isoproterenol-induced myocardial ischemia model rats with everted intestinal sac models. Intestinal sac fluid samples were collected in different part of intestine(duodenum, jejunum, ileum, colon) at different time after administration of different concentration of P. orientale extract(5.0,10.0, 20.0 mg·mL~(-1)). An UPLC-TQD method was employed for the determination of six components including orientin, isoorientin, vitexin, protocatechuic acid, kaempferol-3-O-ß-D-glucoside and quercitrin in the intestinal sac samples. The absorption rate and cumulative absorption were calculated to analyze the intestinal absorption characteristics of six components in normal and myocardial ischemia model rats. The P-glycoprotein(P-gp) inhibitor was applied to investigate influence of intestinal absorption of six components in P. orientale extract. The results showed that the main absorption sites were concentrated on the duodenum at low concentration, while they were the colon at the medium concentration and the ileum at high concentration in control groups. In the condition of myocardial ischemia model, the main absorption sites focus on the ileum and jejunum at low concentration; the main absorption sites were in the ileum at the medium concentration and main absorption sites were the duodenum and ileum at high concentration. Compared with the normal group, the absorption rate and cumulative absorption of the six components significantly decreased in the model group. P-gp inhibitor markedly increased the absorption rate and cumulative absorption of six components in the model group, inferring that the 6 components may be the substrates of P-gp, and the mechanism needs further study. In this study, it is revealed that the six components of P. orientale extract can be absorbed into the intestinal sac, and it is an effective method to assess the intestinal absorption characteristics of P. orientale extract through everted intestinal sac model, providing data support for the clinical application and further development of P. orientale.

Segmental absorption of helicid in rat everted intestinal sac model: A preliminary study / 中国临床药理学与治疗学

AIM: To investigate the absorption of helicid in different segments of intestine based on rat everted intestine sac model. METHODS: To establish a high-performance liquid chromatography method for simultaneous determination of helicid and its metabolite. Krebs-ringer solution containing helicid was added to everted intestine sacs of different segments (duodenum, Jejunum, ileum and colon). Drug concentration in sacs was determined at different time points (5, 10, 15, 30, 45, 60, 75, 90 min). Adsorptions of helicid in four intestinal segments were compared. RESULTS: This high-performance liquid chromatography was successfully applied to the simultaneous determination of helicid and its metabolite. Absorption of helicid was rapid and time-dependent. The absorption and metabolism of helicid in duodenum segment were higher than these in other segments. CONCLUSION: The duodenum segment is the main site of segmental absorption and metabolism of helicid. This is the first report on intestinal segment metabolism of helicid.

Intestinal absorption characteristics of Polygonum orientale extract in normal and isoproterenol-induced myocardial ischemia model rats via everted intestinal sac models / 中国中药杂志

The present study is to investigate the absorption characteristics of the main components in Polygonum orientale extract in normal and isoproterenol-induced myocardial ischemia model rats with everted intestinal sac models. Intestinal sac fluid samples were collected in different part of intestine(duodenum, jejunum, ileum, colon) at different time after administration of different concentration of P. orientale extract(5.0,10.0, 20.0 mg·mL~(-1)). An UPLC-TQD method was employed for the determination of six components including orientin, isoorientin, vitexin, protocatechuic acid, kaempferol-3-O-β-D-glucoside and quercitrin in the intestinal sac samples. The absorption rate and cumulative absorption were calculated to analyze the intestinal absorption characteristics of six components in normal and myocardial ischemia model rats. The P-glycoprotein(P-gp) inhibitor was applied to investigate influence of intestinal absorption of six components in P. orientale extract. The results showed that the main absorption sites were concentrated on the duodenum at low concentration, while they were the colon at the medium concentration and the ileum at high concentration in control groups. In the condition of myocardial ischemia model, the main absorption sites focus on the ileum and jejunum at low concentration; the main absorption sites were in the ileum at the medium concentration and main absorption sites were the duodenum and ileum at high concentration. Compared with the normal group, the absorption rate and cumulative absorption of the six components significantly decreased in the model group. P-gp inhibitor markedly increased the absorption rate and cumulative absorption of six components in the model group, inferring that the 6 components may be the substrates of P-gp, and the mechanism needs further study. In this study, it is revealed that the six components of P. orientale extract can be absorbed into the intestinal sac, and it is an effective method to assess the intestinal absorption characteristics of P. orientale extract through everted intestinal sac model, providing data support for the clinical application and further development of P. orientale.

Study on Absorption Characteristics of Gastrodia elata Powder with Different Particle Sizes Based on Rat Everted Intestinal Sac Model in vitro / 中国药房

OBJECTIVE：To compar e the absorpt ion characteristics of gastrodin ，parishin A ，parishin B and parishin C of Gastrodia elata powder，and to explore the effect of particle size on intestinal absorption of above components. METHODS ：Based on everted intestinal sac model ，using accumulative absorption amount （Q）and absorption rate constant （Ka）as indexes ，UPLC-MS/MS method was used to determine the absorption of gastrodin ，parishin A ，parishin B and parishin C from different doses （2.5，5，10 g/L） of G. elata powder with different particle sizes （fine powder 146 μm，superfine powder 52 μm，ultrafine powder 37 μm）in different segments（duodenum，jejunum，ileum and colon ）. RESULTS ：Q and Ka of gastrodin and parishin B （intestinal segment ），Q（colon） and Ka（ileum and colon ）of parishin C in 2.5 g/L G. elata superfine powder ；Q and Ka of gastrodin （intestinal segment ），Q and Ka of parishin B （duodenum，jejunum，ileum）and Ka of parishin C （colon）in 2.5 g/L G. elata ultrafine powder ；Q of gastrodin （duodenum），Q of parishin A and parishin B （intestinal segment ）and Q of parishin C （duodenum，jejunum）in 5 g/L G. elata superfine powder ；Q（duodenum jejunum ，colon）and Ka（intestinal segment ）of gastrodin ，Q of parishin B （duodenum，ileum and colon）and Q of parishin C （duodenum，ileum）in 5 g/L G. elata ultrafine powder ；Q and Ka of parishin B （jejunum，ileum），Q of parishin C （jejunum，ileum）in 10 g/L G. elata superfine powder as well as Q（colon）and Ka（duodenum）of gastrodin ，Q （duodenum，ileum，colon）and Ka（duodenum，colon）of parishin B ，Q（duodenum，ileum）and Ka（duodenum）of parishin C in 10 g/L G. elata ultrafine powder were all increased significantly ，compared with the same dose of G. elata fine powder （P＜0.05 or P＜0.01）. Ka of parishin A （jejunum）and Q of parishin C （duodenum）in 2.5 g/L G. elata superfine powder ；Ka of parishin A （jejunum，ileum）， Q and Ka of parishin C （duodenum，jejunum）in 2.5 g/L G. elata ultrafine powder ；Ka of gastrodin （jejunum，ileum and colon ），Ka of parishin A （colon），Ka of parishin B （ileum）and Ka of parishin C （jejunum，ileum）in 5 g/L G. elata superfine powder ；Ka of gastrodin and parishin C （jejunum，ileum and colon ），Q（jejunum，colon）and Ka（colon）of parishin A ，Ka of parishin B （jejunum，ileum）in 5 g/L G. elata ultrafine powder ；Q and Ka of parishin A （ileum）in 10 g/L G. elata superfine powder ；Q（duodenum）and Ka（jejunum） of parishin A ，Ka of parishin C （jejunum）in 10 g/L G. elata ultrafine powder were decreased significantly ，compared with the same dose of G. elata fine powder （P＜0.05 or P＜0.01）. Q of gastrodin （colon），Q（colon）and Ka（ileum，colon）of parishin A ，Q and Ka of parishin B （jejunum，colon），Q and Ka of parishin C （ileum，colon）in 2.5 g/L G. elata fine powder ；Q and Ka of gastrodin （colon），Q（ileum，colon）and Ka（jejunum，ileum，colon）of parishin A ，Ka of parishin C （colon）in 2.5 g/L G. elata superfine powder；Q（colon）and Ka（jejunum，ileum，colon）of parishin A and C ，Q and Ka（ileum，colon）of parishin B in 2.5 g/L G. elata ultrafine powder ；Q and Ka of gastrodin ，parishin A and C （colon），Ka of parishin B （colon）in 5 g/L G. elata fine powder ；Q and Ka of gastrodin and parishin A （colon），Q and Ka of parishin C （jejunum，ileum，colon）in 5 g/L G. elata superfine powder ；Q and Ka of gastrodin（ileum，colon），Q of parishin A （jejunum，ileum，colon），Q and Ka of parishin B （jejunum，colon），Q（jejunum，colon） and Ka（jejunum，ileum，colon）of parishin C in 5 g/L G. elata ultrafine powder ；Q of gastrodin （colon），Q and Ka of parishin A ，B and C （jejunum，ileum，colon）in 10 g/L G. el ata fine powder ；Q of gastrodin （colon），Q and Ka of parishin A and C （jejunum， ileum，colon），Q and Ka of parishin B （colon）in 10 g/L G. elata superfine powder ；Q（colon）and Ka（jejunum，ileum，colon）of gastrodin，Q and Ka of parishin A and C （jejunum，ileum，colon），Q（jejunum，ileum，colon）and Ka（ileum，colon）of parishin B in 10 g/L G. elata ultrafine powder were decreased significantly ，compared with duodeum of the same group （P＜0.05）. Q and Ka of gastrodin（jejunum）in 2.5 g/L G. elata superfine pow

Desalted Duck Egg White Peptides: Promotion of Calcium Uptake and Structure Characterization.

The effects of desalted duck egg white peptides (DPs) on calcium absorption were investigated in three models: Caco-2 cell monolayer model, Caco-2 cell population model, and everted intestinal sac model. DPs were found to enhance calcium transport and may do so by acting as calcium carriers and interacting with the cell membrane to open a special Ca(2+) channel, whereas the paracellular pathway may make only a minor contribution. Structure characterization demonstrated the important roles of seven crucial peptides, such as VSEE and LYAEE, in binding calcium and promoting calcium uptake. Three synthetic peptides (VHSS, VSEE, and VHS(p)S(p)) potently induced calcium transport in Caco-2 monolayers, with VHS(p)S(p) being the most effective. This research expands the understanding of the mechanism of cellular calcium uptake by DPs as well as highlights an opportunity for recycling an otherwise discarded processing byproduct.