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.

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.

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