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Study On The The Biological Expression Of Coptis-Evodia In Absorption Model

Posted on:2012-09-09Degree:DoctorType:Dissertation
Country:ChinaCandidate:X J HuangFull Text:PDF
GTID:1114330335466299Subject:Pharmacy
Abstract/Summary:PDF Full Text Request
The topic was based on a more comprehensive overview of progress of Coptis& Evodia in recent years and drug compatibility of intestinal absorption model. And try to use in vitro and in vivo models of chemical drug absorption in the study of Chinese herbal compound medicine.Through establishing the absorption of chemicals in vitro and in vivo models, used fingerprinting method.LC-MS-MS ect. to contrast the changes of chemical composition of Coptis-Evodia on front&after the compatibility and metabolic. Attempt to clarify the expression of the chemical composition of fingerprints, combined with pharmacokinetic parameters, investigate the law of compatibility of bcrbcrine drug.ObjectiveThough studying the absorption of expression of the intestinal absorption and Caco-2 cell model of the Coptis-Evodia by different ratios, investigate the law of compatibility of berberine drug.Methods1 By using HPLC&fingerprinting technology, of comparethe the differences in chemical composition of single Coptis decoction. Evodia single decoction, and different ratio of Coptis-Evodia decoction from the overall perspective, comprehensive study on the chemical composition of compatibility.2 Used one-way perfusion to study intestinal absorption in rats of different ratio of coptis-Evodia. anesthetized and fixed the rats, open the abdominal cavity along the midline at the xiphoid under 2cm. isolated intestines to be investigated, intubatedand ligated both ends of the incision, perfused each drug in accordance with 0.2mL·min-1 of 30min. collected perfusate to determined by HPLC'3 Plus 0.5 mL of drug in the side-A of Caco-2 cell layer.and plus 1.5mL HBSS solution in side- B.and then placed the transwell plates in the culture box at 37℃. Collect 0.5mL accept liquid from the side-B at 0.30,60.90.120 min,and immediately add equal amount of HBSS solution.calculate the absorption characteristics which composition can express and extent.4 Oral administrating in rabbits after anesthesia, collected lmL blood from the carotid artery at fixed time points, centrifuge 3000rpm×l0min and get plasma samples, that were injected into the chromatography after treatment and get sample concentration.5 Animals were assigned randomly and take each dose once a day,1 h after the last administration, advancing studies of glacial in mice induced by acetic acid, fever in rats induced by endotoxin and texting intestinal propulsion rate in the small intestine of mice.Results1 After Combinating of Coptis and Evodia, the dissolution of each component of Coptis were significantly reduced, but the dissolution rate is related to the proportion of Coptis and Evodia,the greater proportion of Coptis,or the smaller proportion of Evodia, the greater the dissolution rate was. The compatibility of Coptis and Evodia is conducive to the dissolution of the main alkaloids of Evodia.2 Different Intestines and concentration had no significant effect on the intestinal absorption of different ratios of Coptis- Evodia,but with the increasing in the proportion of Coptis, the drug absorption rised.6:1 of Coptis and Evodia is most ratio that promoted the intestinal absorption of active ingredients in Coptis and Evodia.3 Papp(transport rate) in Caco-2 cell main of ingredient Coptis and Evodia. which Papp of palmatine in 6:1 of Coptis-Evodia was higher than 1:1 and 2:1, the difference was significant.4 The kinetic parameters of Berberine. palmatine and jatrorrhizine was not significantly correlated to the ratio of Coptis & Evodia. but CL of three alkaloids in 2:1 of Coptis-Evodia were smaller. t1/2βwere higher, indicating that this compatibility was mainly distributing to the surrounding tissue in the body.52:1&6:1 of Coptis - Evodia had obvious analgesic effect, could shorter the incubation period and reduce the role of writhing:6:1 and 2:1 of Coptis-Evodia had a certain influence in reducing fever in rats rectal temperature:1:1 and 6:1 of Coptis-Evodia had some antidiarrheal effect.
Keywords/Search Tags:Coptis, Evodia, absorption, expression
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