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1.
Article in Chinese | WPRIM | ID: wpr-921785

ABSTRACT

The present study investigated the differences in pharmacokinetics and intestinal absorption of six alkaloids in Sanmiao Pills and Simiao Pills in rats and explored the different efficacies of the two formulae. After oral administration of Sanmiao Pills and Simiao Pills in rats, blood samples were collected at different time points. Samples were prepared for the determination of six alkaloids in plasma by UPLC-MS/MS. The chromatography was performed on an ACE Excel 3 C_(18 )column with acetonitrile-0.1% formic acid in water as the mobile phase for gradient elution. Analytes were detected in the positive ion mode. Plasma concentrations and pharmacokinetic parameters were calculated. Intestinal absorption of alkaloids was investigated by single-pass intestinal perfusion and absorption parameters of ingredients were calculated. The results showed that the UPLC-MS/MS method for simultaneous determination of concentrations of six alkaloids in plasma was developed and validated by methodological investigations, such as specificity, calibration curves, precision, accuracy, recovery, matrix effect, and stability. The results of the pharmacokinetic assay revealed that C_(max) and AUC values of phellodendrine, berberine, magnoflorine, berberrubine, and jatrorrhizine in Simiao Pills were significantly increased, and CL/F values were reduced as compared with those in Sanmiao Pills, which indicated the increase in plasma concentrations of alkaloids. The intestinal absorption parameters K_(a )and P_(eff) values of phellodendrine, berberine, and jatrorrhizine in Simiao Pills were higher than those in Sanmiao Pills. The intestinal absorption and plasma concentrations of alkaloids in Simiao Pills were significantly higher than those in Sanmiao Pills, suggesting that the composition of Simiao Pills was more conducive to the alkaloids into the blood to resist inflammation and lower uric acid.


Subject(s)
Alkaloids , Animals , Chromatography, High Pressure Liquid , Chromatography, Liquid , Drugs, Chinese Herbal , Intestinal Absorption , Rats , Reproducibility of Results , Tandem Mass Spectrometry
2.
Article in Chinese | WPRIM | ID: wpr-878930

ABSTRACT

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.


Subject(s)
Animals , Intestinal Absorption , Intestines , Isoproterenol , Myocardial Ischemia/chemically induced , Polygonum , Rats , Rats, Sprague-Dawley
3.
Article in Chinese | WPRIM | ID: wpr-879177

ABSTRACT

To study the effect of self-assembled nanoparticles from Shaoyao Gancao Decoction(SGD-SAN) on the encapsulation, in vitro release and intestinal absorption of the main components of Baishao. Particle size analysis and morphological observation were used to verify the formation of SGD-SAN in the decoction. The entrapment efficiency(EE) of SGD-SAN on the main components of Baishao was determined by ultrafiltration centrifugation. The dialysis bag method was used to study the in vitro release of the main components of Baishao with pH 6.8 phosphate buffer solution as the release media. Single-pass intestinal perfusion study was performed to investigate the effect of SGD-SAN on the absorption of the main components of Baishao. The results showed that there were nanoparticles in the SGD, and the particle sizes and PDI of SGD-SAN were about 200 nm and 0.38, respectively. SGD-SAN was irregularly spherical under transmission electron microscope(TEM). The EEs of albiflorin, paeoniflorin and benzoylpaeoniflorin in SGD-SAN were 33.78%±1.03%,33.61%±0.90%,88.53%±0.58%, respectively. The release characteristics of albiflorin, paeoniflorin and benzoylpaeoniflorin from SGD-SAN showed a slow-release effect on pH 6.8 phosphate buffer solution media. SGD-SAN could significantly enhance the absorption of albiflorin, paeoniflorin and benzoylpaeoniflorin in the ileum. The results of this study indicated that SAN could be formed during the mixed decoction of Baishao and Gancao, and SGD-SAN could encapsulate the components of Baishao, with a certain slow-release effect, and the formation of SAN facilitated the absorption of drugs in the ileum.


Subject(s)
Drugs, Chinese Herbal , Intestinal Absorption , Intestines , Nanoparticles
4.
Article in Chinese | WPRIM | ID: wpr-879135

ABSTRACT

The absorption is the key to the resulted efficacy of orally administered drugs and the small intestine is the main site to absorb the orally administered drug. In this paper, internationally recognized human colon adenocarcinoma cell line(Caco-2) monola-yer model which can simulate small intestinal epithelial cell was used to comparatively study the absorption and transportation diffe-rences of total coumarins and main individual coumarin in Angelica dahurica 'Yubaizhi' by separately using 6-and 12-well plates. It was found that apparent permeability coefficient(P_(app)) values of oxypeucedanin hydrate, byakangelicin and phellopterin were at the quantitative degree of 1 × 10~(-5) cm·s~(-1) when the individual administration was conducted independently, indicating that they were well-absorbed compounds. P_(app) ratio of their bi-directional transportation was close to 1, indicating that they can be absorbed across Caco-2 monolayer by passive diffusion mechanism without carrier mediation during the transportation. The similar trend of transportation was also observed for imperatorin, isoimperatorin and bergapten. The P_(app) values of oxypeucedanin hydrate, byakangelicin and bergapten were at quantitative degree of 1 × 10~(-5) cm·s~(-1) when the administration of total coumarins in Angelica dahurica 'Yubaizhi' was conducted, indicating that they were well-absorbed compounds. The results were consistent with those of independent administration of individual coumarins. Whereas, the P_(app) values of imperatorin, phellopterin and isoimperatorin in the total coumarins decreased, indicating that the interaction between compounds may exist although the P_(app) value ratio of bi-directional transportation was between 0.5 and 1.5. The results laid the foundation for intestinal absorption study of Angelica dahurica 'Yubaizhi' coumarins in compound Chinese medicine.


Subject(s)
Angelica , Caco-2 Cells , Coumarins , Drugs, Chinese Herbal , Humans , Intestinal Absorption , Plant Roots
5.
Article in Chinese | WPRIM | ID: wpr-879055

ABSTRACT

The rat everted intestinal sac model was adopted to investigate the absorption of total flavonoids from Coreopsis tinctoria in different intestinal segments. Cyaniding-3-O-β-D-glucoside, chlorogenic acid, flavanomarein, quercetagetin-7-O-β-D-glucoside, iso-okanin, marein and 3,5-dicaffeoylquinic acid which as the major chemical components of total flavonoids from C. tinctoria were selec-ted as the study objects to evaluate the absorption characteristics of each component in different intestinal segments. The results showed that the absorption of seven components of total flavonoids at different intestinal segments was in consistent with zero order absorption rate. The K_a of chlorogenic acid, flavanomarein, quercetagetin-7-O-β-D-glucoside, isookanin and 3,5-dicaffeoylquinic acid increased with increasing of concentration of total flavonoids(P<0.05), indicating that the intestinal absorption of these five components was passive transport. The K_a of cyaniding-3-O-β-D-glucoside and marein showed a weak concentration dependence, suggesting that the absorption of them may be an positive and passive co-existing mode. The result of absorption in different intestinal segments showed that cyaniding-3-O-β-D-glucoside, chlorogenic acid, flavanomarein, quercetagetin-7-O-β-D-glucoside, marein and 3,5-dicaffeoylquinic acid were mainly absorbed in ileum, while isookanin was mainly absorbed in jejunum. The total flavonoids of C. tinctoria are selectively absorbed in intestinal tract, the rat everted intestinal sac model can be used to evaluate the multi-component intestinal absorption characteristics of total flavonoids from C. tinctoria.


Subject(s)
Animals , Chlorogenic Acid , Coreopsis , Flavonoids , Intestinal Absorption , Plant Extracts , Rats
6.
Horiz. méd. (Impresa) ; 19(3): 40-48, Set. 2019. ilus, graf, tab
Article in Spanish | LIPECS, LILACS, LIPECS | ID: biblio-1022378

ABSTRACT

Objetivo: Evaluar el potencial antihiperglicémico de la infusión de Gentianella gilgiana (Reimers) Fabris ex J.S. Pringle en la absorción intestinal de glucosa in vitro en Rattus norvegicus cepa Holtzman con diabetes inducida químicamente. Materiales y métodos: Estudio de tipo experimental y analítico. Se realizó el tamizaje fitoquímico de la planta. Para el estudio in vitro se utilizaron veinte ratas albinas machos, a las que se les indujo diabetes utilizando aloxano monohidratado (Sigma-Aldrich, Saint Louis, MO, EE. UU.) en dosis de 120 mg/kg p.c, vía intraperitoneal, y luego fueron distribuidas al azar en dos grupos de diez ratas albinas cada uno. Luego de diez días fueron sacrificados para extraerles un segmento intestinal con la técnica del saco intestinal evertido, y medir el transporte y absorción de glucosa. En el grupo control (intestinos evertidos incubados en solución Krebs-Henseleit glucosado) y en el grupo experimental (intestinos incubados en solución Krebs Henseleit glucosado más la infusión de Gentianella gilgiana al 10% p/v), se tomaron muestras basales de los líquidos de incubación, luego otras muestras a los 15, 30, 45 y 60 minutos para cuantificar la glucosa de los compartimentos mucoso y seroso mediante el método enzimático de la glucosa oxidasa. Resultados: Se evidenciaron menores concentraciones de glucosa absorbida en compartimento seroso intestinal del grupo experimental (G. gilgiana) con diferencia estadísticamente significativa respecto al control (p< 0,05). Conclusiones: La infusión de Gentianella gilgiana (Reimers) Fabris ex J.S. Pringle presenta potencial antihiperglicémico significativo que disminuye la absorción intestinal de glucosa in vitro en ratas albinas diabéticas.


Objective: To evaluate the antihyperglycemic potential of the Gentianella gilgiana (Reimers) Fabris ex J.S. Pringle infusion for in vitro intestinal glucose absorption in Rattus norvegicus of the Holtzman strain with chemically-induced diabetes. Materials and methods: The study had an experimental and analytical design. A phytochemical screening of the whole plant was carried out. For the in vitro study, twenty male albino rats were induced with diabetes using alloxan monohydrate (Sigma-Aldrich, Saint Louis, MO, USA) at a dose of 120 mg/kg bw administered by intraperitoneal route, and then randomly distributed into two groups of ten albino rats each. After ten days, they were sacrificed to extract an intestinal segment using the everted intestinal sac technique, and measure the glucose transport and absorption. In the control group (everted intestines incubated in Krebs-Henseleit solution containing glucose) and the experimental group (intestines incubated in Krebs-Henseleit solution containing glucose plus the Gentianella gilgiana (Reimers) Fabris ex J.S. Pringle infusion at 10% w/v), basal samples of fluids were taken from incubation, and then other samples were taken at 15, 30, 45 and 60 minutes to quantify the glucose from the mucous and serous compartments using the glucose oxidase enzymatic method. Results: Lower concentrations of absorbed glucose were observed in the intestinal serous compartment of the experimental group (G. gilgiana) with a statistically significant difference compared to the control group (p <0.05). Conclusions: The Gentianella gilgiana (Reimers) Fabris ex J.S. Pringle infusion exhibits a significant antihyperglycemic potential by decreasing the in vitro intestinal glucose absorption in diabetic albino rats.


Subject(s)
Rats , Hyperglycemia , Gentianella , Diabetes Mellitus , Intestinal Absorption
7.
Article in English | WPRIM | ID: wpr-760619

ABSTRACT

BACKGROUND/OBJECTIVES: Consumption of cholesterol-rich foods, such as eggs, has a minimal effect on circulating cholesterol levels in healthy humans. To gain insight, we investigated whether phospholipids rich in eggs (EPL) interfere with intestinal cholesterol absorption in vivo. MATERIALS/METHODS: To investigate the acute effect of EPL on intestinal cholesterol absorption, male C57BL/6J mice were orally administered with 6, 11, or 19 mg of EPL for three days. We also tested the effect of chronic EPL consumption on cholesterol metabolism in the small intestine and the liver in mice with diet-induced hypercholesterolemia. Male C57BL/6J mice were fed a high fat/high cholesterol (HF/HC; 35% fat, 0.25% cholesterol, w/w) diet for 4 weeks to induce hypercholesterolemia, and subsequently the mice were either fed 0, 0.4 or 0.8% (w/w) of EPL for 6 weeks. RESULTS: Intestinal cholesterol absorption was significantly decreased by the highest dose of acute EPL administration compared to control. Chronic EPL supplementation did not significantly alter intestinal cholesterol absorption nor plasma levels of total cholesterol and low-density lipoprotein cholesterol. In the small intestine and the liver, EPL supplementation minimally altered the expression of genes which regulate cellular cholesterol levels. CONCLUSION: Although chronic EPL consumption was not able to counteract hypercholesterolemia in HF/HC-fed mice, acute EPL administration decreased intestinal cholesterol absorption. This study provides in vivo evidence that acute administration of PLs in eggs prevent cholesterol absorption in the intestine, suggesting a mechanism for a minimal effect of egg consumption on circulating cholesterol levels.


Subject(s)
Absorption , Animals , Cholesterol , Diet , Eggs , Humans , Hypercholesterolemia , Intestinal Absorption , Intestine, Small , Intestines , Lipoproteins , Liver , Male , Metabolism , Mice , Ovum , Phosphatidylcholines , Phospholipids , Plasma
8.
Article in Chinese | WPRIM | ID: wpr-771502

ABSTRACT

To investigate the active fraction from Bletilla striata in Caco-2 cell monolayer,so as to explore its absorption mechanism of oral administration preliminarily.Active fraction from B.striata in Caco-2 cell monolayer was analyzed by UPLC-Q-TOF and detected by UPLC-MS/MS,and the effects of different concentrations,pH and P-glycoprotein inhibitors on Caco-2 cells Monolayer were investigated.Six compounds were isolated from the active fraction of B.striata in Caco-2 cell monolayer by UPLC-Q-TOF,and identified as B6,B12,B14,B17,B19 and B23,with concentration dependence.Within the 0-180 min,the uptake of B12 and B14 had a time dependence,while B6,B17,B19 and B23 tended to saturate after 60 min.All of the components had a good absorption in an acidic environment.B6 had a good absorption at pH 6.0,while the other components B12,B14,B17,B19 and B23 had a good absorption at pH4.0.The absorption of the 6 main components of B.striata were not be affected by P-glycoprotein inhibitors(verapamil/cyclosporin A).Compared with the control group,there was no difference in the absorption of B6 and B12,and the absorption of B14,B17,B19 and B23 increased,but with no significant difference.The absorption characteristic of B.striata extract across the Caco-2 cell monolayer is probably passive diffusion,and the absorption process was not affected by P-glycoprotein.


Subject(s)
Biological Transport , Caco-2 Cells , Chromatography, Liquid , Humans , Intestinal Absorption , Orchidaceae , Chemistry , Plant Extracts , Pharmacology , Tandem Mass Spectrometry
9.
Article in Chinese | WPRIM | ID: wpr-773736

ABSTRACT

The intestinal absorption characteristics of ten iridoid glycosides and phenolic acids in the Pterocephali Herba were evaluated via rat intestinal valgus model. The intestinal sac fluids at different time after administration of high,medium and low concentrations of Pterocephali Herba extract were collected and ten chemical components in fluid samples were detected by UPLC-PDA. Accumulative absorbed doses( Q) and absorption rate constants( Ka) of ten chemical constituents were calculated,while proportions between Pterocephali Herba extract and intestinal absorption liquid were compared. The results showed that the intestinal absorption of 10 chemical components was linear absorption( R2>0. 9) at different concentrations,which accorded with the zero-order absorption rate. The absorption rate constant was related to the concentration of the drug and the intestinal site,which indicated that intestinal adsorption mechanism of the components were passive diffusion and active transport. Proportions of chemical constituents in intestinal sac fluid were different from those in Pterocephali Herba extract. Therefore,those ten chemical components in Pterocephali Herba extract can be absorbed in whole intestine. Everted intestinal sac model can be used to evaluate intestinal absorption characteristics of ingredients in Pterocephali Herba extract effectively.


Subject(s)
Animals , Caprifoliaceae , Chemistry , Drugs, Chinese Herbal , Pharmacokinetics , Intestinal Absorption , Intestines , Plant Extracts , Pharmacokinetics , Rats , Rats, Sprague-Dawley
10.
Article in Chinese | WPRIM | ID: wpr-773669

ABSTRACT

Single-pass intestinal perfusion( SPIP) is the common carrier of biopharmaceutics classification system( BCS) to study compound permeability. With the application and deepening study of BCS in the field of traditional Chinese medicine( TCM),SPIP model is becoming more and more common to study the intestinal absorption of TCM ingredients. Based on the limitations of the SPIP model in some researches on TCM permeability,it was speculated in this study that aglycone may be more suitable than the glycoside to study the intestinal absorption problem by using SPIP model. Furthermore,applicability of aglycone components was analyzed and evaluated. In this study,with quercetin,daidzein,formononetin,genistein and glycyrrhetinic acid used as research objects,the quantitative study of SPIP was used to evaluate the intestinal permeability of these aglycones and to predict the effective permeability coefficient( Peff) and absorption fraction( Fa) in human body. By combining studies comparison and analysis on multiple permeability research methods and prediction of human body absorption of aglycones in physiological-based pharmacokinetic models,this paper can further illustrate that the SPIP model is a good tool for studying the permeability of aglycones and predicting human absorption,which can provide data foundation and theoretical reference for researches on SPIP technique and BCS in intestinal absorption of TCM ingredients.


Subject(s)
Biopharmaceutics , Humans , Intestinal Absorption , Intestines , Medicine, Chinese Traditional , Perfusion , Permeability
11.
Article in Chinese | WPRIM | ID: wpr-773668

ABSTRACT

For the effects of multi-component environment on the solubility and permeability of single components,and the problems of biopharmaceutical attribute classification of single components in the compound prescriptions environment,baicalein was used as the research object in this study to investigate the biopharmaceutic attributes of single-component and their traditional Chinese medicine( TCM) biopharmaceutic attributes in the multi-component environment of Gegen Qilian Decoction. Shaking flask method,intrinsic dissolution rate test and HPLC were used to determine solubility of baicalein. Markers specified by FDA were utilized as permeable boundary reference materials to verify the applicability of the single-pass intestinal perfusion method( SPIP),and the quantitative research on the permeability of baicalein was also conducted. It is concluded that baicalein could be categorized as BCS-Ⅱ drug based on its low solubility and high intestinal permeability values,and it may be categorized into CMMBCS-I in the multi-component environment of Gegen Qilian Decoction due to its poor solubility but enhanced solubility and permeability in compound environment. This study could provide verification ideas for clinical determination of the best human oral dose of baicalein,and provide the data basis for the study of biopharmaceutics classification system of Chinese materia medica( CMMBCS).


Subject(s)
Biopharmaceutics , Classification , Drugs, Chinese Herbal , Chemistry , Flavanones , Chemistry , Humans , Intestinal Absorption , Materia Medica , Classification , Permeability , Solubility
12.
Article in Chinese | WPRIM | ID: wpr-773113

ABSTRACT

To study the compatibility rule of Simao Yongan Decoction,the rat single pass intestinal perfusion model in situ was used in this study. On the basis of early research,the five kinds of anti-inflammatory active ingredients,i.e. chlorogenic acid,liquiritin,hyperoside,angoroside C and isochlorogenic acid C in Simao Yongan Decoction were selected as research objects. The contents of the above five actives compounds with various compatibility combinations and in different intestinal segment perfusates were determined by using the method of ultra-performance liquid chromatography-mass spectrometry( UPLC-MSn). The kinetic parameters of intestinal absorption of the five anti-inflammatory active ingredients were calculated,which could be used to evaluate the intestinal absorption of each component in different combinations. The results showed that the absorption parameters of liquiritin in ileum were highest in Glycyrrhizae Radix et Rhizoma single herb,while the absorption parameters of other four components in ileum and duodenum were highest in the compatible combinations. Among them,the absorption parameters of chlorogenic acid in ileum and duodenum were highest in the whole prescription compatibility; ischlorogenic acid C showed higher absorption levels in the whole prescription and the herb compatibility of Lonicerae Japonicae Flos-Scrophulariae Radix-Glycyrrhizae Radix et Rhizoma. However,the absorption levels of hyperoside and angoroside C in different compatibilities were quite different in ileum and duodenum. In this study,the intestinal absorption of five anti-inflammatory active ingredients in Simiao Yongan Decoction with different compatibility combinations was investigated,revealing that the absorption of active ingredients varied with the different compatibility combinations and different intestinal segments. At the same time,the above research also indicated that the absorption of active ingredients could be obviously promoted by the compatibility of compound prescriptions,laying a foundation for the research on the compatibility rule of Simiao Yongan Detection from the biological point of view.


Subject(s)
Animals , Drugs, Chinese Herbal , Pharmacokinetics , Intestinal Absorption , Intestines , Phytochemicals , Pharmacokinetics , Rats
13.
Article in Chinese | WPRIM | ID: wpr-773084

ABSTRACT

The intestinal absorption properties of four main effective components(gallic acid, ocinolglucoside, ethyl gallate and penta-O-galloyl-β-D-glucose) in Rhus chinensis extracts were investigated by in situ single-pass intestinal perfusion model in rats. The liquid accumulation of perfusion was corrected by gravimetry. The HPLC method was established to determine the concentration of the four effective components in the intestinal perfusion. It showed significant differences(Pethyl gallate>gallic acid>ocinolglucoside, with significant differences between them(P<0.05). In conclusion, gallic acid, orpheolglucoside, ethyl gallate and pentacyl-glucose could be absorbed in the whole intestine. Their absorption rate and permeation ability were related to the intestinal section and the perfusate concentration. These results indicated potential active transport or facilitated diffusion in the intestinal transport process of the four effective components.


Subject(s)
Animals , Chromatography, High Pressure Liquid , Hydroxybenzoates , Metabolism , Intestinal Absorption , Perfusion , Phytochemicals , Metabolism , Rats , Rhus , Chemistry
14.
Article in Chinese | WPRIM | ID: wpr-771708

ABSTRACT

Nuciferin is the main active ingredients in Nelumbinis Folium, which was proved to have good hypolipidemic, antioxidative and anti-inflammatory bioactivities. Currently, pharmacokinetic studies of nuciferin showed different results based on different animal models. evaluation experiments were low-cost, stable and controllable. Biopharmaceutical classification system(BCS) was an effective and reliable simulation method to evaluate the bioavailability of oral drugs. It was a scientific framework for classifying drugs or active pharmaceutical ingredients(API) according to their solubility and impermeability . In the study, BCS was applied in an active ingredient in traditional Chinese medicine(TCM), which was consisted of numerous chemical components. To study the equilibrium solubility of nuciferine, ideal solution model, Ape blat model and polynomial model were adopted. The permeability was measured based on partition coefficient(logP) and distribution coefficient(logD). Besides, apparent permeabilities of Caco-2 cells and murine intestine tissues were evaluated. Nuciferine was classified as BCSⅠ, since it had a good solubility and permeability in all methods under acidic conditions. However, in neutral and alkaline environments, nuciferine was classified as BCSⅣ by using everted intestinal sac. It indicated that the species of experimental animals has a significant influence on the absorption of nuciferine. This experiment can provide data support to the prediction in a complex environment(medicinal materials and absorbed parts). The application of BCS on TCM ingredients provided a new method to evaluate and screen out the druggability of TCM ingredients.


Subject(s)
Animals , Aporphines , Chemistry , Biological Availability , Biological Products , Classification , Biopharmaceutics , Caco-2 Cells , Humans , Intestinal Absorption , Mice , Nelumbo , Chemistry , Permeability , Plant Leaves , Chemistry , Solubility
15.
Article in Chinese | WPRIM | ID: wpr-771693

ABSTRACT

To investigate the absorptive characteristics of Inula cappa extract based on the rat everted intestinal sac method . Nine representative ingredients in I. cappa extract were selected as the study objects. An UPLC-MS/MS method was established to determine and detect their cumulative absorption amount for expounding the absorptive characteristics of ingredients in different intestinal sections. According to the results, the transport mechanism of 8 compounds showed passive diffusion by the reverted gut sac method. And scopolin was actively transported in the intestine. The best absorption site of chlorogenic acid was duodenum. The best absorption site of cryptochlorogenic acid, 1,3--dicaffeoylquinic acid, luteolin-7-glucoside and 3,4--dicaffeoylquinic acid were jejunum. The best absorption site of neochlorogenic acid, scopolin, 4,5--dicaffeoylquinic acid and 3,5--dicaffeoylquinic acid was ileum. The absorption of all the compounds was affected by pH and bile. All of the nine ingredients in I. cappa extract could be absorbed in intestines, but with differences in the absorption rate, the best absorptive site and mechanism, indicating that the intestinal absorption of I. cappa extract was selective.


Subject(s)
Animals , Chromatography, High Pressure Liquid , Intestinal Absorption , Intestines , Inula , Chemistry , Plant Extracts , Pharmacology , Rats , Rats, Sprague-Dawley , Tandem Mass Spectrometry
16.
Article in Chinese | WPRIM | ID: wpr-771539

ABSTRACT

Intestinal absorption liquid was prepared by using everted intestinal sac method; meanwhile, its recipes were decomposed or restructured. Platelet aggregation activity was examined by biochemical tests and a microplate reader. One or more kinds of Chinese medicines which displayed inhibiting activity in Naoxintong Capsules were screened through separation and combination of prescription. The results showed that Naoxintong Capsules could inhibit ADP-induced platelet aggregation. Recipe decomposition and restructuring results showed that Salviae Miltiorrhizae Radix et Rhizoma, Paeoniae Radix Rubra, Cinnamomi Ramulus and Hirudo were the main effective medicines in inhibiting platelet aggregation. Furthermore, Cinnamomi Ramulus played a vital role in inhibiting activity among those four kinds of Chinese medicines. Coumarin derived from intestinal absorption liquid of Cinnamomi Ramulus had inhibiting activity in the range of 50-200 μmol·L⁻¹, and other ingredients such as cinnamyl alcohol and cinnamaldehyde also had inhibiting activities. In conclusion, Salviae Miltiorrhizae Radix et Rhizoma, Paeoniae Radix Rubra, Cinnamomi Ramulus and Hirudo are the main components for inhibiting ADP-induced platelet aggregation, and Cinnamomi Ramulus has the most strongest inhibiting activity in Naoxintong Capsules.


Subject(s)
Adenosine Diphosphate , Capsules , Drugs, Chinese Herbal , Intestinal Absorption , Platelet Aggregation
17.
Int. j. morphol ; 35(3): 877-882, Sept. 2017. ilus
Article in English | LILACS | ID: biblio-893067

ABSTRACT

Reducing nitrogen nutrients concentration in dairy food is economic for pig industry. Here, we used finishing pig as model to investigate the effect on colon mucosal barrier and nutrients absorption after reducing crude protein (CP) in dietary from 16 % to 13 %. The results showed that crypt depth, cells, claudin-1 and E-cadherin expression level will not be changed, which implied the integrity of colon mucosal structure. Furthermore, the expressions of ASCT1, EAAT3 and SGLT1 in colon were also maintained at normal levels in 13 % CP dietary. Interestingly, the CAT1 and GLUT2 expression were increased significantly after reducing CP level to 13 %, which might be attributed to the compensatory nutrients absorption. This study implied that 13 % CP was sufficient to maintain normal colon structure and will not change intestinal morphology, which provided a basis for an ideal economic protein feed formula.


La reducción de concentración de nitrógeno en los alimentos lácteos es económicamente favorable para la industria porcina. En este trabajo se utilizó el cerdo de acabado como modelo para investigar el efecto sobre la barrera de la mucosa del colon y la absorción de nutrientes después de reducir la proteína bruta (CP) en la dieta del 16 % al 13 %. Los resultados mostraron que la profundidad de la cripta, las células globulares, el nivel de expresión de Claudin-1 y E-cadherina no cambiaron, lo que implicaría la integridad de la estructura de la mucosa del colon. Además, las expresiones de ASCT1, EAAT3 y SGLT1 en el colon también se mantuvieron en niveles normales en el 13 % de la dieta de CP. Sin embargo, la expresión de CAT1 y GLUT2 incrementó significativamente después de reducir el nivel de CP a 13 %, lo que podría atribuirse a la absorción de nutrientes compensatorios. Este estudio indicó que el CP del 13 % era suficiente para mantener la estructura normal del colon y no cambiaría la morfología intestinal, lo que proporcionó una base para una fórmula económica ideal para la alimentación con proteínas.


Subject(s)
Animals , Colon/metabolism , Diet, Protein-Restricted , Intestinal Mucosa/metabolism , Swine , Intestinal Absorption
18.
Rev. Nutr. (Online) ; 30(1): 13-22, Jan.-Feb. 2017. tab, graf
Article in English | LILACS | ID: biblio-845572

ABSTRACT

ABSTRACT Objective: This study aimed to compare the intestinal absorption of iron and calcium between soy-based and cow's milk-based infant formulas in weanling rats. Methods: Twenty male Wistar rats, twenty-one days old on the first day of weaning, were used in this experiment, divided in two Groups, one Group was fed soy protein-based infant formula the other, cow's milk protein-based infant formula. During the study period (ten consecutive days) the animals received food and water ad libitum. Hematocrit and hemoglobin were evaluated on the first, fifth, and tenth days by the Wintrobe and cyanomethemoglobin methods. Feces and urine were collected, beginning on the fifth day, for three consecutive days. On the tenth day, hepatic iron content was also analyzed. Hepatic iron as well as fecal and urinary iron and calcium analyses were performed using an atomic absorption spectrophotometer. At thirty-one days of age, the animals were anesthetized with ketamine and xylazine and sacrificed by exsanguination via the vena cava. Results: The final concentration of hemoglobin in the group soy-based infant formula and milk-based infant formula were: 10.3±1.3g/dL and 10.9±1.0g/dL (p=0.310). The apparent absorption of iron and calcium, in that order, were: 73.4±10.2% and 70.2±9.5%; 97.2±0.7% and 97.6±1.0% (p=0.501; p=0.290). The apparent calcium retention was: 88.4% ±2.2 and 88.6±2.6% (p=0.848). Hepatic iron content was: 522.0±121.1mg/g and 527.8±80.5mg/g (p=0.907) . Conclusion: Intestinal iron and calcium absorption from soy-based infant formula is similar to that from milk-based infant formula in weanling rats.


RESUMO Objetivo: Este estudo objetivou comparar a absorção intestinal de ferro e cálcio entre fórmulas infantis à base de leite de vaca e de soja em ratos recém-desmamados. Métodos: Vinte ratos machos Wistar, com 21 dias de vida e no primeiro dia do desmame foram utilizados neste experimento, divididos em dois grupos: um alimentado com fórmula infantil à base de proteína de soja e o outro com fórmula infantil à base de proteína do leite de vaca. Durante o período de estudo (10 dias consecutivos), os ratos receberam dieta e água ad libitum. Hematócrito e hemoglobina foram mensurados no primeiro, quinto e décimo dia pelo método de Wintrobe e da cianometaemoglobina. As fezes e a urina foram recolhidas a partir do quinto dia durante durante três dias consecutivos. No décimo dia, o conteúdo de ferro hepático também foi analisado. O conteúdo de ferro hepático e a análise de ferro e cálcio nas fezes e na urina foram realizados utilizando espectrofotômetro de absorção atômica. Aos 31 dias de vida, os animais foram anestesiados com ketamina e xilasina e sacrificados por exsanguinação da veia vaca. Resultados: A concentração final de hemoglobina no grupo fórmula infantil à base de soja e fórmula infantil à base de leite de vaca foram 10,3±1,3g/dL e 10,9± 1,0g/dL (p=0,310), respectivamente. A absorção aparente de ferro e cálcio foi de: 73,4±10,2% e 70,2±9,5%, para o primeiro grupo; e 97,2±0,7% e 97,6±1,0%, para o segundo (p=0,501; p=0,290). A retenção aparente de cálcio foi: 88,4±2,2% e 88,6±2,6% (p=0,848). O teor de ferro hepático foi: 522,0±121,1µg/g e 527,8±80,5µg/g (p=0,907), respectivamente. Conclusão: A absorção intestinal de ferro e cálcio da fórmula infantil à base de soja é similar à da fórmula infantil à base de leite em ratos recém-desmamados.


Subject(s)
Animals , Rats , Intestinal Absorption , Proteins , Calcium , Soy Milk , Breast-Milk Substitutes , Iron
19.
Braz. j. med. biol. res ; 50(11): e6353, 2017. tab, graf
Article in English | LILACS | ID: biblio-888951

ABSTRACT

This study aimed to investigate the absorption mechanism of three curcumin constituents in rat small intestines. Self-emulsification was used to solubilize the three curcumin constituents, and the rat in situ intestinal perfusion method was used to study factors on drug absorption, including drug mass concentration, absorption site, and the different types and concentrations of absorption inhibitors. Within the scope of experimental concentrations, three curcumin constituents were absorbed in rat small intestines through the active transport mechanism.


Subject(s)
Animals , Male , Female , Adjuvants, Pharmaceutic/pharmacology , Curcumin/analogs & derivatives , Curcumin/pharmacokinetics , Enzyme Inhibitors/pharmacokinetics , Intestinal Absorption , Intestine, Small/metabolism , Reference Values , Time Factors , Uncoupling Agents/pharmacology , Verapamil/pharmacology , Probenecid/pharmacology , Reproducibility of Results , Chromatography, High Pressure Liquid/methods , Rats, Sprague-Dawley , ATP-Binding Cassette Transporters/antagonists & inhibitors , 2,4-Dinitrophenol/pharmacokinetics , Curcumin/chemistry , Multidrug Resistance-Associated Proteins/analysis , Multidrug Resistance-Associated Proteins/antagonists & inhibitors , Emulsions , Perfusion Imaging/methods , Intestinal Absorption/drug effects , Intestine, Small/drug effects
20.
Clinical Endoscopy ; : 26-30, 2017.
Article in English | WPRIM | ID: wpr-67670

ABSTRACT

The incidence of obesity is increasing, and more definitive treatment modalities are needed. Endoluminal procedures, including restrictive endoscopic procedures, endoscopic gastroplasty, and malabsorptive endoscopic procedures, can reduce weight in obese patients and control obesity-related comorbidities. Malabsorptive endoscopic interventions also offer the potential for an ambulatory procedure that may be safer and more cost-effective compared with laparoscopic surgery. Malabsorptive endoscopic intervention can induce weight reduction and improve obesity-related metabolic parameters, despite complications such as device migration, obstruction, and abdominal pain. Improvement in technique will follow the development of new devices.


Subject(s)
Abdominal Pain , Comorbidity , Endoscopy , Gastroplasty , Humans , Incidence , Intestinal Absorption , Laparoscopy , Obesity , Weight Loss
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