• Title/Summary/Keyword: bile acid absorption

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Preparation and Evaluation of Solid lipid Microspheres Containing Cyclosporine A (사이클로스포린을 함유한 고형 지질미립구의 제조와 평가)

  • 양수근;박준상;최영욱
    • YAKHAK HOEJI
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    • v.39 no.5
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    • pp.487-494
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    • 1995
  • Solid lipid microspheres (SLMs) were prepared using various lipids and solidifying agents, in order to enhance the gastrointestinal absorption of Cyclosporine A (Cs A) which is a practically water-insoluble drug with low systemic bioavailability. Egg lecithin and HCO-60 (polyoxyethylated 60 mol, hydrogenated castor oil) were used as lipids. Stearic acid and stearyl alcohol were used as solidifying agents. Emulsion concentrates containing Cs A were prepared by mixing the melted lipid and solidifying agent with water, employing bile salts as a cosurfactant. SLMs were obtained by dispersing the warm emulsion concentrate in cold distilled water under mechanical stirring, followed by freeze drying. Physical characteristics of each SLM were investigated by particle size analysis, optical microscopy and scanning electron microscopy. Mean particle size of SLMs was in the range of 30 to 40.mu.m. The SLMs were in good appearance with spherical shape before freeze drying, but were deformed partially after freeze drying. Drug loading efficiencies of SLMs were observed as high as 80 to 90% in average. The systemic bioavailability of Cs A from different SLM formula was investigated in rats following oral administration. Cs A in whole blood was extracted and assayed by HPLC. SLMs revealed the higher bioavailabilities than the standard formula based on the marketed product. SLMs might have several advantages over standard formula for enhanced gastrointestinal absorption, controlled release properties, high loading capacity of the water-insoluble drug, and feasibility of solid dosage forms with better stability in storage.

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Biliary and Urinary Excretion of DWP305, the Combined Preparation of Ursodeoxycholic Acid and Silymarin for Hepatic Disorders in Rats (흰쥐에서 UDCA와 Silymarin을 함유한 간장질환 치료용 의약조성물(DWP305)의 담즙 및 요중 배설)

  • Nam, Kweon-Ho;Kim, Dong-O;Cho, Jae-Youl;Yeom, Je-Ho;Kim, Young-Man;Yoo, Eun-Sook;Yu, Young-Hyo;Park, Myung-Hwan
    • YAKHAK HOEJI
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    • v.38 no.6
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    • pp.646-653
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    • 1994
  • The pharmacokinetics of DWP305, a new combined preparation for hepatic disorders was examined in rats. DWP305 was composed of ursodeoxycholic acid(UDCA), Cardus marianus extract(silymarin 74.5%), fursulthiamine and riboflavin tetrabutyrate(RTB). Especially, this study was focused on the possibilities of drug interaction that the administration of DWP305 may affect the oral absorption of each component. After oral administration of DWP305 and each component drug to rats, the biliary excretion of silybin and tauroursodeoxycholic acid(TUDCA), and the urinary excretion of vitamins were measured by HPLC up to 48 hours. The cumulative amount of TUDCA or silybin in bile was not significantly different between DWP305 and UDCA/silymarin administered groups at doses of 25 and 100 mg/kg. In the case of vitamin study, the urinary thiamine excretion of equivalent molar fursulthiamine administered group was significantly higher than that of thiamine administered group. Urinary riboflavin level of equivalent molar RTB administered group was lower than that of riboflavin administered group, but not significant. These results suggest that the combined preparation may not affect the oral absorption of each component in respect of drug interaction. Also, fursulthiamine and RTB were more effective in oral absorption than thiamine and riboflavin, respectively.

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Effect of Low-Molecularization on Rheological Properties of Alginate (알긴산의 물성에 미치는 저분자화의 영향)

  • LEE Dong-Soo;KIM Hyeung-Rak;PYEUN Jae-Hyeung
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.31 no.1
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    • pp.82-89
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    • 1998
  • Partial hydrolyzing condition for low-molecularized alginate and rheological properties such as viscosity, solubility, emulsitying ability, oil absorption capacity, bile acids binding and metal ion binding of the low-molecularized alginates from the sea mustard ( Undaria pinnatifida) and giant kelp (Macrocystis pyrifera) were investigated. Alginate from sea mustard was regularly hydrolyzed with the increase of HCl concentration in the range of 0.2 N to 0.5 N and with the prolonged reaction time at $100^{\circ}C$. The molecular weight of alginate was decreased to a part of 100 after hydrolysis for 50 min with 0.3 N HCl. The ratio of mannuronate to guluronate was increased with the acid hydrolysis and total yield was estimated to be $75\%\~80\%$. Low-molecularization of alginate was featured in the apparent decrease of viscosity, whereas solubility, emulsifying ability, and bile acids binding ability were increased with the low-molecularization. Oil absorption capacity of the acid$\cdot$alkali soluble alginate was slightly higher than that of the water soluble alginate. Metal ion binding capacity was the highest in acid$\cdot$alkali soluble alginate, and decreased with the low-molecularization.

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Stress-induced Changes of Taurine Transporter Activity in the Human Colon Carcinoma Cell Line(HT-29)* (스트레스를 유발시킨 인체 소장상피세포주(HT-29) 모델에서 타우린수송체 활성의 변화*)

  • 윤미영;박성연;박태선
    • Journal of Nutrition and Health
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    • v.34 no.2
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    • pp.150-157
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    • 2001
  • Intestinal absorption of dietary taurine is one of the regulatory component maintaining taurine homeostasis along with renal reabsorption, bile acid conjugation and secretion, and de nobo synthesis of taurine in mammals. Recent observations of decreased enterocytic levels of taurine in response to trauma, infection and surgical insults, postulate the possibility that intestinal taurine absorption might be impaired in such stressed conditions. The aim of the present study was to evaluate changes in enterocytic taurine transporter activity using the human intestinal colon carcinoma cell line, HT-29, in various stress-induced conditions. Pretreatment of the HT-29 cells with dexamethasone, a stress hormone(0.1,1,10 or 100$\mu$M) for 3 hrs, or with E coli heat-stable enterotoxin(10, 100, or 200nM) for 30 minutes in order to induce the condition of enterotoxigenic infection did not influence taurine uptake as compared to the value found in control cells. In contrast, pretreatment of the cells with cholera toxin(10, 100, 500, or 1000ng/ml)for 3hr or 24hr significantly decreased taurine uptake by HT-29 cells to 40~50% of the value found in untreated control cells. Kinetic studies of the taurine transporter activity were conducted in control and cholera toxin treated HT-29 cells with varying taurine concentrations(2~60$\mu$M) in the uptake medium. Pretreatment of the cells with cholera toxin(100ng/ml) for 3hr did not influence the Vmax, but resulted in a 55% increase in the Michaelis-Menten constant(Km) of the taurine transporter compared to those in control cells. These results suggest that cholera toxin-induced reduction in taurine transporter activity in HT-29 cells is associated with decreased affinity of the taurine transporter without altering the amount of transporter protein. Intestinal taurine absorption appears to be reduced in the condition of water-borne diseases caused by bacteria such as V. cholerae. This might influence the taurine status of infants and young children more readily, an age group in which the prevalence of intestinal infection is high and the role of intestinal absorption is crucial for maintaining the body taurine pool. (Korean J Nutrition 34(2) : 150-157, 2001)

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Dietary Fiber and Cholesterol Metabolism (식이섬유와 콜레스테롤 대사)

  • Kang, Hee-Jung;Song, Young-Sun
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.26 no.2
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    • pp.358-369
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    • 1997
  • Hypercholesterolemia is a main risk factor to develop cardiovascular disease, a major cause of death in Korea currently. Dietary factors which shows hypocholesterolemic effect have been reported, which includes plant proteins, unsaturated fatty acids, milk, calcium, flavonoids. Numerous animal and human studies confirmed the pronounced hypocholesterolemic effects of soluble dietary fiber, such as psyllium husk, pectin, sodium alginate, guar gum. Several hypotheses have been proposed to explain the hypocholesterolemic effect of dietary fiber, including binding of bile acids by fiber, interference of lipid absorption and reduced hepatic cholesterol synthesis by propionate, a product of soluble dietary fiber fermentation. Several other hypotheses have been proposed, and these hypotheses are not mutually exclusive.

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Investigation of the Effects of Oat and Barley Feeding on Performance and Some Lipid Parameters in Table Ducks

  • Orosz, Szilvia;Husveth, Ferenc;Vetesi, Margit;Kiss, Laszlo;Mezes, Miklos
    • Asian-Australasian Journal of Animal Sciences
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    • v.20 no.7
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    • pp.1076-1083
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    • 2007
  • The effects of barley and oat feeding in table duck were investigated. During a 49-day growing period a corn-based diet was supplemented by 45% barley and 45% oats (isonitrogenously and iso-energetically), respectively. Daily feed intake, FCR-, and weight gain were measured. Abdominal fat, liver, and gizzard weights were determined and dry matter, protein, fat content and fatty acid composition of femoro-tibial muscles and liver fat were measured on the $35^{th}$, $42^{nd}$ and $49^{th}$ days of age. Feeding 45% barley caused a decrease of growth rate ($p{\leq}0.05$) during the first 4 weeks, which was followed by a rapid, compensatory growth from the $6^{th}$ week of age ($p{\leq}0.05$). Both barley and oat supplementation increased protein ($p{\leq}0.05$), while decreasing fat ($p{\leq}0.05$) and dry matter ($p{\leq}0.05$) content of the liver. Feeding of 45% oats in the diet decreased the monounsaturated fatty acid ($p{\leq}0,05$) and increased the n-6 ($p{\leq}0,05$), n-3 ($p{\leq}0,05$) and total polyunsaturated ($p{\leq}0,05$) fatty acid content of the intramuscular fat owing to the high proportion of soluble non-starch polysaccharides (NSP) in the diet. This might be explained by the more pronounced decrease in digestibility of saturated than unsaturated fatty acids in birds fed a soluble NSP-enriched diet. This result might be caused by the "cage effect" of soluble NSP trapping the bile salts which are more important for the absorption of saturated than polyunsaturated fatty acids.

Effect of Alfalfa Saponin on the Serum Cholesterol Level in Rats (알팔파 사포닌이 흰쥐 혈청 콜레스테롤 농도에 미치는 영향)

  • Cho, Young-Su;Horigome, Takao
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.18 no.4
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    • pp.430-434
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    • 1989
  • Alfalfa saponin was isolated from the roots of alfalfa(Medicage sativa L.) and incoporated at the level of 0.2% and 0.4% cholesterol-free diets and cholesterol enriched-diets. Wistar male rats weighing approximately 80g were fed with for 21 days. The serum lipids and fecal excretion lipids of the rats were determined and the result obtained are as follows. 1. Alfalfa saponin contained 36.4% medicagenic acid. 2. The feeding of alfalfa saponin increased cholesterol excretion but not bile acid excretion. 3. Alfalfa saponin showed hypocholesterolemic activity at 0.4% level in both the diets with and without cholesterol but the effect was not observed at 0.2% level in a diet. 4. It was indicated that the hypocholesterolemic effect of alfalfa saponin was associated with the decreased absorption of cholesterol from alimentary canal.

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Effects of black chokeberry on cholesterol metabolism in HepG2 cells (블랙 초크베리가 HepG2세포에서 콜레스테롤 대사에 미치는 효과)

  • Lee, Sang Gil;Kim, Bohkyung
    • Korean Journal of Food Science and Technology
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    • v.54 no.4
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    • pp.398-402
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    • 2022
  • Black chokeberry (Aronia melanocarpa), a rich source of polyphenols, exerts hypocholesterolemic effects. However, little is known about its effects on the regulation of the hepatic cholesterol metabolism and the underlying mechanisms. In the present study, the effects of polyphenol-rich black chokeberry extract (CBE) on hepatic cholesterol metabolism were investigated by measuring the expression of genes involved in the absorption, de novo synthesis, and efflux of cholesterol in HepG2 cells. There was a significant reduction in the expression levels of genes involved in cholesterol metabolism, the low-density lipoprotein receptor, 3-hydroxy-3-methylglutaryl coenzyme A reductase, and sterol regulatory element-binding protein 2, in CBE-treated HepG2 cells. Meanwhile, CBE increased the expression levels of genes involved in cholesterol and bile acid efflux. The expression levels of mitochondrial fatty acid oxidation genes increased, whereas those of lipogenic genes decreased following CBE treatment. These data suggest that the consumption of black chokeberry may be beneficial for the prevention of hypercholesterolemia.

Effects of Angelica keiskei on Lipid Metabolism in Rats (Angelica keiskei가 흰쥐의 지질대사에 미치는 영향)

  • Park, Jeong-Ro;Park, Seok-Kyu;Cho, Young-Sook;Chun, Soon-Sil;Choi, Seong-Hee;Park, Jong-Cheol
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.26 no.2
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    • pp.308-313
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    • 1997
  • To investigate the effects of Angelica keiskei Koidz on cholesterol metabolism, male Sprague Dawley rats were fed diets containing 5% of A. keiskei flour for 6 weeks. A. keiskei decreased plasma contents of total cholesterol, LDL-cholesterol and triglyceride while showing no change in HDL-cholesterol, resulting in reduction of atherosclerotic index. Decrease in liver concentration of triglyceride and increases in fecal excretion of cholesterol, total neutral steroid and bile acid were also observed. Those results suggest that A. keiskei improves hypercholesterolemia through, at least in part, reducing the absorption of cholesterol and enhancing the catabolism of cholesterol to bile acids.

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Health Improvement and Treatment Effect of Probiotics (프로바이오틱스의 건강증진과 질병치료 효능)

  • Baek, Young-Mi;Kim, Kyung-Soon;Lee, Yeon-Weol;Cho, Chong-Kwan;Yoo, Hwa-Seung
    • Journal of Haehwa Medicine
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    • v.19 no.1
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    • pp.25-34
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    • 2010
  • Background : The human being and the bacteria have accomplished a balance and have coexisted each other during long time. Probiotics have evolved with the human host to exist and the result they have operated profitably to human host. So it requires that the functions of probiotics are expounded in view of Traditional Korean Medicine. Aim : Suggest the functions of probiotics in view of Traditional Korean Medicine. Method : The author's research has been performed to review the related references. Results : Probiotics assist the absorption of the lactose, proteins and minerals and product several kinds of vitamins, organic acids. Probiotics suppresses the growth of noxious bacteria and the production of harmful substances or gases. They absorbed and discharge the bile acid, and thus help us maintain the optimal level of blood cholesterol concentration. They can reinforce the immune response of the mucous membrane and control the hypersensitivity immune reaction such as asthma, atopy on the other hand. Probiotics have right functions as above and so can be applied widely in treatment of various disease and symptom. Conclusion : Considering the functions of probiotics in view of Traditional Korean Medicine, they participate in our spleen-earth-system (digestion and synthesis) and liver-wood-system (regulation of digestion, metabolism, internal secretion etc.), assist the function of lung-metal system(respiration and regulation of water metabolism) and regulate wi-chi (reinforce/control immune system). Consequently, hereafter there would be a necessity of control a circumstance in treatment of various diseases under these categories that probiotics should be able to do their right functions inside the human body.