• 제목/요약/키워드: in vitro absorption

검색결과 288건 처리시간 0.028초

Intestinal absorption of aloin, aloe-emodin, and aloesin; A comparative study using two in vitro absorption models

  • Park, Mi-Young;Kwon, Hoon-Jeong;Sung, Mi-Kyung
    • Nutrition Research and Practice
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    • 제3권1호
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    • pp.9-14
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    • 2009
  • Aloe products are one of the top selling health-functional foods in Korea, however the adequate level of intake to achieve desirable effects are not well understood. The objective of this study was to determine the intestinal uptake and metabolism of physiologically active aloe components using in vitro intestinal absorption model. The Caco-2 cell monolayer and the everted gut sac were incubated with $5-50{\mu}M$ of aloin, aloe-emodin, and aloesin. The basolateral appearance of test compounds and their glucuronosyl or sulfated forms were quantified using HPLC. The % absorption of aloin, aloe-emodin, and aloesin was ranged from 5.51% to 6.60%, 6.60% to 11.32%, and 7.61% to 13.64%, respectively. Up to 18.15%, 18.18%, and 38.86% of aloin, aloe-emodin, and aloesin, respectively, was absorbed as glucuronidated or sulfated form. These results suggest that a significant amount is transformed during absorption. The absorption rate of test compounds except aloesin was similar in two models; more aloesin was absorbed in the everted gut sac than in the Caco-2 monolayer. These results provide information to establish adequate intake level of aloe supplements to maintain effective plasma level.

RF 전자기장 생체 영향 실험에서 통계적 방법을 통한 전자기장 노출 불확실성 분석 (The analysis of RF dosimetric uncertainties by using statistical method at in-vivo and in-vitro experiments)

  • 최성호;김남
    • 한국전자파학회:학술대회논문집
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    • 한국전자파학회 2003년도 종합학술발표회 논문집 Vol.13 No.1
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    • pp.74-78
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    • 2003
  • This paper shows the dosimetric uncertainties of electromagnetic field at in-vivo and in-vitro experiments. For more accurate consequences of these researches, we have tried to find out any correlations among output power, power density and specific absorption rate(SAR) with the results of in-vivo, in-vitro tests and SAR reports of cellular phone and PDA. In the case of in-vivo tests, the power density has close statistical correlations with SAR value and in the event of in-vitro tests, the output power has considerable statistical correlations with SAR containing duty factor. On the other hand, we found that both power density and output power don't have any close correlations with SAR. And, we obtained fitted regression form among frequency, power density and SAR containing duty factor through multiple linear regression analysis.

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Enhancement of Heparin and Heparin Disaccharide Absorption by the Phytolacca americana Saponins

  • Cho, So-Yean;Sim, Joon-Soo;Kang, Sam-Sik;Jeong, Choon-Sik;Linhardt, Robert-J;Kim, Yeong-Shik
    • Archives of Pharmacal Research
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    • 제26권12호
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    • pp.1102-1108
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    • 2003
  • We studied the effects of phytolaccosides, saponins from Phytolacca americana, on the intestinal absorption of heparin in vitro and in vivo. The absorption enhancing activity of these compounds (phytolaccosides B, $D_2$, E, F, G and I) was determined by changes in transepithelial electrical resistance (TEER) and the transport amount of heparin disaccharide, the major repeating unit of heparin, across Caco-2 cell monolayers. With the exception of phytolaccoside G, all of them decreased TEER values and increased the permeability in a dose-dependent and time-dependent manner. In vitro, phytolaccosides B,$D_2$, and E showed significant absorption enhancing activities, while effects by phytolaccoside F and I were mild. In vivo, phytolaccoside E increased the activated partial thromboplastin time (APTT) and thrombin time, indicating that phytolaccoside E modulated the transport of heparin in intestinal route. Our results suggest that a series of phytolaccosides from Phytolacca americana can be applied as pharmaceutical excipients to improve the permeability of macromolecules and hydrophilic drugs having difficulty in absorption across the intestinal epithelium.

Phthalate 3종에 대한 경피투과 특성 연구 (Characteristics of Percutaneous Absorption for Three Kinds of Phthalate)

  • 정덕채;윤철훈;엄미선;황현석;백정훈;최진호
    • 한국환경보건학회지
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    • 제39권4호
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    • pp.360-368
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    • 2013
  • Objectives: Phthalates are used in a large variety of products including as coatings of pharmaceutical tablets, film formers, stabilizers, dispersants, emulsifying agents, and suspending agents. They have been the subject of great public concern in recent years. The extensive uses of this material have attracted attention and issues regarding its safety have been raised. Methods: In this study, three types of phthalate skin permeation were studied using matrixes such as ointments, creams and lotions in vitro. The absorption of phthalate diesters [Dimethyl phthalate (DMP), Di-n-propyl phthalate (DPP) and Di-n-pentyl phthalate (DNPP)] using film former has been measured in vitro through rat skin. Epidermal membranes were set up in Franz diffusion cells and their permeability to PBS measured in order to establish the integrity of the skin before the phthalates were applied to the epidermal surface. Results: Absorption rates for each phthalate ester were determined and permeability assessment made to quantify any irreversible alterations in barrier function due to contact with the esters. Types of phthalate in vitro experimental results quickly appeared in the following order DMP > DPP ${\geq}$ DNPP. Conclusions: In the experimental results, lotion> cream> ointment, and the permeation rate of lotion with a great amount of moisture was the fastest. Skin permeation rate is generally influenced by the chemical characteristics of a given chemical, such as molecular weight and lipophilicity. As the esters became more lipophilic and less hydrophilic, the rate of absorption decreased.

관류 랫드 장관모델에서의 케토프로펜의 흡수기전 연구 (Mechanistic Studies of Ketoprofen Absorption in Perfused Rat Intestine Model)

  • 김미정
    • Journal of Pharmaceutical Investigation
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    • 제37권2호
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    • pp.73-78
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    • 2007
  • The aim of this study was to investigate the absorption properties of ketoprofen. The in-situ perfusion model has advantages over in vitro models as it provides intact lymphatic and blood flow circulation. The absorption properties of six different concentrations of ketoprofen have been studied in single pass in-situ rat intestine model. $^{14}C-PEG$ 4000 was used as a permeability marker and the possibility of an energy dependent contribution to ketoprofen absorption was also Investigated using the metabolic inhibitor sodium azide. Three different concentrations of sodium azide were studied to examine its effect on absorption of ketoprofen from the rat intestine. The findings of this study suggest that mono-carboxylic type drugs like ketoprofen cause permeability changes in the intestine. This is shown by the increase in absorption of $^{14}C-PEG$ 4000 as the concentration of ketoprofen is increased. However, the trend for ketoprofen permeability is to decrease over the concentration ranges. It was observed that the Papp values for ketoprofen with sodium azide shows a trend towards reduction in the amount of ketoprofen absorbed from the rat intestine which was significantly different (p<0.05) from that of ketoprofen with sodium azide 3.0mM. This indicates that sodium azide has an affect on the absorption of ketoprofen. The pH of all the perfusion solutions was altered to ${\sim}pH\;6.7$ by the buffering capacity of the small intestine secretions. The results suggest that mechanisms other than passive diffusion may be involved in ketoprofen absorption. This would be consistent with the involvement of active transport or saturatable processes in the absorption of drugs containing monocarboxylic acid group, as has been previously suggested from in vitro data.

케토푸로펜 소프트 히드로겔의 항염증효과 (Anti-inflammatory Activity of Ketoprofen Soft Hydrogel)

  • 이은경;신영희;이치호
    • Journal of Pharmaceutical Investigation
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    • 제29권2호
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    • pp.137-143
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    • 1999
  • Ketoprofen together with various permeation enhancers was incorporated into a novel soft hydrogel which is semi-solid in a container and to form a thin film within a few minutes after applying on the skin. The effect of various enhancers on the skin permeation of ketoprofen from a soft hydrogel was investigated using in vitro and in vivo method. In vitro rat skin permeation of ketoprofen from soft hydrogel was conducted using modified Keshary-Chien diffusion cells. In vivo ketoprofen absorption was also investigated in rats, and the results were compared with that of commercial products. Anti-inflammatory activities were determined using carrageenan-induced paw edema method and adjuvant-induced arthritis method in rats. The anti-inflammatory activity of ketoprofen soft hydrogel formulation with that of commercial products were compared. In vitro as well as in vivo studies showed that $HPE-101^{\circledR}$ was the most effective skin permeation enhancer among those used in this study. Addition of an adhesive (polyisobutylene) in the soft hydrogel decreased skin permeation of ketoprofen. Paw edema and anti-arthritis tests showed that soft hydrogel containing $HPE-101^{\circledR}$ was more effective than the commercial products, which was consistent with the in vivo absorption experiment results.

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인삼 성분이 Ethanol의 장관내 흡수에 미치는 영향 (Effect of Ginseng on the Intestinal Absorption of Ethanol)

  • 허근;최종원
    • 약학회지
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    • 제27권2호
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    • pp.163-168
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    • 1983
  • The effect of ginseng butanol fraction (total sponin) on the absorption rate of ethanol in rat intestine was examined. Ginseng butanol fraction showed inhibitory effect on the intestinal absorption of ethanol in situ as well as in vitro test. Ginseng butanol fraction markedly decreased the ethanol blood level, delayed onset time of ethanol effect and shortened sleeping time when it was adminstered orally together with ethanol. These results suggest that ginseng may alter the ethanol blood level by decreasing the intestinal absorption of ethanol.

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배합약물(配合藥物)의 흡수(吸收)에 관(關)한 생물약제학적(生物藥劑學的) 연구(硏究) 1. Salicylamide에 항(抗) Histamine제(劑)를 배합(配合)하였을 때의 흡수효과에 관(關)하여 (A Biopharmaceutical Study on the Absorption of Some Compounding Drugs)

  • 김재완
    • Journal of Pharmaceutical Investigation
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    • 제1권1호
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    • pp.78-84
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    • 1971
  • The comparative studies were made on Salicylamide, used individually and compounded with antihistaminics as regards. (1) the absorption rate through isolated rat small intestine (in vitro) (2) the absorption rate through rat small intestine (in vivo), and the following effects were found. 1. The Absorption velosity of 2 m Mole gm. of salicylamide in the small intestine were decreased, when the agents compounded with tripelennamine indicating the greatest absorption inhibition in the case of m Mole gm. of tripelennamine. 2. The Absorption velosity of 2m Mole gm. of salicylamide in the small intestine were decreased, when the agents compounded with diphenhydramine indicating the greatest absorption inhibition in the case of 2m Mole gm. of diphenhydramine. 3. The Absorption velosity of 2m Mole gm. of salicylamide in the small intestine were increased, when the agents compounded with chlorpheniramine indicating the greatest absorption augmentation in the case of 0.2m Mole gm. of chlorpheniramine.

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Fabrication of Compound K-loaded Polymeric Micelle System and its Characterization in vitro and Oral Absorption Enhancement in vivo

  • Hong, Sun-Mi;Jeon, Sang-Ok;Seo, Jo-Eun;Chun, Kyeung-Hwa;Oh, Dong-Ho;Choi, Young Wook;Lee, Do Ik;Jeong, Seong Hoon;Kang, Jae Seon;Lee, Sangkil
    • Bulletin of the Korean Chemical Society
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    • 제35권11호
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    • pp.3188-3194
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    • 2014
  • Compound K (CK) was formulated as polymeric micelles (PM) using Pluronic$^{(R)}$ F-127 to enhance the oral absorption of CK, an intestinal bacterial metabolite of ginseng protopanaxadiol saponin. The physicochemical properties of Ck-loaded PM were characterized and an in vitro transport study using the Caco-2 cell system as well as an in vivo pharmacokinetic study using SD rats was carried out. The hydrodynamic mean particle size of CK-loaded PM (CK-PM) was $254{\pm}23.45nm$ after rehydration and the drug loading efficiency was ca. 99.9%. The FT-IR spectroscopy, X-ray diffraction, differential scanning calorimetry and scanning electron microscopy data supported the presence of a new solid phase in the PM. The $P_{app}$ value of in vitro Caco-2 cell permeation of CK-PM and the oral absorption of CK was enhanced about 1.2-fold and 2.6-fold compared to CK suspension, respectively, showing that the present PM formulation enabled an enhancement of oral CK absorption.

In vitro에서 시스테인에 대한 흰쥐의 경피 흡수 (In vitro, Percutaneous absorption for Rat about cysteine)

  • 정덕채;오은하;국원근
    • 한국응용과학기술학회지
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    • 제25권2호
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    • pp.137-143
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    • 2008
  • Chemicals for cosmetics, including skin, the skin absorbs some of the research in the field of science or pharmacy recently, about the environment and the health of the heightened interest in skin absorption, and many other human attributes and absorption evaluation studies are underway in various areas. In this study, The effects of commercial permanent wave products to skin which are composed with cysteine and bases using rat. Results are as follows; the content of penetration 4 hours later with steady state and no significant changeable after 20 hours later. In cysteine groups lag time and permeability coefficient of young skin is 3.32hr and $0.102{\mu}g/cm^2{\cdot}hr$, lag time and permeability coefficient of old skin is 4.04hr and $0.106{\mu}g/cm^2{\cdot}hr$. In conclusion of study lag time and permeability coefficient in old skin and wounded skin are faster than healthy skin. We notified that fine rinkle and rash of skin were changeable in the case of treating with permanent wave drugs than normal skin.