• Title/Summary/Keyword: plasma protein binding

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A Comparative Study of the Influence of Miflumic Acid and Phenylbutazone on Warfarin-Plasma Protein Binding (약-약 상호작용 연구(IV) Warfarin의 혈장단백 결합에 대한 Niflumic Acid 및 Phenylbutazone의 영향 비교)

  • 조윤성;양중익
    • YAKHAK HOEJI
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    • v.24 no.2
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    • pp.97-100
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    • 1980
  • To determine in vitro effects of phenylbutazone and niflumic acid on warfarin binding to rabbit serum protein, warfarin was added to the rabbit plasma, and the bound fraction was determined by warfarin-protein complex fluorescence. The bound fraction was decreased by phenylbtazone and niflumic acid. From this effect niflumic acid was found to have the more potent ability to displace warfarin from protein binding sites than phenylbutazone.

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Binding of Nalidixic Acid with Plasma Protein -On the Species Difference in Binding- (Nalidixic Acid와 혈장단백(血漿蛋白)과 결합(結合)에 관(關)한 연구(硏究) -동물(動物)의 종속차(種屬差)에 대(對)하여-)

  • Kim, Shin-Keun
    • Journal of Pharmaceutical Investigation
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    • v.6 no.1
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    • pp.14-17
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    • 1976
  • Binding of nalidixic acid with plasma of male and female rats, dogs, and rabbits was studied in vitro using the method of equilibrium dialysis in 1/15 mole phosphate buffer (pH 7.4). Rat plasma had the most extensive binding capacity followed by dog and rabbit plasma, and the plasma of female had more extensive capability than male in rat and rabbit but it was reversed in dog.

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Prediction of the Concentration of Diphenylhydantion in the Brain Using a Physiological Pharmacokinetic Hybrid Model

  • Song, Sae-Heum;Shim, Chang-Koo;Lee, Min-Hwa;Kim, Shin-Keun
    • Archives of Pharmacal Research
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    • v.13 no.3
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    • pp.221-226
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    • 1990
  • A physiological pharmacokinetic hybrid model was developed in order to predict the disposition kinetics of diphenylhydantoin (DPH) in the brain from the plasma conentration data of DPH. The model was constructed under the assumptions of well-stirred, plasma flow-limited and lienar tissue diposition kinetics of DPH. DPH was administered intravenously to the rats at a dose of 10 mg/kg together with/without sodium salicylate (SA;10 mg/kg) and the DPH concentrations in the plasma and brain were determined. Plasma protein binding of DPH concentrations in the plasma and brain were determined. Plasma protein binding of DPH was also determined using equilibrium dialysis technique. Then the model was tested for its predictability of DPH concentrations in the brian from the plasma data of DPH. It was found that the predicted values of DPH concentrations in the brian were in fair agreement with the experimental values in the rats of both treatments. The 2-fold increase in the brain concentration of DPH by SA-coadinistration was predicted well from the plasma concentration and plasma free fraction ($f_p$) data of DPH using the model. Therefore, the hybrid model was concluded to be very useful for the prediction of the concentrations of DPH in the brain from the plasma concentration data. Finally, DPH concentrations in the human brian was calculated using this model from plasma DPH data in the literature, yet the scale-up of this model to the human is not convinced.

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Effects of pH, Temperature, and Protein Content on Water Binding Capacity of Hog Plasma Protein (pH, 온도, 단백질함량에 따른 돼지혈장 단백질의 보수력 변화)

  • Kim, J.B.;Yi, Y.H.
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.18 no.2
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    • pp.195-198
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    • 1989
  • The water binding capacity (WBC) of hoe plasma protein was investigated. The centrifugal condition for optimal separation of plasma from hog blood was fixed at 1400 g-force. The WBC of 5%-plasma-protein-solution eel increased rapidly between pH 6 and 7 but gradually after pH 7 at $85^{\circ}C$ for 30 min. The higher heating temperature demonstrated the higher WBC of 5%-plasma-protein-solution gel at pH 7 within short period of time. The WBC of 5%-plasma-protein-solution gel increased rapidly at the beginning of heating. The WBC per gram of plasma protein at pH 7 and $85^{\circ}C$ for 30 min decreased as protein concentration of the plasma solution increased.

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Study on the Protein Binding of Anti-cancer Agent, 2"-O-benzoylcinnamaldehyde, using Ultrafilteration and Flurescence Spectrometry

  • Ren , Shan;Kim, Dae-Duk;Lee, Chi-Ho
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.242.3-243
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    • 2003
  • The compound of 2"-O-benzoylcinnamaldehyde(CB-ph) is a derivative of 2"-hydroxycinnamaldehyde whcih is a methanol extract of cinnamomum cassia blume. It"s a new anti-cancer agent which has been showed to inhibit the growth of various tumor cells in vitro and in vivo. In order to investigate the effective drug concentration and bio-distribution of CB-ph, the plasma protein binding was studied. In this study, the degree of the binding of Cb-ph to various serum proteins, the binding parameters, the binding site of CB-ph in human serum albumin, and the effect of some extensive protein-binding drugs on the protein binding of CB-ph in human serum ablumin were investigated respectively by ultrafilteration and fluorescence spectrometry. (omitted)

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Malonyl Amino Acids and Their Esters as Psychoactive Agents I

  • Jain, Dilip;Tripathi, Meena;Kohli, D.V.;Uppadhyay, R.K.
    • Archives of Pharmacal Research
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    • v.15 no.2
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    • pp.184-186
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    • 1992
  • Malonic acid amides were synthesized using different amino acids and their esters. THe synthesized compounds were evaluated for their sedative activity on rats. Potentiating effect of all the compounds on pentobarbitone induced sleep on rats was observed. Plasma protein binding studies were also carried out and it was observed that the synthesized compounds have low plasma protein binding as compared to barbiturates.

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Effect of 2-Methylaminoethyl-4,4'-Dimethoxy-5, 6, 5' ,6'-Dimethyl­enedioxybiphenyl-2-Carboxylic Acid-2'-Carboxylate Monohydro­chloride (DDB-S) on Indocyanine Green (ICG) Clearance in Rats

  • Lee Kyoung-Jin;Kim Jae-Ryung;Lee Chi-Ho
    • Archives of Pharmacal Research
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    • v.28 no.1
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    • pp.115-119
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    • 2005
  • The clearance of ICG, a known hepatic blood flow marker was investigated in rats in order to examine whether DDB-S influences hepatic blood flow. The effect of DDB-S on the protein binding and blood-to-plasma partition of ICG was measured. The steady-state plasma concentration of ICG was monitored before and after co-administration of various concentration of DDB-S, and ICG clearance was estimated from the steady-state concentration and the infusion rate of ICG. There was no significant difference in protein binding and blood-to-plasma partition of ICG with and without addition of DDB-S (10, 20, and 40 ${\mu}g/mL)$. When ICG was infused into DDB-S pretreated rats, the steady-state concentrations of ICG decreased and the calculated ICG clearance increased. However, no dose-dependency of ICG Css on DDB-S Css was observed. Since DDB-S did not affect the protein binding and blood-to-plasma partition of ICG, the increased clearance of ICG with co-administration of DDB-S seems to be due to the increased hepatic blood flow by DDB-S.

Surface modification of polymeric membranes for low protein binding

  • Higuchi, Akon;Tamai, Miho;Tagawa, Yoh-Ichi;Chang, Yung;Ling, Qing-Dong
    • Membrane and Water Treatment
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    • v.1 no.2
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    • pp.103-120
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    • 2010
  • Surface modification of microfiltration and ultrafiltration membranes has been widely used to improve the protein adsorption resistance and permeation properties of hydrophobic membranes. Several surface modification methods for converting conventional membranes into low-protein-binding membranes are reviewed. They are categorized as either physical modification or chemical modification of the membrane surface. Physical modification of the membrane surface can be achieved by coating it with hydrophilic polymers, hydrophilic-hydrophobic copolymers, surfactants or proteins. Another method of physical modification is plasma treatment with gases. A hydrophilic membrane surface can be also generated during phase-inverted micro-separation during membrane formation, by blending hydrophilic or hydrophilic-hydrophobic polymers with a hydrophobic base membrane polymer. The most widely used method of chemical modification is surface grafting of a hydrophilic polymer by UV polymerization because it is the easiest method; the membranes are dipped into monomers with and without photo-initiators, then irradiated with UV. Plasma-induced polymerization of hydrophilic monomers on the surface is another popular method, and surface chemical reactions have also been developed by several researchers. Several important examples of physical and chemical modifications of membrane surfaces for low-protein-binding are summarized in this article.

Improvement of crop traits using auxin binding protein gene abp57 (옥신 호르몬 결합단백질 ABP57 유전자를 이용한 작물의 형질개선)

  • Kim, Dong-Hern;Lee, Keun-Pyo
    • Journal of Plant Biotechnology
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    • v.38 no.2
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    • pp.137-142
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    • 2011
  • Auxin is a group of small natural and synthetic molecules having diverse regulatory functions in plant growth and development. In this review, two auxin binding proteins identified by biochemical experiments to measure their auxin binding activities and biochemical functions are described. ABP1, a 22 kDa auxin binding protein, shows strong auxin binding affinity and possibly plays an important role in plant development, although its biochemical function are still unclear. ABP57, a 57 kDa soluble protein from rice shoots, has both of IAA binding activity and the plasma membrane proton pump activation. Although it is yet to be accomplished, the improvement of agronomic traits using auxin binding proteins is worth to be considered, since auxin is known to be related to such a diverse crop traits.

Effect of Phenobarbital on the Nonlinear Pharmacokinetics of Naproxen (나프록센의 비선형 체내동태에 미치는 페노바르비탈의 영향)

  • Lee, Yong-Bok;Chae, Myung-Ae;Koh, Ik-Bae
    • Journal of Pharmaceutical Investigation
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    • v.27 no.2
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    • pp.109-117
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    • 1997
  • In order to elucidate the effect of phenobarbital (PB) on the nonlinear pharmacokinetic behavior of naproxen (NAP), we compared the dose dependent hepatic intrinsic clearance, biliary excretion and protein binding of NAP in control rats to those in the PB-pretreated rats which were intraperitoneally pretreated with PB sodium (75 mg/kg) once a day for four days. NAP was injected via femoral (1.5 mg/kg) and portal(0.25, 0.5, 1.5, 15 and 30 mg/kg) vein to the control and PB-pretreated rats, respectively. And also, we measured the plasma free fraction of NAP with the equilibrium dialysis method and the biliary excreted total amounts of NAP in both rats. Plasma free fraction of NAP was decreased in lower concentration than $150\;{\mu}g/ml$ of NAP due to PB pretreatment. In higher concentration, however, plasma free fraction was increased. These in vitro results suggest that the total protein concentration was increased but the total binding capacity of NAP to protein was decreased by PB-pretreatment. The total plasma clearance and the hepatic intrinsic clearance of NAP had similar values in both groups, respectively. And, both clearances of NAP were significantly increased by PB-pretreatment. Even though the plasma free fractions of NAP in both groups were constantly remained within the concentration range according to the increase of administration dose, the hepatic intrinsic clearances of NAP were significantly increased in both groups with the increased dose. And, the biliary excreted total amounts of NAP were significantly increased by PB-pretreatment at the lower dose, but decreased at the higher dose. These in vivo results suggest that NAP represents the uncommon nonlinear pharmacokinetic behavior that the hepatic intrinsic clearance was enhanced with the increased dose, and that PB enhances further the hepatic intrinsic clearance of NAP with the increased dose due to its enzyme induction effect.

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