• Journal of Pharmaceutical Investigation
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• 제23권1호
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• pp.1-9
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• 1993

The endothelial cell of brain capillary called the blood-brain barrier (BBB) has carrier-mediated transport systems for nutrients and drugs. The mechanism of the BBB transport of basic and acidic drugs has been reviewed and examined for endogenous transport systems in BBB in WKY and SHRSP. Acidic drugs such as salicylic acid and basic drugs such as eperisone are taken up in a carrier mediated manner through the BBB via the monocarboxylic acid and amine transport systems. The specific dysfunction for the choline transport at the BBB in SHRSP would affect the function of the brain endothelial cell and brain parenchymal cell. The utilization of the endogenous transport systems of monocarboxylic acid and amine could be promising strategy for the effective drug delivery to the brain.

• Archives of Pharmacal Research
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• 제6권2호
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• pp.109-114
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• 1983

A mechanism of taurine transfer across the rat small intestine was elucidated by using the in situ recirculation perfusion or loop method. Taurine uptake was saturable, Km= 39.9 mM, and energy dependent, and required sodium. The close structural analogues, aminomethane sulfonic acid, .gamma.-amino-butyric acid, hypotaurine, and .betha.-alanine, reduced significantly taurine uptake when present in 10-fold excess. The .alpha.-amino acid, glycine, did not inhibit uptake. Hence, all of these findings lead to a conclusion that a carrier-mediated transport system for taurine exists in the small intestine.

• Bulletin of the Korean Chemical Society
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• 제17권12호
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• pp.1109-1111
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• 1996

The Podand Ⅰ (Figure 1) has been studied as cation carrier in a bulk liquid membrane system. Ag+ and some other transition metal ions (M2+=Cu, Ni, Co, Zn, and Cd) have been transported using the podand as carrier in a bulk liquid membrane system. Studies on the transport of equimolar mixtures of two or three competing components have also been carried out with the same system. Ag+ exhibited a higher transport rate than the other M2+ in the competitive experiments. Ligand structure and the equilibrium constant for complex formation are important parameters in the transport of the metal ions.

• 환경위생공학
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• 제11권2호
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• pp.21-26
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• 1996

In our previous studies, we reported that lead intoxicated nerve cell by inhibition of the Na$^{+}$-K$^{+}$ ATPase activity and reduction of myo-inositol in nerve cell. As the second series of experiments, in order to understand toxic mechanism of lead for nerve cell, the characteristics of myo-inositol transport system and the effect of lead on its system have been studied in the sciatic nerves of control and lead-treated rats. A lead intoxicated animal model was induced by feeding diet containing lead to Sprague-Dawley rat for two weeks. Four weeks aged Sprague-Dawley rats were divided into three group : normal control group, 10ppm-lead treated group, 100ppm-lead treated group. All rats were sacrified at the end of two weeks. The rate o myo-inositol transport by sciatic nerve isolated from lead-treated rat was significantly decreased compared with that of control rat. This deficit results from that myo-inositol transport system which is carrier mediated and sodium-potassium dependent was inhibited by the lead treatment (both 10ppm and 100ppm) due to increase of the Km value without affecting Vmax value for myo-inositol carrier. These observations suggest that the toxic mechanism of lead on nerve myo-inositol transport system might be a change of affinity without change of maximum transport velocity for carrier.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1997년도 춘계학술대회
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• pp.57-63
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• 1997

Animal and clinical investigations have shown that fluoroquinolones, new quinolone antibacterial agents (NQs), are well absorbed across the intestinal tract, with a bioavailability of 60-90% after oral administration. Although some types of carrier-mediated intestinal transport mechanisms have been reported for enoxacin (ENX), ofloxacin (OFLX) and sparfloxacin (SPFX), recent results using a human intestinal epithelial cell line, Caco-2, indicated a passive or nonsaturable transport of SPFX, one of the most hydrophobic NQs. The mechanism underlying the intestinal absorption of NQs is still largely unknown. The distribution of NQs into peripheral tissues including erythrocytes is very rapid and their tissue-to-plasma concentration ratios (Kp) are considerably larger than those of inulin (an extracellular fluid space marker), in spite of almost complete ionization of NQs at the physiological pH. Our findings suggest that OFLX and lomefloxacin (LFLX) are taken up by rat erythrocytes via a transport system common to that of a water-soluble vitamin, nicotinic acid.

• Bulletin of the Korean Chemical Society
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• 제16권1호
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• pp.33-36
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• 1995

Macrocyclic ligands have been studied as cation carriers in a supported liquid membrane system. Cd2+ has been transported using nitrogen substituted macrocycles as carriers and several divalent metal ions (M2+=Zn, Co, Ni, Cu, Pb, Mg, Ca, and Sr) have been transported using DBN3O2, DBN2O2and PolyNtnoen as carriers in a supported liquid membrane system. Competitive Cd2+-M2+ transport studies have also been carried out with the same system. Ligand structure, stability constant, membrane solvent and carrier concentration are also important parameters in the transport of metal ions.

• Bulletin of the Korean Chemical Society
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• 제9권5호
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• pp.292-295
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• 1988

Macrocyclic ligands have been studies as cation carriers in a bulk liquid membrane system. $Cu^{2+}$ has been transported using nitrogen substituted macrocycles as carriers and several transition metal ions($M^{n+}\;=\;Mn^{2+},\;Co^{2+},\;Ni^{2+},\;Cd^{2+},\;Pb^{2+}\;and\;Ag^{+}$) have been transported using $DBN_3O_2,\;DBN_2O_2,\;Me_6N_414C4$ and DA18C6 as carriers in a bulk liquid membrane system. Competitive $Cu^{2+}-M2^+$ transport studies have also been carried out for the same system. In single cation transport experiments, the best macrocyclic ligand for transport is a ligand that gives a moderately stable rather than very stable complex in the extraction. However, when both cations are present in the source phase, the cation which forms the most stable complex with carrier is favored in transport over other cations. Generally, the nitrogen substiituted macrocycles transport $Cu^{2+}$ selectively over $Mn^+$. Ligand structure, equilibrium constant (or stability constant) for complex formation, source phase pH and carrier concentration are also important parameters in transport experiments.

• Journal of Pharmaceutical Investigation
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• 제28권1호
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• pp.25-33
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• 1998

Intestinal absorption of ${\beta}-lactam$ antibiotics and angiotensin converting enzyme(ACE) inhibitors has been shown to use the carrier-mediated transport system. In vitro experiments have established that the efficacy of uptake by enterocytes depends on an inwardly directed proton gradient. It was suggested that benazepril was mediated by tripeptide transport system and that amoxicillin was transported by dipeptide transport carrier. The aim of this study is to assess the influence of amoxicillin on the intestinal absorption of benazepril using in vitro diffusion chamber and in situ single pass perfusion technique in the rat in order to elucidate whether the above transport systems are competitive or not. We obtained the gastrointestinal pemeability coefficient of amoxicillin, benazepril and both of them using in vitro diffusion chamber. And also the gastrointestinal absorption clearance of amoxicillin, benazepril and both of them using in situ single-pass perfusion method at steady state were calculated. Amoxicillin and benazepril were analyzed by HPLC. The results by the use of diffusion chamber in vitro indicated that the apparent intestinal permeability coefficient of benazepril was significantly(p<0.01) decreased by amoxicillin(45.2%) and vice versa significantly(p<0.01) decreased(89.1%). The results by the in situ gastrointestinal single-pass perfusion method indicated that the intestinal absorption clearance of benazepril was significantly(p<0.05) decreased by amoxicillin (40.2%) and vice versa significantly(p<0.05) decreased(54.8%). These results might suggest that they share the same peptide carrier pathway for oral absorption.

• 약학회지
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• 제38권2호
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• pp.114-122
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• 1994

A study on the absorption mechanism of cefixime(CF), an oral ${\alpha}-amino$ group deficient cephalosporin antibiotic, has been undertaken through the rat jejunum and nasal cavity using an in situ simultaneous perfusion technique developed in our laboratory. CF was well absorbed in the jejunum and nasal cavity of rats at pH 5.0, but not at pH 7.0. CF absorption was studied over four orders of magnitude in concentration to determine saturability. Disappearance of CF in the perfusate followed first-order kinetics at all tested concentrations. The apparent first-order absorption rate constant was found to be dependent on the concentration over the range of $0.1\;mM{\sim}3\;mM$ in the jejunum and nasal cavity of rats. Inhibitors were added to determine the competitive inhibition of CF absorption. The presence of L-tyrosine, L-phenylalanine, alanine-alanine, glycine-glycine and cefadroxil produced the significant inhibition of CF absorption in the nasal cavity and jejunum. However, there was no evidence of the inhibition in the presence of cefazolin. In addition, The CF absorption in the nasal cavity and jejunum was inhibited significantly by ouabain and 2,4-dinitrophenol(DNP). This study suggested that CF is absorbed across the rat nasal cavity and jejunum by carrier-mediated transport mechanism and energy consuming system.

• Korean Membrane Journal
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• 제4권1호
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• pp.36-40
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• 2002

The diffusion coefficients of ions in the reverse transport system using the carrier mediated membrane were estimated from the diffusional membrane permeabilities and the ion activity in membrane system. In the aqueous alkali metal ions-membrane system diffusional flux of alkali metal ions driven by coupled proton was analyzed. The aqueous phase I contained NaOH solution and the aqueous phase II also contained NaCl and HCl mixed solution. The concentration of Na ions of both phases were $10^{0},\;10^{-1},\;10^{-2},\;5{\times}10^{-1}\;and\;5{\times}10^{-2}\;mol{\cdot}dm^{-3}$ and the concentration of HCI in aqueous phase II was always kept at $1{\times}10^{-1}\;mol{\cdot}dm^{-3}$. Moreover, the carrier concentration in liquid membrane was $10^{-2}\;mol{\cdot}dm^{-3}$. The results indicated that the diffusion coefficients depend strongly on the concentration of both phases electrolyte solution equilibriated with the membrane. The points were interpreted in terms of the energy barrier theory. Furthermore, eliminating the potential terms from the membrane equation was derived.