• Journal of Pharmaceutical Investigation
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• v.27 no.2
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• pp.125-131
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• 1997

Ethoxycarbonyloxyethyl ester of ceftezole (CFZ-ET) was synthesized as a prodrug by esterification of ceftezole (CFZ) with ethoxycarbonyloxyethyl chloride and was confirmed by spectroscopic analyses. CFZ-ET was more lipophillic than CFZ as assessed by n-octanol and water partition coefficients at various pH. CFZ-ET itself did not show any microbiological activity in vitro, but showed substaintial microbiological activity after oral administration of CFZ-ET, indicating that CFZ-ET is converted to microbiologically active metabolite, probably CFZ, in the body. When CFZ-ET was incubated in blood, liver and intestine homogenates of rabbits, liver homogenate showed the fastest conversion of CFZ-ET. CFZ-ET appears rapidly metabolized in the liver when given orally due to the hydrolysis of the ester to CFZ, the parent drug of CFZ-ET. In vivo metabolism of CFZ-ET to CFZ was confirmed in rabbit by HPLC analysis. CFZ-ET were higher than those in the serum samples taken after oral administration of equivalent amount of CFZ. Oral bioavailability of CFZ-ET was 1.5-fold higher than that of CFZ in rabbits because of enhanced lipophilicity and absorption. Based on these findings, CFZ-ET appears useful as a prodrug of CFZ to improve the oral bioavailability of CFZ.

• Journal of Korean Society on Water Environment
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• v.20 no.3
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• pp.296-300
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• 2004

The rejection properties of 6 aromatic pesticides were evaluated by a continuous flow system equipped with a hollow fiber NF membrane. Different from the separation experiment of batch cell, the rejection and the removal could be calculated exactly because the concentration of feed, permeate and retentate was separately obtained. The lowest and the highest rejection were found in carbaryl(54.8%) and methoxychlor(99.2%), respectively, and the removals were always shown higher than rejections. This may be caused by some reasons such as the solute adsorption on the membrane, the variation of feed concentration. Although molecular weight, molecular width regarded as solute characteristics and log P(n-octanol/water partition coefficient) as hydrophobicity could be applied to explain the rejection property, these factors should be considered together for better analysis. According to the higher relationship between log B(solute permeability) and molecular weight, it was revealed that the solute separation with this membrane was influenced more by molecular weight.

• Journal of Soil and Groundwater Environment
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• v.27 no.6
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• pp.11-21
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• 2022

Sorption of phenanthrene (PHE) and pyrene (PYR) in several sorbents, i.e., natural soil, BionSoil^®, Pahokee peat, vermicompost and Devonian Ohio Shale and a surfactant (hexadecyltrimethyl ammonium chloride)-modified montmorillonite (HDTMA-M) were investigated. Pyrene exhibited higher sorption tendency than phenanthrene, as predicted by its higher octanol to water partition coefficient (K_ow). Several sorption models: linear, Freundlich, solubility-normalized Freundlich model, and Polanyi-Manes model (PMM) were used to analyze sorption isotherms. Linear isotherms were observed for natural soil, BionSoil^®, Pahokee peat, vermicompost, while nonlinear Freundlich isotherms fitted for Ohio shale and HDTMA-M. The relationship between sorption model parameters, organic carbon content (f_oc), and elemental C/N ratio was studied. In the binary competitive sorption of phenanthrene and pyrene in natural soil, competition between the solutes caused reduction in the sorption of each solute compared with that in the single-solute system. The ideal adsorbed solution theory (IAST) coupled with the single-solute Freundlich model was not successful in describing the binary competitive sorption equilibria. This was due to the inherent nature of linear sorption of phenanthrene and pyrene in natural soil. The result indicates that the applicability of IAST for the prediction of binary competitive sorption is limited when the sorption isotherms are inherently linear.

• Applied Chemistry for Engineering
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• v.16 no.6
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• pp.778-784
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• 2005

It has been found that the addition of cosurfactant is necessary in order to expand three phase region containing middle phase microemulsion in ternary systems containing alkyl ethoxylate (AEO) nonionic surfactant, commercial lubricant and water. Phase behavior in the surfactant systems with addition of cosurfactant over a temperature range of 30 to $60^{\circ}C$ showed different trends depending on surfactant, temperature and chain length of alcohol added. For the $C_{12}E_4$ system, addition of n-pentanol and n-hexanol both produced a three phase region over a wide range of temperatures but the middle-phase formed was found to be a $L_3$ or D' phase which would not facilitate solubilization of high molecular weight lubricants. On the other hand, for the $C_{12}E_5$ system, the middle-phase microemulsion was found to be formed with addition of a rather long-chain alcohol such as n-hexanol, n-heptanol, n-octanol, or n-nonanol. The results shown with the addition of cosurfactant was understood in connection with interfacial tension measurements and composition analysis. The inability of the hydrocarbon region of the surfactant films to incorporate the large lubricant molecules and high solubility of a hydrophobic surfactant are thought to be the chief reasons for poor solubilization with D' phase.

• Journal of Life Science
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• v.18 no.11
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• pp.1570-1577
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• 2008

For useful basic data in developing of Omandungi (Styela plicata) processed products, volatile flavor compounds were analyzed to identify the key reaction flavor compounds induced through heat treatment ($100^{\circ}C$, 10 min) in Omandungi -Doenjang (soybean paste) soups and stew. A total of 128 flavor compounds were identified and composed mainly of esters (16), aromatic compounds (14), N-containing compounds (11), alcohols (34), terpenes (5), carbonyl compounds (23), furans (4), hydrocarbons (13), acids (5) and miscellaneous compounds (3). Three groups including aromatic compounds, alcohols and acids were detected in high amounts in Doenjang. However, the levels of C4-C6 series acids (i.e., pentanoic acid having off-flavor) decreased by cooking ($100^{\circ}C$, 10 min), whereas that of furans (i.e., furfural) as heat induced compounds increased 2 times. Alcohols were detected the major group in Omandungi and followed by hydrocarbons and aromatic compounds in that order. In particular, 3 compounds including decenol, 2,6-dimethylheptanol and octanol were the major alcohols of Omandungi. By cooking, the compounds known heat-induced compound, 2-acetyl-2-thiazoline and benzothiazole, were newly formed in Omandungi-Doenjang stew. The alcohols (i.e., decenol, 2,6-dimethylheptanol), hydrocarbons and aromatic compounds derived from Omandungi were supposed to enhance a seafood-like flavor in Omandungi-Doenjang stew.

• Journal of Environmental Health Sciences
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• v.27 no.2
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• pp.108-118
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• 2001

This study was performed to investigate the bioconcentration of IBP, methidathion and piperophos. The BCFs(bioconcentration factor), depuration rate constants for three pesticides in zebrafish(Brachydanio rerio) were measured by OECD guideline 305. The concentration of test pesicides were one-hundredth and one-thousandth concentration of 96-hrs L $C_{50}$ in accordance with OECD guideline 305. The results obtained are summarized as follows: The average BCF values of IBP were 5.31(n=4) and 7.30(n=4) at one-hundredth and one-thousandth concentration of 96-hrs L $C_{50}$ . The average BCF values of methidathion were 8.72(n=4) and 11.25(n=4), the average BCF values of piperophos were 34.30(n=4) and 42.60(n=4). Depuration rate constants of IBP were 0.09( $h^{-1}$ ) and 0.08( $h^{-1}$ ), half-life of IBP were 7.70 and 8.66 at each tested concentration. The concentrations of IBP in zebrafish at low and high concentrations rapidly decreased after 12(0.243$\mu\textrm{g}$/g) and 12 hours(0.040$\mu\textrm{g}$/g). Depuration rate constants of methidathion were 0.40( $h^{-1}$ ), half-life of methidathion were 1.73 at one-hunderdth and of 96-hrs L $C_{50}$ , repectively. The concentrations of methidathion in zebrafish at high concentrations rapidly decreased after 6 hours(0.18 $\mu\textrm{g}$/g). Depuration rate constant of low concentration was no measured because methidathion in zebrafish was depurated in 6 hours. Depuration rate constants of piperophos sere 0.15( $h^{-1}$ ) and 0.44( $h^{-1}$ ), half-life of piperophos were 4.62 and 1.58 at each tested concentration. The concentrations of piperophos in zebrafish at los and high concentrations rapidly decreased after 12(0.26$\mu\textrm{g}$/g) and 6 hours(0.015 $\mu\textrm{g}$/g). It was suggested that high BCF of piperophos was due to high Kow(octanol-water partition coefficient). The possibility of bioconcenration was not likely to be high because of its $K_{DEP}$(depuration rate constant) in the evniroment. It was suggested that low BCF of methidathion showed lowest Kow as well as the most rapid $K_{DEP}$. Therefore, the possibility of bioconcentration was not occured in the enviroment. It was suggested that the BCF dtermined for IBP was lower than that of other pesticides due to high Sw(water solubility), show $K_{DEP}$. Therefore, IBP revealed little bioconcentration effect on in aquatic ecosystem.ystem.

• Archives of Pharmacal Research
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• v.26 no.7
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• pp.526-531
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• 2003

KR-31378 is a new drug candidate intended for the use in the prevention of ischemia-reperfusion damage. The objective of this preformulation study was to determine the physicochemical properties of KR-31378. The n-octanol to water partition coefficients of KR-31378 were 0.0504 at pH 3 and 0.8874 at pH 10. Accelerated stability of KR-31378 in solution and solid state was studied at 5, 40, $60^{\circ}C$. The stability testing indicated that the t90 for the drug in solid was estimated to be 2 years and 128.6 days at $25^{\circ}C$, while the that in aquesou solution was 68.6 days at $25^{\circ}C$. The KR-31378 was also found to be unstable under the relative humidity of 76%, probably because of the hygroscopic nature of the drug. In order to study compatibility of KR-31378 with typical excipients, potential change in differential scanning calorimetry spectrum was studied in 1:1 binary mixtures of KR-31378 and Aerosil, Avicel, Eudragit, lactose, PEG, talc, CMC, PVP, starch. As a result, CMC, PVP, and starch were found to be incompatible with KR-31378, indicating the addition of these excipients may complicate the manufacturing of the formulation for the drug. Particle size distribution of KR-31378 powder was in the size range of 9-93 $\mu$ m with the mean particle size of 37.9 $\mu$ m. The flowability of KR-31378 was apparently inadequate, indicating the granulation may be necessary for the processing of the drug to solid dosage forms. Crystallization of the drug with a number of organic solvents did not lead a crystalline polymorphism. In addition, dissolution of the drug from the powder was adequately rapid at $37^{\circ}C$ in water.

• Analytical Science and Technology
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• v.30 no.4
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• pp.174-181
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• 2017

Bio-liquid is a liquid by-product of the hydrothermal carbonization (HTC) reaction, converting wet biomass into solid hydrochar, bio-liquid, and bio-gas. Since bio-liquid contains various compounds, it requires efficient sampling method to extract the target compounds from bio-liquid. In this research, fatty acid methyl ester (FAME) in bio-liquid was extracted based on hollow fiber supported liquid phase microextraction (HF-LPME) and determined by Gas Chromatography-Flame Ionization Detector (GC-FID) and Gas Chromatography/Mass Spectrometry (GC/MS). The well-known major components of biodiesel, including methyl myristate, palmitate, methyl palmitoleate, methyl stearate, methyl oleate, and methyl linoleate had been selected as standard materials for FAME analysis using HF-LPME. Physicochemical properties of bio-liquid was measured that the acidity was 3.30 (${\pm}0.01$) and the moisture content was 100.84 (${\pm}3.02$)%. The optimization of HF-LPME method had been investigated by varying the experimental parameters such as extraction solvent, extraction time, stirring speed, and the length of HF at the fixed concentration of NaCl salt. As a result, optimal conditions of HF-LPME for FAMEs were; n-octanol for extraction solvent, 30 min for extraction time, 1200 rpm for stirring speed, 20 mm for the HF length, and 0.5 w/v% for the concentration of NaCl. Validation of HF-LPME was performed with limit of detection (LOD), limit of quantitation (LOQ), dynamic range, reproducibility, and recovery. The results obtained from this study indicated that HF-LPME was suitable for the preconcentration method and the quantitative analysis to characterize FAMEs in bio-liquid generated from food waste via HTC reaction.

• Journal of Pharmaceutical Investigation
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• v.33 no.1
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• pp.21-28
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• 2003

Ketorolac tromethamine(KT) is a nonsteroidal agent with potent analgesic and moderate anti-inflammatory activity. The lipid-water partition coefficient of KT was evaluated and KT gel was formulated as a gel containing different pH, different concentrations of polymer (poloxamer 407, carbopol 941), propylene glycol, ethanol and various enhancers. The resulting KT gels were evaluated with respect to their viscosity, in vitro drug permeation rate through hairless mouse skin and stability. In n-octanol and chloroform, the lipid-water partition coefficient of KT was the highest at pH 4 phosphate buffer. The apparent viscosity of KT gel increased with an increase in gel pH, polymer and enhancer concentration. But the apparent viscosity of KT gel decreased with an increase in ethanol concentration. The permeation rate of KT through hairless mouse skin from gels different pH was maximum at pH 4 which is close to KT $pK_{a}$ 3.54. The permeation rate decreased with an increase in polymer, propylene glycol concentration. But the permeation rate increased with an increase in ethanol. The increase of drug concentration from 1 to 3% induced linear increase in permeation rate. The best enhancer was the combination of $Labrasol^{\circledR},\;Transcutol^{\circledR}$, oleic acid and l-menthol. In the accelerated stability test(25, 40 and $50{\circ}C$), pH 5 gel was most stable and pH 4 gel was most unstable for 90 days.

• Journal of Pharmaceutical Investigation
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• v.23 no.3
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• pp.41-50
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• 1993

The iontophoretic delivery across rat skin of quaternary ammonium salts (isopropamide: ISP, pyridostigmine: PS), which are positively charged over a wide pH range, was measured ill vitro. The study showed that: (a) iontophoresis significantly enhanced delivery of ISP and PS compared to respective passive transport; (b) delivery of ISP and PS was directly proportional to the applied continuous direct current density over the range of $0-0.69\;mA/cm^2;$ (c) delivery of ISP and PS was also proportional to the drug concentration in the donor compartment over the range of $0-2{\time}l0^{-2}M:$ (d) sodium ion in the donor compartment inhibited the drug transport possibly due to decreasing the electric transference number of the drug; (e) delivery of ISP and PS increased as the pH of the donor solution increased over the pH range 2-7 suggesting permselective nature of the epidermis, and inhibition of the transference number of the drugs by hydronium ion; (f) some organic anions such as taurodeoxycholate, salicylate and benzoate which form lipophilic ion-pair complexes with ISP inhibited the delivery of ISP. The degree of inhibition by the organic anions was linearly proportional to the extraction coefficient $(K_e)$ of ISP from the partition system with each counteranion between phosphate buffer (pH 7.4) and n-octanol. For PS, however, taurodeoxycholate, but not salicylate and benzoate inhibited the iontophoretic delivery. It suggests that not only sodium ion and hydronium ion but also the counteranions which form lipophilic ion-pairs with quaternary ammonium drugs are not favorable components in formulating the donor solution of the drugs to achieve an effective iontophoretic delivery.