• Journal of Pharmaceutical Investigation
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• v.31 no.3
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• pp.143-150
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• 2001

Butyrolactone ester of ceftezole (CFZ-BL) was synthesized by esterification of ceftezole (CFZ) with ${\alpha}-bromo-{\gamma}-butyrolactone$. The synthesis was confirmed by spectroscopic analysis. CFZ-BL was more lipophilic than CFZ when the lipophilicity was assessed by partition coefficients between n-octanol and water at various pH. CFZ-BL itself did not show any microbiological activity in vitro, but serums taken after oral administration of CFZ-BL showed substaintial microbiological activity indicating that CFZ-BL is converted to microbiologically active metabolite, probably CFZ, in the body. The conversion was confirmed by in vitro incubation study, in which CFZ-BL was incubated in some body tissues of rabbit. Liver homogenate showed fastest conversion of CFZ-BL among the tissues tested (blood and intestine). Thus, CFZ-BL appeares to be rapidly metabolized in the liver to CFZ following oral administration. The metabolism process appears to be hydrolysis of the ester to CFZ, the parent drug of CFZ-BL. In vivo metabolism of CFZ-BL to CFZ was confirmed by analying CFZ by HPLC. CFZ concentration in the serum samples taken after oral administration of CFZ-BL were higher than those in the serum samples taken after oral administration of equivalent amount of CFZ. Oral bioavailability of CFZ-BL, a prodrug of CFZ, was 1.45-fold higher than that of CFZ in rabbits possibly due to enhanced lipophility and absorption of the prodrug.

• Journal of Pharmaceutical Investigation
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• v.31 no.4
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• pp.217-224
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• 2001

To develop a novel transdermal delivery system of loxoprofen (LP), a potent antiinflammatory and analgesic agent, the effects of various vehicles and penetration enhancers on the skin permeation of LP from solution formulations were investigated. The permeation rate of LP through excised guinea pig skin was measured using a side-by-side permeation system at $32^{\circ}C$. The solubilities of LP in various vehicles were determined by the equilibrium solubility method, and partition coefficients $(P_c)$ were determined. The solubility of LP increased in the rank order of water & isopropyl myristate (IPM) & glyceryl dicaprylate/dicaprate & propylene glycol dicaprylate/caprate & propylene glycol laurate (PGL) & polyethylene glycol 400 & diethylene glycol monoethyl ether (DGME) & ethanol. n-Octanol-water $P_c$ value was 15.5. Among pure vehicles tested, IPM and PGL showed highest fluxes of $89.9{\pm}5.0$ and $45.4{\pm}0.3\;{\mu}g/cm^2/hr$ from saturated solutions, respectively. However, it was not possible to demonstrate any correlation between the solubility of LP and its permeation rate, indicating the change in the barrier property of the skin and/or carrier mechanisms by vehicles tested. The addition of DGME to IPM or PGL markedly increased the solubility of LP, but the permeation rate did not decrease when the concentration of DGME in the cosolvent was increased upto 40%. The addition of linoleic acid (3%) in the cosolvent slightly increased the permeation rate, but others such as lauroyl sarcosine, fatty alcohols and fatty acids tested did not show enhancing effect. In conclusion, the DGME-IPM or DGME-PGL cosolvent system proved to be a good vehicle to enhance the skin permeation of LP.

• Archives of Pharmacal Research
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• v.26 no.12
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• pp.1002-1008
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• 2003

Ferulic acid (3-methoxy, 4-hydroxy cinnamic acid) is a flavoid component possessing antioxidant property. The compound is currently under development as a new drug candidate for the treatment of the dementia. The objective of this preformulation study was to determine the physicochemical properties of ferulic acid. The n-octanol to water partition coefficients of ferulic acid were 0.375 and 0.489 at the pHs of 3 and 10, respectively. Accelerated stability study for ferulic acid indicated that the t 90 value for the drug was estimated to be 459 days at $25^{\circ}C$. Ferulic acid was also found to be unstable under the relative humidity of more than 76%, probably because of the hygroscopic nature of the drug. In order to study compatibility of ferulic acid with typical excipients, potential change in differential scanning calorimetry spectrum was studied in 1: 1 binary mixtures of ferulic acid and typical pharmaceutical excipients (e.g., Aerosil, Avicel, CMC, Eudragit, lactose, PEG, PVP, starch and talc). Avicel, CMC, PVP and starch were found to be incompatible with ferulic acid, indicating the addition of these excipients may complicate the manufacturing of the formulation for the drug. Particle size distribution of ferulic acid powder was in the size range of 10-190 $\mu$m with the mean particle size of 61 $\mu$m. The flowability of ferulic acid was apparently inadequate, indicating the granulation may be necessary for the processing of the drug to solid dosage forms. Two polymorphic forms were obtained by recrystallization from various solvents used in formulation. New polymorphic form of ferulic acid, Form II, was obtained by recrystallization from 1,4-dioxane. The equilibrium solubility for Form I was approximately twice of that for Form II. The dissolution rate of Form II was higher than that of Form I in the early phase (<6 min). Therefore, these physicochemical information has to be taken in the consideration for the formulation of ferulic acid.

• Journal of the Korean Ceramic Society
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• v.32 no.5
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• pp.594-600
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• 1995

Spherical alumina gel powders were produced by hydrolysis of aluminum sec-butoxide (Al(sec-OC4H9)3) in a n-octanol/acetonitrile mixed solvent. The enlargement of particle size was induced by increasing HPC (hydroypropylcellulose) concentration (0.005, 0.1, and 0.05 g/ι) and emulsion-state aging time (10 min and 360 min). Mean particle sizes of dried alumina gel powders increased from 1.4 ${\mu}{\textrm}{m}$ to 3.5${\mu}{\textrm}{m}$ at 10-min emulsion-state aging time and from 1.9${\mu}{\textrm}{m}$ to 4.1${\mu}{\textrm}{m}$ at 360-min emulsion-state aging time as HPC concentration increased from 0.005 g/ι to 0.05 g/ι. At the same HPC concentration, particle size of dried alumina gel powder increased with increasing of emulsion-state aging time from 10 min to 360 min. The increase in the average particle size of dried alumina gel powder with increase in HPC concentration was interpreted as the enlargement of particles from alkoxide emulsions unprotected by HPC. The produced dried gel powder calcined at 115$0^{\circ}C$ for one hour transformed to $\alpha$-alumina.

• Journal of the Korean Society of Safety
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• v.7 no.2
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• pp.63-70
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• 1992

The aim of this research is to obtain a basic quantitative understanding of the effect of a noncondensable gas on the absorption of water vapor by a $H_2O$ / LiBr combination with n-octanol as the surfactant. Nonflowing aqueous solutions of LiBr (40,45,50 mass％) were exposed to saturated water vapor following the addition of an n-octanol sufactant (0.01 and 0.6 mass％). A small amount of a noncondensable gas (air) was allowed into the absorber (0.03 volume％) and its effect was analyzed by measuring the amount of water vapor absorbed. This study will aid to predict the performance of heat pump and safety operating condition when the noncondensable gas is not allowed in the absorber The results indicate that, in the presence of small amounts of a noncondensable gas, vapor absorption enhancement ratios are less than half o( those obtained under the same experimental conditions when a noncondensable gas is not present (1). The presence of a noncondensable gas causes the partial vapor pressure of air to increase at the vapor / liquid interface, which results in an instability of vapor absorption rate nd. hence, in an inhibition of interfacial disturbance.

• Korean Chemical Engineering Research
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• v.50 no.6
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• pp.969-979
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• 2012

In this study, the effects of cosurfactant on phase equilibrium and dynamic behavior were studied in systems containing nonylphenol ethoxylate (NP) surfactant solutions and nonpolar hydrocarbon oils. All the cosurfactants used during this study such as n-pentanol, n-octanol and n-decanol acted as a hydrophobic additive and the hydrophobic effect was found to increase with both increases in chain length and amount of addition of a cosurfactant. Dynamic behavior studies under hydrophilic conditions showed that the solubilization of hydrocarbon oil by NP micellar solution is controlled by an interface-controlled mechanism rather than a diffusion-controlled mechanism. Both spontaneous emulsification of water into oil phase and expansion of oil drop were observed under lipophilic conditions because of diffusion of surfactant and water into oil phase. Under conditions of a three phase region including a middle-phase microemulsion, both rapid solubilization and emulsification of oil into aqueous solutions were found mainly due to the existence of ultralow interfacial tension.

• Korean Chemical Engineering Research
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• v.50 no.6
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• pp.1021-1026
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• 2012

The transient mass transfer in a single droplet system consisting of 1-octanol (continuous phase)/aqueous succinic acid solution (dispersed phase) was investigated in the presence of chemical reaction, which is acid/anion exchange reaction of succinic acid and tri-n-octylamine (TOA). This succinic acid extraction by TOA can be considered to occur at the interface between organic and aqueous phase, that is, heterogeneous reaction system. The basic properties of the system such as viscosity, density, distribution coefficient, terminal velocity of droplet, and diffusion coefficient were measured experimentally or calculated theoretically, and used for theoretical calculation of characteristic parameters of mass transfer later. The effects of succinic acid concentration on the terminal velocity was negligible in the existence of TOA, although the terminal velocity increases with succinic acid concentration in the absence of TOA. On the contrary, the terminal velocity decreases with TOA concentration. While droplets falls through organic phase, the trajectory of droplets is observed to oscillate around its vertical path. A mass trnasfer cell was prepared to monitor the mass transfer behavior in a single droplet and used to measure the mean concentration of succinic acid inside droplet. The results are expressed with dimensionless parameters. Under 50 g/L succinic acid condition, the system with 0.1 mol/kg TOA showed that the molar flux decreases in proportion to the decrease of concentration gradient, while in the case of 0.5 mol/kg TOA Sh increases rapidly with time indicating the molar flux of succinic acid decreases relatively slowly compared to the decrease in concentration gradient.

• Food Science of Animal Resources
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• v.32 no.6
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• pp.810-819
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• 2012

This study investigated the chemical composition, meat quality and volatile flavor compounds in loin and top round of Hanwoo beef (n=126) depending on different age groups (G1, <5; G2, 6-8; G3, >9 years old). The intramuscular fat content (%) was higher for loin and top round of G1 (p<0.05) than that in the other groups. There was no difference in age groups for the top round; however, the loin of G1 had lower protein content (p>0.05). Total collagen content was lower in the top round of G3 (p<0.05). The loin and top round muscles of G1 had higher $a^*$ values and lower Warner Bratzler shear force values than that in the other age groups (p<0.05). The loin muscles of G1 were lower in percentage of cooking loss and higher in the water holding capacity than the loin in the other groups (p<0.05). The loin of G1 had lower total content of saturated fatty acids, whereas the top round of G1 had higher total content of monounsaturated fatty acids and lower total content of polyunsaturated fatty acids than that in the other age groups (p<0.05). Alanine was the highest free amino acid in the loin of Hanwoo beef, followed by glutamine, glycine, isoleucine and proline. The loin of G1 had higher contents of threonine, alanine, valine, methionine, phenylalanine, leucine and lysine than those in the other groups (p<0.05). The loin of G3 contained higher 3-methylbutanal, furfural, octanal, 1-(acetyloxy)-2-propanone, 1-octanol, 2,5-dimethylpyrazine and 2-ethyl-2,5-dimethylpyrazine in volatile flavor components than the loin in G1(p<0.05).

• Korean Journal of Food Science and Technology
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• v.34 no.4
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• pp.625-630
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• 2002

Raw pine-mushrooms (Tricholoma matsutake Sing.) of four grades and those frozen were analyzed for proximate composition, smell pattern, volatile flavor compounds, and sensory evaluation. Proximate compositions of raw pine-mushrooms (A-C, regular grade) were $89.48{\sim}90.77%$ moisture, 6.81% ash excluding D (below regular grade) sample, $2.24{\sim}2.52%$ crude lipid, and $16.19{\sim}20.01%$ crude protein. Proximate compositions of frozen pine-mushrooms preserved for 6 months at -20 and $-70^{\circ}C$ showed no difference compared with raw pine-mushrooms. Results of smell pattern and multidimensional analysis revealed raw pine-mushrooms showed no differences among samples, but frozen pine-mushrooms differed significantly depending on the grade. Volatile flavor compounds of pine-mushrooms were analyzed using a purge and trap method with GC/MSD. Twenty-nine volatile compounds were identified, among which alcohols such as 1-octen-3-ol, 2-octen-1-ol, 3-methyl-butanol, and n-octanol were commonly found in all pine-mushroom samples. In sensory attributes, raw pine-mushrooms were not significantly different at 5% level, and sample D of frozen pine-mushrooms scored lower than samples $A{\sim}C$.

• Korean Journal of Food Science and Technology
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• v.45 no.3
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• pp.285-292
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• 2013

This study was carried out to validate the safety of ametoctradin residues in agricultural commodities by developing an official analysis method. An analytical method was developed and validated using HPLC-PDA detectors. The samples were extracted with methanol, subsequently partitioned with dichloromethane and purified with florisil column chromatograph using acetone/hexane (30/70, v/v) as solvent. The method was validated by using grape, hulled rice, mandarin, and potato spiked with ametoctradin at 0.05 and 5.0 mg/kg, and pepper at 0.05 and 2.0 mg/kg. Average recoveries were 76-114.8% with relative standard deviation less than 10%, and the limit of detection and limit of quantification were 0.0125 and 0.05 mg/kg, respectively. The result of recoveries and overall coefficient of variation of the laboratory results from Gwangju regional Food and Drug Administration (FDA) and Daejeon regional FDA was accorded with Codex Alimentarius Commission Guideline (CAC/GL 40). Based on these results, this method was found to be appropriate for ametoctradin residue determination and can be used as the official method of analysis.