• Journal of Pharmaceutical Investigation
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• v.23 no.2
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• pp.61-69
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• 1993

Prodrug of cefazolin (CFZ) was prepared with the objective of improving its oral bioavailability. Cefazolin phthalidyl ester (CFZ-PT) was synthesized and evaluated as potential prodrug form. The successful synthesis of CFZ-PT was identified by spectroscopic analysis. Partition coefficient studies showed that CFZ-PT is more lipophilic than CFZ and the ester was hydrolyzed enzymatically into the parent drug in blood, liver and intestinal homogenates. The pharmacokinetic characteristics of CFZ-PT and CFZ were compared following oral administrations to rabbits. Serum CFZ concentration was determined by HPLC method and the ester compound (prodrug) was not detected in serum following oral administration of CFZ-PT. CFZ-PT did not have antimicrobial activity in vitro against Bacillus subtilis ATCC 6633, whereas CFZ-PT in serum after oral administration to rabbits had antimicrobial activity. From above observations, it was noted that CFZ-PT is rapidly hydrolyzed to CFZ in the body and the bioavailability of CFZ-PT was increased by 3.5-fold than that of CFZ. From these results of this study, it was concluded that CFZ-PT may be a novel prodrug of CFZ which can improve the oral absorption of CFZ.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1996.04a
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• pp.286-286
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• 1996

In order to elucidate the mechanism of action of transdermal absorption-enhancing compounds, i.e., pyrrolidone derivatives (2-pyrrolidone, 1-methyl-2-pyrrolidone, 1-ethyl-2-pyrrolidone, 1,5-dimethyl-pyrrolidone and 5-methyl-2-pyrrolidone), multilamellar liposome was prepared from the simulated stratum corneum lipid and employed as a model system for the barrier function of the stratum corneum. The liposomal membrane of the stratum corneum lipid liposome (SCLL) behaves as an osmometer and has an excellent barrier function. In addition, its phase transition temperatures are similar to those of human stratum corneum intercellular lipid region. Therefore, SCLL seems to be a useful skin model. To estimate the barrier function of SCLL, the osmotic behavior of SCLL was measured in the presence of pyrrolidone derivatives and the effect on the phase transition temperature of SCLL was also investigated using differential calorimetry. Above a certain concentration (MLAC), enhances perturb the barrier function of the liposome. The relationship between MLACs and the partition coefficient of the pyrrolidone derivatives was observed; the greater the partition coefficients, the smaller the MLAC. This suggests that the more hydrophobic enhancers penetrate into the lipid layer more easily and reduce the barrier function of membrane more effectively. The results of differential scanning thermograms of the SCLL suggest that the pyrrolidone derivatives had incorporated into the lipid layer in the liposome and increased the fluidity of the lipid layer in the liposome. Such activity might have some correlation with the transdermal absorption-enhancing activity these compounds.

• Journal of Pharmaceutical Investigation
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• v.25 no.4
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• pp.323-330
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• 1995

Ceftezole pivaloyloxymethyl ester(CFZ-PV) was synthesized to improve oral absorption and bioavailability of parent drug by esterification of ceftezole(CFZ) with chloromethyl pivalate. The successful synthesis of CFZ-PV was conformed by spectroscopic analysis. Partition coefficient studies showed that CFZ-PV is more lipophillic than CFZ. The pharmacokinetic characteristics of CFZ-PV and CFZ were compared following oral administrations of these compounds to rabbits. The amount of CFZ in plasma was determined with an HPLC method. The ester compound (prodrug) was not detected in plasma following oral administration of CFZ-PV, and although CFZ-PV had not microbiological activity in vitro, the plasma taken after oral administration of CFZ-PV had microbiological activity. From above observations, it was noted that CFZ-PV is rapidly hydrolyzed to CFZ in the body. And the oral absorption of CFZ-PV was increased by yielding 2-fold bioavailability rather than CFZ. Therefore, CFZ-PV could be a novel prodrug of CFZ which can improve the oral bioavailability of CFZ.

• Korean Journal of Clinical Pharmacy
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• v.8 no.2
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• pp.133-138
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• 1998

Phthalimidyl ester of ceftezole (CFZ-PT) was synthesized as a prodrug by esterification of ceftezole (CFZ) with N-bromophthalimide. CFZ-PT was more lipophilic than CFZ when the lipophilicity was assessed by partition coefficients between n-octanol and water at various pH. The pharmacokinetic characteristic of CFZ-PT and CFZ preparations were compared following oral administrations of these compounds to rabbits. CFZ-PT is expected to be metabolized rapidly to CFZ in the body. The metabolism process appears to be hydrolysis of the ester to CFZ, the parent drug of CFZ-PT. In vivo metabolism of CFZ-PT to CFZ was confirmed in rabbit by HPLC analysis. CFZ concentration in the serum samples taken after oral administration of CFZ-PT(equivalent amount of CFZ) were released and higher than those of CFZ. Oral bioavailability of CFZ-PT was 1.9 fold higher than at of CFZ in rabbits because of enhanced lipophilicity and absorption. Finally, it was concluded that CFZ-PT appears useful as a prodrug of CFZ to improve the oral bioavailability of CFZ.

• 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.

• KSII Transactions on Internet and Information Systems (TIIS)
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• v.15 no.9
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• pp.3458-3481
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• 2021

Existing methods for blind identification of linear block codes without a candidate set are mainly built on the Gauss elimination process. However, the fault tolerance will fall short when the intercepted bit error rate (BER) is too high. To address this issue, we apply the reverse algebra approach and propose a novel "two-step-screening" algorithm by solving the linear error equations on the binary Galois field, or GF(2). In the first step, a recursive matrix partition is implemented to solve the system linear error equations where the coefficient matrix is constructed by the full codewords which come from the intercepted noisy bitstream. This process is repeated to derive all those possible parity-checks. In the second step, a check matrix constructed by the intercepted codewords is applied to find the correct parity-checks out of all possible parity-checks solutions. This novel "two-step-screening" algorithm can be used in different codes like Hamming codes, BCH codes, LDPC codes, and quasi-cyclic LDPC codes. The simulation results have shown that it can highly improve the fault tolerance ability compared to the existing Gauss elimination process-based algorithms.

• Journal of Pharmaceutical Investigation
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• v.35 no.2
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• pp.71-74
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• 2005

The aim of this study was to analyze characteristics of the barrier function of excised porcine buccal mucosa to the test compounds, estradiol, propranolol HCI, melatonin, and mannitol with a wide range of partition coefficient values. The permeability of melatonin was measured through frozen, stored, and fresh porcine buccal mucosa to examine the impact of storage conditions on the permeability of porcine buccal mucosa. The results demonstrated that the ex vivo permeability of the porcine buccal mucosa was greater for more lipophilic solutes, which was consistent with a series of molecules transported by passive transepithelial diffusion. The melatonin permeation profiles through frozen, stored, and fresh mucosa illustrated that damage was incurred by the freezing process of the mucosal tissue, leading to loss of the barrier function and thereby an increased permeation coefficient. It can be observed that the influence of compound lipophilicity on the association of the compounds with buccal mucosa was clear. The relationship between permeation coefficient and Log P values for the four compounds investigated demonstrated a proportional relationship, further confirming the importance of the lipophilicity of a compound to permeate the buccal mucosa. These results showed that the ex vivo porcine buccal mucosa model is a suitable tool to screen oral mucosal permeability.

• Applied Chemistry for Engineering
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• v.7 no.2
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• pp.237-244
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• 1996

Liquid-liquid extractions by use of microporous hollow fiber modules are fast compared with conventional extraction equipment because of the large surface area per volume. In these modules, the extractant and feed can be contacted at high speed and two flows are completely independent, so there are no problems with loading and channeling. In this paper, it was investigated the extraction selectivities for liquid-liquid extraction of Fe(II) and Ni(II) from dilute aqueous solution into TOA (tri-n-octylamine) and EHPNA (bis(2-ethylhexyle)hydrogenphosphite) as organic extractants by using the hydrophobic hollow fiber module. To determine the rate controlling step for mass transfer in hollow fibers, we also examined the effect of inside and outside flow rates of the hollow fiber module. From these experiments, we identified for the extraction of system with high partition coefficient in hydrophobic hollow fibers, mass transfer in the inside aqueous feed dominated the overall mass transfer, and in this paper, correlation between $K_w$ and $v_t$ was obtained as $K_w{\frac{d}{D}}=6.22\(\frac{d^2v_t}{LD}\)^{1/3}$ On the other hand, for the system with low partition coefficient, the resistance in the inside of hollow fibers was much less than membrane resistance because the extraction was not simple in the micropore. Thus, for systems with high partition coefficients, hydrophobic hollow fibers would be a better choice.

• Journal of Environmental Health Sciences
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• v.48 no.2
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• pp.75-85
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• 2022

Background: Various types of semi-volatile organic compounds (SVOCs) exist in the public's living environment. They occur in different forms in terms of their physical and chemical properties and partition coefficients. As a consequence, indoor exposure to SVOCs occurs via various routes, including inhalation of air and airborne particles, skin contact, and dust intake. Objectives: To propose a method for assessing human exposure to the SVOCs occurring in the air of an indoor environment, the concentrations of SVOCs in house dust and organic films measured in a real residential environment were estimated in terms of gas-phase concentration using the partition coefficient. Assessment of inhalation exposure to SVOCs was performed using this method. Methods: Phthalates were collected from samples of house dust and organic films from 110 households in a real residential environment. To perform an exposures assessment of the phthalates present in organic films, gas-phase concentration was calculated using the partition coefficient. The airborne gas-phase concentrations of phthalates from the house dust and organic films were estimated and exposure assessment was performed based on the assumption of inhalation exposure from air. Results: As a result of the exposure assessment for gas-phase phthalates from house dust and organic films, preschool children showed the highest level of inhalation of phthalates, followed by school children, adults, and adolescents. Conclusions: This study includes the limitation of not considering different SVOCs exposure pathways in the health impact assessment, including those of phthalates in the indoor living environment. However, this study has the significance of performing exposure assessment based on exposure to SVOCs present in indoor air that originated from organic films in the indoor residential environment. Therefore, the results of this study should be useful as basic data for exposure and health risk assessments of SVOCs associated with organic films in the indoor environment.

• Journal of Korean Society for Atmospheric Environment
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• v.26 no.5
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• pp.517-532
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• 2010

After establishment of Banwol industrial complex in 1987, Ansan city becomes the largest industrial sector development in Gyeonggi-do, Korea. As the population and industrial activity grow over this region, toxic air pollutants, particularly POPs (Persistent Organic Pollutants) from various emission sources have been major public concerns. Air samples for POPs monitoring were collected at the industrial sites ($A_2$), residential sites ($B_1$, $B_2$), commercial site (C), and rural/remote site (D) of the area of Ansan during 2008 with a prolonged industrial sampling site $A_1$ from 2001 to 2008. All samples were analysed for 2,3,7,8 substituted-polychlorinated dibenzo-p-dioxin and dibenzofurans (PCDD/Fs) and dioxin like polychlorinatd diphenyls (dl-PCBs). In site $A_1$, a steady decline of their concentrations from 2003 to 2008 was observed due to the reinforced emission guideline from waste incinerators. The average concentration of the PCDD/Fs and dl-PCBs ranged between 0.118 pg-TEQ/$m^3$ (rural/remote site D) and 0.532 pg-TEQ/$m^3$ (industrial area $A_2$). These level were generally consistent with previous studies in Gyeonggi-do, while higher than other places. Most of PCDD/Fs congener were partitioned into particle phase, whereas dl-PCBs were partitioned into gas phase. The logarithm of gas-particle partition coefficient $K_P$ of dl-PCBs and PCDD/Fs were well correlated with sub-cooled liquid vapor pressure $P_L$. The slope $m_T$ of log $K_P$ versus log $P_L$ for PCDD/Fs (-1.22) and dl-PCBs (-1.02) in industrial area ($A_2$) were high compared to other residential/commercial area. It suggests that this area was likely influenced by the direct emission source of PCDD/Fs and dl-PCBs. To simulate the partition of PCDD/Fs and dl-PCBs between gas and particle phase, Junge-Pankow model ($P_L$-base) and $K_{oa}$ model were applied. It was found that J-P model was more suitable than the $K_{oa}$ model in this study.