• Korean Journal of Fisheries and Aquatic Sciences
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• v.18 no.2
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• pp.131-138
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• 1985

The preservative effect of modified-atmosphere storage on the shelf-life of packed semi-salted and dried mackerel, Scomber japonicus, was examined. The semi-salted and dried mackerel fillets were packed in laminated plastic film bags (polyester/nylon/casted polypropylene: $12{\mu}m/15{\mu}m/60{\mu}m,\;15{\times}16cm$) filled with air (control, C), nitrogen gas (N), deoxygenized air (O) prepared by using free-oxygen absorber enclosed in the bag, in vacuum(V), and stored at $5^{\circ}C$. The quality of packed sample during the storage were examined in terms of viable cell counts of bacteria, thiobarbituric acid(TBA) value, perozide value(POV), volatile basic nitrogen(VBN), trimethylamine(TMA), adenosine triphosphate(ATP) and its related compounds and sensory evaluation. The results obtained are as follows: The pH of all the samples was in the range of $6.1{\pm}0.2$, and the contents of VBN and amino nitrogen of them increased during storage. In color values, L value(lightness) decreased while a and b values (red and yellow) revealed a tendency to increase during storage. The viable cell counts of the control sample(C) increased to $3.0{\times}10^6/g$ after 15 days storage but those of the other samples(V, N and O)were in the range of $2{\sim}6{\times}10^5/g$ after 20 days storage. The content of TMA increased during storage, but the histamine content showed a little change during storage and its content of all samples were less than 16 mg/100g. The inosinic acid(IMP) was rapidly degraded while inosine and hypoxanthine increased during storage. The TBA value of the control(C) reached a peak in 9 days and then decreased gradually while that of the sample(O) showed a little change during storage. The changes in POV of all the samples during storage showed a similar tendency to the TBA value. Fatty acid composition of raw mackerel consists of $35.6\%$ of saturated acid, $30.3\%$ of monoenoic acid and $34.2\%$ of polyenoic acid. The major fatty acid of the sample products were oleic acid($C_{18:1}$), palmitic acid($C_{16:0}$), docosahexaenoic acid($C_{22:6}$). The contents of polyenoic acid such as $C_{22:6},\;C_{20:5}$ decreased during storage while the other fatty acids showed a little change. From the results of sensory evaluation, the shelf-life of the control sample(C) was about 7 days and that of sample(V), (N) and (O) was about 15 days. It was concluded that deoxygenized atmosphere(free-oxygen absorber enclosed in the bag) was a good condition for preserving the quality of semi-salted and dried mackerel.

• Economic and Environmental Geology
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• v.35 no.5
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• pp.379-393
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• 2002

Within the Boseong-Jangheung area of Korea, five hydrothermal gold (-silver) quartz vein deposits occur. They have the characteristic features as follows: the relatively gold-rich nature of e1ectrurns; the absence of Ag-Sb( -As) sulfosalt mineral; the massive and simple mineralogy of veins. They suggest that gold mineralization in this area is correlated with late Jurassic to Early Cretaceous, mesothermal-type gold deposits in Korea. Fluid inclusion data show that fluid inclusions in stage I quartz of the mine area homogenize over a wide temperature range of 200$^{\circ}$ to 460$^{\circ}$C with salinities of 0.0 to 13.8 equiv. wt. % NaCI. The homogenization temperature of fluid inclusions in stage II calcite of the mine area ranges from 150$^{\circ}$ to 254$^{\circ}$C with salinities of 1.2 to 7.9 equiv. wt. % NaCI. This indicates a cooling of the hydrothermal fluid with time towards the waning of hydrothermal activity. Evidence of fluid boiling including CO2 effervescence indicates that pressures during entrapment of auriferous fluids in this area range up to 770 bars. Calculated sulfur isotope composition of auriferous fluids in this mine area (${\delta}^34S$_{{\Sigma}S}$$\textperthousand$) indicates an igneous source of sulfur in auriferous hydrothermal fluids. Within the Sobaegsan Massif, two representative mesothermal-type gold mine areas (Youngdong and Boseong-Jangheung areas) occur. The ${\delta}^34S values of sulfide minerals from Youngdong area range from -6.6 to 2.3$\textperthousand$ (average=-1.4$\textperthousand$, N=66), and those from BoseongJangheung area range from -0.7 to 3.6$\textperthousand$ (average=1.6$\textperthousand$, N=39). These i)34S values of both areas are comparatively lower than those of most Korean metallic ore deposits (3 to 7TEX>$\textperthousand$). And, within the Sobaegsan Massif, the ${\delta}^34S values of Youngdong area are lower than those of Boseong-Jangheung area. It is inferred that the difference of ${\delta}^34S values within the Sobaegsan Massif can be caused by either of the following mechanisms: (1) the presence of at least two distinct reservoirs (both igneous, with ${\delta}^34S values of < -6 $\textperthousand$ and 2$\pm$2 %0) for Jurassic mesothermal-type gold deposits in both areas; (2) different degrees of the mixing (assimilation) of 32S-enriched sulfur (possibly sulfur in Precambrian pelitic basement rocks) during the generation and/or subsequent ascent of magma; and/or (3) different degrees of the oxidation of an H2S-rich, magmatically derived sulfur source ${\delta}^34S = 2$\pm$2$\textperthousand$) during the ascent to mineralization sites. According to the observed differences in ore mineralogy (especially, iron-bearing ore minerals) and fluid inclusions of quartz from the mesothermal-type deposits in both areas, we conclude that pyrrhotite-rich, mesothermal-type deposits in the Youngdong area formed from higher temperatures and more reducing fluids than did pyrite(-arsenopyrite)-rich mesothermal-type deposits in the Boseong-Jangheung area. Therefore, we prefer the third mechanism than others because the ${\delta}^34S values of the Precambrian gneisses and Paleozoic sedimentary rocks occurring in both areas were not known to the present. In future, in order to elucidate the provenance of ore sulfur more systematically, we need to determine ${\delta}^34S values of the Precambrian metamorphic rocks and Paleozoic sedimentary rocks consisting the basement of the Korean Peninsula including the Sobaegsan Massif.

• Journal of Korean Society of Forest Science
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• v.80 no.1
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• pp.54-71
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• 1991

To classify and analyze the forest communities and their structures, the vegetation in Mt. Joghe was investigated from July, 1980 to August, 1989. The results obtained are as follow ; 1. A total of 750 kinds of vascular plant(49 orders, 122 families, 434 genera, 627 species, 1 subspecies, 111 varieties and 11 forma)were observed in Mt. Ioghe. The newly observed plant species were Dioscorea quingueloba, Spiranthes sinensis, Cephalanthera falcata, Angelica gigas, Clematis patents, Paeonia obovata, Hibiscus mulabilis, Ainsliaea acerifolia, Dictamnus dasycarpus, Cynachum ascyrifolia, Vaccinium koreanum, Erythrortium japonicum, Indigofera kirilowii (17species), Broussonetia kazinoki var, humillis, Euonymus, fortunei var. radicans, Juniperus communis var, nippnnica, Callicarpa japonica var. radicans, Joniperus communis var. rzipponica, Callicarpa japonica var. taquetii (4 varieties) and L indera obtusiloba for. billosum (1 forma). 2. The life spectrum of flora in Mt. Joghe was classified into $CH-D_1-R_5-e$ type. Distribution area was identical to Southern type by Nakai, Lee, and Yim. A few subtropical species were also observed. 3. Simpson's species diversity index(Ds) was 0.9 and Shannon-Weiner's diversity index (H') was 1.004. These indice suggest that the vegetation in Mt. Joghe is of complicated forest communities. 4. Pte-Q was 1.81 which was higher than the nationwide mean of 1.68. Urbanization Index (UI) was 28.75 for naturalized plant species, and 17.49 for exotic woody plant species, which were similar to those of Mt. Baekun and Mt. Naejang. 5. The forest vegetation of Mt. Joghe was grouped in 3 vegetation types : 7 natural plant Communities dominated by Quercus serrat, Quercus acutissima, Quercus variabilis, Carpinus laxiflora, Pinus derasiflora and Platycarya strobilacea, 8 substitutional plant communities Styrax japonica, Stewartia koreana, Lindera erytlrrocarpa, Zelkova serrata, Rhtrs chinensis, Controversa, and Frzrxirtus manrlshurica, and 7 plantation Communities composed of Pinus koraiensis, Pinus rigida, Magnolia nbnvata, Chamecyparis obkrsa, Larie ieptolepis, Castanea crenata and Cryptomeria japonica. 6. Actual vegetation maps and profile diagrams were made by phytosocialogical classification. 7. As the important and unique species in Mt. Joghe, Lindera sericea, Penicaria tilitorme, Hex macropoda, Hex macropoda for. pseudo-macropoda, Steroartia koreana, Adenopkora palustris and Corylop.,is coreana, which were also seported by Lee(1977), Kim and Yark(1989), were identified and Vaccinium coreanum, Cremastra appendiculinium, Juniperus comminis van. nipponica, Cephalanthera falcata, Broussortetia kazinoki var. humilis, paeonia obovata, Deutzia prunifolia, Dictamnus dasyarpus, Angelica gigics and Bupleurum falcatum were odditionally observed.

• Tuberculosis and Respiratory Diseases
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• v.46 no.3
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• pp.350-362
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• 1999

Background: Acute Respiratory failure which is developed after extubation in the weaning process from mechanical ventilation is an important cause of weaning failure. Once it was developed, endotracheal reintubation has been done for respiratory support. Noninvasive Positive Pressure Ventilation (NIPPV) has been used in the management of acute or chronic respiratory failure, as an alternative to endotracheal intubation, using via nasal or facial mask. In this study, we evaluated the usefulness of NIPPV as an alternative method of reintubation in patients who developed acute respiratory failure after extubation. Method: We retrospectively analyzed thirty one patients(eighteen males and thirteen females, mean ages $63\pm13.2$ years) who were developed acute respiratory failure within forty eight hours after extubation, or were extubated unintentionally at medical intensive care unit(MICU) of Asan Medical Center. NIPPV was applied to the patients. Ventilatory mode of NIPPV, level of ventilatory support and inspiratory oxygen concentration were adjusted according to the patient condition and results of blood gas analysis by the attending doctors at MICU. NIPPV was completely weaned when the patients maintained stable clinical condition under 8 $cmH_2O$ of pressure support level. Weaning success was defined as maintenance of stable spontaneous breathing more than forty eight hours after discontinuation of NIPPV. Respiratory rate, heart rate, arterial blood gas analysis, level of pressure support, and level of PEEP were monitored just before extubation, at thirty minutes, six hours, twenty four hours after initiation of NIPPV. They were also measured at just before weaning from NIPPV in success group, and just before reintubation in failure group. Results: NIPPV was successfully applied to thirty-one patients of thirty-two trials and one patient could not tolerated NIPPV longer than thirty minutes. Endotracheal reintubation was successfully obviated in fourteen patients (45%) among them. There was no difference in age, sex, APACHE III score on admission at MICU, duration of intubation, interval from extubation to initiation of NIPPV, baseline heart rate, respiratory rate, arterial blood gas, and $PaO_2/FiO_2$ between the success and the failure group. Heart rate and respiration rate were significantly decreased with increase $SaO_2$ after thirty minutes of NIPPV in both groups(p<0.05). However, in the patients of failure group, heart rate and respiratory rate were increased again with decrease in $SaO_2$ leading to endotracheal reintubation. The success rate of NIPPV treatment was significantly higher in the patients with COPD compared to other diseases(62% vs 39%) (p=0.007). The causes of failure were deterioration of arterial blood gas without aggravation of underlying disease(n=9), aggravation of undelying disease(n=5), mask intolerance(n=2), and retained airway secretion(n=l). Conclusion: NIPPV would be a useful therapeutic alternative which can avoid reintubation in patient who developed acute respiratory failure after extubation.

• Tuberculosis and Respiratory Diseases
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• v.44 no.6
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• pp.1343-1352
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• 1997

Background : Heat-treated cells are known to be protected from lysis by TNF, which is considered to play a central role in the pathogenesis of sepsis-induced acute lung injury. The objective of the study was to investigate the effect of heat shock response by heat-pretreatment on the acute lung injury of the rats induced by intratracheally administered TNF-$\alpha$, Methods : We intratracheally instilled either saline or TNF (R&D, 500ng) with and without heat pretreatment in Sprague-Dawley rats weighing 250~350 g. The heated rats were raised their rectal temperature to $41^{\circ}C$ and was maintained thereafter for 13 minutes at 18 h before intratracheal administration of saline or TNF. After 5 h of intratracheal treatment, lung leak, lung myeloperoxidase activity (MPO) and heat shock proteins were measured in rats. Lung leak index was defined as counts per minute of $I^{25}$ in the right lung divided by counts per minutes of $I^{25}$ in 1.0 ml of blood. All data are expressed as means ${\pm}$SE. Results : There is no difference in acute lung leak index ($0.099{\pm}0.024$ vs $0.123{\pm}0.005$) among the rats given saline intratracheally with and without heat pretreatment, but MPO activity showed a decreased tendency in heat-pretreated rats ($4.58{\pm}0.79\;U/g$) compared with heat-unpretreated rats ($7.32{\pm}0.97\;U/g$) (P=0.064). Rats administered TNF intratracheally with heat-pretreatment had decreased lung leak index ($0.137{\pm}0.012$) and lung MPO activity ($5.51{\pm}1.04\;U/g$) compared with those of heat-unpretreated and TNF-administered rats ($0.186{\pm}0.016$, $14.34{\pm}1.22\;U/g$) (P<0.05 in each). There were no significant difference of lung leak index and MPO activity between TNF-treated rats with heat-pretreatment and saline-treated rats with and without heat-pretreatment. Conclusion : The heat shock response attenuated neutrophil recruitment and acute lung leak induced by intratracheal instillation of TNF-in rats.

• Journal of Animal Science and Technology
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• v.46 no.2
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• pp.283-294
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• 2004

Air quality in the livestock waste compost pilot plant at the Colligate Livestock Station was assessed to quantity the emissions of aerial contaminants and evaluate the degree of correlation between them for different operation strategies; with the ventilation types and agitation of compost pile, in this study. The parameters analyzed to reflect the level of air quality in the livestock waste compost pilot plant were the gaseous contaminants; ammonia, hydrogen sulfide, and odor concentration, the particulate contaminants; inhalable dust and respirable dust, and the biological contaminants; total airborne bacteria and fungi. The mean concentrations of ammonia, hydrogen sulfide, and odor concentration in the compost pilot plant without agitation were 2.45ppm, 19.96ppb, and 15.8 when it was naturally ventilated, and 7.61ppm, 31.36ppb, and 30.2 when mechanically ventilated. Those with agitation were 5.50ppm, 14.69ppb, and 46.4 when naturally ventilated, and 30.12ppm, 39.91ppb, and 205.5 when mechanically ventilated. The mean concentrations of inhalable and respirable dust in the compost pilot plant without agitation were 368.6${\mu}g$/$m^3$ and 96.0${\mu}g$/$m^3$ with natural ventilation, and 283.9${\mu}g$/$m^3$ and 119.5${\mu}g$/$m^3$ with mechanical ventilation. They were also observed with agitation to 208.7${\mu}g$/$m^3$ and 139.8${\mu}g$/$m^3$ with natural ventilation, and 209.2${\mu}g$/$m^3$ and 131.7${\mu}g$/$m^3$ with mechanical ventilation. Averaged concentrations of total airborne bacteria and fungi in the compost pilot plant without agitation were observed to 28,673cfu/$m^3$ and 22,507cfu/$m^3$ with natural ventilation, and 7,462cfu/$m^3$ and 3,228cfu/$m^3$ with mechanical ventilation. They were also observed with agitation to 19,592cfu/$m^3$ and 26,376cfu/$m^3$ with the natural ventilation, and 18,645cfu/$m^3$ and 24,581cfu/$m^3$ with the mechanical ventilation. It showed that the emission rates of gaseous pollutants, such as ammonia, hydrogen sulfide, and odor concentration, in the compost pilot plant operated with the mechanical ventilation and with the agitation of compost pile were higher than those with the natural ventilation and without the agitation. While the concentrations of inhalable dust and total airborne bacteria in the compost pilot plant with the natural ventilation and with the agitation, the concentrations of respirable dust and total airborne fungi in the compost pilot plant with the mechanical ventilation and agitation were higher than those with the natural ventilation and without the agitation of compost pile. It was statistically proved that indoor temperature and relative humidity affected the release of particulates and biological pollutants, and ammonia and hydrogen sulfide were believed primary malodorous compounds emitted from the compost pilot plant.

• Journal of Food Hygiene and Safety
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• v.34 no.3
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• pp.227-234
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• 2019

An analytical method was developed for the determination of oxytetracycline in agricultural products using the QuEChERS (Quick, Easy, Cheap, Effective, Rugged and Safe) method by liquid chromatography-tandem mass spectrometry (LC-MS/MS). After the samples were extracted with methanol, the extracts were adjusted to pH 4 by formic acid and sodium chloride was added to remove water. Dispersive solid phase extraction (d-SPE) cleanup was carried out using $MgSO_4$ (anhydrous magnesium sulfate), PSA (primary secondary amine), $C_{18}$ (octadecyl) and GCB (graphitized carbon black). The analytes were quantified and confirmed with LC-MS/MS using ESI (electrospray ionization) in positive ion MRM (multiple reaction monitoring) mode. The matrix-matched calibration curves were constructed using six levels ($0.001{\sim}0.25{\mu}g/mL$) and coefficient of determination ($r^2$) was above 0.99. Recovery results at three concentrations (LOQ, $10{\times}LOQ$, and $50{\times}LOQ$, n=5) were from 80.0 to 108.2% with relative standard deviations (RSDs) less than of 11.4%. For inter-laboratory validation, the average recovery was in the range of 83.5~103.2% and the coefficient of variation (CV) was below 14.1%. All results satisfied the criteria ranges requested in the Codex guidelines (CAC/GL 40-1993, 2003) and the Food Safety Evaluation Department guidelines (2016). The proposed analytical method was accurate, effective and sensitive for oxytetracycline determination in agricultural commodities. This study could be useful for safety management of oxytetracycline residues in agricultural products.

• The Korean Journal of Pharmacology
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• v.16 no.2 s.27
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• pp.55-70
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• 1980

The pharmacological and microbiological studies of Cefoperazone (T-1551, Toyama Chemical Co., Japan) were conducted in vitro and in vivo. The studies included stability and physicochemical characteristics, antimicrobial activity, animal and human pharmacokinetics, animal pharmacodynamics and safety evaluation of Cefoperazone sodium for injection. 1) Stability and physicochemical characteristics. Sodium salt of cefoperazone for injection had a general appearance of white crystalline powder which contained 0.5% water, and of which melting point was $187.2^{\circ}C$. The pH's of 10% and 25% aqueous solutions were 5.03 ana 5.16 at $25^{\circ}C$. The preparations of cefoperazone did not contain any pyrogenic substances and did not liberate histamine in cats. The drug was highly compatible with common infusion solutions including 5% Dextrose solution and no significant potency decrease was observed in 5 hours after mixing. Powdered cefoperazone sodium contained in hermetically sealed and ligt-shielded container was highly stable at $4^circ}C{\sim}37^{\circ}C$ for 12 weeks. When stored at $4^{\circ}C$ the potency was retained almost completely for up to one year. 2) Antimicrobial activity against clinical isolates. Among the 230 clinical isolates included, Salmonella typhi was the most susceptible to cefoperazone, with 100% inhibition at MIC of ${\leq}0.5{\mu}g/ml$. Cefoperazone was also highly active against Streptococcus pyogenes(group A), Kletsiella pneumoniae, Staphylococcus aureus and Shigella flexneri, with 100% inhibition at $16{\mu}g/ml$ or less. More than 80% of Escherichia coli, Enterobacter aerogenes and Salmonella paratyphi was inhibited at ${\leq}16{\mu}/ml$, while Enterobacter cloaceae, Serratia marcescens and Pseudomonas aerogenosa were somewhat less sensitive to cefoperagone, with inhibitions of 60%, 55% and 35% respectively at the same MIC. 3) Animal pharmacokinetics Serum concentration, organ distritution and excretion of cefoperazone in rats were observed after single intramuscular injections at doses of 20 mg/kg and 50 mg/kg. The extent of protein binding to human plasma protein was also measured in vitro br equilibrium dialysis method. The mean Peak serum concentrations of $7.4{\mu}g/ml$ and $16.4{\mu}/ml$ were obtained at 30 min. after administration of cefoperazone at doses of 20 mg/kg and 50 mg/kg respectively. The tissue concentrations of cefoperazone measured at 30 and 60 min. were highest in kidney. And the concentrations of the drug in kidney, liver and small intestine were much higher than in blood. Urinary and fecal excretion over 24 hours after injetcion ranged form 12.5% to 15.0% in urine and from 19.6% to 25.0% in feces, indicating that the gastrointestinal system is more important than renal system for the excretion of cefoperazone. The extent of binding to human plasma protein measured by equilibrium dialysis was $76.3%{\sim}76.9%$, which was somewhat lower than the others utilizing centrifugal ultrafiltration method. 4) Animal pharmacodynamics Central nervous system : Effects of cefoperazone on the spontaneous movement and general behavioral patterns of rats, the pentobarbital sleeping time in mice and the body temperature in rabbits were observed. Single intraperitoneal injections at doses of $500{\sim}2,000mg/kg$ in rats did not affect the spontaneous movement ana the general behavioral patterns of the animal. Doses of $125{\sim}500mg/kg$ of cefoperazone injected intraperitonealy in mice neither increased nor decreased the pentobarbital-induced sleeping time. In rabbits the normal body temperature was maintained following the single intravenous injections of $125{\sim}2,000mg/kg$ dose. Respiratory and circulatory system: Respiration rate, blood pressure, heart rate and ECG of anesthetized rabbits were monitored for 3 hours following single intravenous injections of cefoperazone at doses of $125{\sim}2,000mg/kg$. The respiration rate decreased by $3{\sim}l7%$ at all the doses of cefoperazone administered. Blood pressure did not show any changes but slight decrease from 130/113 to 125/107 by the highest dose(2,000 mg/kg) injected in this experiment. The dosages of 1,000 and 2,000 mg/kg seemed to slightly decrease the heart rate, but it was not significantly different from the normal control. All the doses of cefoperazone injected were not associated with any abnormal changes in ECG findings throughout the monitering period. Autonomic nervous system and smooth muscle: Effects of cefoperazone on the automatic movement of rabbit isolated small intestine, large intestine, stomach and uterus were observed in vitro. The autonomic movement and tonus of intestinal smooth muscle increased at dose of $40{\mu}g/ml$ in small intestine and at 0.4 mg/ml in large intestine. However, in stomach and uterine smooth muscle the autonomic movement was slightly increased by the much higher doses of 5-10 mg/ml. Blood: In vitro osmotic fragility of rabbit RBC suspension was not affected by cefoperazone of $1{\sim}10mg/ml$. Doses of 7.5 and 10 mg/ml were associated with 11.8% and 15.3% prolongation of whole blood coagulation time. Liver and kidney function: When measured at 3 hours after single intravenous injections of cefoperaonze in rabbits, the values of serum GOT, GPT, Bilirubin, TTT, BUN and creatine were not significantly different from the normal control. 5) Safety evaluation Acute toxicity: The acute toxicity of cefoperazone was studied following intraperitoneal and intravenous injections to mice(A strain, 4 week old) and rats(Sprague-Dawler, 6 week old). The LD_(50)'s of intraperitonealy injected cefoperazone were 9.7g/kg in male mice, 9.6g/kg in female mice and over 15g/kg in both male and female rats. And when administered intravenously in rats, LD_(50)'s were 5.1g/kg in male and 5.0g/kg in female. Administrations of the high doses of the drug were associated with slight inhibition of spontaneous movement and convulsion. Atdominal transudate and intestinal hyperemia were observed in animals administered intraperitonealy. In rats receiving high doses of the drug intravenously rhinorrhea and pulmonary congestion and edema were also observed. Renal proximal tubular epithelial degeneration was found in animals dosing in high concentrations of cefoperazone. Subacute toxicity: Rats(Sprague-Dawley, 6 week old) dosing 0.5, 1.0 and 2.0 g/kg/day of cefoperazone intraperitonealy were observed for one month and sacrificed at 24 hours after the last dose. In animals with a high dose, slight inhibition of spontaneous movement was observed during the experimental period. Soft stool or diarrhea appeared at first or second week of the administration in rats receiving 2.0g/kg. Daily food consumption and weekly weight gain were similar to control during the administration. Urinalysis, blood chemistry and hematology after one month administration were not different from control either. Cecal enlargement, which is an expected effect of broad spectrum antibiotic altering the normal intestinal microbial flora, was observed. Intestinal or peritoneal congestion and peritonitis were found. These findings seemed to be attributed to the local irritation following prolonged intraperitoneal injections of hypertonic and acidic cefoperazone solution. Among the histopathologic findings renal proximal tubular epithelial degeneration was characteristic in rats receiving 1 and 2g/kg/day, which were 10 and 20 times higher than the maximal clinical dose (100 mg/kg) of the drug. 6) Human pharmacokinetics Serum concentrations and urinary excretion were determined following a single intravenous injection of 1g cefoperazone in eight healthy, male volunteers. Mean serum concentrations of 89.3, 61.3, 26.6, 12.3, 2.3, and $1.8{\mu}g/ml$ occured at 1,2,4,6,8 and 12 hours after injection respectively, and the biological half-life was 108 minutes. Urinary excretion over 24 hours after injection was up to 43.5% of administered dose.

• Tuberculosis and Respiratory Diseases
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• v.55 no.1
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• pp.69-87
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• 2003

Background : LB20304(gemifloxacin) is a new fluoroquinolone antibacterial agent with excellent activity against both Gram-negative and Gram-positive organisms. In vitro studies using clinical isolates have shown gemifloxacin to be highly active against penicillin-resistant strains of S. pneumoniae and in contrast to other reference quinolones, gemifloxacin retained good activity against clinical isolates of S. pneumoniae that were resistant to other members of the quinolone class. Therefore, gemifloxacin is thought to be effective in treating acute bacterial exacerbation of chronic bronchitis(AECB). The objective of this study was to evaluate the efficacy and safety of oral gemifloxacin at doses of 160mg or 320mg once daily for 7 days for the treatment of AECB in Korean adult population. Methods : This was a randomized, multicenter, double-blind, parallel group Phase II study to assess the clinical and antibacterial efficacy and safety of oral gemifloxacin for the treatment of AECB. Treatment Group A (67 patients) took oral gemifloxacin 160mg once daily for seven days and treatment Group B (70 patients) took oral gemifloxacin 320mg once daily for seven days. Results : The demographic profiles of the two treatment groups were similar. The clinical response at follow-up was 84.2% in the gemifloxacin 160-mg group, and 88.7% in the gemifloxacin-320 mg group, showing no statistically significant difference between two treatment groups(p=0.49). The clinical response at the end of therapy was 96.5% in the 160-mg group, and 96.4% in the 320-mg group. The bacteriological response at the end of therapy and follow-up were 81.8% and 78.9%, respectively, in the 160-mg group, and 86.4% and 84.2%, respectively, in the 320-mg group, showing no statistically significant difference between two treatment groups(p=0.68 and 0.68, respectively). S. pneumoniae(12 isolates) and H. influenzae(10 isolates) were the most prevalent pathogens. The MICs were lower for gemifloxacin than other quinolones against these key pathogens, and for S. pneumoniae, the MICs for gemifloxacin were considerably lower(${\leq}0.03$ ug/mL) than those for other quinolones, beta-lactams and macrolides. In the period on-therapy plus 30 days post-therapy, a total of 18 patients(26.9%) in the gemifloxacin 160mg group and 22 patients(31.4%) in the 320mg group reported at least one adverse event(AE). The most frequently reported AE was abdominal pain(3/67 patients, 4.5%) in the gemifloxacin 160mg group and increased level of hepatic enzyme(5/70 patients, 7.1%) in the 320mg group. The overall AE profiles for the two treatment groups were similar. Two out of 67 patients(3.0%) in the gemifloxacin 160mg group and 1/70 patients(1.4%) in the 320mg group reported at least one serious AE, however, none of which was considered by the investigator to be of suspected or probable relationship to study medication. Conclusion : The results of this study showed that gemifloxacin at doses of 160mg or 320mg once daily for 7 days in the treatment of acute exacerbations of chronic bronchitis(AECB) in adult Koreans was a very effective and safe treatment both clinically and bacteriologically.

• Tuberculosis and Respiratory Diseases
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• v.50 no.2
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• pp.182-195
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• 2001

Background : Idiopathic pulmonary fibrosis(IPF) is a devastating illness for which there is little effective treatment. The key cytokines currently implicated in the fibrotic process are the transforming growth factor-${\beta}_1$(TGF-${\beta}_1$), tumor necrosis factor-$\alpha$(TNF-$\alpha$), endothelin-1(ET-1) and interferon-$\gamma$(IFN-$\gamma$). The rat model for paraquat-induced pulmonary fibrosis was chosen to investigate the role of ET-1 in this disease. Both ET-1 and TGF-${\beta}_1$ expression in lung lesions were examined using immunohistochemical staining. After $Bosentan^{(R)}$ administration, an orally active ET-$l_A$ and ET-$1_B$ receptor antagonist, the degree of pulmonary fibrosis and ET-1 and TGF-${\beta}_1$ expression were analyzed. Method : Sprague-Dawley rats were divided into three groups, the control group, the fibrosis group, and the fibrosis-$Bosentan^{(R)}$-treated group. The animals were sacrificed periodically at 1, 3, 5, 7, 10, 14 days after administering saline or paraquat. The effects between groups were compared with the results of light microscopy and immunohistochemical staining for ET-1 and TGF-${\beta}_1$. The degree of fibrosis was evaluated by H&E and Masson's trichrome staining, which were graded by a computerized image analyzer. The degree of immunohistochemical staining was categorized by a semi-quantitative analysis method. Results : The lung collagen content had increased in the paraquat instillated animals by day 3, and continued to increase up to day 14. A daily treatment by gavage with $Bosentan^{(R)}$ (100mg/kg) did not prevent the increase in collagen deposition on the lung that was induced by paraquat instillation. There were increased immunohistochemical stains of ET-1 on the exudate, macrophages, vascular endothelial cells and pneumocytes in the paraquat instillated group. Furthermore, TGF-${\beta}_1$ expression was higher on the exudate, macrophages, some inflammatory cells, pneumocytes( type I, and II), vascular endothelium and the respiratory epithelial cells around the fibrotic area. After Bosentan treatment, there were no definite changes in ET-1 and TGF-${\beta}_1$ expression. Conclusion : Fibrosis of the Paraquat instillated group was more advanced when compared with the control group. In addition, there was increased ET-1 and TGF-${\beta}_1$ expression around the fibrotic area. ET-1 is associated with lung fibrosis but there was little effect of the ET-1 receptor blocker($Bosentan^{(R)}$) on antifibrosis.Background : Idiopathic pulmonary fibrosis(IPF) is a devastating illness for which there is little effective treatment. The key cytokines currently implicated in the fibrotic process are the transforming growth factor-${\beta}_1$(TGF-${\beta}_1$), tumor necrosis factor-$\alpha$(TNF-$\alpha$), endothelin-1(ET-1) and interferon-$\gamma$(IFN-$\gamma$). The rat model for paraquat-induced pulmonary fibrosis was chosen to investigate the role of ET-1 in this disease. Both ET-1 and TGF-${\beta}_1$ expression in lung lesions were examined using immunohistochemical staining. After $Bosentan^{(R)}$ administration, an orally active ET-$1_A$ and ET-$1_B$ receptor antagonist, the degree of pulmonary fibrosis and ET-1 and TGF-${\beta}_1$ expression were analyzed. Method : Sprague-Dawley rats were divided into three groups, the control group, the fibrosis group, and the fibrosis-$Bosentan^{(R)}$-treated group. The animals were sacrificed periodically at 1, 3, 5, 7, 10, 14 days after administering saline or paraquat. The effects between groups were compared with the results of light microscopy and immunohistochemical staining for ET-1 and TGF-${\beta}_1$. The degree of fibrosis was evaluated by H&E and Masson's trichrome staining, which were graded by a computerized image analyzer. The degree of immunohistochemical staining was categorized by a semi-quantitative analysis method. Results : The lung collagen content had increased in the paraquat instillated animals by day 3, and continued to increase up to day 14. A daily treatment by gavage with $Bosentan^{(R)}$ (100mg/kg) did not prevent the increase in collagen deposition on the lung that was induced by paraquat instillation. There were increased immunohistochemical stains of ET-1 on the exudate, macrophages, vascular endothelial cells and pneumocytes in the paraquat instillated group. Furthermore, TGF-${\beta}_1$ expression was higher on the exudate, macrophages, some inflammatory cells, pneumocytes( type I, and II), vascular endothelium and the respiratory epithelial cells around the fibrotic area. After Bosentan treatment, there were no definite changes in ET-1 and TGF-${\beta}_1$ expression. Conclusion : Fibrosis of the Paraquat instillated group was more advanced when compared with the control group. In addition, there was increased ET-1 and TGF-${\beta}_1$ expression around the fibrotic area. ET-1 is associated with lung fibrosis but there was little effect of the ET-1 receptor blocker($Bosentan^{(R)}$) on antifibrosis.