• Journal of Pharmaceutical Investigation
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• v.33 no.2
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• pp.135-140
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• 2003

Fluconazole is an orally active bis-triazole antifungal agent, which is used in the treatment of superficial and systemic candidiasis and in the treatment of cryptococcal infections in patients with the acquired immuno deficiency syndrome (AIDS). The purpose of the present study was to evaluate the bioequivalence of two fluconazole capsules, Diflucan (Pfizer Pharmaceuticals Korea Inc.) and Flucona (Korean Drug Pharmaceuticals Co., Ltd.), according to the guidelines of Korea Food and Drug Administration (KFDA). The fluconazole release from the two fluconazole capsules in vitro was tested using KP VII Apparatus II method at 0.1 M hydrochloride dissolution media. Twenty normal male volunteers, $23.60{\pm}1.88$ years in age and $63.57{\pm}6.17\;kg$ in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After three capsules containing 50 mg as fluconazole was orally administered, blood was taken at predetermined time intervals and the concentrations of fluconazole in serum were determined using HPLC method with UV detector. The dissolution profiles of two fluconazole capsules were very similar at 0.1 M hydrochloride dissolution media. Besides, the pharmacokinetic parameters such as $AUC_t,\;C_{max}\;and\;T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_t$ and $C_{max}$ and untransformed $T_{max}$. The results showed that the differences in $AUC_t,\;C_{max}\;and\;T_{max}$ between two capsules based on the Diflucan were 4.96%, 5.65% and -13.76%, respectively. There were no sequence effects between two capsules in these parameter. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log(0.8) to log(1.25) $(e.g.,\;log(1.01){\sim}log(1.08)\;and\;log(1.00){\sim}log(1.12)\;for\;AUC_t\;and\;C_{max},\;respectively)$, indicating that Flucona capsule is bioequivalent to Diflucan capsule.

• Korean Journal of Weed Science
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• v.12 no.1
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• pp.39-45
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• 1992

This experiment was conducted to evaluate the effect of gibberellin biosynthesis retardants as used by rice lodging inhibitors on the gibberellin antagonism, auxin interation, ethylene evolution and growth of second crops. Results obtained can be summarized as follows. Inabenfide, paclobutrazol and uniconazole markedly inhibited the epicotyl elongation of mung bean. Inhibiting effect of epicotyl by these chemicals was markedly stimulated by gibberellic acid, thus showing clear antagonism between these chemicals and gibberellic acid. Significantly large number of roots were formed in the mung bean cuttings which were rooted in the paclobutrazol and uniconazol of 1 ppm. The higher the concentration, the more the number of roots forms. It was guessed that these effect was closely related with auxin. Ethylene evolution was a little stimulated in the leaf of rice under the treatment of inabenfide, paclobutrazol and uniconazole at earlier stage(5 DAT), however it was suppressed at later stage(10, 30 DAT) at higher concentration. The effect of gibberllin biosynthesis inhibitors to second crops retarded tomato plants without influencing the height of barley. The treatment of paclobutrazol and uniconazol which is triazole-type more severely inhibited than that of inabenfide which is isonicotinanilide-type. The more the concentration, the less the height of tomato plants.

• Journal of Life Science
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• v.29 no.7
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• pp.755-761
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• 2019

Kojic acid (KA) is produced by Aspergillus oryzae-sort of like mushrooms, which is commonly called as koji in Japan. KA is used as a chelation agent and a preservative preventing oxidative browning of fruits. KA also shows antibacterial and antifungal properties. Because KA stops the production of melanin by inhibiting tyrosinase in the biosynthetic pathway from tyrosine to melanin in skin, it has been applied as a skin lightening ingredient in cosmetics. Since some animal studies have shown that high amounts of KA had side effects such as in liver, kidney, reproductive, cardiovascular, gastrointestinal, respiratory, brain, and nervous system, more efficient KA derivatives are needed to be developed in order to safely apply as a skin lightening ingredient. A series of KA derivatives via conjugated with triazole by click reaction were synthesized and their in vitro tyrosinase inhibitory activities were evaluated. Most of all KA derivatives have shown in moderate tyrosinase inhibitory activities. In case of KA-hybrid compound, 1~3 have shown tyrosinase inhibitory activities about 50~10,000 times more effective tyrosinase inhibitor compared to KA itself. Specifically, the $IC_{50}$ value of KA-hybrid compound, 2 was $0.0044{\pm}0.74{\mu}M$ against tyrosinase. It is about 10,000 times more effective tyrosinase inhibitor compared to KA itself ($IC_{50}=45.2{\pm}4.6{\mu}M$).

• Korean Journal of Environmental Agriculture
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• v.15 no.1
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• pp.25-36
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• 1996

This study was carried out to isolate some bacterial strains which had potentiality of good degrader of fungicides from herbicide free soil and to clarify degradation of a fungicide mycrobutanyl[2-p-chlorophenyl-2-(1H-1,2,4-triazole-1-ylmethyl)-hexanenitrile]. Ten strains of the gram-positive and the gram-negative bacteria were isolated and identified. Most of them vigorously proliferated at 55ppm of mycrobutanil, but the stains were not grown when more than 70ppm of this fungicide were treated Staphylococcus spp. I, Actinobacillus spp. III, and another I of the isolated bacteria degraded more than 35% of the treated mycrobutanil. These three strains could utilize mycrobutanil as nitrogen and carbon sources. Mycrobutanil was rapidly decomposed by these strains when applied once or three times. Tested bacteria gradually increased in growth when mycrobutanil was applied repeatedly. Degradation of mycrobutanil and growth of these bacteria were greater in pH 5.5, and they were high in the order of $28^{\circ}C$ > $18^{\circ}C$ > $38^{\circ}C$.

• The Korean Journal of Mycology
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• v.50 no.4
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• pp.281-289
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• 2022

Fusarium head blight is an important disease of small grains. It is mainly caused by members of the Fusarium graminearum species complex (FGSC). Barley and wheat growers spray fungicides, especially demethylation-inhibitor fungicides, to suppress the disease. The objective of this study was to examine the changes in the sensitivity of the FGSC population to the triazole fungicide, propiconazole. A total of 124 and 350 isolates of FGSC were obtained from barley and wheat in Jeolla Province during 2010-2016 and 2020-2021, respectively. The species identity and trichothecene chemotypes of the FGSC isolates were determined based on polymerase chain reaction assays targeting translation elongation factor 1-alpha and TRI12 genes, respectively. Sensitivity to propiconazole was determined based on the effective concentration that reduced 50% of the mycelial growth (EC₅₀) using the agar dilution method. Of all isolates, F. asiaticum with the nivalenol chemotype was the most common (83.9% in 2010-2016 and 96.0% in 2020-2021), followed by F. asiaticum with the 3-acetyl deoxynivalenol chemotype (12.1% in 2010-2016 and 2.9% in 2020-2021). The EC₅₀ values of the isolates collected in 2010-2016 and 2020-2021 ranged from 0.0180 to 11.0166 ㎍/mL and 1.3104 to 17.9587 ㎍/mL, respectively. The mean EC₅₀ value of the isolates increased from 3.8648 ㎍/mL in 2010-2016 to 5.9635 ㎍/mL in 2020-2021. The baseline resistance to propiconazole was determined to be 7 ㎍/mL, based on the EC₅₀ value of isolates collected in 2010-2016, and the ratio of resistant isolates increased from 9.7% in 2010-2016 to 28.6% in 2020-2021.