• Journal of Pharmaceutical Investigation
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• v.30 no.1
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• pp.51-54
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• 2000

A column-switching high performance liquid chromatographic method has been developed for the determination of a fluconazole in human plasma. Each plasma sample was centrifuged for 10 min at 5000 g. After an aliqout of the supernatant was taken to nylon microcentrifuge filter, these samples were centrifuged for 10 min at 5000 g. An aliqout of the supernatant was injected directly onto the HPLC column. Deionized water was run for 2 min at a flow rate of 1.0 ml/min to retain fluconazole in an extration column, while proteins and endogenous interferences were eluted to the waste. The analyte was then back-flushed onto an analytical column, $C_{18}$ reversed-phase column. The mobile phase for analytical column, 0.01 M sodium acetate (pH 5.0)-methanol (65:35, v/v), was run at a flow rate of 1.0 ml/min. The column effluent was monitored by ultraviolet detection at 261 nm. The retention time for fluconazole was 11.76 min in human plasma. The detection limit for fluconazole in human plasma was $0.2\;{\mu}g/ml$. No interference from endogenous substances was observed.

• YAKHAK HOEJI
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• v.45 no.4
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• pp.357-365
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• 2001

The purpose of this study is to investigate the influence of cyclodextrins (CDs) and different acids on the solubility of fluconazole, and o formulate its more concentrated parenteral aqueous solution. Solubility studies of fluconazole with 7-CD, 2-hydroxypropyl-$\beta$-CD (HPCD), sulfobutyl ether $\beta$-CD (SBCD) and dimethyl-$\beta$-CD(DMCD) were performed. The aqueous solubility of fluconazole was measured in different concentrations of different acids with or without addition of CDs. Solubility of fluconazole increased in the rank order of $\beta$-CD$^1$H-NMR studies confirmed the formation of an inclusion complex of fluconazole with HPCD. It was also shown by the NMR studies that the complex formed was a 1:1 complex. Among the different acids used, maleic acid and phosphoric acid increased solubility of fluconazole. The lower the pH of solution is, the more fluconazole dissolved, regardless of acids. Addition of HPCD (50 mM) to acid solutions increased the solubility about two times. New fluconazole injections at a dose of 10 mg/ml could be prepared in aqueous solutions containing 10% HPCD or 15% SBCD. These parenteral solutions did not form any precipitates at 4$^{\circ}C$ and was very stable at elevated temperatures. These results demonstrate that it is possible to develop a parenteral aqueous solution of fluconazole with a smaller injection volume using HPCD or SBCD.

• Journal of Gastric Cancer
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• v.9 no.1
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• pp.31-35
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• 2009

Most gastric candida infections have been reported in immune-insufficient patients with peptic ulcer, but there have been few reports on gastric candidiasis with malignant ulcer in the stomach. We experienced a case of candida infection with gastric carcinoma in a 72-year-old female with diabetic mellitus. The endoscopic view showed multiple whitish necrotic plaques with a huge ulcer in the body of the stomach. The pathologic findings showed that budding yeast and pseudohyphae had infiltrated through the ulcerated stomach wall and the stomach wall contained tubular adenocarcinoma. After treatment with Fluconazole medication for 14 days, the patient underwent total gastrectomy along with D2 lymph node dissection. For the final pathologic results, there was no evidence of any remnant candidiasis, and the patient was discharged without specific complications. Through our experience and with reviewing articles about gastric candidiasis, we recommend that the gastric candidiasis that is accompanied with gastric malignancy should be treated before administering definite treatments for the gastric cancer.

• Pediatric Infection and Vaccine
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• v.28 no.2
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• pp.124-131
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• 2021

Cryptococcus neoformans is a fungus that primarily causes opportunistic infections in immunocompromised hosts. It can also cause various infections in immunocompetent patients. Pulmonary cryptococcosis involving the lymph node is relatively rare in immunocompetent patients. In this report, a previously healthy 17-year-old girl presented with high-grade fever and persistent cough. Chest X-ray and computed tomography (CT) scan revealed an anterior mediastinal conglomerate mass that expanded to the right supraclavicular area. Ultrasound-guided gun biopsy revealed histological evidence of cryptococcosis. Immunological screening tests did not identify immunodeficiency. She recovered completely with a combination therapy of amphotericin B and flucytosine for 2 weeks, followed by fluconazole for 8 months. The characteristics of cryptococcosis involving the mediastinal lymph node and the lung should be understood, and the possibility of cryptococcosis even in immunocompetent hosts should be considered.

• Journal of Pharmaceutical Investigation
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• v.39 no.3
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• pp.207-216
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• 2009

Fluconazole is used as an orally administrated antifungal drug for the treatment of tinea corporis, candidiasis including skin mycotic pneumonia infections. The dosage of fluconazole varies with indication ranging from 50 mg/day to 400 mg/day. The fluconazole capsule 50 mg (3 capsules daily) is already available in Korean market. To improve the patient compliance, a fluconazole tablet 150 mg (once a day administration) was developed recently. The purpose of this study was to evaluate the bioequivalence of three doses of fluconazole capsule 50 mg (Diflucan 50 mg, Pfizer Korea Inc., as a reference drug) and a single dose of fluconazole tablet 150 mg (Plunazol 150 mg, Daewoong Pharm. Co., Korea) according to the guidelines of the Korea Food and Drug Administration (KFDA). The bioequivalence for three capsules of Diflucan 50 mg and a single tablet of Plunazol 150 mg was investigated in twenty-four healthy male volunteers under a randomized 2${\times}$2 crossover trial design. The average age of twenty-four volunteers was 24.78${\pm}$3.27 year-old, average height was 175.56${\pm}$5.45 cm and average weight was 67.24${\pm}$6.86 kg. After three capsules of Diflucan 50 mg or a single tablet of Plunazol 150 mg were orally administered, blood was taken at predetermined time intervals and the plasma concentrations of fluconazole in plasma were determined using LC-MS-MS. The 90% confidence intervals for the main parameters of statistical results after logarithmic transformation were AUCt 0.9272-1.0084 and Cmax 0.8423-0.9544 respectively, which are in the range of log 0.8 to log 1.25 and the statistical results of additional parameters (AUClast, t1/2 and MRT) were also in the 90% confidence interval that is in the range of log 0.8 to log 1.25. Therefore, the results of this study confirm the bioequivalence of three capsules of Diflucan 50 mg to one tablet of Plunazol 150 mg.

• Korean Journal of Food Science and Technology
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• v.48 no.3
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• pp.241-246
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• 2016

The object of this study was to develop an alternative way to treat human skin pathogens using marine algae. During this study, we observed that the ethanolic extract of the edible brown algae [Sargassum serratifolium (C. Agardh) C. Agardh] exhibited potential antimicrobial activity against pathogenic commensal bacteria related with acne vulgaris (Propionibacterium acnes, Staphylococcus epidermidis, Staphylococcus aureus and Pseudomonas aeruginosa), and Candida albicans which causes cutaneous candidiasis. Among the solvent-soluble fractions from the ethanolic extract, a hexane-soluble fraction showed the strongest antimicrobial activity against all tested human skin pathogens with MIC values ranging from 32 to $512{\mu}g/mL$. In addition, the hexane fraction exhibited a synergistic antimicrobial activity with commercial antibiotics used in the treatment of acne vulgaris or cutaneous candidiasis. Thus, this study suggests that S. serratifolium extract could be a potential source of natural antimicrobial agents or a pharmaceutical component against human skin pathogens.

• 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.