• Journal of Pharmaceutical Investigation
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• 제30권1호
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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.

• 약학회지
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• 제45권4호
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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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• 제9권1호
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• pp.31-35
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• 2009

위장관 칸디다증은 대개는 면역성이 저하된 경우에 기회 감염으로 발현되는 것이 일반적이다. 위장관 칸디다증 중식도 칸디다증이 가장 많은 빈도를 차지하고 있고 주로 면역기능이 억제된 환자에서 잘 발생하지만 드물게 건강한 성인에서도 보고된다. 현재까지는 양성 위궤양에 병발된 위장관 칸디다증이 흔히 보고되었지만 위선암에서 발견된 칸디다증은 비교적 드물다. 저자들은 속쓰림과 소화불량을 주소로 내원한 72세 여자환자에서 수술전 위선암과 칸디다증으로 진단되어 fluconazole을 경구투여를 통하여 칸디다증을 치료한 후 위전절제술을 시행한 증례를 경험하였다. 본 증례의 경험과 문헌 검색을 통하여, 저자들은 위암 수술 전 위암과 함께 위 칸디다증을 진단받은 환자에 대하여 칸디다에 대한 약물 치료 후 수술을 권유하는 바이다.

• Pediatric Infection and Vaccine
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• 제28권2호
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• pp.124-131
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• 2021

Cryptococcus neoformans는 주로 면역이 저하된 환자에서 기회 감염을 일으키는 진균이다. 그러나 면역이 정상인 환자에서도 다양한 감염을 일으킬 수 있다. 림프절을 침범한 폐 크립토코쿠스증은 정상 면역을 가진 사람에서는 상대적으로 드물게 발생한다. 고열과 지속적인 기침을 주소로 병원에 온 17세 여자 청소년이 가슴X선 영상검사 및 컴퓨터단층촬영에서 전방 종격동에서 우측 쇄골하 부위까지 침범된 종괴를 보여 초음파 유도하 총생검 검사로 크립토코쿠스증을 진단하였다. 각종 면역 검사에서는 이상 소견이 발견되지 않았다. 환자는 2주간 암포테리신 B와 플루시토신으로 치료 후 8개월간 플루코나졸로 치료하였고 완쾌되었다. 본 증례를 통해 크립토코쿠스증의 특징을 이해하고 정상 면역 환자에게서도 크립토코쿠스증이 발생할 수 있음을 염두에 두고 진단을 내리는 것이 바람직하겠다.

• Journal of Pharmaceutical Investigation
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• 제39권3호
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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.

• 한국식품과학회지
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• 제48권3호
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• pp.241-246
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• 2016

S. aureus, S. epidermidis, P. aeruginosa, P. acnes와 C. albicans는 사람의 피부에서 발생하는 질병과 밀접한 관련을 가지는 대표적인 병원성 미생물로 알려져 있다. 본 연구에서는 해조류 중에서도 항균 활성에 대한 연구가 미미한 모자반을 대상으로 피부 병원균에 대한 항균 효과를 조사하였다. 국내의 연해에 자생하는 7종의 모자반 추출물 중에서 disc diffusion assay와 MIC assay를 통해 가장 뛰어난 항균 효과를 나타낸 톱니모자반을 후속 연구를 위한 후보 물질로 선정하고 연구를 진행하였다. 톱니모자반 추출물의 유기용매 분획층 중에서, 노말-헥세인 분획층이 S. aureus, S. epidermidis, P. aeruginosa, P. acnes 및 C. albicans에 대한 MIC값이 $32-256{\mu}g/mL$로 가장 뛰어난 항균 활성을 나타내었다. 이에 피부 병원균들에 대한 치료제로 사용되고 있지만 내성균의 출현으로 효능이 거의 없는 항생제들인 테트라사이클린, 에리트로마이신, 린코마이신과 플루코나졸과 항균 활성이 뛰어난 것으로 나타난 톱니모자반의 노말-헥세인 분획층과의 병용 사용에 의한 항균 시너지 효과를 조사하였다. 그 결과, 톱니모자반 노말-헥세인 분획층과 이들 항생제와의 병용 사용에 의해 피부 병원균에 대한 항생제와 톱니모자반 노말-헥세인 분획층의 MIC값이 4-32배 감소되었고, 톱니모자반 노말-헥세인 분획층과 이들 항생제와의 병용 시 median FIC값이 0.26-0.55로 항균 시너지 효과를 나타내었다. 즉, 항생제와 톱니모자반 노말-헥세인 분획층과의 병용 사용은 피부 병원균에 대한 이들 항생제의 감수성을 회복시키는데 크게 기여하는 것으로 나타났다.

• Journal of Pharmaceutical Investigation
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• 제33권2호
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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.