• 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.

• 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.