A randomized, open-label pharmacokinetic comparisonof two oral formulations of fluconazole 150 mg in healthy adult volunteers

Jovanović, Dušan; Kilibarda, Vesna; Ciric, Biljana; Vučinić, Slavica; Srnić, Danica; Vehabović, Midhad; N, Potogija

doi:10.1016/j.clinthera.2005.10.016

Cited by 16 publications

(20 citation statements)

References 10 publications

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“…The 90.0% C.I.s for the ratio of test medication to reference were within the range of 80.0-125.0%, which is acceptable according to USFDA and KFDA [19,20]. Moreover, the pharmacokinetic values obtained during the present study were similar to those of previous reports from Thailand, Saudi Arabia and Serbia and Montenegro [5,8,11,16], indicating that the generic differences involved do not affect the disposition of FLA. Thus, the bioequivalence study results indicated that the absorption of the 1 × 150 mg FLA tablet is comparable to that of the 3 × 50 mg capsules.…”

Section: Application To Bioequivalence Studysupporting

confidence: 89%

“…The protocol for the stability study included: (a) freeze-thaw stability, which was determined after three freeze (−70 • C)-thaw cycles on consecutive days, (b) short-term stability, which was determined by exposing samples to room temperature for 24 h, (c) long-term stability, which was determined after keeping the plasma samples frozen at −70 • C for 30 days, (d) postpreparative stability, which was determined after keeping the samples in auto-sampler at 4 • C for 24 h and (e) working solution stability, which was determined by exposing working solutions containing FLA or I.S. to room temperature for 6 h. The protocol was based on criteria recommended by USFDA [16].…”

Section: Stabilitymentioning

confidence: 99%

“…Several HPLC methods for determining FLA levels in human plasma have been described [7][8][9][10][11][12][13][14][15][16]. The majority utilize ultraviolet detection (UV) and a reversed-phase octadecylsilyl (C 18 ) column.…”

Section: Introductionmentioning

confidence: 99%

“…However, existing methods have shortcomings in terms of pharmacokinetic studies, i.e., a narrow concentration range (LLOQ ≥ 0.2 g/mL) [7][8][9][10][11][12][13], lengthy running times (>10.0 min) [7,[9][10][11][13][14][15][16] and the lack of an internal standard (I.S.) [8][9][10]12,16]. Therefore, a sensitive and a short chromatographic run-times of HPLC-UV analytical method is required to quantify FLA levels in human plasma to support pharmacokinetic and bioequivalence studies.…”

Section: Introductionmentioning

confidence: 99%

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An optimized analytical method of fluconazole in human plasma by high-performance liquid chromatography with ultraviolet detection and its application to a bioequivalence study

Kim¹,

Im²,

Kang³

et al. 2007

Journal of Chromatography B

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Section: Application To Bioequivalence Studysupporting

confidence: 89%

Section: Stabilitymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

An optimized analytical method of fluconazole in human plasma by high-performance liquid chromatography with ultraviolet detection and its application to a bioequivalence study

Kim¹,

Im²,

Kang³

et al. 2007

Journal of Chromatography B

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“…Its mechanism of action, like that of the other azoles, is related to its ability to alter the membrane permeability of yeasts and other fungi by inhibiting the synthesis of ergosterol. Inhibition of P-450 lanosterol 14-alpha-demethylase dependent causes accumulation of sterols methylated depletion ergosterol and inhibition of cell growth (Alnaim et al, 2007;Jovanović et al, 2005;Pore et al, 2006).…”

Section: Introductionmentioning

confidence: 99%

Validation of high-performance liquid chromatographic method for analysis of fluconazole in microemulsions and liquid crystals

Silva

Santos

Luz

et al. 2014

Braz. J. Pharm. Sci.

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In recent decades, there has been a significant increase in the incidence of fungal diseases. Certain fungal diseases cause cutaneous lesions and in the usual treatment, generally administred orally, the drug reaches the site of action with difficulty and its concentration is too low. An approach much explored in recent years is the development of nanotechnology-based drug delivery systems, and microemulsions (ME) and liquid crystals (LC) are promising. ME and LC were developed with oleic acid or copaiba oil as the oil phase, propoxyl (5OP) ethoxyl (20 OE) cetyl alcohol as surfactant and water. An analytical method to assess the incorporation of fluconazole (FLU) in the systems under study was validated according to guidelines of the International Conference on Harmonization (ICH) guidelines and the Brazilian Food, Drug and Sanitation Agency (ANVISA). The method was conducted on a C18-RP column (250 × 4.6 mm i.d.), maintained at room temperature. The mobile phase consisted of acetonitrile and water (50:50, v/v), run at a flow rate of 1.0mL/min and using ultraviolet detection at 210nm. The chromatographic separation was obtained with a retention time of 6.3min, and was linear in the range of 20-400 µg/mL (r 2 =0.9999). The specificity showed no interference of the excipients. The accuracy was 100.76%. The limits of detection and quantitation were 0.057 and 0.172 µg.mL -1 , respectively. Moreover, method validation demonstrated satisfactory results for precision and robustness. The proposed method was applied for the analysis of the incorporation of FLU in ME and LC, contributing to improve the quality control and to assure the therapeutic efficacy.Uniterms: Nanotehcnology. Microemulsions. Liquid crystals. High-performance liquid chromatography/ qualitative analysis. Fluconazole. Nas últimas décadas, houve aumento significativo na incidência de doenças fúngicas. Certas doenças fúngicas provocam lesões cutâneas, sendo que no tratamento usual, geralmente administrado por via oral, o medicamento chega ao local de ação com dificuldade, em concentração muito baixa. Uma abordagem muito explorada nos últimos anos é o desenvolvimento de sistemas de administração de fármacos baseados em nanotecnologia, como as microemulsões (ME) e cristais líquidos (LC). ME e LC foram desenvolvidos com o ácido oleico ou óleo de copaíba como fase oleosa, álcool cetílico propoxilado (5 OP) e etoxilado (20 OE) como tensoativo e água. Método analítico para avaliar a incorporação de fluconazol (FLU) nos sistemas em estudo foi validado de acordo com as diretrizes da Conferência Internacional de Harmonização (ICH) e Agência Nacional de Vigilância Sanitária (ANVISA). O método foi desenvolvido empregando coluna C18-RP (250 x 4,6 mm id), mantida à temperatura ambiente. A fase móvel consistiu de acetonitrila e água (50:50, v/v), executado a uma taxa de fluxo de 1,0 mL/min e com detecção ultravioleta a 210 nm. A separação cromatográfica foi obtida com o tempo de retenção de 6,3min, e mostrou-se linear no intervalo de 20-400 µg/mL (r 2 =0,9999). Pelo e...

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Pharmacokinetics and Bioequivalence of Fluconazole Capsules Manufactured in France and China in Healthy Chinese Participants: Open‐Label, Randomized, Single‐Dose, 2‐Way, Crossover Bioequivalence Study Under Fasted and Fed Conditions

Chen

Qing

Ying

et al. 2023

Clinical Pharm in Drug Dev

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This was an open-label, randomized study in healthy Chinese participants to assess the bioequivalence of 2 fluconazole 150-mg capsules under fasted and fed conditions. The study consisted of 2 treatment periods, separated by a 14-day washout period. Thirty-six participants were enrolled, with 18 participants each in the fasted and fed groups. In each treatment period, participants received a single oral dose of the test or reference fluconazole 150-mg capsule. After washout, participants received the alternate treatment. Blood samples for pharmacokinetic analysis were collected from 1 hour before dosing to 72 hours after dosing. The median plasma concentration-time profiles were similar for both treatments under fasted and fed conditions. Bioequivalence of fluconazole between the 2 capsules was demonstrated as 90% confidence intervals of the geometric mean ratios for the maximum plasma concentration and area under the plasma concentration-time curve from time 0 to 72 hours after dosing under fasted and fed conditions were within the acceptable range of 80%-125%. Overall, 7 participants reported at least 1 treatment-emergent adverse event; all were mild in severity. No serious adverse events or deaths were reported. The test fluconazole capsule was bioequivalent to the reference capsule, and a single dose was well tolerated. Clinicaltrials.gov ID: NCT03621072

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A randomized, open-label pharmacokinetic comparisonof two oral formulations of fluconazole 150 mg in healthy adult volunteers

Cited by 16 publications

References 10 publications

An optimized analytical method of fluconazole in human plasma by high-performance liquid chromatography with ultraviolet detection and its application to a bioequivalence study

An optimized analytical method of fluconazole in human plasma by high-performance liquid chromatography with ultraviolet detection and its application to a bioequivalence study

Validation of high-performance liquid chromatographic method for analysis of fluconazole in microemulsions and liquid crystals

Pharmacokinetics and Bioequivalence of Fluconazole Capsules Manufactured in France and China in Healthy Chinese Participants: Open‐Label, Randomized, Single‐Dose, 2‐Way, Crossover Bioequivalence Study Under Fasted and Fed Conditions

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