Liquid chromatographic determination of ketoconazole, a potent inhibitor of CYP3A4-mediated metabolism

Bruijn, Peter de; Kehrer, Diederik F.S.; Verweij, Jaap; Sparreboom, Alex

doi:10.1016/s0378-4347(00)00573-9

Cited by 18 publications

(13 citation statements)

References 17 publications

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“…Alkalinization of samples, proposed by several authors [7,9,14,16] did not improve the results, thus it was not adopted in this method. In addition, tedious and time consuming preparation procedures, such as sample evaporation and reconstitution aiming for lower limits of detection, were eliminated.…”

Section: Sample Preparationmentioning

confidence: 99%

“…Among them microbiological assays [4,5] lack specificity because they are based on measurement of antifungal activity, which may not only be due to ketoconazole but to other bioactive plasma components or metabolites as well. HPLC methods with UV [6][7][8][9][10][11][12], fluorescence [13,14], electrochemical [15] and MS-MS [16] detection have been reported in plasma samples. Chen et al [16] have summarized the limitations of all the above HPLC methods.…”

Section: Introductionmentioning

confidence: 99%

“…Chen et al [16] have summarized the limitations of all the above HPLC methods. More specifically, main drawbacks of the existing HPLC methods with UV detections are either high detection limits (>50 ng/ml) [8][9][10][11][12], or complicated and time consuming sample preparation procedures including liquid-liquid extraction, evaporation and reconstitution in order to lower LODs [6][7][8]12] or long total time elution time (>20 min) with the internal standard eluted after ketoconazole [7][8][9][10] or lack of internal standard [6,11,12]. The aim of the present work was to develop and validate a simple, fast and reliable isocratic RP-HPLC method with UV detection for the determination of ketoconazole in plasma samples.…”

Section: Introductionmentioning

confidence: 99%

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Optimization and validation of a high-performance liquid chromatographic method with UV detection for the determination of ketoconazole in canine plasma

Vertzoni

Archontaki

2006

Journal of Chromatography B

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Section: Sample Preparationmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Optimization and validation of a high-performance liquid chromatographic method with UV detection for the determination of ketoconazole in canine plasma

Vertzoni

Archontaki

2006

Journal of Chromatography B

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“…24,25 This paper describes the development and optimization of a new analytical method combining SPE of CLO and KET residues in milk from dairy cattle and their subsequent analysis by a previously validated HPLC-UV method.…”

Section: Introductionmentioning

confidence: 99%

SPE-HPLC method for determination of ketoconazole and clotrimazole residues in cow's milk

Beigi¹,

Imani²,

Payehghadr³

et al. 2011

J. Braz. Chem. Soc.

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Um método simples confirmatório para determinação em HPLC-UV de resíduos de cetoconazol e clotrimazol em leite de vaca, após extração da fase sólida (SPE), é relatado neste artigo. Foram removidos das amostras proteínas e lipídeos por tratamento com acetonitrila e conseqüente extração em n-hexano. Os extratos foram posteriormente limpos e concentrados através de extração em fase sólida. Os analitos foram determinados quantitativamente usando um método validado de cromatografia líquida de alta eficiência. O método foi linear no intervalo de 0,1 a 1,0 µg mL -1 para ambos analitos. Os limites de detecção e quantificação para os analitos foram iguais a 0,01 e 0,1 µg mL -1 , respectivamente. Parâmetros importantes que influenciam a eficiência da extração foram investigados e otimizados. O método proposto foi aplicado à análise de amostras de leite. Foram obtidas recuperações satisfatórias no intervalo de 95,9 a 101,78%, usando SPE.A simple confirmatory method for HPLC-UV determination of ketoconazole and clotrimazole residues in cow's milk after solid phase extraction (SPE) is reported in this article. The samples were deprived of proteins and lipids by treating with acetonitrile and consequent extraction in n-hexane. Extracts were further cleaned-up and concentrated via solid phase extraction. The analytes were determined quantitatively using a validated high performance liquid chromatography method. The method was linear in the range of 0.1-1.0 µg mL -1 for both analytes. Limits of detection and quantification for both analytes were equal to 0.01 and 0.1 µg mL -1 , respectively. Important parameters influencing the extraction efficiency were investigated and then optimized; the proposed method was applied to the analysis of milk samples. Satisfactory recoveries were obtained in the range of 95.9-101.78% using SPE.

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“…They include volumetric, 3) spectrophotometric, [4][5][6][7][8][9][10][11][12][13][14][15][16][17][18] spectrofluorimetric methods, [19][20][21] capillary electrophoresis method, 22,23) thin layer chromatography, 24,25) gas chromatography 26,27) and high performance liquid chromatographic methods. [28][29][30][31][32][33][34][35][36][37][38][39][40] However, the imidazole antifungal derivatives are susceptible for the degradation due to the effect of temperature, oxygen, light and pH and the degraded products may be pharmacologically inactive. In addition, there are many antifungal pharmaceutical preparations containing some corticosteroid hormones and the pharmacopeial methods don't report any method for the determination of these drugs either in presence of their degradation products or in presence of corticosteroid hormones.…”

mentioning

confidence: 99%

Stability Indicating Methods for the Determination of some Anti-fungal Agents Using Densitometric and RP-HPLC Methods

Mousa

El-Kousy

El‐Bagary

et al. 2008

CHEMICAL & PHARMACEUTICAL BULLETIN

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There are more than 100000 different species of fungi, many of which are beneficial to food and fermentation industries; however, hundreds are pathogenic to plants and a few hundreds have been shown to cause infection in humans. 1)Treatment of fungal infections is considerably more difficult than that of a bacterial infection as many fungal infections occur in poorly vascularised or avascular tissues. 2)Ketoconazole (KT), clotrimazole (CL), miconazole nitrate (MN) and econazole nitrate (EN) (Fig. 1) are imidazole derivatives which represent a large and emerging group of synthetic antifungal agents.Several methods for the determination of ketoconazole, clotrimazole, miconazole nitrate and econazole nitrate, have been described in the literature. They include volumetric, 3) spectrophotometric, [4][5][6][7][8][9][10][11][12][13][14][15][16][17][18] spectrofluorimetric methods, [19][20][21] capillary electrophoresis method, 22,23) thin layer chromatography, 24,25) gas chromatography 26,27) and high performance liquid chromatographic methods. [28][29][30][31][32][33][34][35][36][37][38][39][40] However, the imidazole antifungal derivatives are susceptible for the degradation due to the effect of temperature, oxygen, light and pH and the degraded products may be pharmacologically inactive. In addition, there are many antifungal pharmaceutical preparations containing some corticosteroid hormones and the pharmacopeial methods don't report any method for the determination of these drugs either in presence of their degradation products or in presence of corticosteroid hormones.In this study simple, rapid precise and selective densitometric and HPLC method for the determination of some antifungal drugs KT, CL, MN, and EN in pure form or in the presence of their degradation products were developed. The methods were successfully applied to determine these drugs in pharmaceutical dosage forms and in presence of some corticosteroid hormones. ExperimentalMaterials and Reagents Ketoconazole (KT) Sedico Pharmaceutical Co., 6 October City-Egypt. The purity of the sample was found to be 99.82Ϯ1.157 applying a non-aqueous titration pharmacopoeial method. 3)Clotrimazole (CL) Pharcopharmaceuticals, Alexandria-Egypt. The purity of the sample was found to be 99.87Ϯ1.856 applying a non-aqueous titration pharmacopoeial method. 3)Miconazole nitrate (MN) Minapharm-Egypt. The purity of the sample was found to be 99.776Ϯ1.695 applying a non-aqueous titration pharmacopoeial method. Control and Research; Cairo, Egypt. Received February 26, 2007; accepted September 30, 2007; The HPLC method determined mixtures of CL or EN with their degradation products which were separated and quantified on a Zorbax C8 column. Elution was carried out using methanol : phosphate buffer pH 2.5 (65 : 35 v/v) as a mobile phase at a flow rate of 1.5 ml/min and UV detection at 220 nm for CL. For EN, a mixture of methanol : water containing 0.06 ml triethylamine pH 10 (75 : 25 v/v) was used as a mobile phase at a flow rate of 1.5 ml/min and UV detection at 225 nm. ...

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Liquid chromatographic determination of ketoconazole, a potent inhibitor of CYP3A4-mediated metabolism

Cited by 18 publications

References 17 publications

Optimization and validation of a high-performance liquid chromatographic method with UV detection for the determination of ketoconazole in canine plasma

Optimization and validation of a high-performance liquid chromatographic method with UV detection for the determination of ketoconazole in canine plasma

SPE-HPLC method for determination of ketoconazole and clotrimazole residues in cow's milk

Stability Indicating Methods for the Determination of some Anti-fungal Agents Using Densitometric and RP-HPLC Methods

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