Simultaneous determination of the two main metabolites of deflazacort in human plasma by high-performance liquid chromatography

Bernareggi, A.; Poletti, P.; Zanolo, G.; Zerilli, L. F.

doi:10.1016/0731-7085(87)80021-3

Cited by 12 publications

(7 citation statements)

References 4 publications

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“…Plasma concentrations of 21HDFZ were analysed by high‐performance liquid chromatography according to the method of Bernareggi, Poletti, Zanolo, and Zerilli (). The HPLC system was equipped with a model 305 and 306 pumps, 811C dynamic mixer, 805 manometric module, 115 UV detector (Gilson, Middleton, USA), and a model SIL‐10ADVP autoinjector (Shimadzu, Kyoto, Japan) connected to a computer with a Shimadzu Class‐VP™ Chromatography Data System programme (Shimadzu, Columbia, USA).…”

Section: Methodsmentioning

confidence: 99%

“…Plasma concentrations of 21HDFZ were analysed by highperformance liquid chromatography according to the method of Bernareggi, Poletti, Zanolo, and Zerilli (1987 (500 ng of prednisolone) were added to a 10 ml glass tube and mixed by shaking. After that the specimen was extracted in two serial steps, with 10 and 5 ml of methylene chloride also by shaking for 10 min, at 300 inversions per min.…”

Section: Methodsmentioning

confidence: 99%

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Pharmacokinetics of deflazacort in rabbits after intravenous and oral administration and its interaction with erythromycin

Escudero

Marı́n

Cárceles

et al. 2017

Vet Pharm & Therapeutics

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The pharmacokinetic of deflazacort after intravenous and oral administration and the effect of erythromycin on the disposition of deflazacort in rabbits were investigated.A parallel study was carried out in twelve rabbits. The plasma concentration-time profiles of deflazacort were determined after intravenous and oral administration of single dosages of 5 mg/kg in the presence and absence (baseline) of multiple dose erythromycin regimens. Plasma concentrations of 21-desacetyldeflazacort were determined by HPLC. Plasma concentration-time curves were analysed by compartmental pharmacokinetic and noncompartmental methods. The t ½λz values following intravenous and oral administration were 3.67 and 4.96 hr, respectively. The apparent volume of distribution at steady-state (V ss ) was 4.08 ± 0.31 L/kg, this value indicates that deflazacort is widely distributed into the extravascular tissues. Moreover, bioavailability after oral administration of deflazacort (F = 87.48%) was high.Pharmacokinetic analysis after both routes of administration revealed a significant reduction in total body clearance, a significant increase in mean residence time, half-life and plasma concentrations of the steroid in the presence of multiple dose erythromycin. The results indicated the influence of the erythromycin on deflazacort disposition, which is consistent with a pharmacokinetic-type interaction in the elimination of the drug from the body. Moreover, this interaction should be considered to avoid adverse effects when using both drugs concomitantly.

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Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Pharmacokinetics of deflazacort in rabbits after intravenous and oral administration and its interaction with erythromycin

Escudero

Marı́n

Cárceles

et al. 2017

Vet Pharm & Therapeutics

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“…In man, deflazacort is rapidly desacetylated to deflazacort-21 alcohol (DF-210H), which is further metabolized to 6B-hydroxy-DF-210H. DF-210H is reported to be the major species determined in plasma; deflazacort was not detected (Bernareggi et al, 1987). An assay to quantitate DF-210H in human plasma at concentrations of 1 ng/mL was required to support the clinical development of deflazacort.…”

Section: Introduction Deflazacort ((11 ~L6)-21-(acetyloxy-(ll-hydroxmentioning

confidence: 97%

“…These procedures utilized liquid-liquid extraction (Bernareggi et al, 1987) or solid-phase C-18 extraction (Chan, 1991), each coupled with a normal-phase liquid chromatographic separation using ultraviolet detection. Lower limits of quantitation were 5 and 10ng/mL DF-210H for these assays, respectively.…”

Section: Introduction Deflazacort ((11 ~L6)-21-(acetyloxy-(ll-hydroxmentioning

confidence: 99%

Quantitative determination of 21‐hydroxy‐deflazacort in human plasma using gradient semi‐microbore liquid chromatography

Reynolds¹,

Burmaster²,

Eichmeier³

1994

Biomedical Chromatography

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A sensitive and selective liquid chromatographic procedure to quantitate the deflazacort metabolite 21-hydroxy-deflazacort (DF-21OH) in human plasma was developed and validated. DF-21OH and fludrocortisone acetate (internal standard, IS) were isolated from human plasma (2 mL) by solid-phase extraction onto C-18 cartridges. Potential interferences were selectively removed and analytes were eluted with ethyl acetate. Following evaporation, the residue was reconstituted for HPLC analysis. Separation was achieved by gradient elution using a 5 microns YMC Basic column (2.0 x 100 mm) with mobile phases consisting of 20% methanol and 50% acetonitrile in 50 mM phosphate buffer (pH 3) at a temperature of 50 degrees C. Flow rate was maintained at 0.3 mL/min., and analytes were quantified spectrophotometrically at 246 nm. The assay was validated over the range 1.0 to 500 ng/mL DF-21OH. Calibration curves were prepared using a weighted (1/concentration) nonlinear quadratic regression algorithm. Peak-height ratios were proportional to the amount of DF-21OH added to plasma. Assay precision (%RSD) ranged from 4.2 to 11%, with a corresponding assay accuracy (% relative error) of +/- 2.8%. Absolute recovery of DF-21OH from plasma was 78-86% over the concentration range. The minimum quantitation limit was 1.0 ng/mL.

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“…Several high performance liquid chromatographic (HPLC) methods have been reported for determination of DFZ and its metabolites in biological fluids (Bernareggi et al, 1987;Santos-Montes et al, 1994;Reynolds, Burmaster, Fichmeier, 1994;Hirata et al, 1994;Möllmann et al, 1995;Rao et al, 1996;Santos-Montes, Isquierdo-Hornillos, 1999;Ifa et al, 2000). However, there is no official method for DFZ analysis in any of the pharmacopoeia.…”

Section: Introductionmentioning

confidence: 99%

Spectrophotometric and HPLC determination of deflazacort in pharmaceutical dosage forms

Scremin

Piazzon

Silva

et al. 2010

Braz. J. Pharm. Sci.

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(DFZ) is a glucocorticoid used as an anti-inflammatory and immunosuppressant drug. No official methods are available for DFZ determination in pharmaceutical formulations. The objective of this study was to develop, validate and compare spectrophotometric (UV and colorimetric) and highperformance liquid chromatography (HPLC) methods, for the quantitative determination of DFZ in tablets and oral suspension. For the UV method, ethanol was used as the solvent, with detection at 244 nm. The colorimetric method was based on the redox reaction with blue tetrazolium in alkaline medium, with detection at 524 nm. The method by HPLC was carried out using a C 18 column, mobile phase consisting of acetonitrile:water (80:20, v/v) with a flow rate of 1.0 mL min -1 and detection at 244 nm. The methods proved linear (r > 0.999), precise (RSD < 5%) and accurate (recovery > 97%). Statistical analysis of the results indicated that the UV and HPLC methods were statistically equivalent, while the values obtained for the colorimetric method differed significantly from the other methods. O deflazacorte (DFZ) é um fármaco glicocorticóide usado como antiinflamatório e imunossupressor. Métodos oficiais não estão disponíveis para a determinação de DFZ em formas farmacêuticas. Este estudo teve como objetivo desenvolver, validar e comparar métodos por espectrofotometria (UV e colorimetria) e cromatografia líquida de alta eficiência (CLAE), na determinação quantitativa de DFZ em comprimidos e suspensão oral. O método por UV utilizou etanol como solvente, com detecção em 244 nm. O método colorimétrico foi baseado na reação de redução com azul de tetrazólio em meio alcalino, com detecção em 524 nm. O método por CLAE utilizou coluna C 18 ; fase móvel constituída de acetonitrila:água (80:20, v/v), com fluxo de 1,0 mL min -1 e detecção em 244 nm. Os métodos foram lineares (r > 0,999); precisos (RSD < 5 %), e exatos (recuperação > 97%). As análises estatísticas dos resultados obtidos indicaram que os métodos por UV e por CLAE foram estatisticamente equivalentes, enquanto os valores obtidos para o método colorimétrico diferiram significativamente dos demais métodos.Unitermos: Deflazacorte/determinação quantitativa. Cromatografia líquida de alta eficiência/análise quantitativa. Espectrofotometria/análise quantitativa. Medicamentos/análise quantitativa.

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Simultaneous determination of the two main metabolites of deflazacort in human plasma by high-performance liquid chromatography

Cited by 12 publications

References 4 publications

Pharmacokinetics of deflazacort in rabbits after intravenous and oral administration and its interaction with erythromycin

Pharmacokinetics of deflazacort in rabbits after intravenous and oral administration and its interaction with erythromycin

Quantitative determination of 21‐hydroxy‐deflazacort in human plasma using gradient semi‐microbore liquid chromatography

Spectrophotometric and HPLC determination of deflazacort in pharmaceutical dosage forms

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