Comparative biotransformation and disposition studies of nabumetone in humans and minipigs using high-performance liquid chromatography with ultraviolet, fluorescence and mass spectrometric detection

Nobilis, Milan; Kopeckỳ, J.; Kvĕtina, J; Svoboda, Zbyněk; Pour, Milan; Kuneš, Jiřı́; Holčapek, Michal; Kolářová, Lenka

doi:10.1016/s0731-7085(03)00171-7

Cited by 38 publications

(37 citation statements)

References 16 publications

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“…[13][14][15][16][17] As such, minipigs are becoming more frequently used for toxicological and PK studies of small molecules. [18][19][20] Recently, minipigs have been used to test the immunogenicity of therapeutic proteins; 21,22 however, limited data exist for the pharmacokinetics of macromolecules in minipigs. [23][24][25] In particular, to the best of our knowledge, there are no studies that describe the PK of mAbs in minipigs.…”

Section: Resultsmentioning

confidence: 99%

Minipig as a potential translatable model for monoclonal antibody pharmacokinetics after intravenous and subcutaneous administration

Zheng¹,

Tesar²,

Benincosa

et al. 2012

mAbs

125

110

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Section: Resultsmentioning

confidence: 99%

Minipig as a potential translatable model for monoclonal antibody pharmacokinetics after intravenous and subcutaneous administration

Zheng¹,

Tesar²,

Benincosa

et al. 2012

mAbs

125

110

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“…The method for 6-MNA determination was applied with only minor modifications from Nobilis et al (2003). Shortly, the separation and detection of 6-MNA and naproxen (20 M, ISTD) was performed by high-performance liquid chromatography/UV (HP 1100; Agilent Technologies, Waldbronn, Germany) equipped with a LiChrospher 100 RP-18 column (100 ϫ 3 mm, 5-m particle size; Merck, Darmstadt, Germany).…”

Section: Methodsmentioning

confidence: 99%

A Predominate Role of CYP1A2 for the Metabolism of Nabumetone to the Active Metabolite, 6-Methoxy-2-naphthylacetic Acid, in Human Liver Microsomes

Turpeinen¹,

Hofmann²,

Klein³

et al. 2009

Drug Metabolism and Disposition

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ABSTRACT:Nabumetone, a widely used nonsteroidal anti-inflammatory drug, requires biotransformation into 6-methoxy-2-naphthylacetic acid (6-MNA), a close structural analog to naproxen, to achieve its analgesic and anti-inflammatory effects. Despite its wide use, the enzymes involved in metabolism have not been identified. In the present study, several in vitro approaches were used to identify the cytochrome P450 (P450) enzyme (

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“…4 Paracetamol (PAR), 4-hydroxyacetanilide is a widely-used analgesic and antipyretic drug. 5 T h e l i t e r a t u r e s u r vey r eve a l s t h a t s eve r a l chromatographic methods have been used for the analysis of NAB in biological fluids [6][7][8][9][10][11] and in pharmaceutical formulations. [10][11][12] Also colorimetric 13 and micellar stabilized room temperature phosphorescence quantitation 14 of NAB as single component, or in combinations with other drugs, has been reported.…”

Section: Introductionmentioning

confidence: 99%

Simultaneous HPTLC determination of nabumetone and paracetamol in combined tablet dosage form

Gandhi¹,

Ranher²,

Deshpande³

et al. 2011

J. Braz. Chem. Soc.

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Um novo método de cromatografia em camada delgada de alta eficiência (HPTLC) para determinação simultânea de nebumetona e paracetamol em forma combinada em comprimido foi desenvolvido e validado. As separações foram efetuadas em placas de alumínio prerrecobertas com sílica gel 60 F 254 utilizando tolueno:propanol-2:ácido acético (8:2:0.1, v/v/v) como fase móvel. A determinação quantitativa das bandas foi feita por varredura densitométrica a 236 nm. Os fatores de retenção calculados para nebumetona e paracetamol foram 0,78 ± 0,03 e 0,32 ± 0,03, respectivamente. O método foi validado com relação à linearidade, exatidão, precisão e robustez. A curva de calibração mostrou-se linear dentro do intervalo de 50-250 ng por banda de ambas as drogas. O método tem sido aplicado com sucesso nas análises das drogas em formulações farmacêuticas. As porcentagens de precisão de ensaio (média ± desvio padrão) foram 99,89 ± 1,15 para nabumetona e 101,10 ± 0,71 para paracetamol, ambos de comprimidos disponíveis comercialmente.A new simple high performance thin layer chromatographic method (HPTLC) for simultaneous determination of nabumetone and paracetamol in combined tablet dosage form was developed and validated. The separations were carried out on Merck aluminum plates precoated with silica gel 60 F 254 , using toluene:2-propanol:acetic acid (8:2:0.1, v/v/v) as mobile phase. Quantitative determination of bands was done by densitometric scanning at 236 nm. The calculated retention factors for nabumetone and paracetamol were 0.78 ± 0.03 and 0.32 ± 0.03, respectively. The method was validated with respect to linearity, accuracy, precision and robustness. The calibration curves showed to be linear over a range of 50-250 ng per band for both drugs. The method has been successfully applied for the analysis of drugs in pharmaceutical formulation. The percentages of assay (mean ± S.D.) were 99.89 ± 1.15 for nabumetone and 101.10 ± 0.71 for paracetamol, both of commercially available tablets.

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Comparative biotransformation and disposition studies of nabumetone in humans and minipigs using high-performance liquid chromatography with ultraviolet, fluorescence and mass spectrometric detection

Cited by 38 publications

References 16 publications

Minipig as a potential translatable model for monoclonal antibody pharmacokinetics after intravenous and subcutaneous administration

Minipig as a potential translatable model for monoclonal antibody pharmacokinetics after intravenous and subcutaneous administration

A Predominate Role of CYP1A2 for the Metabolism of Nabumetone to the Active Metabolite, 6-Methoxy-2-naphthylacetic Acid, in Human Liver Microsomes

Simultaneous HPTLC determination of nabumetone and paracetamol in combined tablet dosage form

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