High-performance liquid chromatographic analysis of mometasone furoate and its degradation products

Teng, Xiao Wei; Foe, Kuncoro; Brown, Kenneth; Cutler, David J.; Davies, Neal M.

doi:10.1016/s0731-7085(01)00408-3

Cited by 28 publications

(20 citation statements)

References 13 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The degradation profile of MF in human plasma was reported previously [15] (products D1, D3, D2 and D4 reported correspond to products A, B, C and D reported here). The half-life of MF was (18.4 AE 4.3 h, n=4).…”

Section: Degradation In Human Plasma and Effect Of Esterase Inhibitorssupporting

confidence: 83%

“…PMSF at concentrations 1 and 10 mm reduced the apparent degradation rate constant (k obs ) of MF by 12% and 19%, respectively. The degradation profile of MF in PMSF treated plasma was very similar to that in untreated human plasma [15]. EDTA 10 mm or SDS 70 mm significantly inhibited the decomposition of MF in human plasma, with k obs reduced by 83% and 79%, respectively.…”

Section: Degradation In Human Plasma and Effect Of Esterase Inhibitorsmentioning

confidence: 59%

See 1 more Smart Citation

Mometasone furoate degradation and metabolism in human biological fluids and tissues

Teng

Cutler

Davies

2003

Biopharm & Drug Disp

Self Cite

View full text Add to dashboard Cite

The in vitro metabolic and non-metabolic degradation kinetics of mometasone furoate (MF) was investigated in selected human biological fluids and subcellular fractions of tissues. Qualitative and quantitative differences in transformation profiles of MF were observed among human biological media. Degradation was the major event in plasma and urine with four new degradation products identified; A: 21-chloro-17alpha-hydroxy-16alpha-methyl-9beta,11beta-oxidopregna-1,4-diene-3,20-dione 17-(2-furoate), B: 9alpha,21beta-dichloro-11beta,21alpha-dihydroxy-16alpha-methylpregna-1,4,17,20-tetraen-3-one 21-(2-furoate), C: 21beta-chloro-21alpha-hydroxy-16alpha-methyl-9beta,11beta-oxidopregna-1,4,17,20-tetraen-3-one 21-(2-furoate), and D: 21-chloro-17alpha-hydroxy-16alpha-methyl-9beta,11beta-oxidopregna-1,4-diene-3,20-dione. A, B and C were predominant and D was minor in plasma while A and C were predominant in urine. Hydrolysis of the 17-ester bond of MF was not a major event in plasma. The turnover of MF in plasma was faster than that in phosphate buffers of pH 7.4. Metabolism of MF occurred primarily and rapidly in liver, appreciably in intestine, but negligibly in in vitro lung tissue. While 6beta-hydroxylation was a major metabolic pathway for MF in microsomes of both human liver and intestine, other parallel and subsequent metabolism pathways could also be involved. If these degradation and metabolic products are also formed and active in humans in vivo, both MF and its 'active' products need to be taken into account when determining the systemic bioavailability of MF and in establishing concentration-effect relationships with this drug.

show abstract

Section: Degradation In Human Plasma and Effect Of Esterase Inhibitorssupporting

confidence: 83%

Section: Degradation In Human Plasma and Effect Of Esterase Inhibitorsmentioning

confidence: 59%

Mometasone furoate degradation and metabolism in human biological fluids and tissues

Teng

Cutler

Davies

2003

Biopharm & Drug Disp

Self Cite

View full text Add to dashboard Cite

show abstract

“…There was some information about so far unidentified degradation products of MF in human plasma and simulated lung fluid. 17 In aqueous buffer solutions degradation pathways such as epoxide formation, hydrolysis, and ester group migration were observed. 18 In rat extrahepatic tissues and fluids only slow degradation of MF into four products was reported.…”

Section: Discussionmentioning

confidence: 99%

“…In human plasma, unidentified degradation products of MF were detected. 17 Further experiments revealed a pH-dependent degradation of MF in aqueous systems. 18 In rat tissues and fluids metabolism and degradation was observed.…”

Section: Introductionmentioning

confidence: 98%

Human Receptor Kinetics, Tissue Binding Affinity, and Stability of Mometasone Furoate

Valotis

Neukam

Elert

et al. 2004

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

“…appropriate for first order kinetics. Classical methods are rather slow, and so it is usually necessary to extract some of the reaction mixture and then stop the reaction so that no further reaction takes place during the analysis (Teng et al, 2001;Chancellor et al, 2008;Katsuda& Toshiro, 2009, Pierre et al, 2009Stepensky et al, 2004). A more sophisticated method is mass spectrometry, gas chromatogram (GC) in conjunction with a mass spectrometer and high-performance Liquid Chromatography combined with Mass Spectrometry (LC-MS or LC-MS/MS) have been used to detect concentrations.…”

Section: Introductionmentioning

confidence: 99%

Application of Tandem Mass Spectrometry in Chemical Kinetics

Qiao¹

2012

Tandem Mass Spectrometry - Applications and Principles

View full text Add to dashboard Cite

High-performance liquid chromatographic analysis of mometasone furoate and its degradation products

Cited by 28 publications

References 13 publications

Mometasone furoate degradation and metabolism in human biological fluids and tissues

Mometasone furoate degradation and metabolism in human biological fluids and tissues

Human Receptor Kinetics, Tissue Binding Affinity, and Stability of Mometasone Furoate

Application of Tandem Mass Spectrometry in Chemical Kinetics

Contact Info

Product

Resources

About