Enantioselective determination of sibutramine and its active metabolites in human plasma

Kang, Wonku; Bae, Kyoungjin; Noh, Keumhan

doi:10.1016/j.jpba.2009.07.023

Cited by 15 publications

(8 citation statements)

References 7 publications

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“…Literature survey reveals that quantification of sibutramine in pharmaceutical, synthetic/dietary supplements and herbal products was reported using LC–MS [4] , [5] , [6] , [7] and HPLC [8] , [9] , [10] , [11] in biological matrices, e.g. rats [12] , [13] , [14] , [15] , [16] , [17] , [18] . Only a few methods were reported for the quantification of sibutramine and its two metabolites in human plasma using LC–MS/MS [19] , [20] , [21] , [22] , [23] , [24] .…”

Section: Introductionmentioning

confidence: 99%

“…rats [12] , [13] , [14] , [15] , [16] , [17] , [18] . Only a few methods were reported for the quantification of sibutramine and its two metabolites in human plasma using LC–MS/MS [19] , [20] , [21] , [22] , [23] , [24] . Kang et al [21] developed a method with the linearity range of 0.1 – 0.8 ng/mL; they used imipramine as the internal standard and a more complicated solid phase extraction method to isolate sibutramine and its two metabolites.…”

Section: Introductionmentioning

confidence: 99%

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Quantification of sibutramine and its two metabolites in human plasma by LC–ESI-MS/MS and its application in a bioequivalence study

Ponnuru

Challa

Nadendla³

2012

Journal of Pharmaceutical Analysis

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Obesity can be considered as a chronic illness of epidemic proportion and its incidents have increased exponentially in recent years. The use of anti-obesity drugs such as sibutramine is somewhat helpful. There is a need to quantify such drugs in biological samples, which is generally quite difficult. In this report, we developed and validated a simple, sensitive and specific liquid chromatography–tandem mass spectrometry (LC–MS/MS) method for the quantification of sibutramine (SB) and its two metabolites N-des methyl sibutramine (DSB) and N-di desmethyl sibutramine (DDSB) in human plasma. Zorbax SB-C18 (4.6 mm×75 mm, 3.5 μm, 80 Å) analytical column and 5 mM ammonium formate:acetonitrile (10:90, v/v) mobile phase were used for chromatographic separation of SB, DSB and DDSB. Multiple reaction monitoring (MRM) in the positive mode was used to detect SB, DSB and DDSB at m/z 280.3/124.9, 266.3/125.3 and 252.2/124.9, respectively. Liquid–liquid extraction was used for the extraction of analytes and internal standard from human plasma. This method was validated over a linear concentration range of 10.0–10,000.0 pg/mL for SB, DSB and DDSB with correlation coefficients (r) of ≥0.9997. The drug and the two metabolites were stable in plasma samples. The validated method was successfully applied in a bioequivalence and pharmacokinetic study with human volunteers under fasting condition.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Quantification of sibutramine and its two metabolites in human plasma by LC–ESI-MS/MS and its application in a bioequivalence study

Ponnuru

Challa

Nadendla³

2012

Journal of Pharmaceutical Analysis

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“…chromatography-mass spectrometry (LC-MS), [8][9][10][11][12][13][14][15][16] gas chromatography-mass spectrometry (GC-MS) 17,18 and ultra-high-pressure liquid chromatography coupled to quadrupole-time-of-flight (UHPLC-QTOF) mass spectrometry. 19 For applications in pharmaceutical products, there are methods that make use of spectrophotometry [20][21][22] and HPLC.…”

mentioning

confidence: 99%

Development and validation of an analytical method by RP-HPLC for quantification of sibutramine hydrochloride in pharmaceutical capsules

et al. 2011

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Sibutramine is a monoamine re-uptake inhibitor used for the treatment of obesity. In the present study a rapid, sensitive and economical HPLC method was developed and fully validated for analysis of sibutramine HCl in pharmaceutical capsules. HPLC analyses were carried out by using an isocratic elution mode with a mobile phase constituted by sodium phosphate buffer (pH 2.5) and methanol (30 : 70, v/v), flow rate at 1.0 mL min À1, column temperature at 40 C, UV detection wavelength at 225 nm and 20 mL of injection volume. The validation parameters were in accordance with FDA and ICH specifications, showing accuracy, precision, selectivity, robustness and linearity from 4.5 to 19.5 mg L À1 of sibutramine HCl. The limits of detection and quantification were 0.666 and 2.018 mg L À1 , respectively. The validated method is suitable for quality control applications and its advantages over the already existing methods are simplicity and reduced analysis time.

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“…Several reports have been published for the chiral determination of SIB by HPLC techniques, using protein based chiral stationary phase [21], Chiracel OD column [22] or Chiralcel AGP-stationary phase column [23,24].…”

Section: Chiral Separation Of Sibutramine By Chromatographic Methodsmentioning

confidence: 99%

“…The method was validated in accordance with FDA regulations for the validation of bioanalytical methods. The method was successfully applied to quantify SIB and its metabolites stereoisomers plasma concentration in healthy volunteers [24].…”

Section: Chiral Separation Of Sibutramine By Chromatographic Methodsmentioning

confidence: 99%

Analytical Methodologies for the Stereoselective Determination of Sibutramine: An Overview

Vlad

Hancu

Kelemen

et al. 2017

Acta Medica Marisiensis

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Sibutramine is a chiral anti-obesity drug which decreases food intake and increases energy expenditure. In therapy it is used as a racemic mixture; however both pharmacokinetic and pharmacodynamic data have revealed enantioselective behavior of sibutramine and its major active metabolites. Several chromatographic and electrophoretic analytical methods have been published so far for the chiral determination of sibutramine from pharmaceutical preparations and biological samples. The current paper aims to provide a systematic review of the stereochemical aspects and analytical methods used for the enantiodetermination of sibutramine and its active enantiomers covering the last 15 years.

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Enantioselective determination of sibutramine and its active metabolites in human plasma

Cited by 15 publications

References 7 publications

Quantification of sibutramine and its two metabolites in human plasma by LC–ESI-MS/MS and its application in a bioequivalence study

Quantification of sibutramine and its two metabolites in human plasma by LC–ESI-MS/MS and its application in a bioequivalence study

Development and validation of an analytical method by RP-HPLC for quantification of sibutramine hydrochloride in pharmaceutical capsules

Analytical Methodologies for the Stereoselective Determination of Sibutramine: An Overview

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