Simultaneous determination of bambuterol and its two major metabolites in human plasma by hydrophilic interaction ultra-performance liquid chromatography–tandem mass spectrometry

Zhou, Ting; Cheng, Qunpeng; Zou, Chengjuan; Zhao, Ting; Liu, Shan; Pistolozzi, Marco; Tan, Evina; Xu, Ling; Tan, Wen

doi:10.1016/j.jchromb.2014.07.022

Cited by 12 publications

(13 citation statements)

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“…Both bambuterol and monocarbamate bambuterol are BChE inhibitors, inhibiting their own hydrolysis [3][4]. Our previous studies showed that monocarbamate bambuterol contributed significantly to the inhibition of BChE in humans after the administration of normal doses of bambuterol, which resulted in the rate-limiting step during the conversion of bambuterol into its active drug terbutaline [5][6]. Therefore, monocarbamate bambuterol concentrations should always be monitored during the pharmacokinetic studies of bambuterol [6].…”

Section: Introductionmentioning

confidence: 99%

Chiral analysis of bambuterol, its intermediate and active drug in human plasma by liquid chromatography–tandem mass spectrometry: Application to a pharmacokinetic study

Zhou

Liu

Zhao

et al. 2015

Journal of Chromatography B

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Section: Introductionmentioning

confidence: 99%

Chiral analysis of bambuterol, its intermediate and active drug in human plasma by liquid chromatography–tandem mass spectrometry: Application to a pharmacokinetic study

Zhou

Liu

Zhao

et al. 2015

Journal of Chromatography B

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“…The physiologically relevant concentration of BMB and MONO was set at 40 nM to equal the highest sum of BMB, MONO, and TBT concentrations measured in the plasma of healthy volunteers during a pharmacokinetic study of BMB (Zhou et al, 2014b). This value represents a hypothetical minimum concentration of BMB reaching the circulation (i.e., considering plasma protein binding, other metabolisms, distribution to tissues, and elimination of the three species negligible).…”

Section: In Vitro Measurements Of Bche Activitymentioning

confidence: 99%

“…The physiologically relevant concentration of BChE was set at 6.42 U/mL. This value was chosen on the basis of the lowest activity found among the previously cited healthy volunteers (Zhou et al, 2014b). An aliquot of the stock solution of BChE was diluted fourfold in sodium phosphate buffer (50 mM, pH 7.4) and divided in fractions of 12 mL.…”

Section: In Vitro Measurements Of Bche Activitymentioning

confidence: 99%

“…The supernatant (2 mL) was injected into the UPLC-MS/MS system. The chromatographic separation and the detection of BMB, MONO, and TBT were performed by using a method validated for plasma samples (Zhou et al, 2014b). The details of the analysis are reported as Supplemental Material 3.…”

Section: Bmb and Mono Used As Substrates: Simultaneous Quantitation Omentioning

confidence: 99%

“…In light of the recent indications reported by the European Medicines Agency (EMA, 2012), the Food and Drug Administration (U.S. FDA, 2012), and successive suggestions (Yu and Tweedie, 2013), metabolites that are present at 25% of the parent area under time-concentration curve (AUC) or 100% of the parent AUC (Yu and Tweedie, 2013) should be subject of further in vitro characterization of the metabolite as a possible contributor to drugdrug interactions. This is clearly the case of BMB and MONO, because the AUC of MONO (in molar units) was found to be about 300% of the AUC of BMB in a recent pharmacokinetic study (Zhou et al, 2014b). The renewed interest over BMB and the indications of the regulatory bodies emphasized the gaps in the current knowledge of BMB pharmacokinetics, and in particular on the interaction of its primary metabolite, MONO with BChE.…”

Section: Introductionmentioning

confidence: 98%

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Stereoselective Inhibition of Human Butyrylcholinesterase by the Enantiomers of Bambuterol and Their Intermediates

Pistolozzi

Hong

et al. 2014

Drug Metab Dispos

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This work describes the sequential hydrolysis of bambuterol enantiomers and their monocarbamate metabolites (MONO) catalyzed by human butyrylcholinesterase (BChE) as well as the enzyme inhibition resulting from this process. Particular emphasis is given to the contribution given by MONO to the enzyme inhibition because it was not fully characterized in previous works. Bambuterol and MONO enantiomers displayed the same time-and concentrationdependent mechanism of interaction with the enzyme. The hydrolysis kinetics of both bambuterol and MONO was enantioselective, and the (R)-enantiomer of each compound was hydrolyzed fourfold faster than the respective (S)-enantiomer. Even though the enzyme inhibition rates of (R)-and (S)-MONO were much slower than those of their respective bambuterol enantiomers (∼15-fold), both MONO enantiomers showed a significant BChE inhibition when physiologically relevant concentrations of enzyme and inhibitors were used (∼50% of their respective bambuterol enantiomers). The kinetic constants obtained by testing each single compound were used to model the contribution given by MONO to the enzyme inhibition observed for bambuterol. The hydrolysis of MONO enantiomers enhanced the inhibitory power of bambuterol enantiomers of about 27.5% (R) and 12.5% (S) and extended more than 1 hour the duration of inhibition. The data indicate that MONO contribute significantly to the inhibition of BChE occurring in humans upon administration of normal doses of bambuterol. In addition, the hydrolysis of MONO resulted in the rate-limiting step in the conversion of bambuterol in its pharmacologically active metabolite terbutaline; therefore, MONO concentrations should always be monitored during pharmacokinetic studies of bambuterol.

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Micelle‐enhanced spectrofluorimetric method for the rapid determination of bronchodilator terbutaline and its prodrug bambuterol: application for content uniformity test

et al. 2022

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A novel, simple and sensitive spectrofluorimetric approach for determination of terbutaline sulphate (TER) and its prodrug bambuterol (BAM) in their pure and pharmaceutical dosage forms was developed. The suggested approach depends on enhancing the native fluorescence of either TER or BAM at 315 and 297.2 nm after excitation at 277 and 259 nm, respectively, using sodium dodecyl sulphate (SDS) as a micellar medium. In the presence of 0.7% w/v SDS, $1.38-fold and 1.18-fold enhancement is achieved in the relative fluorescence intensity (RFI) of TER and BAM, respectively. The fluorescence-concentration curves were rectilinear over the concentration range 0.8-16 μg ml À1 , with detection limits (LOD) of 0.252 and 0.26 (μg ml À1 ), quantitation limits (LOQ) of 0.76 and 0.79 (μg ml À1 ), determination coefficients (r2) of 0.9981, and slopes of 45.92 and 10.44 for TER and BAM, respectively. The suggested approach was validated in accordance with International Council for Harmonisation criteria and was effectively applied in the analysis of the studied drugs in their commercial tablets. The high sensitivity of the proposed approach allows its application in evaluating the content uniformity testing of the studied drugs in their tablets through using the official United States Pharmacopeia criteria. Statistical analogies of the findings with that of the reported methods showed really good harmony and indicated no major differences in precision and accuracy.

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Simultaneous determination of bambuterol and its two major metabolites in human plasma by hydrophilic interaction ultra-performance liquid chromatography–tandem mass spectrometry

Cited by 12 publications

References 35 publications

Chiral analysis of bambuterol, its intermediate and active drug in human plasma by liquid chromatography–tandem mass spectrometry: Application to a pharmacokinetic study

Chiral analysis of bambuterol, its intermediate and active drug in human plasma by liquid chromatography–tandem mass spectrometry: Application to a pharmacokinetic study

Stereoselective Inhibition of Human Butyrylcholinesterase by the Enantiomers of Bambuterol and Their Intermediates

Micelle‐enhanced spectrofluorimetric method for the rapid determination of bronchodilator terbutaline and its prodrug bambuterol: application for content uniformity test

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