Estimation of tegaserod in human plasma by high-performance liquid chromatography–tandem mass spectroscopy and its application to bioequivalence study

Singh, Sonu Sundd; Patel, Harshvardhan; Sharma, Kuldeep

doi:10.1016/j.aca.2005.10.044

Cited by 6 publications

(5 citation statements)

References 2 publications

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“…Tg-NEs were found to be stable and homogenous under dilution and body temperature, with no appreciable changes over the time in terms of hydrodynamic diameter, PDI and drug payload for 24 h (Figure 5). These results predicted a good stability of the nanoemulsions in the bloodstream, especially since tegaserod has been shown to remain stable in these conditions [70]. The nanoemulsions integrity could be preserved to reach the BBB.…”

Section: Stability Study Of Tg-nes Over Timementioning

confidence: 62%

Active Targeted Nanoemulsions for Repurposing of Tegaserod in Alzheimer’s Disease Treatment

et al. 2021

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Background and Purpose: The activation of 5-HT4 receptors with agonists has emerged as a valuable therapeutic strategy to treat Alzheimer’s disease (AD) by enhancing the nonamyloidogenic pathway. Here, the potential therapeutic effects of tegaserod, an effective agent for irritable bowel syndrome, were assessed for AD treatment. To envisage its efficient repurposing, tegaserod-loaded nanoemulsions were developed and functionalized by a blood–brain barrier shuttle peptide. Results: The butyrylcholinesterase inhibitory activity of tegaserod and its neuroprotective cellular effects were highlighted, confirming the interest of this pleiotropic drug for AD treatment. In regard to its drugability profile, and in order to limit its peripheral distribution after IV administration, its encapsulation into monodisperse lipid nanoemulsions (Tg-NEs) of about 50 nm, and with neutral zeta potential characteristics, was performed. The stability of the formulation in stock conditions at 4 °C and in blood biomimetic medium was established. The adsorption on Tg-NEs of peptide-22 was realized. The functionalized NEs were characterized by chromatographic methods (SEC and C18/HPLC) and isothermal titration calorimetry, attesting the efficiency of the adsorption. From in vitro assays, these nanocarriers appeared suitable for enabling tegaserod controlled release without hemolytic properties. Conclusion: The developed peptide-22 functionalized Tg-NEs appear as a valuable tool to allow exploration of the repurposed tegaserod in AD treatment in further preclinical studies.

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Section: Stability Study Of Tg-nes Over Timementioning

confidence: 62%

Active Targeted Nanoemulsions for Repurposing of Tegaserod in Alzheimer’s Disease Treatment

et al. 2021

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“…The method is limited by time-consuming extraction procedure such as solid phase extraction (SPE) and the LLOQ of 0.20 ng/ml. In our study, because the clinical dosage of tegaserod is lower than Sonu [7], the LLOQ of 0.20 ng/ml is not sensitive enough. Present paper describes a simple, economic and yet sensitive LC-ESI-MS/MS method that can determine tegaserod plasma concentration in humans as low as 0.05 ng/ml using liquid-liquid extraction and can be used to evaluate the pharmacokinetics of tegaserod in humans.…”

Section: Introductionmentioning

confidence: 63%

“…Sonu Sundd Singh et al [7] described the pharmacokinetic parameters in 24 healthy volunteers receiving 6 mg of test and reference tegaserod formulations. The developed method in this paper was successfully used for a pharmacokinetic study in which plasma concentration of tegaserod in 36 healthy Chinese volunteers (Groups A-C) 0.0985 ± 0.0018 0.5085 ± 0.0145 0.5110 ± 0.0120…”

Section: Pharmacokinetic Studymentioning

confidence: 99%

“…Tegaserod has also been estimated in human serum by differential pulse voltammetry [6] with a detection limit of 3.0 × 10.10 M, Sonu [7] has developed an LC-MS/MS method for the bioequivalence study of tegaserod formulation on healthy male human subjects. The method is limited by time-consuming extraction procedure such as solid phase extraction (SPE) and the LLOQ of 0.20 ng/ml.…”

Section: Introductionmentioning

confidence: 99%

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Determination of tegaserod by LC–ESI-MS/MS and its application to a pharmacokinetic study in healthy Chinese volunteers

Zou

Bian

Ding

et al. 2008

Journal of Chromatography B

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“…The drug is not official in any Pharmacopoeia[ 2 – 4 ]. A thorough literature survey revealed a few HPLC-MS[ 5 6 ], HPLC[ 7 ] and spectrophotometric[ 8 9 ] methods for the analysis of TM in plasma and formulations. Voltametry offers a group of highly selective and sensitive methods.…”

mentioning

confidence: 99%

Estimation of tegaserod maleate by differential pulse polarography

Rajput¹,

Raj²

2009

Indian J Pharm Sci

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A highly sensitive differential pulse polarographic method has been developed for the estimation of tegaserod maleate after treating it with hydrogen peroxide solution. The oxidation of tegaserod maleate is a reversible process as the oxidized product could be reduced at hanging mercury drop electrode in a quantitative manner using differential pulse polarography mode. The limit of quantification was 0.1ng/ml. The voltametric peak was obtained at -1.05 volts in presence of 0.1M potassium chloride as supporting electrolyte. The technique could be used successfully to analyze tegaserod maleate in its tablet formulation.

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Estimation of tegaserod in human plasma by high-performance liquid chromatography–tandem mass spectroscopy and its application to bioequivalence study

Cited by 6 publications

References 2 publications

Active Targeted Nanoemulsions for Repurposing of Tegaserod in Alzheimer’s Disease Treatment

Active Targeted Nanoemulsions for Repurposing of Tegaserod in Alzheimer’s Disease Treatment

Determination of tegaserod by LC–ESI-MS/MS and its application to a pharmacokinetic study in healthy Chinese volunteers

Estimation of tegaserod maleate by differential pulse polarography

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