Journal of In Silico & In Vitro Pharmacology

Bio-analytical Validated Method Development and Bioequivalence Study of Serotonin Receptor 5-HT4 Agonist Dihydrobenzofurancarboxamide Derivative used for Chronic Constipation Drug Prucalopride by LC-ESI-MS/MS in Indian Human Plasma

Aim and objective: Clinically, prucalopride is used to treat persistent constipation since it is a serotonin receptor agonist. According to US-FDA and European Medicines Agency (EMA) requirements, a validated bioanalytical technique for prucalopride quantification from human plasma was developed and utilized in a comparative investigation of pharmacokinetics and bioequivalence of the drug.

Method: Prucalopride's protonated precursor ion was 368.1/196.0 m/z, while propranolol's was 260.1/116.0 m/z. When it came to plasma, it was extracted using liquid-liquid technology. It combined with 10 mM ammonium acetate as an aqueous solvent with an apparent pH of 1.20 and 1% formic acid in acetonitrile as an organic solvent at a flow rate of 0.5000 ml/min as the mobile phase. 0.25 ng/ml, 0.50 ng/ml, 1 ng/ml, 2 ng/ml, 4 ng/ml, 8 ng/ml, and 16 ng/ml is used as calibration concentrations.

Result: Peak Concentration Cmax was 4.98 ng/ml ± 0.95 ng/ml for reference preparation at 2.71 hour ± 0.33 hour. (Tmax) and 5.01 ± 1.05 ng/ml for test preparation at 2.64 hour ± 0.28 hour (Tmax).

Conclusion: Using this technique for comparative pharmacokinetics and bioequivalence studies has proven to be a highly selective, sensitive, high recovery, low ion suppression, repeatable, and cost effective approach.

Author(s):

Pallab Mandal, Soumya Chakraborty, Rakesh Bera, Chiranjit Saha, Balaram Ghosh, Sourav Poddar, Sujata Barma, Sanmoy Karmakar, Tapan K Pal

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