Abstract

FORMULATION AND EVALUATION OF CARVEDILOL PHOSPHATE EXTENDED RELEASE TABLETS ALONG WITH AUTO DOCKING ANALYSIS, PREDICTIONS OF PHARMACOKINETICS AND DRUGLIKENESS PROPERTIES STUDIES

S. Selvaraj*, K. Tamilarasan and P. Perumal

Abstract

Introduction: Carvedilol phosphate, a non-selective beta-blocker, is used for the treatment of hypertension and heart failure. Extendedrelease formulations enhance therapeutic efficacy and patient compliance by ensuring prolonged drug release. Aim: This study focuses on the formulation and evaluation of extended-release carvedilol phosphate tablets, including pre-compression and postcompression analysis, in vitro drug release, molecular docking studies, pharmacokinetic predictions, and drug-likeness evaluation. Methods: Extended-release tablets were prepared using hydroxypropyl methylcellulose (HPMC K4M and K100M) via the wet granulation method. Pre-compression parameters such as identification, determination of powder characteristics like tapped density, untapped density, angle of repose, and loss on drying were assessed. Postcompression studies included average weight, group weight, uniformity of weight variation, thickness, hardness, friability, dissolution studies, related substances, and assay using HPLC. Molecular docking (AutoDock) analyzed carvedilol’s binding affinity to beta-adrenergic receptors, while SwissADME predicted pharmacokinetic properties and drug-likeness. Results: All formulations met pharmacopoeial standards for weight uniformity, thickness, and friability. Formulations F2 and F7 exhibited higher hardness. Dissolution studies confirmed extended drug release over 20 hours. Docking studies revealed strong receptor binding, suggesting effective targeting. Pharmacokinetic analysis showed moderate solubility, low bioavailability (0.17), and a favorable metabolic profile. Drug-likeness evaluation indicated compliance with Lipinski’s rule of five, confirming its potential as an oral therapeutic agent. Conclusion: This study successfully developed extended-release carvedilol phosphate tablets with desirable physicochemical properties. Computational studies supported the formulation’s potential for improved therapeutic outcomes.

Keywords: Carvedilol Phosphate, Extended-Release Tablets, Molecular Docking, Pharmacokinetics, Drug-Likeness Properties.