FORMULATION AND EVALUATION OF AZELNIDIPINE FAST DISSOLVING TABLETS

BALA HEMALATHA; ANNE RAMU; SURYADEVARA VIDYADHARA

doi:10.22159/ijap.2025v17i1.52398

Authors

BALA HEMALATHA Acharya Nagarjuna University College of Pharmaceutical Sciences, Acharya Nagarjuna University, Guntur, Andhra Pradesh, India https://orcid.org/0009-0000-0765-7986
ANNE RAMU Department of Pharmaceutics, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chowdavaram, Guntur, Andhra Pradesh, India
SURYADEVARA VIDYADHARA Department of Pharmaceutics, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chowdavaram, Guntur, Andhra Pradesh, India

DOI:

https://doi.org/10.22159/ijap.2025v17i1.52398

Keywords:

Azelnidipine, PEG 6000, Microcrystalline cellulose-polyethylene glycol (MCC-PEG) conjugate, Crospovidone, croscarmellose sodium, Sodium starch glycolate, dissolving tablets

Abstract

Objective: The main aim of the present study was to improve the solubility and rate of dissolution of azelnidipine and thereby increase the oral bioavailability. Azelnidipine is a calcium channel blocker that lowers blood pressure by relaxing blood vessels and relieving pressure on them. Azelnidipine is a Biopharmaceutics Classification System (BCS) class II drug with low bioavailability.

Methods: The present study involves the preparation and evaluation of solid dispersion of azelnidipine by physical mixing, fusion and solvent evaporation method using polyethylene glycol 6000 (PEG 6000) as a carrier. The prepared solid dispersions were evaluated for various parameters like angle of repose, carr’s index, particle size, drug content, Scanning Electron Microscopy (SEM) analysis, Differential Scanning Calorimetry (DSC), X-ray diffraction (XRD) and in vitro dissolution studies. As part of the project, Microcrystalline Cellulose-Polyethylene Glycol (MCC-PEG) Conjugate, a novel superdisintegrant, was developed.

Results: Solid dispersions prepared by fusion (AF 6) in a drug-to-polymer ratio of 1:3 released 99.40% of the drug more quickly than pure drug and other dispersions. The optimized solid dispersion (AF6) was used to prepare fast-dissolving tablets of azelnidipine. In comparison to commercially available and alternative tablet formulations, the study suggests that azelnidipine tablets (AT 13), made with 5% microcrystalline cellulose - Polyethylene glycol conjugate as a super disintegrant, exhibited rapid drug release of 99.92% in 15 minutes. The drug was released in the following order: MCC-PEG Conjugate > Crospovidone > Croscarmellose sodium > Sodium starch glycolate in all tablet preparations containing super disintegrants.

Conclusion: It can be inferred that MCC-PEG conjugate is an efficient super disintegrant by comparing its results with those of available commercial super disintegrants and caused the drug azelnidipine to release rapidly from fast-dissolving tablets

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