Journal article
Improvement of in Vitro Dissolution of the Poor Water-Soluble Amlodipine Drug by Solid Dispersion with Irradiated Polyvinylpyrrolidone

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Publication Details
Author list: Mohamed Mohamady Ghobashy, Dalal Mohamed Alshangiti, Sheikha A. Alkhursani, Samera Ali Al-Gahtany, Fathiah Salem Shokr and Mohamed Madani
Publisher: American Chemical Society: Open Access Titles / American Chemical Society
Publication year: 2020
Journal: ACS Omega
Journal name in source: ACS Omega
Volume number: 5
Issue number: 34
Start page: 21476
End page: 21487
Number of pages: 12
ISSN: 2470-1343
Web of Science ID: 000568645300018
PubMed ID: 32905418
Scopus ID: 85091036703
eISSN: 2470-1343

The aim of this study was to increase both the rates of dissolution and bioavailability of the amlodipine (Amlo) drug. Due to the low cost, high solubility, and amorphous state, polyvinylpyrrolidone (PVP) has been used as a drug carrier in the solid dispersion process. Through applying an irradiation technique, powder of (PVP) is irradiated with six 0–50 kGy irradiation doses. The six irradiated (PVP) samples were characterized using gel permeation chromatography, electron spin resonance, and Fourier transform infrared (FT-IR) spectroscopy. The formulation of six (PVP/Amlo) samples at a ratio of 2:1 wt/wt were characterized using FT-IR spectroscopy and X-ray powder diffraction. In vitro dissolution of (Amlo) drug was assessed in a water solvent at pH 1.2 and pH 7. Results demonstrated that there is a change in the physicochemical properties of irradiated (PVP). FT-IR confirmed that there is an intermolecular H bond between the (Amlo) drug and (PVP) polymer. XRD confirmed that (PVP) changes the crystalline (Amlo) to amorphous amlodipine. Irradiated (PVP) at a dose of 20 kGy released approximately 89% from 40 mg of (Amlo) in 60 s. The in vitro rate of amlodipine dissolution depends on the drug–polymer intermolecular H bond. The rate of (Amlo) dissolution is increased due to the drug–drug intramolecular hydrogen bonding replaced with the drug–polymer intermolecular hydrogen bonding, which reduces the crystal packing. Irradiated (PVP) improved the rate of (Amlo) dissolution compared to unirradiated (PVP).

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Last updated on 2020-02-11 at 13:04