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

[Image: see text] 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 appl...

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Autores principales: Ghobashy, Mohamed Mohamady, Alshangiti, Dalal Mohamed, Alkhursani, Sheikha A., Al-Gahtany, Samera Ali, Shokr, Fathiah Salem, Madani, Mohamed
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2020
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7469126/
https://www.ncbi.nlm.nih.gov/pubmed/32905418
http://dx.doi.org/10.1021/acsomega.0c01910
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author Ghobashy, Mohamed Mohamady
Alshangiti, Dalal Mohamed
Alkhursani, Sheikha A.
Al-Gahtany, Samera Ali
Shokr, Fathiah Salem
Madani, Mohamed
author_facet Ghobashy, Mohamed Mohamady
Alshangiti, Dalal Mohamed
Alkhursani, Sheikha A.
Al-Gahtany, Samera Ali
Shokr, Fathiah Salem
Madani, Mohamed
author_sort Ghobashy, Mohamed Mohamady
collection PubMed
description [Image: see text] 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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spelling pubmed-74691262020-09-04 Improvement of In Vitro Dissolution of the Poor Water-Soluble Amlodipine Drug by Solid Dispersion with Irradiated Polyvinylpyrrolidone Ghobashy, Mohamed Mohamady Alshangiti, Dalal Mohamed Alkhursani, Sheikha A. Al-Gahtany, Samera Ali Shokr, Fathiah Salem Madani, Mohamed ACS Omega [Image: see text] 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). American Chemical Society 2020-08-18 /pmc/articles/PMC7469126/ /pubmed/32905418 http://dx.doi.org/10.1021/acsomega.0c01910 Text en Copyright © 2020 American Chemical Society This is an open access article published under an ACS AuthorChoice License (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html) , which permits copying and redistribution of the article or any adaptations for non-commercial purposes.
spellingShingle Ghobashy, Mohamed Mohamady
Alshangiti, Dalal Mohamed
Alkhursani, Sheikha A.
Al-Gahtany, Samera Ali
Shokr, Fathiah Salem
Madani, Mohamed
Improvement of In Vitro Dissolution of the Poor Water-Soluble Amlodipine Drug by Solid Dispersion with Irradiated Polyvinylpyrrolidone
title Improvement of In Vitro Dissolution of the Poor Water-Soluble Amlodipine Drug by Solid Dispersion with Irradiated Polyvinylpyrrolidone
title_full Improvement of In Vitro Dissolution of the Poor Water-Soluble Amlodipine Drug by Solid Dispersion with Irradiated Polyvinylpyrrolidone
title_fullStr Improvement of In Vitro Dissolution of the Poor Water-Soluble Amlodipine Drug by Solid Dispersion with Irradiated Polyvinylpyrrolidone
title_full_unstemmed Improvement of In Vitro Dissolution of the Poor Water-Soluble Amlodipine Drug by Solid Dispersion with Irradiated Polyvinylpyrrolidone
title_short Improvement of In Vitro Dissolution of the Poor Water-Soluble Amlodipine Drug by Solid Dispersion with Irradiated Polyvinylpyrrolidone
title_sort improvement of in vitro dissolution of the poor water-soluble amlodipine drug by solid dispersion with irradiated polyvinylpyrrolidone
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7469126/
https://www.ncbi.nlm.nih.gov/pubmed/32905418
http://dx.doi.org/10.1021/acsomega.0c01910
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