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

Abstract

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).

Rational Design of Self-Supported CuOx-Decorated Composite Films as an Efficient and Easy-Recycling Catalyst for Styrene Oxidation

“…65 The absorption peak at 2929 cm −1 confirms the presence of asymmetric CH 2 , and the peak at 822 cm −1 represents the characteristic vibrations of PVP rings. 66 The peaks at 1368 cm −1 (COO− symmetric stretching vibrations), 1320 cm −1 (C−H bending vibrations), and 1108 cm −1 (C−O stretching vibrations) belong to CMC. 67,68 These FT-IR results indicate the presence of PVP and CMC in the tested samples.…”

“…The primary microstructure of CuO@rGO-PC was preserved after the recycling test (Figure h). The FT-IR spectra of CuO@rGO-PC and CuO@rGO-PC-R illustrated in Figure f demonstrated vibration bands attributable to −OH (3352 cm –1 ), −CH 2 (2929 cm –1 ), CO (1654 cm –1 ), COO– (1368 cm –1 ), C–H (1320 cm –1 ), and C–O (1108 cm –1 ) groups. − The strong and broad peak at 1654 cm –1 could be assigned to the stretching vibration of CO in PVP rings . The absorption peak at 2929 cm –1 confirms the presence of asymmetric CH 2 , and the peak at 822 cm –1 represents the characteristic vibrations of PVP rings .…”

“…The FT-IR spectra of CuO@rGO-PC and CuO@rGO-PC-R illustrated in Figure f demonstrated vibration bands attributable to −OH (3352 cm –1 ), −CH 2 (2929 cm –1 ), CO (1654 cm –1 ), COO– (1368 cm –1 ), C–H (1320 cm –1 ), and C–O (1108 cm –1 ) groups. − The strong and broad peak at 1654 cm –1 could be assigned to the stretching vibration of CO in PVP rings . The absorption peak at 2929 cm –1 confirms the presence of asymmetric CH 2 , and the peak at 822 cm –1 represents the characteristic vibrations of PVP rings . The peaks at 1368 cm –1 (COO– symmetric stretching vibrations), 1320 cm –1 (C–H bending vibrations), and 1108 cm –1 (C–O stretching vibrations) belong to CMC. , These FT-IR results indicate the presence of PVP and CMC in the tested samples.…”

Solid Dispersion: A Mechanistic and Realistic Approach on Antihypertensive Drug as a Drug Carrier System

“…The rate of dissolution was found to increase as the crystal packing is reduced due to replacement of the drugdrug intermolecular hydrogen bond along with the drugpolymer intermolecular hydrogen bond. 43 SDs prepared using Poloxamer 407 and Poloxamer 188 were able to improve the solubility of amlodipine besylate. 44 The XRD analysis revealed that drugs existed in the amorphous state in the SD in contrast to their crystalline state in the pure form.…”

Computational investigation of metal organic frameworks as potential drug carriers for antihypertensive amlodipine

“…A large variety of nanoparticles have been investigated for encapsulating amlodipine including diamond nanoparticles, 5 nanoemulsions, 6 mesoporous silica nanoparticles, 7 nanostructured lipid, 8 and polyvinylpyrrolidone. 9 However, they suffer from some problems such as insufficient drug adsorption capacity or poor control of drug release. Metal organic frameworks (MOFs), composed of metal ions and organic linkers, not only have the advantages of high pore volume, large surface area, and low density but also offer superior and tunable chemical and structural properties compared with traditional porous materials.…”