Skip to main content

Development of fully amorphous dispersions of a low Tg drug via co-spray drying with hydrophilic polymers

Zhao, M., Barker, S.A., Belton, P.S., McGregor, C., Craig, D.Q.M. (2012) Development of fully amorphous dispersions of a low Tg drug via co-spray drying with hydrophilic polymers. European Journal of Pharmaceutics and Biopharmaceutics, 82 (3). pp. 572-579. ISSN 0939-6411. (doi:10.1016/j.ejpb.2012.07.012) (The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided) (KAR id:78846)

The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided.
Official URL
https://doi.org/10.1016/j.ejpb.2012.07.012

Abstract

The aim of the study was to prepare molecular dispersions of a physically highly unstable amorphous drug, paracetamol (acetaminophen with a Tg of ca. 25°C) via co-spray drying with a variety of polymers. Solid dispersions at a range of drug loadings (10-90%w/w) using hydroxypropyl methylcellulose/acetate succinate (HPMC/HPMC AS), polyvinylpyrrolidone (PVP) and copovidone were produced and characterised by modulated temperature differential scanning calorimetry (MTDSC), thermogravimetric analysis (TGA), X-ray powder diffraction (XRPD), Fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM). PVP-based polymers showed a greater tendency than the HPMC-based group to generate temperature-stable dispersions. In particular, copovidone (Plasdone® S-630) was found to be the most effective of the polymers studied and could formulate molecular dispersions at drug loadings up to and including 40%w/w. However, no evidence for direct drug-polymer interactions was found for such systems as a possible stabilising mechanism. The expected relationship of a higher Tg of the polymer leading to greater stabilisation was not observed, while there was an inverse relationship between viscosity grade and amorphous phase generation. The study has therefore shown that temperature-stable amorphous dispersions of a low Tg drug may be prepared by co-spray drying, particularly using PVP-based polymers.

Item Type: Article
DOI/Identification number: 10.1016/j.ejpb.2012.07.012
Uncontrolled keywords: Acetaminophen, Amorphous, Paracetamol, Pyrrolidone, Solid dispersion, Spray drying, hydroxypropylmethylcellulose acetate succinate, paracetamol, polymer, povidone, aqueous solution, article, differential scanning calorimetry, dispersion, drug solubility, glass transition temperature, heating, hydrogen bond, hydrophilicity, infrared spectroscopy, melting point, miscibility, scanning electron microscopy, spray drying, thermogravimetry, viscometry, viscosity, X ray powder diffraction, Acetaminophen, Calorimetry, Differential Scanning, Drug Carriers, Drug Stability, Methylcellulose, Microscopy, Electron, Scanning, Polymers, Povidone, Pyrrolidines, Spectroscopy, Fourier Transform Infrared, Temperature, Thermogravimetry, Transition Temperature, Vinyl Compounds, Viscosity, X-Ray Diffraction
Divisions: Divisions > Division of Natural Sciences > Medway School of Pharmacy
Depositing User: Susan Barker
Date Deposited: 27 Nov 2019 10:14 UTC
Last Modified: 16 Nov 2021 10:26 UTC
Resource URI: https://kar.kent.ac.uk/id/eprint/78846 (The current URI for this page, for reference purposes)
Barker, S.A.: https://orcid.org/0000-0003-4880-0253
  • Depositors only (login required):