Physicochemical characterisation, drug polymer dissolution and in vitro evaluation of phenacetin and phenylbutazone solid dispersions with polyethylene glycol 8000

Sheraz Khan, Hannah Batchelor, Peter Hanson, Yvonne Perrie, Afzal-Ur-Rahman Mohammed

Research output: Contribution to journalArticle

Abstract

Poor water solubility leads to low dissolution rate and consequently, it can limit bioavailability. Solid dispersions, where the drug is dispersed into an inert, hydrophilic polymer matrix can enhance drug dissolution. Solid dispersions were prepared using phenacetin and phenylbutazone as model drugs with polyethylene glycol (PEG) 8000 (carrier), by melt fusion method. Phenacetin and phenylbutazone displayed an increase in the dissolution rate when formulated as solid dispersions as compared with their physical mixture and drug alone counterparts. Characterisation of the solid dispersions was performed using differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM). DSC studies revealed that drugs were present in the amorphous form within the solid dispersions. FTIR spectra for the solid dispersions of drugs suggested that there was a lack of interaction between PEG 8000 and the drug. However, the physical mixture of phenacetin with PEG 8000 indicated the formation of hydrogen bond between phenacetin and the carrier. Permeability of phenacetin and phenylbutazone was higher for solid dispersions as compared with that of drug alone across Caco-2 cell monolayers. Permeability studies have shown that both phenacetin and phenylbutazone, and their solid dispersions can be categorised as well-absorbed compounds.
LanguageEnglish
Pages4281-4294
Number of pages14
JournalJournal of Pharmaceutical Sciences
Volume100
Issue number10
Early online date10 May 2011
DOIs
Publication statusPublished - Oct 2011

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Phenacetin
Phenylbutazone
Polymers
Pharmaceutical Preparations
Differential Scanning Calorimetry
Fourier Transform Infrared Spectroscopy
Permeability
Caco-2 Cells
In Vitro Techniques
polyethylene glycol 8000
Drug Liberation
Electron Scanning Microscopy
Solubility
Biological Availability
Hydrogen
Water

Keywords

  • solid dispersions
  • PEG 8000
  • phenacetin
  • phenylbutazone
  • FTIR
  • DSC
  • dissolution studies
  • permeability
  • amorphous form

Cite this

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title = "Physicochemical characterisation, drug polymer dissolution and in vitro evaluation of phenacetin and phenylbutazone solid dispersions with polyethylene glycol 8000",
abstract = "Poor water solubility leads to low dissolution rate and consequently, it can limit bioavailability. Solid dispersions, where the drug is dispersed into an inert, hydrophilic polymer matrix can enhance drug dissolution. Solid dispersions were prepared using phenacetin and phenylbutazone as model drugs with polyethylene glycol (PEG) 8000 (carrier), by melt fusion method. Phenacetin and phenylbutazone displayed an increase in the dissolution rate when formulated as solid dispersions as compared with their physical mixture and drug alone counterparts. Characterisation of the solid dispersions was performed using differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM). DSC studies revealed that drugs were present in the amorphous form within the solid dispersions. FTIR spectra for the solid dispersions of drugs suggested that there was a lack of interaction between PEG 8000 and the drug. However, the physical mixture of phenacetin with PEG 8000 indicated the formation of hydrogen bond between phenacetin and the carrier. Permeability of phenacetin and phenylbutazone was higher for solid dispersions as compared with that of drug alone across Caco-2 cell monolayers. Permeability studies have shown that both phenacetin and phenylbutazone, and their solid dispersions can be categorised as well-absorbed compounds.",
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Physicochemical characterisation, drug polymer dissolution and in vitro evaluation of phenacetin and phenylbutazone solid dispersions with polyethylene glycol 8000. / Khan, Sheraz; Batchelor, Hannah; Hanson, Peter; Perrie, Yvonne; Mohammed, Afzal-Ur-Rahman.

In: Journal of Pharmaceutical Sciences, Vol. 100, No. 10, 10.2011, p. 4281-4294.

Research output: Contribution to journalArticle

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T1 - Physicochemical characterisation, drug polymer dissolution and in vitro evaluation of phenacetin and phenylbutazone solid dispersions with polyethylene glycol 8000

AU - Khan, Sheraz

AU - Batchelor, Hannah

AU - Hanson, Peter

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AU - Mohammed, Afzal-Ur-Rahman

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