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. 2017 Feb;7(1):111-124.
doi: 10.1007/s13346-016-0344-5.

Evaluation of the drug solubility and rush ageing on drug release performance of various model drugs from the modified release polyethylene oxide matrix tablets

Saeed Shojaee  1   2 , Ali Nokhodchi  3   4 , Mohammed Maniruzzaman  5
Affiliations

Evaluation of the drug solubility and rush ageing on drug release performance of various model drugs from the modified release polyethylene oxide matrix tablets

Saeed Shojaee et al. Drug Deliv Transl Res. 2017 Feb.

Erratum in

Abstract

Hydrophilic matrix systems are currently some of the most widely used drug delivery systems for controlled-release oral dosage forms. Amongst a variety of polymers, polyethylene oxide (PEO) is considered an important material used in pharmaceutical formulations. As PEO is sensitive to thermal oxidation, it is susceptible to free radical oxidative attack. The aim of this study was to investigate the stability of PEO based formulations containing different model drugs with different water solubility, namely propranolol HCl, theophylline and zonisamide. Both polyox matrices 750 and 303 grade were used as model carriers for the manufacture of tablets stored at 40 °C. The results of the present study suggest that the drug release from the matrix was affected by the length of storage conditions, solubility of drugs and the molecular weight of the polymers. Generally, increased drug release rates were prevalent in soluble drug formulations (propranolol) when stored at the elevated temperature (40 °C). In contrast, it was not observed with semi soluble (theophylline) and poorly soluble (zonisamide) drugs especially when formulated with PEO 303 polymer. This indicates that the main parameters controlling the drug release from fresh polyox matrices are the solubility of the drug in the dissolution medium and the molecular weight of the polymer. DSC traces indicated that that there was a big difference in the enthalpy and melting points of fresh and aged PEO samples containing propranolol, whereas the melting point of the aged polyox samples containing theophylline and zonisamide was unaffected. Graphical abstract ᅟ.

Keywords: Controlled release; Drug release; Drug solubility; Polyox matrices; Stability.

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Conflict of interest statement

The authors declare that they have no conflict of interest.

Figures

Graphical abstract
Graphical abstract
ᅟ
Fig. 1
Fig. 1
The effect of storage time and various molecular weights on drug release of propranolol at (1:1) drug/polymer ratio and stored at 40 °C. a PEO 750/303 effect of MV. b PEO 750. c PEO 303
Fig. 2
Fig. 2
The effect of different relative humidity on the drug release of propranolol at 16–75% RH on storage
Fig. 3
Fig. 3
GPC profiles for PEO 750 fresh compared to 8-week samples stored at 40 °C
Fig. 4
Fig. 4
The effect of storage time and various molecular weights on drug release of theophylline at (1:1) drug/polymer ratio and stored at 40 °C. a PEO 750/303 effect of molecular weight. b PEO 750. c PEO 303
Fig. 5
Fig. 5
The effect of storage time and various molecular weights on drug release of zonisamide at (1:1) drug/polymer ratio and stored at 40 °C. a PEO 750/303 effect of molecular weight. b PEO 750. c PEO 303
Fig. 6
Fig. 6
SEM of various molecular weight PEOs at zero and week 8 storage times that were obtained at 25 °C
Fig. 7
Fig. 7
X-ray diffraction (XRD) patterns of various molecular weights PEO750 and 303 at zero and week 8 storage times
Fig. 8
Fig. 8
DSC thermograms for ground propranolol, theophylline and zonisamide matrix tablets: PEO 750 and 303 before and after storage times of 0, 2, 4 and 8 weeks
See this image and copyright information in PMC

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