Abstract
Anionic polymer sodium carboxymethylcellulose (CELLOGEN® HP-HS and/or HP-12HS) was investigated for its ability to influence the release of three model drugs propranolol hydrochloride, theophylline and ibuprofen from polyethylene oxide (POLYOX™ WSR 1105 and/or Coagulant) hydrophilic matrices. For anionic ibuprofen and non-ionic theophylline, no unusual/unexpected release profiles were obtained from tablets containing a mixture of two polymers. However, for cationic propranolol HCl, a combination of polyethylene oxide (PEO) with sodium carboxymethylcellulose (NaCMC) produced a significantly slower drug release compared to the matrices with single polymers. The potential use of this synergistic interaction can be a design of new extended release pharmaceutical dosage forms with a more prolonged release (beyond 12 h) using lower polymer amount, which could be particularly beneficial for freely water-soluble drugs, preferably for once daily oral administration. In order to explain changes in the obtained drug release profiles, Fourier transform infrared absorption spectroscopy was performed. A possible explanation for the more prolonged propranolol HCl release from matrices based on both PEO and NaCMC may be due to a chemical bond (i.e. ionic/electrostatic intermolecular interaction) between amine group of the cationic drug and carboxyl group of the anionic polymer, leading to a formation of a new type/form of the active (i.e. salt) with sustained release pattern.
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Acknowledgements
The authors are grateful to Dai-Ichi Kogyo Seiyaku and IMCD for generous supply of Na CMC and ibuprofen, Charlotte Penny (Sekisui Diagnostics) for assistance in interpretation of potential chemical interaction and Colorcon for providing Ph.D. scholarship.
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Guest Editors: Michael Repka, Joseph Reo, Linda Felton and Stephen Howard
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Palmer, D., Levina, M., Nokhodchi, A. et al. The Influence of Sodium Carboxymethylcellulose on Drug Release from Polyethylene Oxide Extended Release Matrices. AAPS PharmSciTech 12, 862–871 (2011). https://doi.org/10.1208/s12249-011-9648-4
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DOI: https://doi.org/10.1208/s12249-011-9648-4