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Development and evaluation of injection-molded sustained-release tablets containing ethylcellulose and polyethylene oxide.
Drug Dev Ind Pharm. 2011 Feb; 37(2):149-59.DD

Abstract

PURPOSE

It was the aim of the present study to develop sustained-release matrix tablets by means of injection molding of ethylcellulose (EC) and polyethylene oxide (PEO) mixtures and to evaluate the influence of process temperature, matrix composition, and viscosity grade of EC and PEO on processability and drug release.

METHODS

Formulations consisting of metoprolol tartrate (MPT, concentration: 30%), EC plasticized by dibutyl sebacate, and PEO were extruded and consequently injection molded into tablets. The influence of process temperature (120°C and 140°C), matrix composition, viscosity grade of EC (4, 10, 20, 45, and 100 mPa·s) and PEO (7 × 10(6), 1 × 10(6), and 1 × 10(5) Mw) on processability and drug release was determined.

RESULTS

Formulations consisting of 70% EC and 30% MPT showed incomplete drug release, whereas drug release was too fast for formulations without EC. Higher PEO concentrations increased drug release. Formulations containing 30% metoprolol, EC, and different concentrations of PEO showed first-order release rates with limited burst release. Drug release from direct compressed tablets showed faster drug release rates compared to injection-molded formulations. There was no clear relationship between the molecular weight of EC and drug release. The melting endotherm (113.9°C) of MPT observed in the differential scanning calorimeter thermogram of the tablets indicated that a solid dispersion was formed which was confirmed by X-ray diffractogram. X-ray tomography demonstrated a difference in pore structure between tablets processed at 120°C and 140°C.

CONCLUSION

It was concluded that injection molding can be applied successfully to develop sustained-release PEO/EC matrix tablets.

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Publisher Full Text

Authors+Show Affiliations

Quinten T
Laboratory of Pharmaceutical Technology, Ghent University, Ghent, Belgium.
De Beer T
No affiliation info available
Almeida A
No affiliation info available
Vlassenbroeck J
No affiliation info available
Van Hoorebeke L
No affiliation info available
Remon JP
No affiliation info available
Vervaet C
No affiliation info available

MeSH

Calorimetry, Differential ScanningCelluloseDelayed-Action PreparationsDicarboxylic AcidsExcipientsMetoprololPolyethylene GlycolsTabletsTemperatureTime FactorsTomography, X-Ray ComputedTransition TemperatureViscosityX-Ray Diffraction

Pub Type(s)

Journal Article

Language

eng

PubMed ID

20615154

Citation

Quinten, T, et al. "Development and Evaluation of Injection-molded Sustained-release Tablets Containing Ethylcellulose and Polyethylene Oxide." Drug Development and Industrial Pharmacy, vol. 37, no. 2, 2011, pp. 149-59.
Quinten T, De Beer T, Almeida A, et al. Development and evaluation of injection-molded sustained-release tablets containing ethylcellulose and polyethylene oxide. Drug Dev Ind Pharm. 2011;37(2):149-59.
Quinten, T., De Beer, T., Almeida, A., Vlassenbroeck, J., Van Hoorebeke, L., Remon, J. P., & Vervaet, C. (2011). Development and evaluation of injection-molded sustained-release tablets containing ethylcellulose and polyethylene oxide. Drug Development and Industrial Pharmacy, 37(2), 149-59. https://doi.org/10.3109/03639045.2010.498426
Quinten T, et al. Development and Evaluation of Injection-molded Sustained-release Tablets Containing Ethylcellulose and Polyethylene Oxide. Drug Dev Ind Pharm. 2011;37(2):149-59. PubMed PMID: 20615154.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development and evaluation of injection-molded sustained-release tablets containing ethylcellulose and polyethylene oxide. AU - Quinten,T, AU - De Beer,T, AU - Almeida,A, AU - Vlassenbroeck,J, AU - Van Hoorebeke,L, AU - Remon,J P, AU - Vervaet,C, Y1 - 2010/07/08/ PY - 2010/7/10/entrez PY - 2010/7/10/pubmed PY - 2011/4/14/medline SP - 149 EP - 59 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 37 IS - 2 N2 - PURPOSE: It was the aim of the present study to develop sustained-release matrix tablets by means of injection molding of ethylcellulose (EC) and polyethylene oxide (PEO) mixtures and to evaluate the influence of process temperature, matrix composition, and viscosity grade of EC and PEO on processability and drug release. METHODS: Formulations consisting of metoprolol tartrate (MPT, concentration: 30%), EC plasticized by dibutyl sebacate, and PEO were extruded and consequently injection molded into tablets. The influence of process temperature (120°C and 140°C), matrix composition, viscosity grade of EC (4, 10, 20, 45, and 100 mPa·s) and PEO (7 × 10(6), 1 × 10(6), and 1 × 10(5) Mw) on processability and drug release was determined. RESULTS: Formulations consisting of 70% EC and 30% MPT showed incomplete drug release, whereas drug release was too fast for formulations without EC. Higher PEO concentrations increased drug release. Formulations containing 30% metoprolol, EC, and different concentrations of PEO showed first-order release rates with limited burst release. Drug release from direct compressed tablets showed faster drug release rates compared to injection-molded formulations. There was no clear relationship between the molecular weight of EC and drug release. The melting endotherm (113.9°C) of MPT observed in the differential scanning calorimeter thermogram of the tablets indicated that a solid dispersion was formed which was confirmed by X-ray diffractogram. X-ray tomography demonstrated a difference in pore structure between tablets processed at 120°C and 140°C. CONCLUSION: It was concluded that injection molding can be applied successfully to develop sustained-release PEO/EC matrix tablets. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/20615154/Development_and_evaluation_of_injection_molded_sustained_release_tablets_containing_ethylcellulose_and_polyethylene_oxide_ L2 - https://www.tandfonline.com/doi/full/10.3109/03639045.2010.498426 DB - PRIME DP - Unbound Medicine ER -