Advanced search
1 file | 8.54 MB Add to list

Prilling of API/fatty acid suspensions : screening of additives for drug release modification

Elien De Coninck (UGent) , Valérie Vanhoorne (UGent) , Matthieu Boone (UGent) , G Van Assche, Bruno De Geest (UGent) , Thomas De Beer (UGent) and Chris Vervaet (UGent)
Author
Organization
Abstract
Current study screened additives which could modify the drug release from prills made of an active pharmaceutical ingredient/fatty acid (API/FA) suspension, without negatively influencing the processability and/or stability of the formulation. Therefore, 11 additives (i.e. emulsifiers, pore-formers and FA-based lubricants) were added in a 20% concentration to a paracetamol/behenic acid formulation. Two additives, Kolliphor (R) P338 and P407 provided complete drug release in less than 1 h, as their thermoreversible gel formation resulted in a disintegration of the prills. Lower Kolliphor (R) P338 or P407 concentrations (2.5-10%) resulted in a complete but slower drug release in 24 h as the prills no longer disintegrated and the release mechanism was dominated by pore-formation. Prills with a robust drug release profile (i.e. independent of pH and surfactant concentration of the dissolution medium) were obtained after the addition of >= 5% Kolliphor (R) P338 or P407 to the FA-based formulation. Based on a 6-month stability study, it was concluded that Kolliphor (R) P407 was a suitable additive to modify the drug release profile of API/FA suspension-based prills when formulations were stored below 25 degrees C at low relative humidity.
Keywords
Prilling, Controlled release, Multiparticulate dosage forms, Fatty acids, Paracetamol, Poloxamers, FATTY-ACIDS, POLOXAMERS, DISINTEGRATION, ACETAMINOPHEN, MICROSPHERES, PREDICTION, STABILITY, RHEOLOGY, POLYMER, AGENTS

Downloads

  • (...).pdf
    • full text
    • |
    • UGent only
    • |
    • PDF
    • |
    • 8.54 MB

Citation

Please use this url to cite or link to this publication:

MLA
De Coninck, Elien, et al. “Prilling of API/Fatty Acid Suspensions : Screening of Additives for Drug Release Modification.” INTERNATIONAL JOURNAL OF PHARMACEUTICS, vol. 576, 2020.
APA
De Coninck, E., Vanhoorne, V., Boone, M., Van Assche, G., De Geest, B., De Beer, T., & Vervaet, C. (2020). Prilling of API/fatty acid suspensions : screening of additives for drug release modification. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 576.
Chicago author-date
De Coninck, Elien, Valérie Vanhoorne, Matthieu Boone, G Van Assche, Bruno De Geest, Thomas De Beer, and Chris Vervaet. 2020. “Prilling of API/Fatty Acid Suspensions : Screening of Additives for Drug Release Modification.” INTERNATIONAL JOURNAL OF PHARMACEUTICS 576.
Chicago author-date (all authors)
De Coninck, Elien, Valérie Vanhoorne, Matthieu Boone, G Van Assche, Bruno De Geest, Thomas De Beer, and Chris Vervaet. 2020. “Prilling of API/Fatty Acid Suspensions : Screening of Additives for Drug Release Modification.” INTERNATIONAL JOURNAL OF PHARMACEUTICS 576.
Vancouver
1.
De Coninck E, Vanhoorne V, Boone M, Van Assche G, De Geest B, De Beer T, et al. Prilling of API/fatty acid suspensions : screening of additives for drug release modification. INTERNATIONAL JOURNAL OF PHARMACEUTICS. 2020;576.
IEEE
[1]
E. De Coninck et al., “Prilling of API/fatty acid suspensions : screening of additives for drug release modification,” INTERNATIONAL JOURNAL OF PHARMACEUTICS, vol. 576, 2020.
@article{8654810,
  abstract     = {Current study screened additives which could modify the drug release from prills made of an active pharmaceutical ingredient/fatty acid (API/FA) suspension, without negatively influencing the processability and/or stability of the formulation. Therefore, 11 additives (i.e. emulsifiers, pore-formers and FA-based lubricants) were added in a 20% concentration to a paracetamol/behenic acid formulation. Two additives, Kolliphor (R) P338 and P407 provided complete drug release in less than 1 h, as their thermoreversible gel formation resulted in a disintegration of the prills. Lower Kolliphor (R) P338 or P407 concentrations (2.5-10%) resulted in a complete but slower drug release in 24 h as the prills no longer disintegrated and the release mechanism was dominated by pore-formation. Prills with a robust drug release profile (i.e. independent of pH and surfactant concentration of the dissolution medium) were obtained after the addition of >= 5% Kolliphor (R) P338 or P407 to the FA-based formulation. Based on a 6-month stability study, it was concluded that Kolliphor (R) P407 was a suitable additive to modify the drug release profile of API/FA suspension-based prills when formulations were stored below 25 degrees C at low relative humidity.},
  articleno    = {119022},
  author       = {De Coninck, Elien and Vanhoorne, Valérie and Boone, Matthieu and Van Assche, G and De Geest, Bruno and De Beer, Thomas and Vervaet, Chris},
  issn         = {0378-5173},
  journal      = {INTERNATIONAL JOURNAL OF PHARMACEUTICS},
  keywords     = {Prilling,Controlled release,Multiparticulate dosage forms,Fatty acids,Paracetamol,Poloxamers,FATTY-ACIDS,POLOXAMERS,DISINTEGRATION,ACETAMINOPHEN,MICROSPHERES,PREDICTION,STABILITY,RHEOLOGY,POLYMER,AGENTS},
  language     = {eng},
  pages        = {12},
  title        = {Prilling of API/fatty acid suspensions : screening of additives for drug release modification},
  url          = {http://dx.doi.org/10.1016/j.ijpharm.2020.119022},
  volume       = {576},
  year         = {2020},
}

Altmetric
View in Altmetric
Web of Science
Times cited: