Next Article in Journal
Erythrocytes as Carriers of Therapeutic Enzymes
Next Article in Special Issue
Influence of the Polymer Glass Transition Temperature and Molecular Weight on Drug Amorphization Kinetics Using Ball Milling
Previous Article in Journal
Mesoporous Silica Nanoparticles as Carriers for Therapeutic Biomolecules
Previous Article in Special Issue
Importance of Mesoporous Silica Particle Size in the Stabilization of Amorphous Pharmaceuticals—The Case of Simvastatin
Open AccessArticle

Physicochemical Properties of Poly-vinyl Polymers and Their Influence on Ketoprofen Amorphous Solid Dispersion Performance: A Polymer Selection Case Study

SSPC The SFI Research Centre for Pharmaceuticals, School of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin, Dublin 2, Ireland
*
Author to whom correspondence should be addressed.
Pharmaceutics 2020, 12(5), 433; https://doi.org/10.3390/pharmaceutics12050433
Received: 13 April 2020 / Revised: 2 May 2020 / Accepted: 6 May 2020 / Published: 8 May 2020
(This article belongs to the Special Issue Advances in Amorphous Drug Formulations)
When developing an amorphous solid dispersion (ASD), a prudent choice of polymer is critical to several aspects of ASD performance including: processability, solid state stability and dissolution rate. However, there is little guidance available to formulators to aid judicious polymer selection and a “trial and error” approach is often taken. This study aims to facilitate rational polymer selection and formulation design by generating ASDs using a range of poly-vinyl polymers and ketoprofen as a model active pharmaceutical ingredient (API) and evaluating several aspects of their performance. The molecular weight of the polymer and the ratio of vinyl pyrrolidone to vinyl acetate in the polymer were found to influence the relative humidity at which the relative humidity induced glass transition occurred, as well as the extent of ketoprofen supersaturation achieved during dynamic solubility testing. Interestingly, ASD tablets containing polymers with the vinyl pyrrolidone functional group exhibited higher tensile strengths than those without. This points towards the binder functionality of vinyl pyrrolidone. In conclusion, the physicochemical properties of poly-vinyl polymers greatly influence ketoprofen ASD performance and due regard should be paid to these properties in order to develop an ASD with the desired attributes. View Full-Text
Keywords: amorphous solid dispersion; polymer selection; ketoprofen; relative humidity induced glass transition; supersaturation amorphous solid dispersion; polymer selection; ketoprofen; relative humidity induced glass transition; supersaturation
Show Figures

Graphical abstract

MDPI and ACS Style

Browne, E.; Worku, Z.A.; Healy, A.M. Physicochemical Properties of Poly-vinyl Polymers and Their Influence on Ketoprofen Amorphous Solid Dispersion Performance: A Polymer Selection Case Study. Pharmaceutics 2020, 12, 433.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Search more from Scilit
 
Search
Back to TopTop