Physicochemical Properties of Poly-Vinyl Polymers and Their Influence on Ketoprofen Amorphous Solid Dispersion Performance: A Polymer Selection Case Study
Autor: | Zelalem Ayenew Worku, Anne Marie Healy, Emer Browne |
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Jazyk: | angličtina |
Rok vydání: | 2020 |
Předmět: |
chemistry.chemical_classification
Active ingredient Materials science ketoprofen relative humidity induced glass transition supersaturation Pharmaceutical Science lcsh:RS1-441 Polymer Vinyl polymer Article Amorphous solid lcsh:Pharmacy and materia medica chemistry.chemical_compound chemistry Chemical engineering amorphous solid dispersion polymer selection Vinyl acetate Solubility ketoprofen relative humidity induced glass transition supersaturation Glass transition Dissolution |
Zdroj: | Pharmaceutics Volume 12 Issue 5 Pharmaceutics, Vol 12, Iss 433, p 433 (2020) |
ISSN: | 1999-4923 |
DOI: | 10.3390/pharmaceutics12050433 |
Popis: | 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 &ldquo trial and error&rdquo 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. |
Databáze: | OpenAIRE |
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