Api polymer pharma
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This document summarizes an experiment examining the interaction between active pharmaceutical ingredients (APIs) and binders in tablet formulations using ellipsometry and neutron reflectometry. Ellipsometry was able to categorize sample composites into three groups - no interaction, some interaction, and definite interaction - based on changes in light polarization. Neutron reflectometry provided high definition models of intermixing at the API-binder interface by measuring scattering length density as a function of sample depth. The results from both techniques help understand interfaces between pharmaceutical powders and polymers which influence tabletability.
Api polymer pharma
- 1. Aman Imani Macalester College CHEM 394: Polymer and Macromolecular Chemistry 1
- 2. The players • Active pharmaceutical ingredient/s (API) • Binder (e.g. PVP, starch, cellulose) 2
- 3. The game • Interaction of API and binders – API: acetaminophen (ACM); Sulfamerazine (SMZ) – Binders: Hydroxypropylcellulose (HPC); Polyvinylpyrrolidone (PVP) • Tabletability – Wet granulation • Improved compaction + flow behavior • Overgranulation 3
- 4. Why interfaces b/w powders and polymers? 4
- 5. The referees • Ellipsometry: measures change in polarization of light after reflection and refraction from a film – VASE (variable angle spectroscopic ellipsometer) • Neutron Reflectometry: – Neutrons directed onto sample at low angle – Time-of-flight measured – Reflectivity as a fn. • Intensity of incident beam: intensity of reflected beam 5
- 8. Ellipsometer • Useful for dividing the simulated API composites into 3 categories: – No API-binder interaction (SMZ-PVP) – Some API-binder interaction (SMZ-HPC, ACM-HPC) – Definite API-binder interaction (ACM-PVP) 8
- 10. Neutron Reflectometry • Scattering Length Density (SLD) is a fn. of chemical composition and density • SLD modeled as fn. of depth into sample to provide high definition of the intermixing regions for each category 10
- 13. References • Yeager, John D., Kyle J. Ramos, Changquan C. Sun, Saurabh Singh, Manish Dubey, Jaroslaw Majewski, and Daniel E. Hooks. "Probing Interfaces between Pharmaceutical Crystals and Polymers by Neutron Reflectometry." Molecular Pharmaceutics 9.7 (2012): 1953-961 • "Ellipsometry." Wikipedia. Wikimedia Foundation • James, Michael. "Report on Neutron Reflectometry." (2001) Australian Research Reactor • Berk, N. F., and C. F. Majkrzak. "Analysis of Multibeam Data for Neutron Reflectivity." Langmuir 25.7 (2009): 4145-153 13