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M. Sc. Dominik Borrmann

M. Sc. Dominik Borrmann Foto von M. Sc. Dominik Borrmann

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+49(231)755-3695

Adresse

Fakultät Bio- und Chemieingenieurwesen
Emil-Figge-Str. 70
44227 Dortmund

Raum G2-109a

Crystallization and Dissolution of Pharmaceutical Formulations

Abstract:

The bioavailability of an active pharmaceutical ingredient (API) with low water solubility is enhanced by dissolution in a polymer matrix, generating a so-called amorphous solid dispersion (ASD). This promising type of formulation might destabilize when being exposed to water[1]. This project focusses on the investigation and prediction of the phenomena which occur when an ASD is submerged in an aqueous solution.

 

Description:

ASDs are glassy pharmaceutical formulations where the amorphous API is dissolved in a polymer. An amorphous API has an advantageous dissolution rate and higher solubility compared to the crystalline API[2]. Already when exposing an ASD to ambient humidities, API crystallization[3] or amorphous demixing[4] may occur due to the absorption of water from the air. Undesired phase changes impact significantly the API release and bioavailability. Fundamental knowledge of the occurring diffusion, crystallization and dissolution phenomena will lead to ASD formulations with better understood dissolution performance.

 

Bibliography:

[1] G. Van den Mooter:
"The use of amorphous solid dispersions: A formulation strategy to overcome poor solubility and dissolution rate"
Drug Discov. Today Technol., vol. 9, pp. e79–e85, Jun. 2012.
[2] D. E. Alonzo, G. G. Z. Zhang, D. Zhou, Y. Gao, and L. S. Taylor:
"Understanding the Behavior of Amorphous Pharmaceutical Systems during Dissolution"
Pharm. Res., vol. 27, pp. 608–618, Apr. 2010.
[3] A. Prudic, Y. Ji, C. Luebbert, and G. Sadowski:
"Influence of humidity on the phase behavior of API/polymer formulations"
Eur. J. Pharm. Biopharm., vol. 94, pp. 352–362, Aug. 2015.
[4] C. Luebbert, F. Huxoll, and G. Sadowski:
"Amorphous-Amorphous Phase Separation in API/Polymer Formulations"
Molecules, vol. 22, pp. 1–17, Feb. 2017.