dissolution

Asma Radwan's picture

Mechanistic Understanding of Food Effects: Water diffusivity in GI is an Important Parameter For Prediction of Disintegration of Solid Oral Dosage Forms

Journal Title, Volume, Page: 
Mol. Pharmaceutics, 2013, 10 (6), pp 2283–2290 DOI: 10.1021/mp3006209 Publication Date (Web): April 19, 2013
Year of Publication: 
2013
Authors: 
Asma Radwan
Institute of Pharmacy and Biochemistry, Johannes Gutenberg University, Mainz, Germany
Current Affiliation: 
Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine
Sandro Ebert
Max Planck Institute for Polymer Research, Mainz, Germany
Andrea Amar
Max Planck Institute for Polymer Research, Mainz, Germany
Kerstin Münnemann
Manfred Wagner
Gordon L Amidon
College of Pharmacy, The University of Michigan, 428 Church Street, Ann Arbor, Michigan 48109-1065, United States
Peter Langguth
Institute of Pharmacy and Biochemistry, Johannes Gutenberg University, Mainz, Germany
Preferred Abstract (Original): 

Much interest has been expressed in this work on the role of water diffusivity in the release media as a new parameter for predicting drug release. NMR was used to measure water diffusivity in different media varying in their osmolality and viscosity. Water self-diffusion coefficients in sucrose, sodium chloride, and polymeric hydroxypropyl methylcellulose (HPMC) solutions were correlated with water uptake, disintegration, and drug release rates from trospium chloride immediate release tablets. The water diffusivity in sucrose solutions was significantly reduced compared to polymeric HPMC and molecular sodium chloride solutions. Water diffusivity was found to be a function of sucrose concentration in the media. Dosage form disintegration and drug release was to be affected by water diffusivity in these systems. This observation can be explained by hydrogen bonding formation between sugar molecules, an effect which was not expressed in sodium chloride solutions of equal osmolality. Water diffusivity and not media osmolality in general need to be considered to predict the effect of disintegration and dissolution media on drug release. Understanding the relevance of water diffusivity for disintegration and dissolution will lead to better parametrization of dosage form behavior in gastrointestinal (GI) aqueous and semisolid media.

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