Nifedipine Release From Extended-Release Solid Oral Formulations Using In Vitro Dissolution Testing Under Simulated Gastrointestinal Compression

Abstract

Drug release plays a critical role in defining bioavailability for an extended release solid oral drug products and predictive dissolution tests are desired to establish clinically relevant quality standards for batch release. The objective of this study focuses on exploring the possible impacts of 1 gastrointestinal (GI) parameter for 1 drug: simulated GI contractions on nifedipine release (in 2 extended release solid oral formulations). The 60 mg nifedipine osmotic pump product A, and polymer matrix-based products B and C were examined in the study. An in-house dissolution system was used to simulate various levels of GI contractions on tested samples, and to monitor changes of sample mechanical properties during dissolution testing. The results show that the polymer matrix-based formulation failed to provide controlled release when simulated GI contraction was above 100 g of force. The method may be useful for polymer matrix-based products to assess potential formulation-related interactions with the GI tract during in vivo drug dissolution.