The influence of dissolution conditions on the drug ADME phenomena

作者：Cascone Sara; De Santis Felice; Lamberti Gaetano^*; Titomanlio Giuseppe

来源：European Journal of Pharmaceutics and Biopharmaceutics, 2011, 79(2): 382-391.

DOI：10.1016/j.ejpb.2011.04.003

• Dissolution
• Pharmacokinetic modeling
• Enteric coated
• ADME

In this work, a review of the apparatuses available to mimic what happens to a drug (or to foodstuffs) once ingested is presented. Similarly, a brief review of the models proposed to simulate the fate of a drug administered to a living body is reported. Then, the release kinetics of extended release of diclofenac from a commercial enteric-coated tablet was determined both in a conventional dissolution tester (USP Apparatus 2, Method A) as well as in an apparatus modified to reproduce a given pH evolution, closer to the real one than the one suggested by USP. The two experimental release profiles were reported and discussed; therefore, they were adopted as input functions for a previously proposed pharmacokinetic model. The obtained evolutions with time of plasma concentration were presented and used to assess the effectiveness of the commercial pharmaceutical products. The importance of a correct in vitro simulation for the design of pharmaceutical dosage systems was thus emphasized.

• 出版日期2011-10