Mechanism for Enhanced Absorption of a Solid Dispersion Formulation of LY2300559 Using the Artificial Stomach Duodenum Model

• Published in: Molecular pharmaceutics Vol. 12; no. 4; pp. 1131 - 1140
• Main Authors: Polster, Christopher S, Wu, Sy-Juen, Gueorguieva, Ivelina, Sperry, David C
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 06.04.2015
• Subjects: Acetophenones - chemistry; Acetophenones - pharmacokinetics; Animals; Area Under Curve; Benzoates - chemistry; Benzoates - pharmacokinetics; Biological Availability; Chemistry, Pharmaceutical - methods; Crystallization; Dogs; Drug Design; Duodenum - drug effects; Humans; Hydrogen-Ion Concentration; Intestinal Absorption - drug effects; Madin Darby Canine Kidney Cells; Meglumine - chemistry; Models, Biological; Molecular Structure; Sodium Bicarbonate - chemistry; Solubility; Stomach - drug effects; Tissue Distribution; meglumine; high-shear wet granulation; artificial stomach duodenum; ASD; high-energy solid; amorphous; solid dispersion; bioavailability; pharmacokinetics; supersaturation

An artificial stomach duodenum (ASD) model has been used to demonstrate the performance difference between two formulations of LY2300559, a low-solubility acidic developmental drug. The two formulations investigated were a conventional high-shear wet granulation (HSWG) formulation and a solid disper...