Dissolution media simulating conditions in the proximal human gastrointestinal tract: an update.
OBJECTIVE
The aim of this study was to update the compositions of biorelevant media to represent the composition and physical chemical characteristics of the gastrointestinal fluids as closely as possible while providing physical stability during dissolution runs and short-term storage.


METHODS
Media were designed to reflect postprandial conditions in the stomach and proximal small intestine in the "early", "middle", and "late" phases of digestion. From these "snapshot" media, general media for simulating postprandial conditions were devised. Additionally, media reflecting preprandial conditions in the stomach and small intestine were revisited.


RESULTS
A set of four media is presented. A recently published medium to represent the fasted stomach, FaSSGF, needed no further revision. To simulate the postprandial stomach, a new medium, FeSSGF, is presented. Media representing the upper small intestine in the fed and fasted states were fine-tuned according to physicochemical and biochemical characteristics in vivo. All four media proved to be stable under ambient storage conditions for at least 72 h as well as under usual dissolution test conditions.


CONCLUSIONS
The updated dissolution media can be used to predict formulation performance and food effects in vivo. These media are more physiologically relevant and show better physical stability than their corresponding predecessors.
Jantratid
Ekarat
E
Institute of Pharmaceutical Technology, Johann Wolfgang Goethe University, Frankfurt am Main, Germany.
Janssen
Niels
N
Reppas
Christos
C
Dressman
Jennifer B
JB
D000465:Algorithms; D001646:Bile / Q000378:metabolism; D001826:Body Fluids / Q000502:physiology; D002021:Buffers; D055598:Chemical Phenomena; D002626:Chemistry, Pharmaceutical; D002627:Chemistry, Physical; D003470:Culture Media; D004356:Drug Storage; D004798:Enzymes / Q000737:chemistry; D005079:Excipients; D005215:Fasting / Q000502:physiology; D005745:Gastric Acidity Determination; D005753:Gastric Mucosa / Q000378:metabolism*; D006801:Humans; D007421:Intestine, Small / Q000378:metabolism*; D008055:Lipids / Q000737:chemistry; D009994:Osmolar Concentration; D004364:Pharmaceutical Preparations / Q000378:metabolism; D019518:Postprandial Period / Q000502:physiology; D012997:Solvents; D013500:Surface Tension
D002021:Buffers; D003470:Culture Media; D004798:Enzymes; D005079:Excipients; D008055:Lipids; D004364:Pharmaceutical Preparations; D012997:Solvents