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TRANSCRIPT
Author
Supersaturation as driving force for intestinal absorption resulting in an increased oral bioavailability: case example with
posaconazole
IMI Scientific Symposium– Brussels, Belgium
: Bart HENS
Clinical Aspiration Studies
1 Intubation 2 Positioning 3 Aspiration
Antral aspirates
Duodenal aspirates
Intragastric administration
solution
0 50 100 150 2000
2
4
6
8
Time (min)
pH
0 50 100 150 2000
20
40
60
80
100
Dissolved
Total
Time (min)
Po
saco
nazo
le (
µM
)
Intragastric administration of posaconazole solution
Stomach Duodenum
0 50 100 150 2000
20
40
60
80
100 Total
Dissolved
Time (min)
Po
saco
nazo
le (
µM
)
0 50 100 150 2000
2
4
6
8
Time (min)
pH
Dissolved versus solubility
0 100 200 3000
10
20
30
Dissolved
Solubility
Time (min)
Po
sa
co
na
zo
le (
µM
)
0 100 200 3000
2
4
6
8
Time (min)
pH
Solid dispersion manufactured by hot-melt extrusion in combination with HPMC-AS
Conclusion
• This technique allowed us to study the behavior of a drug in the gastrointestinal tract of humans
• We helped a pharmaceutical company in developing a new drug formulation with a better systemic exposure and, consequently, this helps patients!