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

Bart.hens@kuleuven.be

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!