IMI Scientific Symposium Brussels, Belgium · IMI Scientific Symposium–Brussels, Belgium: Bart...

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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 [email protected]

Transcript of IMI Scientific Symposium Brussels, Belgium · IMI Scientific Symposium–Brussels, Belgium: Bart...

Page 1: IMI Scientific Symposium Brussels, Belgium · IMI Scientific Symposium–Brussels, Belgium: Bart HENS Bart.hens@kuleuven.be. Clinical Aspiration Studies 1 Intubation 2 Positioning

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

[email protected]

Page 2: IMI Scientific Symposium Brussels, Belgium · IMI Scientific Symposium–Brussels, Belgium: Bart HENS Bart.hens@kuleuven.be. Clinical Aspiration Studies 1 Intubation 2 Positioning

Clinical Aspiration Studies

1 Intubation 2 Positioning 3 Aspiration

Antral aspirates

Duodenal aspirates

Intragastric administration

solution

Page 3: IMI Scientific Symposium Brussels, Belgium · IMI Scientific Symposium–Brussels, Belgium: Bart HENS Bart.hens@kuleuven.be. Clinical Aspiration Studies 1 Intubation 2 Positioning

0 50 100 150 2000

2

4

6

8

Time (min)

pH

0 50 100 150 2000

20

40

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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

Page 4: IMI Scientific Symposium Brussels, Belgium · IMI Scientific Symposium–Brussels, Belgium: Bart HENS Bart.hens@kuleuven.be. Clinical Aspiration Studies 1 Intubation 2 Positioning

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

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8

Time (min)

pH

Solid dispersion manufactured by hot-melt extrusion in combination with HPMC-AS

Page 5: IMI Scientific Symposium Brussels, Belgium · IMI Scientific Symposium–Brussels, Belgium: Bart HENS Bart.hens@kuleuven.be. Clinical Aspiration Studies 1 Intubation 2 Positioning

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!