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Absorbtion of Bioactive Compounds

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Presentation on theme: "Absorbtion of Bioactive Compounds"— Presentation transcript:

1 Absorbtion of Bioactive Compounds
Absorbtion from GI tract

2 Certain ionic compounds may go thru as ion-pair
Crossing the membrane Passive transport / diffusion Rate  Conc. absortion site (1. order kinetics) % Drug absorbed  lipophilicity Size of molecule Certain ionic compounds may go thru as ion-pair

3 Active transport / Carrier mediated transport
Less common Structural recemblanse with for instance nutritional compound Transport against conc. gradient Mechanism saturated at high conc. Competition for carrier molecules, compounds with structural resemblance

4 logP - P: Partition coefficient between n-octanol and water
Most drugs: Passive diffusion Low lipophilicity unionized form - low absorbtion logP - P: Partition coefficient between n-octanol and water

5 Bad kinetics -- Need for improved structure
Pharmacokinetics Mathematic descript. of A) Biolog. processes affecting drugs B) Biolog. processes affected by drugs drugs Mathematical expressions to describe temporal changes in drug conc. Determine constrains related to ADME processes Optimal dossage regime (how much drug, how often etc.) Bad kinetics Need for improved structure

6 The terapeutic window Min. tox. conc (MTC) Min. effective conc (MEC)
Therapeutic index = TD50 : ED50 Window size - Disease severity

7 Compartment models Two compartment model One compartment modell
The whole body = central compartment Drug rapidly distributed thru out the body Central compartment (plasma etc) Peripher compartment (certain tissue, organs etc)


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