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Absorbtion of Bioactive Compounds

Absorbtion of Bioactive Compounds. Absorbtion from GI tract. 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.

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Absorbtion of Bioactive Compounds

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  1. Absorbtion of Bioactive Compounds Absorbtion from GI tract

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

  5. 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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