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Absorbtion of Bioactive Compounds

Explore the absorption mechanisms of bioactive compounds from the gastrointestinal tract, including passive diffusion and active transport. Learn about factors influencing drug absorption such as lipophilicity and molecule size, and delve into pharmacokinetics to understand drug distribution in the body and optimal dosage regimes.

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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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