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  • Physical/Chemical Properties of Drugs: Ability To Approach Receptors

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    rahmianggriawan
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    This document discusses the physical and chemical properties that determine a drug's ability to cross cell membranes and reach receptor sites. Small molecule drugs can cross cell membranes through diffusion, which is dependent on a drug's permeability coefficient and partition coefficient. The partition coefficient, which indicates a drug's solubility in oil versus water, is the most important factor for pharmacokinetics and predicting a drug's properties. An example shows how the ionization state of a weak acid drug affects its diffusion from the stomach to the blood and back.

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    Biofar, absorpsi obat

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    ABS OBAT OK

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    This document discusses the physical and chemical properties that determine a drug's ability to cross cell membranes and reach receptor sites. Small molecule drugs can cross cell membranes through diffusion, which is dependent on a drug's permeability coefficient and partition coefficient. The partition coefficient, which indicates a drug's solubility in oil versus water, is the most important factor for pharmacokinetics and predicting a drug's properties. An example shows how the ionization state of a weak acid drug affects its diffusion from the stomach to the blood and back.

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    © All Rights Reserved
    Download as PPT, PDF, TXT or read online from Scribd
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    14 views9 pages

    Physical/Chemical Properties of Drugs: Ability To Approach Receptors

    Uploaded by

    rahmianggriawan
    This document discusses the physical and chemical properties that determine a drug's ability to cross cell membranes and reach receptor sites. Small molecule drugs can cross cell membranes through diffusion, which is dependent on a drug's permeability coefficient and partition coefficient. The partition coefficient, which indicates a drug's solubility in oil versus water, is the most important factor for pharmacokinetics and predicting a drug's properties. An example shows how the ionization state of a weak acid drug affects its diffusion from the stomach to the blood and back.

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    of 9

    Physical/Chemical Properties

    of Drugs
    Ability to Approach Receptors
    Small Mols Cross Cell Membrs
    Diffn lipid
    Diffn aqueous
    pores traversing
    lipid bilayer
    BUT most pores
    too small to
    accomm most
    drugs
    Transmembr
    carrier prot
    Pinocytosis
    Not impt for small
    mols
    Diffusion
    Number mols crossing membr per unit
    area in unit time; depends on
    Permeability coefficient (P)
    Diffusivity
    Diffusion coefficient
    Doesnt differ much between drugs
    Solubility in membr
    Partition coefficient (solubility oil/solubility water)
    Most impt to pharmacokinetics
    Used as predictor of drug properties




    secobarbital thiopental barbital
    Ex: Stomach Blood
    Assume weak acid drug (HA) w/ pKa=6.0
    Assume [HA]=1.0
    Stomach pH=1.0
    1.0-6.0=log [A-]/[HA]
    1.0x10
    -5
    =[A-]
    Little ionized drug
    Blood pH=7.0
    10=[A-]
    Much ionized drug
    Expect stomach-to-plasma traverse BUT not
    plasma-to-stomach
    Book ex: more basic drug (how do we know?)
    Plasma Digestive Tract

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