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BioavailabilityDistribution Absorption and Transport.

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Presentation on theme: "BioavailabilityDistribution Absorption and Transport."— Presentation transcript:

1 BioavailabilityDistribution Absorption and Transport

2 Volume of Distribution The volume of distribution is given by the following equation: Therefore the dose required to give a certain plasma concentration can be determined if the V D for that drug is known. The V D is not a physiologic value; it is more a reflection of how a drug will distribute throughout the body depending on several physicochemical properties, e.g. solubility, charge, size, etc. V D is often calculated per weight of body – it is not volume any more!

3 MedicationV d / kg body weight heparin0.05-0.1 insulin0.05-0.1 warfarin0.1-0.2 sulfamethoxazole0.1-0.2 glibenclamide0.1-0.2 atenolol0.1-0.2 NXY-0590.1-0.2 tubocurarine0.2-0.4 theophylline0.4-0.7 ethanol0.7-0.9 neostigmine0.7-0.9 phenytoin0.7-0.9 methotrexate1-2 indometacin1-2 paracetamol1-2 diazepam1-2 lidocaine1-2 glyceryl nitrate2-5 morphine2-5 propranolol2-5 digoxin2-5 chlorpromazine2-5 nortriptyline2-5 chloroquine200

4 V D Proportion of Drug in body water 0.140% 0.1527% 1 4% 10 0.4%

5 Two compartment model Blood Tissue

6 Mode of entry of drugs/toxins Skin transport Respiratory route Oral route

7 Organ pH Surface Area Time Stomach1-3up to 5 m 2 0.5-20 h Small Intestine5-7200 m 2 2 h Colon7-8up to 52 h – 1 week logC Time

8 DrugBioavailability VD (L/kg weight) Diazepam1000.5-2 Morphine15-603-5 Pentobarbital950.7-10 Tetrahydrocannabinol 69-11 V D Proportion of Drug in body water 0.140% 0.1527% 1 4% 10 0.4%

9 Surface Area Diffusion Coefficient Solubility Concentration in bulk Diffusion Layer thickness Solid

10 BiLayer Membrane pH 1 pH 2 Passive Transport Hydrophobic area Aqeous area


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