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B.P.C Presentation
B.P.C Presentation
Factors Influencing
Absorption
pH Partition Hypothesis
(Drug pka, Lipophilicity, GI pH & Limitations)
• According to Brodie et.al, drug compounds with a molecular weight greater than 100 are
primarily transported across the biomembrane through passive diffusion.
• Drug – weak acid or base degree of ionisation depends on the pH of biological fluid.
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• Click tostatement
The above edit Master title
of the hypothesis wasstyle
based on the assumption that:
i. The GIT is a simple lipoidal barrier to the transport of drugs.
ii. Larger fraction of unionised drugs faster the absorption.
iii. Greater the lipophilicity (Ko/w) of the unionised drug better the absorption.
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Henderson-Hasselbalch
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Determine the amount of drug that exists in unionised form is a function of the
dissociation constant (pKa) of the drug and pH of the drug and pH of the fluid at the
absorption site.
* 100
pH = pKa + log (Ionised drug) %Drug Ionised = 10 (pH-pKa)
(Unionised drug) 1+10 (pH - pKa)
Biological members are usually lipoidal in nature therefore, the lipid solubility of the drug is a
major parameter for its absorption.
Example – Opium alkaloids like morphine, thebaine and codeine (contain two, zero and one
hydroxyl groups, respectively).
• It is reported that the absorption rate decreased by enhancing the polarity of
molecules.
Perfect hydrophilic-lipophilic balance (HLB) should be there in the structure of the drug for
optimum bioavailability
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It is a measure of the degree of distribution of a drug between several organic solvents and
an aqueous solvent.
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Limitations title
of the pH style
– partition
hypothesis
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1.Click
Presence
to editof a virtual
Master titlemembrane
style
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This led to suggestions that a virtual pH, also called the microclimate
pH
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2. Absorption title drugs
of ionised style
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3. Influence of GI surface area
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andtoresidence
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time of style
drug
But both acidic and basic drugs are more rapidly absorbed from the
intestine because of
• Its large surface area
• Resident time of the drug in the intestine
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4. Presence of aqueous
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diffusion style
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Despite its limitations, the pH-partition theory is still useful in the basic
understanding of drug absorption and the movement of drugs between
various body compartments.
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Thank-You
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