Oral Bioavailability

GROUP 3
 GROUP MEMBERS
NAME REG NO
ISHAKA AHMAD 17/X/18552/PS
BAGUMA MICHEAL 17/U/3413/PS
ODOI YONA 17/U/9486/PS
KAWEESA HENRY 17/U/18782/PS
EGARU LAZARUS 17/U/19785/PS
NIWAHA HILDA 17/U/928
OGWAL PETER 17/U/991
TURYAMUSIMA WISE 17/U/1916/PS
MUKIMA NJERI TERESIA(SR)
AIYA CATHERINE LALAM 17/U/42
NABIRYE HUSUNA 17/U/711
KIIZA LORETA MARGARET 17/U/19927/PS
ASHIRAF LUBEGA 16/U/19248/PS
NABULIME ANGELA RINAH 17/U/20165/PS
 Oral Bioavailability the fraction of an orally administered dose of drug that reaches the systemic
circulation unchanged
The rate determining steps in absorption of orally administered drugs are:
1. Rate of dissolution
2. Rate of drug permeation through the bio-membrane.
 Dissolution is the rate determining step for hydrophobic & poorly aqueous soluble drugs.
E.g. Griseofulvin & Spironolactone.
 Permeation is the rate determining step for hydrophilic & highly aqueous soluble drugs.
E.g. Cromolyn sodium OR Neomycin.
spirinolactone Griseofulvin Cromolyn sodium
 The rate and extent of dissolution of the drug is a major factor in controlling the
absorption of that drug.
 The rate of dissolution depends on the surface area of the solid, which is
dependent on both physical nature of the dosage form of the drug and chemical
structure of the drug.
Hydrophilic drugs have a higher rate of dissolution
than the lipophilic drugs eg introduction of hydroxyl
groups into the structure of a lead( minaprine) will
produce analogues with an increased hydrophilic
nature and a lower lipophillicity. It provides a centre
for hydrogen bonding
 Examples of other groups that increase hydrophilicity are amino groups, carboxylic groups and
sulphonic groups
 An optimum or balance of these groups is needed because excess of them may make the drug
too hydrophilic and will make the drug too polar leading to poor permeation across the lipid
membranes
 Eg acyclovir (bioavailability 15-20%)

Acyclovir structure
Lipophilicity

 For a drug to be absorbed it has to be transported across the lipid membranes, it

has to be lipophilic (an optimum is need)
 Eg introduction of methyl groups, fluorine and chlorine increases lipophilicity of
the drugs(decreases hydrophilicity). This increases the partition coefficient of
these drugs
Benzenze and toluene Acetatamide and Propanamide
REFEENCES

 1. Foye’s principles of medicinal chemistry 7th edition 2013

 2. Fundamentals of Medicinal Chemistry by Gareth Thomas 1st edition 2000