SUDHAKAR LAKAVATH

PG. SECOND YEAR

Drugs has to cross membranes for absorption,
distribution, metabolism & excretion.
This is achieved by translocation of drug from one
side of the biological barrier to the other
(biotranport).
How drugs are biotransported across membranes
& how their physico-chemical properties influence
their biotransportation.
Major transport mechanisnms
Passive diffusion- Nonionised/lipid soluble/weak
acid or base
Carrier mediated transport
 Facilitated diffusion- amino acids, antimetaboloites,
antiviral, B12, thiamine, riboflavin etc
 Active transport- 5FU by GI, Glycosides by liver,
Sympathomimmetic amines by neural tissues
Pinocytosis-Liposomes, Insulin crosses BBB, antigens
Filteration- GF of urea, alc, sugar, Proteins through cap
Absorption Via GIT
Mouth-(Alkaline), lipophilic, basic drugs are absorbed
better. Abs is faster due to thin mucosa, high vascularity
but surface area is limited.
Stomach- (pH 1-4), lipophilic, acidic & neutral drugs
are better absd
Intestine- (pH 6-8), lipophilic, basic & neutral drugs
are better absd. Even lipophilic acidic drugs are absd due
to large surface area. Major site of drug absorption
Colon & rectum- (pH 6-8), lipophilic, basic & neutral
drugs are better absd but to a lesser extent compared to
intestine.
Methods of delaying absorption`
 Using an appropriate dosage form

 Changing the physical characteristics of the drug

 Adding a vasoconstrictor drug or applying a

tourniquet
Factors affecting drug absorption
Aqueous solubility
Concentration
Area of absorbing surface
Vascularity of the absorbing surface
Route of administration