Biopharmaceutics Lecture 1
Biopharmaceutics Lecture 1
1 By: Merga D.
Outline
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Introduction
Barriers of drug
transport
Mechanisms of drug
transport
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Learning outcomes
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Introductory activity
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What is Pharmaceutics?
discipline of pharmacy that deals with all
aspects of the process of turning a new
chemical entity into a medication able to be
safely and effectively used by patients
put at its most simplistic, it converts a
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Introduction…
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Biopharmaceutics
a branch of pharmaceutical sciences that concerns the
interrelationship b/n
the physicochemical properties of a drug
the dosage form in which the drug is given
the route of administration
on the rate and extent of systemic drug absorption
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Introduction…
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enteral
Other route (transdermal, inhalation, intranasal
Ophthalmic)
for systemic absorption
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In intravenous route,
a drug is introduced directly into the bloodstream
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Clinical
IV effect
E
injection Drug at site (s) L Unchanged
of action I drug
A M excreted
B I
DISTRIBUTIO
S N N
O A
Drug at site R
Bound unbound T
of P
administration drug drug I
T O metabolis
(extravascular)
I N m
O DISTRIBUTIO
N N Metabolites
excreted
Fig.: Drug ADME Drug in tissues (including
blood cells) & other fluid of
By: Sintayehu distribution
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A 6/29/2021
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of response
it is desired to obtain these concentrations rapidly
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body
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factors
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Barriers to Drug Transport
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Barriers to Drug Transport…
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Barriers to Drug Transport…
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Barriers to Drug Transport…
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Epithelia
Epithelia are a collection of cells
Epithelia…
There are several morphologically distinct
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Barriers to Drug Transport…
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secretion
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Barriers to Drug Transport…
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Transitional epithelium
This is composed of several layers of cells of
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Barriers to Drug Transport…
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layers
Site
vagina
Function
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Barriers to Drug Transport…
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epithelia
Overcoming these barriers to absorption is
one of the most important considerations in
the DD process
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Mechanisms of drug transport
31 By: Merga D.
Mechanisms…
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Mechanisms…
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Trans-cellular pathways
Passive diffusion:
transport for relatively small lipophilic molecules
many drugs transported via this route
drug molecules pass across cell membrane via a region
of high concentration to a region of lower concentration
i.e. from lumen to blood
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Trans-cellular pathways…
Carrier-mediated transport:
The drug require carrier or transporter to
cross membrane
carrier-mediated transport
Two main types carrier-mediated transport
Active transport and
Facilitated diffusion
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Trans-cellular pathways…
Active transport: materials transported
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Trans-cellular pathways…
Facilitated diffusion:
Drugs are transported down the concentration gradient
does not require an energy
butdoes require a concentration
gradient
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Trans-cellular pathways…
Endocytosis:
Endocytosis is the process by which the plasma
membrane of the cell invaginates and the
invaginations become pinched off, forming small
intracellular membrane-bound vesicles that enclose
a volume of material
Thus material can be transported into the cell
primary mechanism of transport of macromolecules
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Trans-cellular pathways…
Endocytosis can be further subdivided into four main
processes:
pinocytosis
receptor-mediated endocytosis
phagocytosis
transcytosis
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Trans-cellular pathways…
Pinocytosis:
the engulfment of small droplets of extracellular fluid
by membrane vesicles
The cell will internalize material regardless of its
metabolic importance to that cell
The fat-soluble vitamins A, D, E and K are absorbed via
pinocytosis
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Trans-cellular pathways…
Receptor-mediated endocytosis
Many cells within the body have receptors on
Trans-cellular pathways…
Phagocytosis
can be defined as the engulfment by the cell membrane
of particles larger than 500 nm.
This process is important for the absorption of polio
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Trans-cellular pathways…
Transcytosis
the process by which the material internalized by the
membrane domain is transported through the
cell and secreted on the opposite side
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Para-cellular pathway
transport of materials in the aqueous pores b/n the cells
transport ions such as calcium and for the transport of
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