Drug Product

and
Delivery System formulation
(General Considerations)
 a.
Design of the
appropriate dosage
form or delivery
system
 General considerations
The design of the appropriate dosage form or delivery system depends on 8
things
 General considerations

1. Physical and chemical

properties of the drug
Definition
- The chemical or physical characteristics
of the drug

Consideration:s
-The physical and chemical
properties of the API, such as
solubility, particle size, etc.
 General considerations
2. Dose of the drug
Definition
- The specified medication taken
at a time

Consideration:s
--Wether a large or small dose is
needed.

–The frequency of the doses, and

the patient’s acceptance and
compliance of the product
 General considerations
3. Route of
administration
Definition
-is the path by which a drug, fluid,
or other substance is taken into the
body.

Consideration:s
-Various drugs work differently on
different routes.
-It can be the that the route of
administration is oral, topical,
parenteral, transdermal, inhalation, and
etc.
 General considerations
4. Type of drug delivery
system desired
Definition
- The drug delivery system that
the manufacturer’s want in to
design
Consideration:s
--This involves the
manufacturer’s ideas,
decisions, and future plans.

-Various factors are taken into

account here.
 A. Design of the appropriate dosae form or delivery system depends
on:
5. Desired Therapeutic Effect
Definition
● is a consequence of the medical treatment
of any kind, the results of which are judged
to be desirable and beneficial

Consideration:
● Drug may be intended for rapid relief of
symptoms, slow extended action given once per
day, or longer for chronic; some drug may be
intended for local action or systemic action.
 A. Design of the appropriate dosae form or delivery system depends
6. Physiologic release of the drug
on:

from the delivery system

Definition
● Physiologic: conforming to the normal
function or state of the body or a tissue or
organ

Consideration:
● How stomach emptying, GI residence time, and
gastric window
 A. Design of the appropriate dosae form or delivery system depends
on:
7. Bioavailability of the drug at the
absorption site
Definition
● Bioavailability: refers to the percentage of
the drug that reaches systemic circulation
unchanged

Consideration:
● Rate: the amount or rate of drug absorption from
the given dosage form
● Duration: how long does the drug present into
the blood strem
 A. Design of the appropriate dosae form or delivery system depends
on:
8. Pharmacokinetics and Pharmacodynamics
of the drug
Definition
● Pharmacokinetics: what the body does to the drug
● Pharmacodynamics: what the drug does to the
body

Consideration:
● the desired therapeutic response of the type/
frequency of adverse reaction to the drug
 b.
Bioavailability
Bioavailability
Measurement of the rate
& extent of systemic
absorption of the
therapeutically active
drug.
“ The route of administration and the
dose of a drug have a significant
impact on both the rate and extent
of bioavailability.
“ The difference in drug bioavailability
may be manifested by observing the
difference in the therapeutic
effectiveness of a drug product.
These processes may include the
following:
Dissolution
Process through
which solid, gaseous
or liquid substances
dissolve in a solvent
Disintegration to produce a
Disaggregation
Breaks down the drug solution Division or breaking up
into tiny fragments or into constituent parts
granules to improve
their solubility
 03
Convection and
diffusion
Of the drug molecules to the absorpbing
surface
Diffusion = is a solute transport across a
semi – permeable membrane molecules
move from an area of higher to an area
of lower concentration.
Ex:
• absorption of drug
• Permeation through biological tissue
• Reabsorption in the nephron

Convention = is a process where solute pass

across the semi-permeable membrane
along with the solvent in response to a
positive transmembrane pressure.
Ex.
• Transport of O2, nutrients, drugs and
other molecules by the blood.
• Paracellular mechanism of small water-
soluble molecules
• Transport of molecules through a
porous matrix
04 Absorption - of the drug
across cell membrane into the
systemic circulation.
C. Rate-limiting step
 Rate-limiting step

In a series of kinetic or
rate processes, the rate at
which the drug reaches
the systemic circulation is
determined by the
slowest of various steps
involved in the sequence.
“
In the process of drug disintegration,
dissolution, and absorption, the rate
at which drug reaches the
circulatory system is determined by
the slowest step in the sequence.
“ For drugs that have very poor
aqueous solubility, the rate at which
the drug dissolves (dissolution) is
often the slowest step and therefore
exerts a rate-limiting effect on drug
bioavailability.
“ In contrast, for a drug that has a
high aqueous solubility, the
dissolution rate is rapid, and the rate
at which the drug crosses or
permeates cell membranes is the
slowest or rate-limiting step.
 In general, for drug products that

“
slowly release the drug from the
formulation such as extended- or
controlled-release formulations or
for drug products where dissolution
of the drug is the rate-limiting step in
the appearance in the systemic
circulation, with a discriminating
dissolution method, the probability
of establishing a predictive in vitro–
in vivo correlation (IVIVC) is higher. .
Alternative Resources