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UNIT I
V.MANIMARAN
LECTURER
DEPARTMENT OF PHARMACEUTICS
SRM COLLEGE OF PHARMACY
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Formulation science for drug development and dosage form design, Study notes of Pharmacy
Formulation science for drug development and dosage form design
Typology: Study notes
2016/2017
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UNIT I^ V.MANIMARAN^ LECTURER^ DEPARTMENT OF PHARMACEUTICS^ SRM COLLEGE OF PHARMAC
Y
CONTENTS
INTRODUCTION
OBJECTIVES
PRELIMINARY STUDIES
BULK CHARACTERIZATIONS
ANALYTICAL MEASURES
CONCLUSION
REFERENCES
2
OBJECTIVES
The
main
objective
is
to
generate
information
useful to the formulation in developing most stableand bioavailable dosage form that mass can beproduced.
4
Why
is
Preformulation
Important
It describes the process of optimizing the delivery of drug
thorough
determination
of
physical,
chemical
properties
of
new
drug
molecule
that
affect
drug
performance and development of an efficacious stableand safe dosage form.
Preformulation
studies
on
a
new
drug
molecule
provide useful information for subsequent formulationof a physicochemically stable and biopharmaceuticallysuitable dosage form.
5
Organic
salts
are
more
water
soluble
than
un
–ionized
molecule.
Prodrug are
synthetic
derivative
of
drug
molecule
Pharmaceutical
improvement
from
prodrug include
stabilization
,increase
or
decrease
of
solubility
crystallinity,
taste
,odour
e.
g.Erythromycin esolate
Once
the
optimum
molecular
form
of
drug
has
been
selected
formulation
development
begin
there
task
in
drug
development
process.
7
BULK
CHARACTERIZATION
8
BULK
CHARACTERIZATION
SOLUBILITY
ANALYSIS
CRYSTALLINITY
&POLYMORPHISM
HYGROSCOPICITY
FINE
PARCTICLE
CHARACTERIZATION
BULK
DENSITY
POWDER
FLOW
PROPERTIES
IONIZATION CONSTANT –Pka
PH SOLUBILITY PROFILE
COMMON ION EFFECT –Ksp
THERMAL EFFECTS
SOLUBILIZATION
PARTITION COEFFICIENT
DISSOLUTION
STABILITY
ANALYSIS
STABILITY
IN
TOXICOLOGY
FORMULATION
SOLUTION
STABILITY
PH
RATE
PROFILE
SOLID
STATE
STABILITY
BULK
STABILITY
COMPATIBILITY
Changes
with
internal
structure
alter
crystal
habit
while
chemical
changes
produces
both
change
in
internal
structure
crystal
habit
Characterization
of
solid
form
involves
Verifying
that
the
solid
is
expected
chemical
compound.
Characterizing
internal
structure
Describing
habit
of
crystal.
The
internal
structure
of
compound
can
be
classified
in
following
way.
10
11
Chemical compound
habits
Internal structure
crystalline
amorphous
Single entity
Molecular adduct
polymorphs
Nonstoichiometricinclusion compound
Stoichiometricsolvates (hydrates)
channel
layer
Cage(clathrate)
Analytical
method
used
for
characterization
Microscopy
Differential
scanning
calorimetry
Infrared
spectroscopy
Thermogravimetric
analysis
X
‐ray
diffraction
13
MICROSCOPY:
In
this
technique
substances
are
examined
under
the
microscope.
It
gives
information
about
shape,
thickness,
particle
size,
etc.
of
drug
molecules.
By
this
method
we
can
study
crystal
morphology,
difference
between
polymorphic
character
of
molecule.
14
Differential
Scanning
Colorimetry
16
Infrared
spectroscopy
The study of the interaction of electromagnetic radiationwith
vibrational
and
rotational
resonances
within
a
molecular structure is termed as IR Spectroscopy.
IR has the ability to differentiate isomers groups such as Cis
‐trans double bond compound.
Gives
an
information
regarding
functional
group
present in new drug molecule.
FT
‐IR use for both qualitative and quqntitative analysis
of sample.
17
.^
X
RAY
DIFFRACTION
When a beam of non homogenous x
‐rays is allowed to pass
through a sample the x
‐ray beam is diffracted & it is recorded by
means of photographic plates.
Single Crystal X
‐ray provides the most complete information
about the solid state.
It is used to differentiate the amophous and crystalline forms.
This method is tedious, time consuming & hence unsuitable for
routine use.
19
B. Polymorphism^
polymorphism is the ability of the compound to crystallize as more than one distinct crystalline species with different internalstructure.
Formation
of
different
polymorphs
depends
on
solvents,
temperature, pressure, rate of cooling, etc.
Polymorphic
transitions
can
also
occur
during
milling,
granulating, drying and compressing operations
Different
polymorphs
vary
in
physical
properties
such
as
dissolution, solid
‐state stability, compatibility
, etc
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