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PHARMACEUTICAL

SUSPENSIONS AND
EMULSIONS
PHARMACEUTICAL
SUSPENSIONS AND
EMULSIONS
EmuIsion: Liquid drug in liquid vehicle:
Suspension: Solid drug in liquid vehicle
Coarse Dispersions
Oil-in-water emulsions (o/w)
Water-in-oil (w/o)
(Lyophobic colloids)
Reasons for Use Reasons for Use
Drug is insoluble
Drug is more stable in
suspension or emulsion
There is a need to control the
rate of release of the drug
Drug has bad taste (oral)
Routes of Administration Routes of Administration
Oral
Ocular
Otic
Rectal
Parenteral
Topical
I. FormuIation of
Suspensions
I. FormuIation of
Suspensions
etting
Wetting agent
eII FormuIated
Suspension
Resuspend easily upon shaking
Settle rapidly after shaking
Homogeneous mix of drug
Physically and chemically stable
during its shelf life
Sterile (parenteral, ocular)
Gets into syringe (parenteral, ocular)
ExternaI" Forces Acting
on ParticIes
V(8-8
o
)g
2-5 3m
Gravity
Brownian Movement
Sedimentation
equilibrium: Gravity is
neutralized by
Brownian movement
SettIing and Aggregation
The suspension shall
form loose networks of
flocks that settle rapidly,
do not form cakes and
are easy to resuspend.
Settling and aggregation
may result in formation of
cakes (suspension) that
is difficult to resuspend or
phase separation
(emulsion)
flock
cake
Sediment VoIume
F=0.5 F=1.0 F=1.5
F={volume of sediment V
u
}/{original volume V
o
}
V
o
V
u
V
o
V
u
DLVO: OptimaI Distance
Distance
Energy
Attraction
Repulsion
Attraction
No flocks can form
ControIIed FIoccuIation
eta-potential
F=V
u
/V
o
Caking Caking
Non-caking
Flocculating Agent
+
+
-
Flocculating agent
changes zeta-
potential of the
particles (it can be
electrolyte,
charged surfactant
or charged polymer
adsorbing on a
surface).
f the absolute
value of the zeta-
potential is too high
the system
deflocculates
because of
increased repulsion
and the dispersion
cakes.
II. FormuIation of
EmuIsions
II. FormuIation of
EmuIsions
EmuIsification
Emulsifier
HLB and Use of Surfactants HLB and Use of Surfactants
HLB ca. 1 to 3.5: Antifoams
HLB ca. 3.5 to 8: Water-in-Oil Emulsifiers
HLB ca. 7 to 9: Wetting and spreading agents
HLB ca. 8 to 16: Oil-in-Water Emulsifiers
HLB ca. 13 to 16: Detergents
HLB ca. 15 to 40: Solubilizers
Amphiphilic surfactants are characterized by
the hydrophilic-lipophilic balance (HLB): a
relative ratio of polar and non-polar groups in
the surfactant
Required HLB Required HLB
Calculate the required HLB for the oil phase of the following
o/w emulsion: cetyl alcohol 15 g., white wax 1g. Lanolin 2 g,
emulsifier (q.s.), glycerin 5 g. water 100 g.
Required HLB Fraction
(from reference)
Cetyl alcohol 15 x 15/18 12.5
White wax 12 x 1/18 0.7
Lanolin 10 x 2/18 1.1
Total required HLB 14.3
HLB needed for emulsification of the oil phase. f
there are several oil ingredients the required HLB
is calculated as a sum of their respective required
HLB multiplied by the fraction of each.
HLB of Surfactant Blend HLB of Surfactant Blend
hat is the HLB of the mixture of 40 % Span 60
(HLB = 4.7) and 60 % Tween 60 (HLB = 14.9)?
HLB of mixture:
4.7 x 0.4 + 14.9 x 0.6 = 10.8
In what proportion should Span 80 (HLB = 4.3) and
Tween 80 (HLB = 15.0) be mixed to obtain
"required" HLB of 12.0?
4.3
.
(1-x) + 15
.
x = 12 x = 0.72
72 % Tween 80 and 28 % Span 80
Surfactant blends are commonly used to obtain
desired emulsifying properties.

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