Preparation 13: Basic Preparation 14: Mineral Oil Preparation 15: Preparation 16:

Emulsion Emulsion COD Eucalyptus Oil

Emulsion

● Offi. title: ​Basic ● Offi. title:​ Mineral Oil ● Offi. title: ● Offi. title:
emulsion emulsion, USP COD Liver Oil Eucalyptus Oil
(Non-Official) ● Category:​ Cathartic emulsion, emulsion
● Category: ● Uses:​ Laxative USP (Non-Official)
Cathartic ​(cleanse ● Synonyms: ​Liquid ● Category: ● Category:
or purge) Petrolatum emulsion and Vitamin Expectorant ​(helps
● Uses:​ Vehicle, Liquid Paraffin Emulsion Supplement bring up mucus
Laxative Olei Morrhuae and other material
● Synonyms: - --> Basic concepts: ● Uses:​ To from the lungs,
Primary Emulsions supply vitamin bronchi, and
--> Basic concepts: - Initial emulsion formed after A and D trachea)
A. Emulsion incorporating all the appropriate ● Synonyms: ● Uses:​ Expectorant
- Dispersion in amounts of oil, water, and gum Emulsion Olei in chronic
which dispersed depending on the method used Morrhuae bronchitis
- A.k.a “Emulsion Nucleus” ● Synonyms: ​-
phase is --> Ingredients
composed of Acacia mucilage 1. COD Liver Oil: --> Ingredients
​small globules of - Acacia dissolved in water by ​Active ingredient, 1. Eucalyptus oil: Active
a liquid trituration internal phase ingredient, internal phase
​distributed - Scientific name: ​Acacia xenical 2. Acacia: ​Natural 2. Acacia: Natural
throughout a - Used as: emulsifying agent emulsifying agent
a. demulcent ​(relieving 3. Purified water: 3. Purified water: External
​vehicle in which
inflammation or irritation) External phase phase
it is immiscible
and suspending agent
B. Internal Phase b. emulsifying agent -->Quality Control --> Quality
- Dispersed c. excipient in making pills /Packaging Control/Packaging
medium and troches ● Appearance: ​White, ● Appearance: ​White,
C. External phase milky, opaque, milky, opaque,
- Dispersion --> Small scale homogeneous homogeneous
extemporaneous methods of - Due to rupturing of - Due to rupturing of the
medium
preparing emulsions the film of the film of the continuous
continuous phase phase
--> Types of Emulsion A. Continental/Dry Gum
1. Oil-in-water Method ● pH:​4.5-5 ● pH:​4.5-5
- Internal phase: ● 4:2:1 method for preparing the ● Pourability: ​Easily ● Pourability: ​Easily
Oleaginous initial or primary emulsion pourable pourable
- External phase: ● 4 parts of oil, 2 parts water, 1 ● Redispersability:​ ● Redispersability:​ Easily
part gum Easily dispersed dispersed upon shaking
Aqueous upon shaking ● Particle size to
● Arrangement
2. Water-in-oil ○ Emulsifier and oil ● Particle size to appearance: > 1 um,
- Internal phase: ○ then water appearance: > 1 um, milky
Aqueous ● Uses a Wedgewood or milky ● Physical stability: No
- External phase: porcelain mortar and pestle → to ● Physical stability: creaming, sedimentation,
Oleaginous ensure proper grinding action No creaming, coalescence, flocculation
reduction of globule size sedimentation, and phase inversion.
3. Multiple emulsion
● Ex: Mineral Oil coalescence, ● Packaging requirement:
- Contains even small flocculation and Preserve in tight
droplets that are Procedure: phase inversion. containers
miscible w/ the → Note:4 parts of oil is first ● Packaging ● Label: Shake well
 continuous mixed with 1 part of gum; Do not requirement: before use
phase/external phase allow contact of oil and gum for Preserve in tight ● Container: 15mL clean
- W/O/W (oil droplet too long, as the gum may absorb containers flint bottle (amber bottle si
the oil ● Label: Shake well COD)
surrounded by
before use
aqueous phase) → Note: Adding 2 parts of water ● Container: 15mL --> Physical Signs of
- O/W/O (water all at once = ensure uniform clean flint bottle Unstable Emulsions
separates internal and distribution (amber bottle si COD) 1. Creaming
external oil phase) - Upward movement, of
- ​Multiple emulsions → Note: The mixture is then *Add the oil in dispersed droplets
are “emulsions of triturated immediately, rapidly increments of 0.5 g - Due to a difference in
and continuously and disperse. density between the
emulsions,” in which
Triturate for at least 5 internal and external
the drops of the → Note: Primary emulsion: mins phase
dispersed phase creamy white appearance and a
themselves contain crackling sounds 2. Sedimentation
smaller dispersed - Downward movement of
droplets of a miscible → Note: the dispersed droplets
liquid a. Add liquid ingredients that are - Due to a difference in
miscible with the external phase density between the
-D ​ roplets have the
with trituration internal and external
same phase with the b. Dissolve solid ingredients phase
external phase before adding to the mixture.
4. Microemulsion = To disperse them evenly and 3. Flocculation
- Thermodynamically so that they are already - Aggregation of the
stable, isotropically clear dissolved before adding it in the dispersed droplets
dispersion of two mixture. - Due to intermolecular
Attraction
immiscible liquids → Note: Add water to volume
and swirl in the mortar = 4. Coalescence
--> Basic Components RFIS→Add more water to reach - Separation of the
of an Emulsion the final/required volume. dispersed and continuous
1. Water phase​: RFIS→To remove the remaining phase
Aqueous mixtures portions of the emulsions - Due to rupturing of the
film of the continuous
2. Oil phase:
B.English/Wet Gum Method phase
Representing ●Trituration of mucilage with oil
hydrocarbon or organic Mucilage → emulsifying agent 5. Phase Inversion
liquids; Ex: Mineral oil, is added to the water - Changing of an
Castor oil, Beeswax, and ●4 parts of oil, 2 parts water, 1 emulsion from one type to
Wool fat part gum another caused by
3. Emulsifying agent: ●Arrangement: changing the phase
○ Emulsifier and water volume ratio
Promote emulsification
○ Then oil
●Ex: COD If O/W is the stable then it
Example of Emulsifying will change to W/O
Agents: Procedure: If W/O is the stable then it
A. Carbohydrates: → Note: 1 part of gum is first will change to O/W
Acacia, Tragacanth, mixed with 2 parts of water.
Agar, Chondrus, and --> Methods of detecting
→ Note:4 parts of oil is added Emulsions (standard:
Pectin slowly in parts = prevent phase aqueous)
separation 1. Dilution Test
-miscible in water
B. Protein materials: → Note:The mixture is then
Gelatin, Egg Yolk, triturated forming emulsion.
and Casein Mixture should be mixed
thoroughly = ensure uniform
C. High molecular
distribution
weight alcohols:
Stearyl Alcohol, → Note: Primary emulsion:
Cetyl Alcohol, and creamy white appearance and a
Glyceryl crackling sounds
Monostearate
D. Wetting agents: → Note:
a. Add liquid ingredients that are
Anionic, Cationic, or
miscible with the external phase
Nonionic with trituration.
b. Dissolve solid ingredients
-->Hydrophile-Lipophile before adding to the mixture.
Balance (HLB System) = To disperse them evenly and
- Provides a so that they are already
systematic method of dissolved before adding it in the
mixture.
selecting mixtures of
emulsifying agent → Note: Add water to volume
- Higher surfactant and swirl in the mortar
HLB value = The RFIS→Add more water to reach
more hydrophilic the final/required volume.
​(water loving) RFIS:→To remove the
- Lower surfactant remaining portions of the
emulsions
HLB value = The
more lipophilic C.Bottle/Forbes Bottle
(​lipids/fat loving) Method
● For preparations of emulsions
--> HLB values with volatile oils or oleaginous
substances with low viscosity.
● Ex: Eucalyptus
● Not for viscous oils: they
cannot be thoroughly agitated in
the bottle when mixed with the
emulsifying agents.
Procedure:
→ Note: Place the emulsifier in a
dry bottle and ​add 2 parts of
oil.​ Cap the mixture and shake
thoroughly = RFIS: To
completely dissolve the
emulsifier; Do not allow contact
of oil and gum for too long, as
the gum may absorb the oil
→ Note: Add ​2 parts of water
with shaking after ​each
addition​, forming the primary
𝐻𝐿𝐵mixture emulsion. Repeat until all water
-O/W = positive
-W/O = negative
-part of emulsion is
diluted in water
2. Conductivity Test
-Conduct electricity
-O/W = Lamp will light
-W/O = Lamp will not light
-pair of electrodes
connect to a lamp and
electrical source is dipped
in emulsion
3. Dye-Solubility Test
-Macroscopic result →
aqueous external phase
can absorb more dye.
-Microscopic
result→aqueous internal
phase can absorb the
dye.
-Dye dissolves in either
layers
-O/W:
a. Macroscopic
- more intense
coloration
b. Microscopic
- Colorless
-W/O:
a. Macroscopic
- Less intense
b. Microscopic
- Colored droplets
-Water-soluble dye→
dissolved in the emulsion.
-Oil-soluble dye→
dissolve in oil phase.
4. CoCl2/ Filter paper
test: (Pink color of filter
paper)
- if aqueous in external
phase = hydrate all CoCl2
present
- if aqueous internal
phase = hydrate apart of
CoCl2 present
-O/W: Blue to pink filter
paper
-W/O: Pink spots on blue
filter paper
=​𝒙𝐻𝐿𝐵a +(1−𝒙)𝐻𝐿𝐵b has been added = RFIS: To - Emulsion is tested on
prevent the separation of two filter paper containing
TO GET THE PERCENT! liquids, and so to reduce CoCl2
interfacial tension.
A = 100(X-HLBb) / (HLBa
5. Fluorescence test
- HLBb) → Note: Add water to volume. - If oleaginous in external
B = 100- A Other ingredients in an aqueous phase = Fluoresce
solution may be added = RFIS: completely
TO GET THE GRAMS! Add water to reach the required - If oleaginous in external
A = % in A x (HLB of volume. phase = Fluoresce in
mineral oil) / 100 parts
--> Ingredients -O/W: Spotty
B = g depends on the
1. Mineral Oil: Active ingredient, fluorescence
prep needed - answer in internal phase -W/O: Continuous
A 2. Acacia: Natural emulsifying fluorescence
agent
If o/w Answers: 3. Syrup: Sweetener
1. Tween 80 = 3.09 4. Vanillin: Flavorant
2. Span 80 = 1.91 5. Alcohol: Preservative; benzoic
acid or sweet orange peel
tincture = can be substitute since
If w/o: it has alcohol content (tincture)
1. Tween 80= 0.327 and benzoic acid requires acidic
2. Span 80 = 4.673 pH so it can be substitute
6. Purified Water: External
Take note: phase
HLB of mineral oil:
*RFIS​→Alcohol should be
1. W/O: 5-6 added as near to the end of the
2. O/W: 12 process to avoid breaking the
emulsion.
--> Use of each Quality Control/Packaging
ingredient in the prep:
1. Liquid petrolatum Official title Mineral Oil
- A.k.a Mineral Oil Emulsion,
- Oil phase/Active USP
ingredient
Appearance White, milky
- RHLB:
opaque,
- 5-6 (W/O) homogenous
- 12 (O/W) mixture
2. Span 80
- Oil soluble emulsifying pH 4.5-5
agent
Pourability Easily
- HLB Value: 4.3 pourable
3. Tween 80
- Water soluble Redistribution Easily
emulsifying agent dispersed on
- HLB Value: 15.0 shaking
4. Purified Water Particle size >1um; Milky
- Continuous phase
--> Reasons for
Physical No creaming,
important steps Stability sedimentation
1. Water must be ​heated , flocculation,
to higher temperature coalescence,
​than the oil because and phase
it will cool faster. inversion
2. Temperature must ​not
exceed 70°C ​because it
can ​denature protein​ ​in
the emulsifying agent
3. Water needs to heat at
65°C while Mineral Oil is
required to heat at 60°C.
4. Constant Stirring is
required

--> Quality Control

● Appearance: ​Creamy,
white, thick
homogeneous
mixture
● Pourability: ​Easily
pourable
● Dispersibility:
Redispersible
● Particle size:
a. Milky​: ​> 1um
b. Blue-White​: 0.1 –
1 um:
c. Gray or
Semi-Transpare
nt​ : 0.05 – 0.1 um
d. Transparent: ​<
0.05 um
● Physical instability:
Flocculation, Creaming,
Coalescence, Breaking

Coalescence:​ Fusion of
small droplets to form a
large droplets

Creaming: ​Isolated oil

droplets combine
• O/W – rise at the top
• W/O–sink to the bottom
Flocculation: ​Two or
more droplets together to
form an aggregate

Breaking: ​Water droplets

and collect in a layer
separate from oil.

--> Packaging, Labeling

and Storage
● Packaging:
○ Preserved in well-
closed containers (15 mL
flint bottle)
○ For viscous emulsions,
wide mouth bottles
should be used.
● Storage:
○ Should be stored in
room temperature
● Label:
○ For viscous emulsion,
“shake thoroughly before
use”
○ For External products,
“for external use only”

--> Types of emulsion

--> Test for identifying
emulsion type

1. Dilution test
Involves the addition of
continuous phase

2. Electrical
Conductivity Test
An emulsion with water
continuous phase will
readily conduct electricity

3. Dye-Solubility Test
a. Water soluble dye
– dissolve in
aqueous phase
b. Oil soluble dye –
dissolve in oil
phase

4. Fluorescence Test
a. W/O – continuous
fluorescence
b. O/W – spotty
fluorescence
5. Cobalt Chloride Test
a. W/O – does not
change color
b. O/W – changes
color
Preparation 17: Kaolin Suspension
● Offi. title: ​Kaolin Suspension
(Non-Official)
● Category: ​Gastrointestinal drug
● Uses:​ Toxin absorbent; For
treatment of diarrhea, Chronic
ulcerative colitis
● Synonyms: ​Kaolin mixture, Native
hydrated aluminum silicate
--> Review of basic concepts
Suspensions:
- Preparations that are containing
finely divided drug particles (the
suspensoid) dispersed somewhat uniformly
in a vehicle in which the drug exhibits
minimum solubility.
- Insoluble dispersed phase (solid) in a
dispersion medium
- The external phase(dispersion/suspending
medium) is generally aqueous in some
instances, ​may be organic or oily liquid for
non oral use.
- Pharmaceutical suspensions can
improve stability of certain
drugs, e.g. Procaine penicillin G.
- Suspensions are formulated for drugs
which are unstable in an aqueous medium
and for insoluble or poorly soluble drugs.
- ​Drugs in suspensions exhibits a higher
rate of bioavailability​ than other dosage
forms
- Suspensions are either in ​Ready-to-use
form or Dry powdered form
--> General features desired in
pharmaceutical suspensions
1. The particle sizes of insoluble dispersed
phase or solids in a suspension must be
about 0.2-10 microns/micrometer
2. A pharmaceutical suspension should
settle slowly ​and must be readily dispersed
Preparation 18: Aluminum
Hydroxide-Magnesium Hydroxide
Suspension
● Offi. title: ​Aluminum
Hydroxide-Magnesium Hydroxide, USP
● Category: ​Antacid and Gastrointestinal
OTC Drug
● Uses:​ ➔ For the relief of acid
indigestion, heartburn, and an upset
stomach ➔ Treat symptoms in patients
with peptic ulcer, gastritis, and gastric
hyperacidity
● Synonyms: ​MAALOX (innovator name),
Alamag Plus and Almacone, Almacone,
Milk of Magnesia
--> Precautions and Side effects
Precautions
● Must not be taken by:
○ People with kidney disease
○ Breastfeeding mothers
○ People who are on a low- salt diet
○ People who are allergic to the
components
Side effects
● Diarrhea
● Constipation
● Loss of appetite
● Unusual tiredness
● Muscles weakness
--> Suspensions
- biphasic dosage forms containing insoluble
solid material suspended in a liquid medium
Advantages
● Chemical stability
● Controlled drug release
● Palatability and patient acceptance
● For drugs with low solubility
● Higher rate of bioavailability
Disadvantages
upon gentle shaking. ● Sedimentation and compaction
3.The suspension should pour out ● Bulky - sufficient care during handling and
readily and evenly from its transport
container. ● Uniform and accurate dose cannot be
4. The particle size of the suspension achieved
should remain fairly constant during long
periods of standing. --> Phases
Continuous / External Phase
--> Flocculated vs Deflocculated - Dispersion Medium (aqueous or oily)
systems: Flocculated systems
Flocculated: Dispersed / Internal Phase
● The dispersed particles are held - Insoluble API
together in loose aggregates
● Dispersed particles lessen the --> General Features of a Desired
elegance of the preparation due to their Suspension
tendency to separate from the dispersion 1. Slow settling; readily dispersed with moderate
medium but they avoid caking and are easy shaking
to reside. 2. Spreads over surface but does not run off;
● Rate of sedimentation is high provide an elastic protective film
● Sediments are rapidly formed 3. Easy to pour yet not watery and no grittiness
● Redispersion of sediments is easy 4. Good syringeability
which can be done by the shaking 5. Parenteral and Ophthalmic
of the bottle/container 6. Suspension must be sterilizable
● The floccules sticks to the side of 7. Stable during shelf-life
the bottle/container 8. Acceptable taste, odor and color
● Appearance: Clear 9. Must not recrystallize during
Storage
Deflocculated:
● The particles exists as separate
Flocculated Deflocculated
entities in this system
● Dispersed particles gives the Particles Aggregates/ Separate
preparation a uniform appearance as they Flocs Entities
tend to settle less rapidly but they can form
a hard cake which is hard to redisperse.
● Rate of sedimentation is low
● Sediments are slowly formed
● Suspension is pleasing in
appearance and they don’t stick to
the sides of the bottle/container
● Appearance: Cloudy Rate of High & rapid Low & slow
Sedimentation
--> Ingredients
● Flocculating agents-increases the degree Sediments Loosely Closely
of flocculation in a suspension and prevent packed; no packed;
caking. The Flocculating agent are only hard cake forms hard
added in preparation B ​as it is a flocculated cake
system. The Flocculating agent in
preparation B is ​Monobasic potassium Redispersion Easily Difficult to
phosphate dispersed redispersed
● Suspending agents- Usually added to
Supernatant Clear Turbid/cloudy
promote pharmaceutical elegance and
dosage uniformity and prevent settling of Overall Unsightly Aesthetically
particles. The suspending agent in both Appearance pleasing
preparations is ​Sodium
Carboxymethylcellulose.
● Active ingredient/suspensoid- is the ​main
component of the pharmaceutical
suspension which performs the
pharmacological activity. The active
ingredient in both preparations is ​Kaolin
● Wetting agent- lowers the surface tension
of a liquid and thus allows it to spread more
easily. The wetting agent in both
preparations is ​Glycerin.
● Dispersion medium- It is the medium in
which the dispersed particles are distributed
uniformly. The dispersion medium in both
preparations is​ ​Purified Water.
● Preservative- It is a natural or synthetic
chemical added to pharmaceutical
preparations to prevent microbial
decomposition. The preservative in both
preparations is ​Sodium Benzoate
--> Quality Control & Packaging
Appearance: ​White liquid with dispersed
particles
pH: ​7.3 (Neutral)
Pourability: ​Easily poured
Dispersibility: ​Easily dispersed upon
shaking
Appearance of sediments:
● Preparation A: Closely packed
● Preparation B: Loosely packed
Sedimentation rate, Sedimentation volume,
Degree of flocculation:
● ​Preparation A: Slow, 0.15, 1
● Preparation B: Fast, 0.75, 5
Physical stability: ​No sedimentation, caking
present and partially soluble internal phase
Physical instabilities:
● Sedimentation- Settling of dispersed
phase which can be ​remedied by gentle
shaking.
● Caking- Aggregation of the settled
dispersed particles forming a hard “cake”
which is hard to redisperse.
Packaging requirement: ​Store in a cool, dry
place away from heat and light
Label: ​Shake well before use
Container: ​15mL amber bottle or flint bottle
Procedure: A
→ Note: Dispense 0.1 g Sodium
Carboxymethylcellulose in 3 mL water.
Set aside.
→ Note: Levigate ​(reduce a substance to a
​ g kaolin
fine powder or smooth paste) 1
Other: Stick to the Does not
sides of the stick to the
bottle sides of the
bottle
--> Basic Components of Suspensions
1. Solvent/Vehicle: where the API / insoluble
drug is dispersed ---Examples: Purified Water
(aqueous), Propylene Glycol (non-aqueous)
2. API: To provide pharmacologic effect
---Examples: Aluminum Hydroxide,
Magnesium Hydroxide
3. Wetting Agents: To disperse solids
in continuous phase; aka “surfactants”
---Examples: Glycerin, Polysorbates, Sorbitan
Esters
4. Flocculating Agents: To “flock” drug particles
and prevent caking ---Examples: Citrates,
Sulfate, Phosphate Salts and Calcium salts
5. Preservatives: To prevent microbial growth
---Examples: Glycerin, Parabens,
Alcohol,
6. Suspending Agents: To increase
viscosity, inhibit agglomeration and decrease
sedimentation; aka “thickeners”
---Example: xanthan gum, acacia
7. Flavoring Agents: For taste-masking
purposes ---Examples: Lemon Oil, Peppermint
8. Sweeteners: To improve palatability
---Examples: Syrup, Aspartame
9. Colorants: To provide a more
aesthetic appearance ---Examples: FD&C Blue
#1 (Brilliant Blue), FD&C Yellow #6 (Sunset
Yellow)
10. Buffering Agents: To resist pH change
---Examples: citrates, carbonates
​--> Use of each ingredient
1. Magnesium Hydroxide & Aluminum
Hydroxide: ​Active Pharmaceutical Ingredient
2. Sodium Citrate:​ Flocculating Agent
3. Glycerin:​ Wetting Agent
4. Purified Water: ​Solvent
5. Simple Syrup: ​Sweetening Agent; thickener
6. Peppermint Oil:​ Flavoring
7. Sodium Benzoate:​ Preservative
--> Stoke’s Equation
- Explains the theory of sedimentation behavior
with 1 mL Glycerin, and mix with the
Sodium Carboxymethylcellulose solution =
Kaolin is levigated in order to prevent
lumping as it is combined with both
carboxymethylcellulose aqueous solution
→ Note: Dissolve 0.01 g Sodium Benzoate
in enough Purified Water, and slowly add
this mixture to the Kaolin
Procedure: B
→ Note: Dispense 0.1 g Sodium
Carboxymethylcellulose in 3 mL water.
Set aside.
→ Note: Levigate ​(reduce a substance to a
fine powder or smooth paste) 1 ​ g kaolin
with 1 mL Glycerin, and mix with 0.15 g
Monobasic Potassium Phosphate dissolved
in enough water. Combine two solutions =
Kaolin is levigated in order to prevent
lumping as it is combined with both
carboxymethylcellulose aqueous solution
→ Note: Dissolve 0.01 g Sodium Benzoate
in enough Purified Water, and slowly add
this mixture to the Kaolin
➔ Sedimentation velocity is directly proportional
to the ​square diameter of particle
◆ Rate of fall of a suspended particle: greater
for larger particles (Solution: Reduce size of
particles)
➔ Greater Difference in density = Higher Rate
of Sedimentation (Solution: Increase viscosity)
◆ Ps ​(density of disperse phase)​ is higher than
Po ​(density of disperse media)​ = particles settle
down
◆ Po is higher than Ps = particles float
➔ Increasing viscosity = Lower Rate of
Sedimentation (Ideal)
◆ Gives rise to problems like pourability and
syringeability
--> Zeta potential
- Determines the ability of a liquid to carry a
solid material in a suspension
- If attractive forces exceed repulsive forces and
particles come together → Flocculation
--> Quality Control and Packaging
Appearance: ​White, opaque liquid with a creamy
consistency; Should appear uniform and elegant
pH: ​7.3 - 8.5
Pourability: ​Easy to pour, yet not watery and no
grittiness
Instability: ​Sedimentation, flocculation, cake
formation; change in color, odour or taste
Packaging: ​Amber bottle; wide-mouth and tight
containers
Labelling: ​“Shake well before use” “Store in a
cool place”
Storage: ​Store in a controlled room temperature
between 15-30 degrees Celsius away from
moisture and heat. Do not allow liquid medicine
to freeze.
--> Physical signs of an unstable suspension
1. Flocculation: ​Particles form loose networks
---Cause: Van der Waals attraction
2. Sedimentation:​ Particles settle down at the
bottom
---Cause: large particle diameter
 3. Caking: ​Formation of non-redispersible
sediments
---Cause: crystal-bridging and close aggregates

4. Stable Suspension:​ Particles are uniformly

dispersed.

5. Crystal Growth
---Cause: Low viscosity; temperature
fluctuations

--> Quality Control Tests for Stability

1. Sedimentation Method
- Sedimentation volume: Most important
parameter

2. Rheological Method
- Viscosity is measured at different time intervals

3. Electrokinetics Method
- Determination of Zeta Potential

4. Micrometric Method
- Particle size is measured; also tests for crystal
growth

5. Temperature Tests
- Fluctuations: crystal formation
- Freezing: cake formation

Preparation 19: Milk of Magnesia Preparation 20: Aluminum Hydroxide Gel

● Offi. title: ​MIlk of Magnesia, USP ● Offi. title: ​Aluminum Hydroxide Gel,
● Category: ​Antacid (​class of USP
medicines that neutralize acid in the ● Category: ​Antacid, Antireflux
stomach​) agents, and Antiulcerants
 ● Uses:​ Antacid, Relief for bowel
problems
● Synonyms: ​Magnesium Hydroxide,
- Magnesia Magma and Rolaids
(calcium carbonate and sodium
hydroxide)
● Offi. def’n: ​A suspension of
Magnesium Hydroxide. Contain not
less than 90% and not more than
115%, the labeled amount being ​80,​
160,​ and ​240mg​ of Mg(OH)2 per
mL, respectively. It may contain oils,​
suitable for flavoring purposes
--> Mechanism of Action
simple chemical reaction (neutralization)
--> Review of basic concepts
Dispersed systems
- Liquid preparations containing
undissolved/ immiscible drug distributed
throughout a vehicle
- Dispersed phase + Dispersion medium
Suspensions
- Two-phase system consisting of finely
divided solid dispersed in a solid, liquid or
gas
- Density of particles is greater than of the
vehicle
*emulsions vs suspensions
- SIMILARITY: mixture of two components
- DIFFERENCE: ​emulsions (​ two
components - two liquids); suspensions
​(two components - any phase)
Milk & magmas
- Suspension with inorganic solids where
there is a tendency for strong hydration and
aggregation giving rise to a gel-like
consistency
Lotion
- Category of liquid suspensions or
dispersions intended for external application Gels ---> ETO YUNG PREP
Gels
- Consisting of either suspensions made up molecules interpenetrated by a liquid
of small inorganic or large organic
molecules in a liquid vehicle
Milk & Magmas Gels and Lotion
● Uses:​ Heartburn, Upset stomach,
Sour stomach, and Acid indigestion
● Synonyms: ​Aluminum hydroxide,
Hydrated Alumina, and Aluminic
Acid
● Offi. def’n: ​Aluminum Hydroxide
Gel is a suspension of ​amorphous
aluminum hydroxide i​n which there
is a partial substitution of carbonate
for hydroxide. It contains the
equivalent of ​not less than 90% and
not more than 110%
*flavorants are added against bitter taste
--> Mechanism of Action
Reaction: Neutralization Al(OH)3 + 3HCl
-> AlCl3 + 3H2O
H2 blockers - called histamine 2
receptors; ex: cemeditine
--> Precautions and Side Effects
A. Side effects
1. Constipation
2. Low phosphate levels: loss of appetite,
unusual tiredness, and muscle weakness
B. Precautions
1. Constipation problems
2. Kidney diseases
3. Breastfeeding mothers
4. Allergies
*Adsorption
--> Common Brands
- Alternagel, Amphojel, Alu-Cap, Dialume,
Alu-Tab, Aloh-Gel
--> Review of Basic Concepts
Solutions
- contains one or more chemical
substances dissolved in suitable solvent.
- consisting of either suspensions made up
of small inorganic particles or large organic
Suspensions
- consisting finely divided solid dispersed in
solid liquid or gas
 Magmas
- Colloid - Homogenous
- Aqueous suspensions of insoluble,
- Large particle - Small particle
inorganic drugs
size (inorganic size (inorganic
solids) solids)
Emulsions
- Particles are - Particles are
- one liquid is dispersed throughout another
dispersed dissolved
liquid in droplet form
(spread/distributed)
Single-Phase/One Phase
- Dissolve in an aqueous or non-aqueous
*ex of colloid: Liquid dispersed in a gas is solvent or combination (homogenous)
--> Fog - A.k.a Organic hydrogels - Uniformly
distributed
--> Use of each ingredient in the prep:
1. Magnesium Sulfate Lotions
- Active Ingredient - Either liquid or semisolid preparations that
2. Sodium Hydroxide contain one or more active ingredients in an
- Active ingredient appropriate vehicle
3. Purified Water
- Dispersion medium Two-Phase --> ETO YUNG PREP
4. 0.1% Citric Acid - Consists of a dispersed phase and a
- Reduce bitterness dispersion medium
- Magnesium hydroxide can react to - Mixotrophic
the glass of the container
--> Factors affecting gel formation
--> Procedure and Reasons for important 1. Temperature
steps - Coarsening (freezing)
2. pH level
- Swelling
3. Addition of agents
- Contributes to the gelation process

--> Use of Ingredients

Direct hydration-​ more commercially used
1. Dissolve 3.0 g Magnesium Sulfate in
6.50mL Purified Water, place in a suitable
capacity vessel and heat to boiling.
RFIS:​ Diluted solutions ensure a fine,
flocculent, gelatinous precipitate of
magnesium hydroxide
2. Dissolve the 1 g Sodium Hydroxide in 1
mL Purified Water.
RFIS: ​Diluted solutions ensure a fine,
flocculent,gelatinous precipitate of
magnesium hydroxide
3. Add slowly to the boiling solution of
1. Sodium carbonate: ​Reacted to
form ALUMINUM HYDROXIDE,
the active ingredient; source of OH
2. Ammonium Alum: ​Reacted to
form ALUMINUM HYDROXIDE, the active
ingredient; source of aluminum hydroxide;
substitute (aluminum chloride)
3. Peppermint Oil: ​Flavorant, Alternatives
(glycerin, sorbitol, sucrose, saccharin, etc. )
4.Sodium Benzoate: ​Preservative
5.Purified Water: ​Dispersion medium
--> Procedure and Reasons for Important
Steps
1. Dissolve 5g of NaCO3.10H2O in 2 mL
hot water and filter (para walang buo buo)
RFIS: ​Hot water increases solubility of
Ammonium alum and sodium carbonate.
2. Dissolve 4g of Ammonium Alum in 1mL
hot water, filter into the carbonate solution
Magnesium Sulfate and continue boiling for
30 minutes
RFIS: ​Lessen sedimentation of the
product on standing
4. Wash with hot Purified Water 5-10x or
more (as shown by testing the supernatant
liquid with BaCl2 TS)
RFIS:​ This is to ensure that all sodium
sulfates are removed and because it is
more soluble in hot water
5. Decant the excess liquid, package and
label.
Chemical Reaction -​
* BaCl2 reacts with Na2SO4 = white heavy
precipitate of BaSO4, very distinct because
of magnesium hydroxide is gelatinous;
supernatant = clear colorless solution
* Sulfate free - BaCl2
--> Quality Control
● Appearance: ​Opaque, white liquid
● pH:​10
*Effect of pH? --> 0.1% Citric Acid *we can
add flavoring oils but not exceeding 0.05%
conc.
● Pourability: ​Not Easily Pourable
● Redispersability: ​Easily redispersed upon
shaking
● Particle Description:
White, gelatinous precipitate (identity:
Magnesium hydroxide​)
● Sedimentation rate: ​Fast
● Physical stabilities: ​NO
Sedimentation, NO Caking, NO Microbial
Growth (microbial count: not exceed 100
CFU and must pass the test that do not
have e. Coli present)
--> Packaging, Labeling and Storage
● Packaging:
○ In tight containers, preferably not
exceeding 35 degrees. Avoid Freezing.
*Freezing = Coarsening
*Temp > 35 degrees celsius = lower/reduce
gel structure
*pH can also affect the gel structure
● Label:
○ “Shake Well Before Use”
● Container:
○ Clean, flint bottle
with constant stirring
RFIS: ​Hot water and agitation causes
dissolution of side product Sodium
sulfate.​ DO NOT use boiling water since it
may cause DECOMPOSITION of API
3. Add 20mL hot water and remove all gas.
Dilute to 400mL with cold water
RFIS: ​Dilution with cold water
recrystallizes Al(OH)3 since it is
insoluble in water
4. Collect & wash the precipitate & suspend
it in 10mL Purified water with 0.01%
Peppermint oil and preserve with 0.1%
Sodium Benzoate
5. Homogenize the resulting gel
RFIS:​ Homogenized to form a uniform
product
6. Decant the excess liquid, package, and
label
4NaCO3*10H2O + NH4Al(SO4)2 =
Al(OH)3 + 2 Na2SO4+ 4 CO2+ NH3 + 10
H2O
--> Homogenization techniques
- + in small quantities
- Incorporate w/ additional agents such as
glycerin and alcohol
- Use mixer to incorporate gelling agent
when mixture has formed vortex to prep
uniform gel
*Why center: para di mag clumps
*Vortex disadvantage: di masyado
madissolve
--> Side Effects of Milk of Magnesia
1. Diarrhea - most common side effect; at
certain dose at specific acid, higher amount
of milk of magnesia (more water ang
naddraw sa intestine) → Magnesium
hydroxide (diarrhea effect) combined with
aluminum hydroxide (constipation effect)
2. Stomach Cramps
3. Nausea
4. Vomiting
--> Quality Control/Packaging
● Appearance: ​White, viscous liquid
● pH:​ 5.5-8
● Pourability: ​Easily pourable
● Redispersability:​ Easily dispersed upon
shaking
● Particle dispersion: ​White gelatinous
precipitate
● Physical stability: ​No syneresis
(c​ ontraction of a gel accompanied by the
separating out of liquid),​ microbial growth,
sedimentation and caking present
● Packaging requirement: Preserve in tight
containers and avoid freezing
● Label: ​“Shake well before use” “Do not
freeze”
● Container: ​15mL clean flint bottle
--> Characteristics of Gels
1. Imbibition
- The taking up of a certain amount of liquid
without a measurable increase in volume.
2. Swelling
- The taking up of a liquid by a gel with an
increase in volume
*Only liquids that solvate a gel can cause
swelling
* pH and presence of electrolytes influence
swelling
3. Syneresis
- On standing, the dispersion medium is
squeezed out and the gel shrinks due to the
attraction between particles of the
dispersed phase
4. Xerogel
- Formed when liquid is removed from the
gel, only framework remains
- Ex: Gelatin sheets, tragacanth ribbons,
and acacia tears
5. Thixotropy
- Reversible gel-sol (on standing -
semisolid, shake- colloid) (ex: ketchup)
- formation with no change in
volume or temperature, a type of
non-Newtonian flow
 Preparation 21: Bentonite Magma ​Preparation 22: Calamine lotion

● Offi. title: ​Bentonite Magma, NF
● Category: ​-
● Uses:​ Suspending agent for
insoluble medicaments (Calamine
Lotion)
● Synonyms: ​Native Colloidal
Hydrated Aluminum Silicate
(NCHAS), Magma Bentoniti (Latin
name), Mineral soap magma,
Wilhinite Soap Clay Magma
● Offi. def’n: ​a preparation of ​5%
bentonite,​ a native colloidal hydrated
aluminum silicate, in purified water.
--> Review of basic concepts
Bentonite Magma
- Composed of 5% bentonite, a native
colloidal hydrated aluminum silicate, and
purified water.
Dispersed systems (Magma)
- It is a dispersion of an exceptional
insoluble particles.
● Offi. title: ​Calamine Topical lotion, USP
● Category: ​Antipruritic (relieve itching),
Astringent (​causing the contraction of
skin cells and other body tissues.)
● Uses:​ Astringent, antipruritic, topical
protectant and soothing lotion to sunburn,
treatment for ivy poisoning, skin
protectant
● Synonyms: ​Native Colloidal Hydrated
Aluminum Silicate (NCHAS), Magma
Bentoniti (Latin name), Mineral soap
magma, Wilhinite Soap Clay Magma
● Offi. def’n: ​Usually are fluid, somewhat
viscid (sticky) suspension dosage forms
for external application to the skin.
→ Review of Basic components
Suspensions
-liquid preparations that contain solid particles
dispersed in a liquid vehicle intended for
application to the skin. Some suspensions
labeled as ‘‘Lotions’’ fall into this category

Milk & Magmas

Lotions Magmas/Milks Gels
- Gel that has a large dispersed phase
particle mass Liquid or Aqueous A.k.a jellies
semisolid suspensions
Lotion prep that of insoluble, Semisolid
- Aqueous suspension of solid that are contain one inorganic systems
applied to the parts of the skin that are not or more drugs that consisting of
damaged active have larger either
ingredients particle size. suspension
Gels in an Thick and made up of
- Semisolid systems that have a dispersions appropriate viscous and small inorganic
composed of either small inorganic particles vehicle does not particles or
or large organic molecules that are being need a large organic
enclosed and interpreted by liquid suspending molecules
agent interpenetrated
--> Use of each ingredient in the prep: by a liquid
1. Bentonite
- Active ingredient
- Clays frequently generated by altering Bentonite magma
volcanic ash - 5% bentonite
- Consists of predominant smectite - Native colloidal hydrated aluminum silicate, in
minerals, that are montmorillonite purified water
2. Purified water Preparation of bentonite magma
- Dispersing medium
- Solvent Mechanical Simple hydration

--> Two methods to prepare Bentonite - Prepared in a - Prepared also by

Magma blender with the sprinkling the
1. Mechanically bentonite added bentonite, in portions,
- First method done w/ the use of a blender directly to the purified upon hot purified
- Bentonite should be directly added to the water while the water, allowing each
H2O while blender is turned on machine is running. portion to be
2. Simple hydration thoroughly wetted
- Used when by scattering the bentonite in without stirring before
different portions, upon adding a hot another portion is
purified water, making every part wet w/o added.
the need to stir, before adding another
portion
- Scattering Tests to assess the quality of Bentonite
- Mixture needs to stand for 24 hours before magma
stirring
Swelling Test Tests the property of
- Swelling
swelling.
--> Procedure and Reasons for
important steps Required mass at the
* Smooth slurry is obtained bottom should occupy
*15 mL magma is needed an apparent volume
*Stand for 5 - 15 minutes before use
not less than 24mL.
Swelling test
pH Test Tests the pH level.
- 2 g of bentonite should be added in
portions of 100 mL water to a 100 mL
glass-stoppered cylinder pH must be not less
- The mass at the bottom should inhabit a than 9.5 but not more
volume of not below 24 mL than 10.5.
- assess quality of bentonite magma
Fineness of Powder Tests the quality of
pH test the powder.
- Should be between 9.5 to 10.5
Particle size should
Fineness of powder
- Particle size between 1 nanometer to 0.5 be 1nm – 0.5um
micrometer
Gel Formation Tests the gel
Gel Formation transition.
- When the bentonite magma is able to
stand peacefully for some time, it forms gel After standing;
(Thixotropic gel) thixotropic gel
- When agitated, its sol form comes back
(semisolid)
--> Quality Control
● Appearance: ​Grayish turbid slurry mixture Upon agitation; sol
● pH: ​9.5 - 10.5 form (liquid/colloid)
● Pourability: ​Not Easily Pourable
● Redispersability: ​Difficult to disperse upon
shaking
● Particle Description: Colloidal (1 nm - 5
micrometer)
● Sedimentation rate: ​Very slow to none
● Physical stabilities: ​No microbial growth
presence, no organic volatile impurities
--> Packaging, Labeling and Storage
● Packaging:
○ Preserve in tight containers
● Label:
○ “Shake Well Before Use”
● Storage requirement:
○ Store in a cool dry place (must not be
freezed)
--> Additional notes:
*Swells up to 12 times when water is added
*if it lowers down to 7, the suspending
agent lowers --> select an alternative
suspending agent
--> Use of ingredients
1. Calamine: ​Active ingr, antipruritic and
astringent
2. Calcium hydroxide: ​Provides astringent
action, dispersion medium; dissolves
bentonite magma and zinc oxide
3. Zinc oxide: ​Provides Astringent action;
Anti microbial; Mixed with calamine to
give its pink color
4. Glycerin: ​Humectant, emollient, wetting
agent
5. Bentonite magma: ​Stabilizing and
suspending Agent
--> Procedure and Reasons for Important
Steps
1. Dilute 2.5 mL Bentonite Magma with an equal
volume of Calcium Hydroxide Topical Solution
2. Mix the powders intimately with the 0.2 mL
Glycerin and about 1 mL of the diluted magma
3. Triturating until a smooth, uniform paste is
formed.
RFIS: I​ntimately mix ingredients to form
uniform particle size.
4. Gradually incorporate the remainder of the
diluted magma
RFIS: ​To​ prevent air​ from being incorporated
(solidifies diluted magma)
5. Finally add enough Calcium Hydroxide
Topical solution to make 10 mL, and shake
--> Quality Control/Packaging
● Appearance: ​Pink, thick, creamy semi liquid
● pH:​ 9-10
● Pourability:​ Not Easily pourable
● Sedimentation rate: ​Very slow to none
● Physical stability: ​No sedimentation, caking
and microbial growth present
--> Packaging, Labeling and Storage
● Packaging:
○ Preserve in tight containers
● Label:
○ “Shake Well Before Use”
● Container:
○ 15 mL clean flint bottle
--> Additional notes
*other synonyms: Lotio Calaminae, Caladryl,
calmoseptine
Narrow mouth amber bottle
 Zinc oxide yung astringent

Preparation 23: White Ointment ​-----

● Offi. title: ​White Ointment, USP

● Category: ​Pharmaceutical
Necessity
● Uses:​ vehicle, emollient
● Synonyms: ​Ointment USP, Simple
Ointment
● Offi. def’n: ​White ointment is an
ointment consisting of 5% white wax
and 95% of white petrolatum

--> Review of basic concepts

Semi-solid dosage forms
- Includes ointments, creams, gels, pastes,
plasters and glycerogelatins
- Ointments are semi solid prep intended for
external application to the skin or mucous
membrane

--> Types of Ointments

1. Medicated
- Contain ​medicament​ either dissolved or
dispersed in the vehicle as fine powders or
in form of micronized powder

2. Non medicated
- ​Vehicles ​for prep or medicated ointments
or can be used for their physical effect

--> Properties
a. Non sensitizing
b. Water washable
c. Non irritating
d. Permanent, pliable, smooth
e. Efficient release of medicament at
site of application

--> Types of ointment bases

a. Oleaginous bases
b. Absorption bases
c. Water removable bases
d. Water soluble bases

A. Oleaginous bases

---Properties:
○ Hydrophobic
○ Occlusive (​To close, obstruct, or prevent
the passage; ​increase moisture​ levels in
skin by providing a physical barrier to
epidermal water loss​)
○ Emollient effect (​having the quality of
softening or soothing the skin​)
○ Allows incorporation of small quantity
aqueous solutions or hydrophilic agents

---Advantages
○Remains on the skin without drying out for
a period of time
○Provides the best emollient and occlusive
property

---Disadvantages
○ Stains on clothes
○ Hard to wash off
○ Greasy

---Examples
○ Petrolatum, USP
○ White Petrolatum, USP
○ Yellow Ointment, USP
○ White Ointment, USP

B. Absorption bases

---Properties:
○ Less occlusive
○ Emollient effect
○ Allows incorporation of small quantity
aqueous solutions or hydrophilic agents

---Advantages
○ Can be used as vehicle for drugs that are
not stable in aqueous environment
○ Used for incorporation and aqueous
components to hydrocarbon bases

---Disadvantages
○ Stains on clothes layer
○ Hard to wash off because of external
hydrocarbon layer
○ Greasy

---Examples
○ Hydrophilic petrolatum
○ Lanolin, USP
○ Aquaphor - refined hydrophilic petrolatum;
takes up 3 times of its weight in water;
medication is used as a moisturizer to treat
or prevent dry, rough, scaly, itchy skin and
minor skin irritations

C. Water removable bases

---Properties:
○ Contains ​hydrophilic and lipophilic
compounds
○ Can be diluted with water
○ Most commonly used base
○ Has resemblance to creams because of
its oil in water property

---Advantages
○ Washable with water because of its
aqueous external phase
○ Faster release rate of drug when applied

---Disadvantages
○ Not occlusive

---Examples
Hydrophilic ointment, USP

D. Water soluble bases

---Properties:
○ Used for better incorporation of solids and
non aqueous substance in which large
amounts of aqueous solutions are
effectively incorporated

---Advantages
○ Water washable
○ Greaseless

---Disadvantages
○ Not occlusive

---Examples
○ Polyethylene Glycol Ointment, NF

Water number
○ Defined as the number of water in grams
that can be incorporated into 100 g base
without losing its consistency

--> Formula
White Wax (0.5 g): Stiffening agent
White petrolatum (9.5g): ointment base -->
oleaginous base
--> Procedure
1. Melt the white wax in a suitable dish
in a warm water bath of 60-70
2. Add white petrolatum when wax has
completely melted
3. Continue heating until liquefied
4. Remove from the heat, stir

--> Methods of Preparation

1. Incorporation

A. In solid
○ An amount of ointment approximately
equal in size to the drug is added to the
drug
○ Spatulate the mixture
○ By geometric dilution, add the ointment
continuously until all of it is consumed

RFIS:
1. With mortar and pestle or with a
spatula and ointment slab, the
incorporation process is done. If the
parts to be used react with metals
2. To ensure even distribution in the
base, Geometric dilution is
performed
3. The production of a gritty substance
would be prevented by reducing
particle size

B. In liquid
○ The aqueous solution is incorporated into
a small amount of hydrophilic base. The
mixture will then be added to the
hydrophobic bases

RFIS:
Before incorporation, the capacity of the
base to absorb liquids should be determine

2. Fusion

- Components with the​ highest

melting point are melted first
- Other components must be added
next
- Uses porcelain dish and heat
involved
- White wax has higher melting point
than white petrolatum thus, it will be
the first one to be melted

RFIS:
 1. Heat labile and volatile
components are added last
2. Decomposition (broken down into
simpler organic or inorganic matter)
can be prevented if components are
not exposed to high temperature
areas

--> Quality Control

Appearance: viscous, semisolid
preparations containing either dissolved or
suspended ingredients

Label: For external use only

- Keep out of reach of children
- In addition to labeling requirements,
USP direct that it must also include
type of base used

Pourability: Not pourable

Physical Instability:
- Changes in particle size,
consistency
- Coalescence
- Bleeding​ - fluid components of prep
separate at the top of the ointment
- Change in drug release rate
- Loss of drug content uniformity
- Formation of granules or grittiness
(having a rough texture)

--> Packaging, Labeling and Storage

Packaging and packaging:
- Must be stored in large mouth of
ointment jar, metals or plastic tubes
- In well closed containers to protect
against contamination
- In cool place to protect against
product separation due to heat

ADDITIONAL NOTES:

1. Occlusion - it traps water in the skin,

preventing evaporation or absorption into
the occlusive material.

2.Humectant - it increases water holding

capacity of the stratum corneum.

3.Lubrication - adding slip or glide on the

surface of the skin.

4. Emollient - Soften or soothe the skin by

 filling spaces between skin flakes and
creating a smooth skin surface

Oleaginous Absorption Water/Oil Oil/Water Water-miscible

ointment Bases Ointment Emulsion Emulsion /Water soluble
Bases Ointment Ointment Ointment
Bases Bases Bases

Composition Oleaginous Oleaginous Oleaginous Oleaginous base Polyethylene

compounds base + w/o base + water + water (>45% Glycols (PEGs)
surfactant (<45% w/w) + w/w) + o/w
w/o surfactant surfactant (HLB
(HLB <= 8) >= 9)

Water Content Anhydrous anhydrous hydrous hydrous anhydrous,hydr

ous

Affinity for Hydrophobic hydrophilic hydrophilic hydrophilic hydrophilic

water

Spreadability Difficult Difficult Moderate to Easy Moderate to

easy easy

Washability Nonwashable Nonwashable Non- or poorly Washable Washable

washable

Stability Oils poor; Oils poor, Unstable, Unstable, Stable

hydrocarbons hydrocarbons especially alkali especially alkali
better better soaps and soaps and
natural colloids natural colloids;
nonionics better

Drug Solids or oils (oil Solids, oils, and Solids, oils, and Solids and Solids and
Incorporation solubles only) aqueous aqueous aqueous aqueous
Potential solutions (small solutions (small solutions (small solutions
amounts) amounts) amounts)

Drug release poor Poor, but > Fair to good Fair to good Good
potential oleaginous

Occlusiveness yes yes sometimes no no

Uses Protectants, Protectants, Emollients, Emollients, Drug vehicles

emollients (+/-), emollients (+/-), Cleansing vehicles for
vehicles for vehicles for creams,vehicles Solid, liquid , or
hydrolyzable aqueous for Solid, liquid , non hydrolyzable
drugs solutions, or non drug
solids, and non hydrolyzable
 hydrolyzable drug
drugs

Examples White Hydrophilic Cold cream Hydrophilic PEG ointment

petrolatum, petrolatum, type, Hydrous Ointment,
White ointment, Anhydrous Lanolin, Rose Dermabase,
yellow ointment Lanolin, Water Ointment, Velvachol,
Aquabase, Hydrocream, unibase
Aquaphor Eucerin, Nivea
Polysorb

General review of basic concepts

Semisolid Dosage forms

● Drug category consisting of semisolid products
● Intended for ​topical application
● Can also be applied to the are medicated or non ​ mucous membranes of the body
● Are medicated or non medicated
○ Non-medicated - physical effects as protectants or lubricants
● Local and systemic effects
○ Local - kung san lang nilagay un lang mag eeffect
○ Systemic - kumakalat

Creams vs ointments vs Pastes

Creams Ointments Pastes

Semisolid Semisolid Semisolid

preparations preparations preparations
containing one intended for intended for
or more external application to
medical agents application to the skin
dissolved or the skin or
dispersed in mucous Contain a
either W/O membranes, larger
emulsion, an and can be percentage
O/W emulsion, medicated or (up to 25%)
or in another non of solid
type of water medicated material​ than
washable base ointments.

*creams are more prefer can be easily applied and remove

*non medicated - as protectants, lubricants and sometimes as emollient

Definition of Concepts

A. Gels: ​Semisolid systems ​consisting of dispersions in an aqueous liquid vehicle

rendered jelly like due to the addition of a gelling agent; ​a.k.a. jellies
 B. Plasters: ​Solid or semisolid adhesive masses​ spread on a backing of paper, fabric,
moleskin or plastic
C. Powders:​ ​Dry mixtures of finely divided ​medicinal and ​non medicinal agents
intended for ​internal or external use
D. Dressings: ​Products​ for external application​ that​ resemble ointments​ and are used
for covering for protection
*can be used as a topical antibiotic dressing
(ex: antibacterial dressings: neomycin sulfate for burns)
E. Glycerogelatins: ​Plastic masses ​containing gelatin (15%), glycerin (40%), water
(35%), and an added medicinal substance (​10%) such as​ zinc oxide;​ These are
applied to the ​skin​ for long term application.
F. Cataplasms: ​Consist of a ​soft, moist mass of absorptive materials​; are also called
poultices​, and are intended ​to localize infectious materials in the body
G. Contraceptives: ​Drug products that ​immobilize spermatozoa or prevent ovulation
*immobilize spermatozoa: gellies, creams and aerosols,
*prevent ovulation: Capsules or tablets

Preparation 24: Sulfur Ointment Preparation 25: Zinc Oxide Preparation 26: Hydrophilic
Paste Ointment

● Offi. title: ​Sulfur Ointment, USP
● Category: ​Parasiticide ​(used in
medicine and veterinary medicine
to kill parasites; especially those
other than bacteria or fungi)
● Uses:​ Parasiticide, Keratolytic
(remove warts, calluses and other
lesions in which the epidermis
produces excess skin)​, Used in
the treatment of skin diseases
such as psoriasis and seborrhea
*can be an alternative treatment for
scabies
● Synonyms: ​Unguentum Sulfuris,
Precipitated Sulfur Ointment, Lae
Sulfuris Ointment
● Offi. def’n: ​“Sulfur Ointment
contains not less than 9.5 percent
and not more than 10.5 percent of
Sulfur.”
--> Uses of each ingredient
1. Precipitated sulfur - Active
ingredient
2. Mineral Oil - Levigating agent
(improve ease of wetting the
solid); ​not use as a humectant
● Offi. title: ​Zinc Oxide
Paste, USP
● Category: ​Topical Drug
● Uses:​ Mild astringent,
Antiseptic, Used in
treatment for ivy
poisoning, seborrhea,
eczema, psoriasis, and
pruritus.
● Synonyms: ​Lassar’s Plain
Zinc Paste
● Offi. def’n: ​“Zinc Oxide
Paste contains not less
than 24.0 percent and not
more than 26.0 percent of
ZnO.”
--> Uses of each ingredient
--> Uses of each ingredient
1. Zinc Oxide: Active
ingredient; specifically
protective, antiseptic,
astringent
2. Starch: Binding agent,
thus will make it firm as
well
3. White petrolatum:
Ointment base =
oleaginous base
● Offi. title: ​Hydrophilic
Ointment, USP
● Category: ​Pharmaceutical
necessity
● Uses:​ water removable
ointment base
● Synonyms: ​Lassar’s Plain
Zinc Paste
● Offi. def’n: ​A water-miscible
ointment base for topical
application, composed of a
traditional water-in-oil
emulsion containing
petrolatum and propylene
glycol
1. Methylparaben and
Propylparaben:
Anti-microbial agent
Methylparaben - anti yeast
Antiparaben - anti molds
2. Sodium Lauryl Sulfate: Main
emulsifying agent;
Emulsifier or Surfactant
3. Propylene Glycol:
Humectant
4. Stearyl Alcohol: Stiffening
agent (assist lang siya as
 3. White Ointment - Hydrocarbon
base/oleaginous base
Both levigating agent and wetting agent
mean the same thing and their purpose is RFIS:
to decrease the surface tension between
two ingredients. There are two major
types used in non-sterile compounding.
Glycerin is preferred when an
oil-soluble base is used, while Mineral
Oil is used for water-soluble bases
--> Procedure
1. Levigate 1 g of sulfur with the 1 g of
mineral oil to a smooth paste.
a. Sulfur is first levigated ​in mineral
oil to aid in incorporation.
b. Practice geometric dilution during
incorporation to ensure uniform
distribution and dosage.
c. When levigating, ensure that
there are no visible particles, and
levigate in a figure of 8 pattern.
2. Incorporate with 8 g of white ointment.
--> Quality Control
A. Appearance:
Yellow Homogeneous solid
B. Texture
Surface: Smooth Non-gritty
Spatula spread: Smooth; Non-gritty
C. Feel
Greasiness: Greasy
Water washability: Non water washable
Stiffness: Slightly stiff
Solid Content: Moderate amounts of solid
present.
--> Acceptance Criteria
a. Physical stability: No change in
consistency, coalescence,
bleeding (separation of excessive
amount of fluid), drying out, and
rancidity-- ​spoilage of a food in
such a way that it becomes
--> Procedure
1. Mix the 2 g of Zinc Oxide,
1.5 g of starch and 6.5 g of
white petrolatum
a. Trituration of zinc oxide
and starch = The goal is to
achieve a small particle
size​ in order to deliver a
great amount of
therapeutic activity
*lower particle size = higher
surface area
b. Levigation of mixed
powders w/ petrolatum:
Add the homogeneous
mixture in ​small
increments
We have to make sure
that we ​levigate the first
addition first before
adding more to make
sure that it is distributed
equally.
--> Quality Control
A. Appearance
White homogeneous solid
B. Texture
Surface: Smooth Non-gritty
Spatula spread: Smooth;
Non-gritty
C. Feel
Greasiness: Greasy
Water washability: Non water
washable
Stiffness: Stiff
Solid Content: Large amounts of
solid present.
--> Acceptance Criteria
a. Physical stability: No
change in consistency,
emulsifying if sumobra to =
crystallization)
5. White Petrolatum:
Hydrocarbon base
6. Purified Water: Solvent
--> Procedure
1. Melt 2.5 g stearyl alcohol and 2.5
g white petrolatum on a 75° C
steam bath. (optimum temp to
make emulsion as well)
RFIS:
a. Add stearyl alcohol first to
avoid decomposition.
b. Maintain 75° C temperature
to avoid decomposition of
the oils and to prevent
pre-solidification of the
aqueous components.
c. Perform constant stirring to
avoid waxing
2. Add the 0.0025 g MP, 0.0015 g
PP, 0.1 g SLS, 1.2 g PG, 2.5 g SA
previously dissolved in 3.7 mL
water and warmed to 75° C.
3. Stir the mixture until it congeals.
--> Quality Control
A. Appearance
White, opaque, and homogeneous
semisolid.
D. Texture
Surface: Smooth Non-gritty
Spatula spread: Smooth; Non-gritty
E. Feel
Greasiness: Greasy
Water washability: Non water
washable
Stiffness: Moderately stiff
Solid Content: Very few amounts of
solid present.
 undesirable (and usually bleeding, and drying out; --> Acceptance Criteria
unsafe) for consumption​; there liquefaction (instability) 1. Physical stability: No
could also be microbial growth change in consistency,
--> Packaging coalescence, bleeding,
--> Packaging 1. Packaging requirement: drying out, rancidity and
1. Packaging requirement: Preserve in well closed microbial growth;
Preserve in well closed container container and avoid crystallization (instability)
and avoid prolonged exposure to prolonged exposure to
direct heat. temperatures exceeding --> Packaging
2. Label: ​“For external use only” 30 degrees. 1. Packaging requirement:
3. Container: ​Large-mouth, plastic 2. Label: ​“For external use Preserve in tight containers
ointment jar only” 2. Label: ​“For external use
3. Container: ​Plastic only”
--> Basic tests for ointments ointment jar 3. Container:​ Large-mouth,
Plastic ointment jar
Test Procedure
Additional Notes:
Test of Rate of The test is If the preparation exceeds 30
Absorption performed in-vivo​, degrees celsius
*Discoloration = yellow,
applying the
ointment through lumping
rubbing over a *Liquefaction
definite area of
the skin.​ Over
several periods of
time, the ​urine
and serum
samples are
analyzed for the
quantity of drug
absorbed​. The
rate of absorption
should be
compliant to the
standards set.

Test of A ​definite quantity

Non-Irritancy of ointment​ is
applied ​under
occlusion daily on
the back or
forearm.​ There
should be ​no
visible reaction
such as
erythema in the
area of
application.

Test of Rate of A ​weighed

Penetration quantity of the
preparation is
 applied to a
selected area of
the skin for a
definite period of
time. ​The
remaining
preparation is
weighed and
compared with the
initial quantity.
The value
obtained ​is
divided by the
area and time,
resulting in the
rate of penetration
of the ointment.

Test of Rate of To assess the ​rate

Drug Release of medicament
release,​ a small
amount of the
ointment is placed
on a petri dish
with nutrient agar.
If the medicament
is bactericidal, the
plate is previously
seeded with
suitable
organisms ​such
as S. aureus.
After a period of
incubation, the
zone of
inhibition ​is
measured and
correlated with the
rate of release.

Test of The ​viscosity of

Rheological the preparation
Properties should be
sufficient​ to be
easily removed
from the container
and easily applied
to the skin. ​This
test is performed
using a cone and
plate viscometer.

Test of Content The ​net weight of

Uniformity ten filled ointment
containers ​are
determined. The
results should
match each other
and the labelled
quantity.

Test of The pour plate

Preservative technique is used
Efficacy in determining the
initial number
of microorganisms
present​ in the
preparation.
Solutions of
different samples
of the preparation
are mixed with
Tryptone
Azolectin
(TAT) broth.
These are
inoculated with
the cultures, and
are incubated for
some time. O​n the
14th day, the
number of
vegetative cells
must not be more
than 0.1% of the
initial
concentration.
After 28 days, the
number of
microorganisms
should be below
or equal to the
initial
concentration.

--> USP TESTS

Test Description

Microbial Content Semisolid

Screening preparations are
required to be free
from any microbial
contamination.
The USP states
 the microbial limits
for certain articles.
In the chapter
entitled
“Microbiological
Attributes of
Nonsterile
Pharmaceutical
Products”,
emphasis is
placed on the
strict adherence to
environmental
control and
application of
good
manufacturing
practices​ to
minimize both the
type and number
of microorganisms
in unsterilized
pharmaceutical
products. ​Most
topical ointments
are screened for
the presence of
Staphylococcus
aureus and
Pseudomonas
aeruginosa.

Minimum Fill This test is

performed to
compare the
weight or volume
of a product filled
into each
container with
their labeled
weight or volume.
It helps in
assessing the
content uniformity
of a product. ​The
minimum fill test is
only ​applicable to
containers that
contain not more
than 150 mg or
mL of the
preparation.​ The
USP recommends
 that the average
net content of 10
containers should
not be less than
the labeled
amount.

Assays The quantity of a

drug present in a
unit weight of
ointment can
be determined by
various methods.
These methods
can be in ​the form
of
spectrophotometr
y, titrimetry,
chromatography,
or in some cases,
microbial assays.
While the
selection of a
method is
dependent on
several factors
such as the nature
of the drug,​ the
USP recommends
that
High-Performance
Liquid
Chromatographic
(HPLC) ​assays for
most ointments
due to its
specificity,
accuracy, and
precision.
Microbial assays
are recommended
for preparations
with antibiotics.

Storage and The USP

Labelling recommends
packaging and
storage
requirements for
each official
ointment and
cream. ​For
ointments, these
 are generally
packaged in tight
or well-closed
containers stored
at a cool place or
at controlled room
temperature.​ In
some cases,
special storage
conditions are
recommended, for
example, protect
from light, avoid
exposure to direct
heat, avoid direct
exposure to
sunlight, etc.

As discussed, unlike Zinc Oxide Paste and Sulfur Ointment,

Hydrophilic Ointment, USP does not have any active ingredient
incorporated. It is a specific example of a Water-Removable Base.
To make Hydrophilic Ointment, we make use of White Petrolatum
which is a hydrocarbon/oleaginous base. White petrolatum does not
function as an adjuvant, however, the presence of an emulsifying
agent like SLS facilitates the mixing of our oleaginous phases
(White Petrolatum and Stearyl Alcohol) + aqueous phase
(propylene glycol and water)