POWDERS AND GRANULES
-does not irritate the skin when applied
Powders vs Granules
-a.k.a pulvis
-mixtures of finely divided drugs and/or chemicals used
externally or internally in dry form.
Granules
- Granules are prepared agglomerates of powdered
materials.
-Typically fall within the range of 4- to 12-sieve size
POWDERS
Composition
- Powders are more stable than are liquid dosage forms
and are rapidly soluble, enabling the drug to be
absorbed quickly.
- should be dispensed in tight containers.
-Small particle size in a greater surface area to the
atmosphere= reactive and can absorb large quantities
of gases.
-increase in surface free energy = increase the absolute
solubility of the drug = positive bioequivalence
Historical use
-Convenient mode of administering drugs derived from
hard vegetables
-Example: roots-rhubarb
Barks-cinchona
Woods-charcoal
-Synthetic drugs: Powders were used to administer
insoluble drugs
-Example: calomel, bismuth salts, mercury, and chalk.
Medicated powders
1. Powdered fillers and other pharmaceutical
ingredients to fabricate solid dosage forms as
tablets and capsules
2. Dissolved or suspended in solvents or liquid
vehicles to make various liquid dosage forms
3. Incorporated into semisolid bases in the
preparation of medicated ointments and
creams.
4. Aerosol powders
-administered by inhalation with the aid of dry
powder inhalers (DPIs), which deliver
micronized particles of medication in metered
quantities.
-requirements of Aerosol products will be
discussed later
Topical powders
>should easily adhere to the skin
>should not be passed through at least a No.
100-mesh sieve = minimize skin irritation
-usually consist of:
> base or vehicle: cornstarch or talc;
>adherent: such as magnesium stearate,
calcium stearate, or zinc stearate;
> active ingredient
> aromatic material.
Insufflated powders
-intended to be applied in a body cavity, such as the
ears, nose, vagina, tooth socket, or throat.
-Insufflator or puffer:
>the patient simply “puffs” the desired quantity
of powder onto the affected area or into the
cavity.
>Anti-infectives
>Incorporated with, a moisture-activated
adherent
E.g.: Polyox- ethylene oxide polymer
with a high molecular weight that forms
a viscous, mucoadhesive gel when in
contact with moisture.
Powder fineness
Vegetable and animal drugs
 Very coarse (No. 8): All particles pass
through a No. 8 sieve, and not more than
20% pass through a No. 60 sieve.
 Coarse (No. 20): All particles pass through
a No. 20 sieve, and not more than 40%
pass through a No. 60 sieve.
 Moderately coarse (No. 40): All particles
pass through a No. 40 sieve, and not more
than 40% pass through a No. 80 sieve.
 Fine (No. 60): All particles pass through a
No. 60 sieve, and not more than 40% pass
through a No. 100 sieve.
 Very fine (No. 80): All particles pass
through a No. 80 sieve. There is no limit
to greater fineness.

Different factors which are influenced by particle size
(one per slide)
1. Dissolution rate of particles intended to dissolve
- drug micronization can increase the rate of
drug dissolution and its bioavailability.
2. Suspendability of particles intended to remain
undissolved but uniformly dispersed in a liquid
vehicle (e.g., fine dispersions have particles ~0.5
to 10 μm)
3. Uniform distribution of a drug substance in a
powder mixture or solid dosage form to ensure
dose-to-dose content uniformity
4. Penetrability of particles intended to be inhaled
for deposition deep in the respiratory tract (e.g.,
1 to 5 μm)
5. Lack of grittiness of solid particles in dermal
ointments, creams, and ophthalmic preparations
(e.g., fine powders may be 50 to 100 μm in size)
Different methods by which particle size can be
determined
 Sieving
- particles are passed by mechanical shaking
 Microscopy
- particles are sized through the use of a
calibrated grid background or other measuring
device (range 0.2 to 100 μm)
 Sedimentation rate
-particle size is determined by measuring the
terminal settling velocity of particles through a
liquid medium in a gravitational or centrifugal
environment (range 0.8 to 300 μm).
 Light energy diffraction or light scattering
- particle size is determined by the reduction in
light reaching the sensor as the particle, dispersed
in a liquid or gas, passes through the sensing zone
(range 0.2 to 500 μm)
 Laser holography
-a pulsed laser is fired through an aerosolized
particle spray and is photographed in three
dimensions with a holographic camera
 Cascade impaction
-which is based on the principle that a
particle driven by an airstream will hit a
surface in its path, provided its inertia is
sufficient to overcome the drag force that
tends to keep it in the airstream.
 Online methods for determining particle
sizes during production are available
COMMINUTION OF DRUGS (put pictures)
Small scale
-extemporaneous; done by the order of the physician
Trituration or comminution
-grinding a drug in a mortar to reduce
its particle size.
Levigation
-the process of reducing particle size by
1. Forming a paste of the solid with a
minimum amount of a levigating agent
(Mineral oil and glycerin)
2. Triturating the paste in a mortar or on
slab with a spatula
- used to reduce particle size of ointments
and suspensions and grittiness of the added
powders.
Large scale
-uses mills and pulverizers
Example: FitzMill comminuting machine with a product
containment system
-particles are reduced in size and passed through a
screen of desired dimension to the collection container
through the grinding action of the rapidly moving
blades in the comminuting chamber.
DIFFERENT METHODS OF MIXING POWDERS (insert
pictures)
 Spatulation
- blending small amounts of powders by
movement of a spatula through them or on an
ointment tile.
- For eutectic mixtures
 Trituration
- comminute and to mix powders
-Uses mortar and pestle if there is no special
need of comminution.
 - geometric dilution is used when a small
amount of potent substance is to be mixed with
a large amount of diluent.
 Sifting
- powders are mixed through passing them to
sifters.
- Uniform mixing of drug products
- Not acceptable for the incorporation of potent
drugs into a diluent powder.
 Tumbling
-powder that is mixed in a rotating chamber.
- time consuming.
 Geometric Dilution
- the potent drug is placed with an
approximately equal volume of the diluent in a
mortar and mixed thoroughly by trituration.
- ensure the uniform distribution of the potent
drug.
DIFFERENT ROUTES OF ADMINISTERING MEDICATED
POWDERS
 Most powders are taken orally after mixing
with water.
 Some powders are inhaled for local and
systemic effect.
 Other dry powders are commercally packaged
for constitution with a liquid solvent or vehicle
some for administration orally, some us it as an
injection and vaginal douche.
ADVANTAGES AND DISADVANTAGES OF POWDERS
 Advantage:
- faster rates of dissolution and absorption than
solid dosage forms
-immediate contact with the gastric fluids.
- Flexibility of compounding
- Good chemical stability
 Disadvantage:
- Undesirable taste of the drug
- Time consuming preparation
- Inaccuracy of dose
HYGROSCOPIC VS. DELIQUESCENT VS EFFLORESCENT
POWDERS
Hygroscopic powders will absorb moisture from the air.
Deliquescent powders will absorb moisture from the air
to the extent that they will partially or wholly liquefy.
Efflorescent powder (Table 6.4) is a crystalline powder
that contains water of hydration or crystallization.
REQUIREMENTS OF AEROSOL PRODUCTS
-used in the treatment of asthma and other bronchial
disorders that require distribution of medication deep
in the lungs.
-To accomplish this, the particle size of the micronize is
prepared in the range of 1 micrometer in diameter.
- Crystalline Alpha-lactose monohydrate
- an inert propellant and pharmaceutical diluent
-aid the fomulation’s flow properties and
metering uniformity and to protect the powder
from humidity.
BULK POWDERS
 Antacids - sodium bicarbonate and laxatives
(psyllium) which the patient takes by mixing
with water or another beverage before
swallowing (do not include description in
the ppt, use index cards)
 Douche powders - dissolved in warm water
by the patient for vaginal use
example: Massengil powder
 Medicated powders for external
application to the skin
examples:
- topical anti-infectives (bacitracin
zinc and polymyxin B sulfate)
- antifungals (tolnaftate)
 Brewer's yeast complex vitamins and other
nutritional supplements
DIVIDED POWDERS
-Each divided portion of powder may be placed on a
small piece of paper that is folded to enclose the
medication.
-Latin - Chartulae, Abbr. “charts” or chartula
-Method used is called “block and divide”
 Some commercially prepared
premeasured products available in
folded papers or pockets:
- headache powders
- powdered laxatives (psyllium
mucilloid, cholestyramine resin)
- douche powders (massengill
powder packets)
 Examples of Finely Divided Powders:
- Oral powders are supplied as finely divided powders or
as effervescent granules
- Douche powders, generally dissolved in warm water
for vaginal use
- Medicated or non medicated powders for external
application usually dispensed in sifter cans for
convenient application to the skin
- Dentifrices or dental cleansing powder
- Denture powders, for dentifricesor for adhesive to
hold dentures
ADVANTAGES OF DIVIDED POWDERS:
•Flexibility
•Rapid therapeutic effect.
•Stability
•Ease of administration
DISADVANTAGES OF DIVIDED POWDERS:
•Time consuming to prepare
•Not well suited for dispensing of many
unpleasant tasting hygroscopic drug.
•Inaccuracy
Block and divide- For non-potent drugs
Steps:
1. Triturate all the powders.
2. Mix the powders.
3. Place the mixed powders in a flat surface (can be a
porcelain or glass plate, pill tile or a large sheet of
paper).
4. Using a spatula, form a square or rectangular block
of the powder having a uniform depth.
5. Cut into the powder lengthwise and crosswise to
delineate the appropriate number of smaller,
uniform blocks
TWO WAYS OF PREPARING GRANULES USING:
a) Wet method
>Basic wet method
Triturate the powders -> Mix the powders ->
moisten the powder mix -> pass through a sieve
-> oven drying
>Fluid bed processing
1. Powders are placed inside a conical piece
equipment.
2. The powders are vigorously dispersed and
suspended while a liquid excipient is
sprayed on.
3. The product dries forming granules.
b) Dry method
- Dry powder is passed through a roll compactor ->
then through a granulating machine.
- The roll compactor processes a fine powder into
dense sheets by forming it through two
mechanically rotating metal rolls running counter
to each other.
 Alternative dry method or slugging
o Compression of powder or powder
mixture into large tablets or slugs on a
compressing machine under 8000 to
12000 lbs. of pressure.
CHARACTERISTICS OF GRANULES WHICH ARE
ADVANTAGEOUS OVER POWDERS
- Granules flow well compared to powders
- Granules are more stable to the effects of
atmospheric humidity and are less likely to cake or
harden upon standing
- Granules are more easily wetted by liquids than
certain light and fluffy powders
CHEMICAL COMBINATION PRESENT IN EFFERVESCENT
GRANULATED SALTS
 Sodium bicarbonate, citric acid, tartaric acid
 Citric acid – for sticking
 Tartaric acid – for crumbling

DIFFERENCE BETWEEN FUSION METHOD AND WET
(DRY NASA GUIDE QUESTIONS PERO PARANG MALI)
METHOD OF PREPARING EFFERVESCENT GRANULES
- Fusion method – the water present in each
molecule of citric acid acts as the binding agent for
the powder mixture
- Wet method – The water added to the alcohol acts
as the binding agent
Examples of medicated powders used in prescription
and non-prescription
o Dulcolax and MiraLAX (laxative)
o Buphenyl (for managing urea cycle disorder)
o Equate (Analgesic)
o Massengill (douche powder)
o Tolnaftate (Anti-fungal)