Powders

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Powders

A Pharmaceutical powder is a mixture of finely


divided drugs or chemicals in a dry form meant
for internal or external use.

Advantages of Powders:

Good chemical stability compared with fluids


useful for bulky drugs with large dose, e.g. indigestion
powder.
Easy to swallow even in large bulk, especially if mixed
with drink, food (useful for stomach- tube feeding)
The smaller particle size of powders causes more rapid
dissolution in body fluids, increases drug
bioavailability, and decreases gastric irritation
compared with tablets

Disadvantages of Powders
1-Time-consuming preparation
2-Inaccuracy of dose- size of measuring
spoon, density of powder, humidity, degree
of settling , fluffiness.
3-Unsuitability for many unpleasant tasting,
hygroscopic and deliquescent drugs

Types of Powders
1- Divided powders
- packets
- cachets
- capsules
2- Bulk (Undivided) powders
- dusting powder
- effervescent powder
- antacids, laxatives, dietary
nutrient supplements.
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Oral divided powder may contain one


or more active ingredients together
with an inert diluent to produce a
minimum quantity of 120 mg.
Oral undivided powder are usually a
simple mixture of the prescribed
medication without additional
ingredients.

Particle Size of Powders

United States Pharmacopeia (USP) classify


powders as: very coarse, coarse, moderately
coarse, fine, and very fine.

These are related to the proportion of powder that


is capable of passing through the openings of
standard sieves of varying fineness in a specified
period while being shaken, generally in a
mechanical sieve shaker.
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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.
Granules fall within the range of 4- to 12-sieve size,
although granulations of powders prepared in the 12- to 20
sieve range are sometimes used in tablet making .
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Effects of Particle Size

Dissolution rate of particles intended to dissolve;


drug micronization can increase the rate of drug
dissolution and its bioavailability

Suspendability of particles intended to remain


undissolved but uniformly dispersed in a liquid
vehicle (e.g., fine dispersions have particle
approximately 0.5 to 10 m)

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Effects of Particle Size


Uniform distribution of a drug substance in a powder
mixture or solid dosage form to ensure dose-to-dose
content uniformity.
Penetrability of particles intended to be inhaled for
deposition deep in the respiratory tract (e.g., 1 to
5m).
Lack of grittiness of solid particles in dermal
ointments, creams, and ophthalmic preparations
(e.g., fine powders may be 50 to 100 m in size).

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Particle Size Determination

Sieving
Particles are passed by mechanical shaking through a
series of sieves of known and successively smaller
size and the proportion of powder passing through or
being withheld on each sieve is determined (range
about 40 to 9,500 m, depending upon sieve sizes).

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Coulter Counter
Coulter
counter
determines
the
volume
distribution
of
particles
suspended
in
an
electrolytecontaining solution. When a particle
passes through a small orifice, it
blocks the electric current. The
information on particle volume is used
for calculating particle size assuming
a spherical shape.
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Other methods

Microscopic analysis (0.2 to 100m)


Sedimentation Rate (0.8 to 300 m)
Light Scattering (0.2 to 500m)
Permeability methods (>1 m)
Laser diffraction analysers(0.02 to
2000m)
Laser holography (1.4 to 100m)
Electronic particle counters

Preparation of Powders
1- Reduction of particle size of all
ingredients to the same range to
prevent stratification.
2- Sieving.
3- Weighing of each ingredient.
4- Mixing.
5- Packaging.

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Reduction of Particle Size


The manually operated procedures are trituration,
pulverization and levigation.
1- Trituration: is used to comminute( reduce particle
size) & to mix powders.
1-A porcelin preferred than glass morter.
2- A glass morter is preferrable for chemicals that stain a
porcelin. When granular or crystalline materials are to
be incorporated in to powdered product ,these
materials are comminuted individually and then blended
together in the morter.
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2- Pulverization
Substance are reduced& subdivided with an additional
material ( i.e solvent) that can be removed easily after
pulverization is complete.
* This technique is applied to
Substances which are gummy and tend to reagglomerate
or which resist grinding. As camphor which is gummy,
so addition of alcohol or other volatile solvent can be
reduced readily to a fine powder.
Similarly, iodine crystals may be comminuted with the aid
of ether.
In both instances the solvent is permitted to evaporate
and the powdered material is recovered

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3- Levigation
In this process
A- paste is first formed by the
addition of a suitable non solvent to
the solid material.
B-Particle-size reduction then
accomplished by rubbing the paste
in a mortar with a pestle or on an
ointment slab using a spatula.
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Methods of Powder Mixing


1- Mechanical Mixing
2- Hand Mixing:
2.1- Spatulation (spatula + tile)
2.2- Trituration (mortar + pestle)
2.3- Tumbling (wide mouth closed
container)

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Mixing of powders
Large-Scale Mixing Equipment

The ideal mixer should


1- produce a complete blend rapidly to avoid
product damage.

2- It should be cleaned and discharged easily


3- be dust-tight
4 require low maintenance and low power
consumption.
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Small-Scale Mixing Equipment


1- Mortar and pestle
* The pharmacist most generally employs the mortar and pestle for
the small-scale mixing
* The mortar and pestle method is a single operation. Thus, it is
particularly useful where some degree of particle-size reduction
as well as mixing is required as in the case of mixtures of
crystalline material.
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Small-Scale Mixing Equipment


2- Spatulation
The blending of powders with a spatula on a tile
or paper used sometimes for small quantities
or when the mortar and pestle technique is
undesirable.
It is not suitable for large quantities of powders
or for powders containing one or more potent
substance because homogenous blending may
not occur.
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Small-Scale Mixing Equipment


3- Sieving
Sieving usually is employed as a pre-or
post-mixing method to reduce loosely held
agglomerates and to increase the overall
effectiveness of blending process.

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Small-Scale Mixing Equipment


4-Tumbling
Powder is mixed in rotating
chamber.
Mixing is thorough but time
consuming. Mostly used in industry

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Extemporaneous Techniques
1.

Use of geometric dilution for the incorporation of small


amounts of potent drugs

Geometric dilution:
Entire quantity of potent drug (x volume) + (x volume)
of the diluents + (2x volume) of the diluents + (4x
volume) of the diluentsrepeated until all the
diluents are used.

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Extemporaneous Techniques
2. Reduction of particle size of all ingredients to
the same range.
3. Sieving when necessary to achieve mixing or
reduction of agglomerates, especially in powders
into which liquids have been incorporated.
4. Heavy trituration, when applicable, to reduce
the bulkiness of a powder.
5. Protection against humidity, air oxidation and
loss of volatile ingredients.
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Powders are prepared most commonly


either as:
1- Divided powders and bulk powders
which are mixed with water prior to
administration
2- Dusting powders which are applied
locally.
3- Dentifrices
4- Insufflations
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Divided Powders
Are dispensed in the form of
individual doses and generally are
dispensed in papers, properly folded
(chartulae). They also may be
dispensed in metal foil, small heatsealed plastic bags or other
containers.
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Divided Powders
- After weighing, comminuting and mixing
the ingredients, the powders must be
divided accurately into the prescribed
number of doses. In order to achieve
accuracy consistent with the other steps in
the preparation, each dose should
be weighed individually and transferred to a
powder paper. Following completion of this
step the powder papers are folded.
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Powder Papers
- Four basic types of powder papers are
available.
1. Vegetable parchment, a thin semi-opaque
moisture-resistant paper.
2. White bond, an opaque paper with no
moisture-resistant properties.
3. Glassine, a glazed, transparent moistureresistant paper.
4. Waxed,( Parrafin) a transparent
waterproof paper.
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Powder Papers
Hygroscopic and volatile drugs can be
protected best by using a waxed
paper, double-wrapped with a bond
paper to improve the appearance of
the completed powder.

Parchment and glassine papers offer


limited protection for these drugs.
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Bulk Powders
may be classified as oral powders, dentifrices, douche
powders, dusting powders, insuffiations and
triturations.
Oral Powders - These generally are supplied as finely
divided powders or effervescent granules.The finely
divided powders are intended to be suspended or
dissolved in water or mixed with soft foods, prior to
administration.
Antacids and laxative powders frequently are
administered in this form

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Dusting Powders
These are locally applied nontoxic preparations that are
intended to have no systemic action.
Requirements:
1- Homogenous and very fine
2- Free from irritation.
3- Flow easily.
4- Have good covering capacity.
5- Have good adsorptive and absorptive capacity.
6- Spread uniformly over body surface.
7- Cling (adhere) to skin surface after application.
8- Protect the skin from irritation caused by friction, moisture
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and chemical irritants.

Dusting Powders
Application:
Medicated dusting powders may be applied either to
intact skin or to open wound and mucous
membranes.
2- powders applied to open wound must be sterilized
3- Particle size should be very small. It is better to be
micronized or those passes through # 100 sieve.
4- Highly sorptive powders should not be used on areas
exude large quantities of fluids to avoid hard crust
formation.
Function:
1-

Lubricants- protective- adsorbents- antiseptic astringents- antiperspirants


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Dusting Powders
Packaging:
Dispensed in sifter- top cans or pressurized
packs (aerosols).
Aerosols protect the powder from air, moisture
and contamination and more convenient for
application.

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Insufflations
- These are finely divided powders
introduced into body cavities such
as the ears, nose, throat, tooth
sockets and vagina. An insufflator
(powder blower) usually is
employed to administer these
products.

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Insufflations

However, the difficulty in obtaining


a uniform dose has restricted their
general use.
Specialized equipment has been
developed for the administration of
micronized powders of relatively
potent drugs. The Norisodrine
Sulfate Aerohaler Cartridge (Abbott)
is an example.
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Douche Powders

These products are completely soluble and are


intended to be dissolved in water prior to use as
antiseptics or cleansing agents for a body cavity.

They most commonly are intended for vaginal use,


although they may be formulated for nasal, otic or
ophthalmic use. Generally, aromatic oils are included
in these powders.

Dispensing in wide-mouth glass jars serves to


protect against loss of volatile materials and
permits easy access by the patient

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Dentifrices

These may be prepared in the form of a


bulk powder, generally containing a soap
or detergent, mild abrasive and an
anticariogenic agent.

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Triturations
-

These are dilutions of potent powdered drugs,


prepared by intimately mixing them with a suitable
diluent in a definite proportion by weight. They were
at one time official as 1 to 10 dilutions.

The pharmacist sometimes prepares triturations of


poisonous substances, eg, atropine, in a convenient
concentration using lactose as the diluent, for use at
the prescription counter.

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Triturations

The correct procedure for preparing such triturations or


any similar dilution of a potent powder medicament, to
insure uniform distribution of the latter, is:
1- Reduce the drug to a moderately fine powder in a
mortar.
2-Add about an amount of diluents & mix well by thorough
trituration in the mortar.
3-Successively add portions of diluent ,triturating after
each addition ,until the entire quantity of diluent has
been incorporated. Under no circomostances should
the entire quantity of of diluent be added at once to the
drug that is to be diluted, ununiform dispersion will be
achieved
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Problems encountered in powder


formulation
1- Hygroscopic and Deliquescent Powder

Problem: Absorption of moisture from air


leading to partial or complete liquefaction.
Solution: A- Applied in a granular form to
decrease the exposed surface to air.
B- Packed in aluminum foil or in plastic film
packets
C- Addition of light magnesium oxide to reduce
the tendency to damp
D- Addition of adsorbent materials such as
starch
Examples: - halide salts (ex. Sod. Iodide)
- Certain alkaloids (physostigmine Hcl)
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Problems encountered in powder


formulation
2- Efflorescent powders

Problem: Crystalline substances which


during storage loose their water of
crystallization and change to powder
(to be efflorescent). The liberated
water convert the powder to a paste
or to a liquid.
Examples: Alum- atropine sulfatecitric acid- codeine phosphate
Solution: Using the anhydrous form,
and treating it in a manner similar to
hygroscopic powders
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Problems encountered in powder


formulation
3- Eutectic Mixtures
Problem: mixture of substances that liquefy when
mixed, rubbed or triturated together. The melting
points of many eutectic mixtures are below room
temperature.
Examples: menthol- thymol- phenol-camphor.
Solution: A- using inert adsorbent such as starch,
talc, lactose to prevent dampness of the powder
B- dispensing the components of the eutectic
mixture separately.

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Problems encountered in powder


formulation
4- Potent Drug
Problem: Limited precision and accuracy of the
used balances to weight small amounts of
potent drugs.
Solution: Drug triturates:
A- Suitable diluents like lactose are mixed with
the potent drug to form 10 - 20%w/w drug
triturates.
B- Very fine powders should be used in the
triturates
C- Geometric dilution to prepare drug triturates
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Problems encountered in powder


formulation
5- Incompatible salts
Problem: Chemically incompatible salts when triturated

together produce discoloration, chemical deterioration or


loss of potency.

Solution:
A- Compounding such substances with minimum pressure
B- Use a convenient method for mixing the powder like
tumbling in a jar or spatulation on a sheet of paper.
C- Each substance should be powdered separately in a
clean mortar and then combined with other ingredients
gently.
D- Powder and dispense separately.

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Problems encountered in powder


formulation
6- Explosive mixtures
Problem: Oxidizing agents(ex. Pot. Salts of
chlorate, dichromate, permanganate and
nitrate- Sod. Peroxide- silver nitrate and silver
oxide) explore violently when triturated in a
mortar with a reducing agent ( ex. sulfidessulfur- tannic acid- charcoal).
Solution:
A- Comminute each salt separately.
B- Subject to a minimum pressure.
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Effervescent Powders

Definition: Mixture of organic acid and alkali


effervesces when subjected to water due to reaction
between the acid and the base with evolution of co 2
Examples: Citric or tartaric acids with sodium
carbonate or bicarbonate
Uses: The liberated carbon dioxide has the
following advantages:
It masks the bitter and nauseous taste.
It promotes gastric secretions.
It acts as a carminative.
psychological impression at the patient. .

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Effervescent Powders

Formulation:
- Bulk powders or divided powders
- Packed in separate packages of
contrasting colors.
- The contents are mixed in a
quantity of water at the time of
dosing.
- The liquid is consumed just after
the reaction begin to subside.
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Effervescent Granules

Definition: Sweetened effervescent


powders formulated as granules.
Granulation:
1- Wet method: By the addition of a
binding liquid (Alcohol is frequently
used).
2- Dry method: Heating effloresced
powder to liberate the water of
crystallization which then acts as the
binding agent

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Effervescent Granules
Wet Granulation

Procedure:
1- The powders are mixed without pressure in
a suitable container.
2- Alcohol is added in portions with stirring
until a dough like mass is formed.
3- The materials are then passed through sieve
# 6.
4- The resulted granules are dried at a
temperature not exceeding 50C.
5- The granules are packed in air tight
containers
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THE
END
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