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Solid Dosage Form  Less convenient for patients to carry

than a small container for capsules or


- are drug substances most frequently are
tablets
administered orally.
 The masking of unpleasant tastes may
- They have a definite shape and volume that
be a problem
contains one or more active ingredients and
 Not a good method of administering
non-active ingredients (excipients).
potent drugs with a low dose
- Excipients are included in the formulations
 Not a suitable method of administering
to facilitate handling, enhance the physical
drugs that are inactivated in the
appearance, improve stability, and aid in
stomach
the delivery of the drug to the bloodstream
 Not well suited for dispensing
after administration
hygroscopic or deliquescent drug
Types of Powders (Method of Administration)
1. Topical powders
2. Insufflated powders
Topical Powders
• They should be impalpable and free flowing
• Easily adhere to the skin
• Passed through at least a No. 100-mesh
sieve to minimize skin irritation
Insufflated Powders
• Insufflated powders are finely divided
powders that are intended to be applied in
a body cavity, such as the ears, nose,
Powders and Granules vagina, tooth socket, or throat.
Powders (Pulvis, in Latin) • Insufflated powders are finely divided
powders that are intended to be applied in
- A dosage form composed of a solid or a body cavity, such as the ears, nose,
mixture of solids reduced to a finely divided vagina, tooth socket, or throat.
state and intended for internal (oral
powder) or external (topical Powder) use. Adherents in insufflated powders
• Divide • PolyoxTM
 Bulk • Moisture-activated adherent
Types of Powders (Packaging) • An ethylene oxide polymer with a high
molecular weight
DIVIDED • Forms a viscous, mucoadhesive gel when in
- chartula or chartulae contact with moisture
- dispensed in the form of individual doses Class of Powders (Physicochemical aspect)
and generally dispensed in papers, properly
folded • Eutectics
• Hygroscopic and deliquescent powders
BULK • Efflorescent powders
- oral powder, dentrifices, douche powder, • Explosive mixtures
dusting powders, insufflations and Eutectics
triturations
• Mixture of substances that liquefy when
Advantage of Powders over Tablets and Capsules mixed, rubbed or triturated together. The
1. Enable easy alteration of the quantity of melting points of many eutectic mixtures
medication for each dose are below room temp.
2. Aid in clinical studies of drug preparations Eutectic Powders
3. Alternative to a drug that may be too bulky
to be prepared in tablet or capsule form • Acetanilide
4. Provide rapid onset of action • Acetophenetidin
• Aminopyrine
Advantage of Powders over Liquid DS • Antipyrine
1. Generally more stable • Aspirin
2. Rapidly soluble • Benzocaine
• Beta-naphthol
Disadvantage of Powders and Granules • Camphor
• Chloral hydrate
• Lidocaine
• Menthol
• Phenacetin
• Phenol
• Phenyl salicylate
• Prilocaine
• Resorcinol
• Salicylic acid
• Thymol
Hygroscopic & Deliquescent 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 Powders
• A crystalline powder that contains water of
hydration or crystallization.
• This water can be liberated either during
manipulations or on exposure to a lowhumidity
environment.
Powder Characterization and Preparation
• Result: powder will become sticky and pasty, or
it may even liquefy. Type of Powder Sieve Size All Sieve Size
Particles Pass Percentage of
Through Particles Pass
Through
Very Coarse (#8 #8 sieve 20% through a
#60 sieve
Coarse (#20) #20 sieve 40% through a
#60 sieve
Moderately #40 sieve 40% through a
Coarse (#40 #80 sieve
Fine (#60) #60 sieve 40% through a
#100 sieve
Very Fine (#80) #80 sieve No limit

Explosive Mixtures
• Powder combinations that may react
violently when mixed together
Particle Size Analysis Powder Preparation – Particle Size Reduction
• SIEVING • Trituration / comminution
- Powders are passed through a series of - -Mortar and pestle (small scale)
sieves of known and successively smaller - Mills and pulverizers (large scale)
size. (40 to 9,500 µm)
• Levigation
• MICROSCOPY
- Mortar and pestle
- Sample powders are sized through the use - -Ointment tile
of a calibrated grid background. (0.2 to 100 - Levigating agent (e.g., mineral oil, glycerin)
µm)
• Pulverization by Intervention
- Mortar and pestle
- additional material (i.e., solvent-alcohol or
other volatile solvent) that is easily
removed after pulverization.
Powder Preparation – Blending / Mixing

• SEDIMENTATION RATE 1. Spatulation


2. Trituration
- Measurement of the terminal settling -Subtype: geometric dilution
velocity of particles through a liquid 3. Sifting
medium in a gravitational or centrifugal 4. Tumbling
environment. (0.8 to 300 µm)
SPATULATION
Particle Size Analysis
- used to blend small amounts of powders
on a sheet of paper or a pill tile. It is not
LIGHT ENERGY DIFFRACTION suitable for large quantities of powders or
for powders that contain potent
- Also known as “Light Scattering.” substances because homogeneous
- Involves the reduction of light reaching the blending may not occur.
sensor as the particles (dispersed in liquid
or gas) passed through the sensing zone. • For eutectic mixtures
(0.2 to 500 µm) - Phenol
• LASER HOLOGRAPHY - Camphor
- Menthol
- Pulsed laser is fired through aerosolized - Thymol
particle spray and is photographed in 3D - ASA
with a holographic camera - Phenyl salicylate
- This allow the particles to be individually
imaged and sized. (1.4 to 100 µm) TRITURATION
 Trituration may be employed both to
comminute and to mix powders. If simple
admixture is desired without special need
for comminution, the glass mortar is
usually preferred.

• CASCADE IMPACTION
- Particles are separated into various size
ranges by successively increasing the
velocity of the air stream, in which they are
carried.

-
TRITURATION Types of Paper used
Subtype: GEOMETRIC DILUTION 1. Simple bond paper (white bond)
2. Vegetable parchment
• Applicable to small amounts of potent
3. Glassine paper
substances to be mixed with a large amount
4. Waxed paper
of diluent.
• ensures uniform distribution of the potent
substance.

SIFTING
• Powders are mixed by passing them
through sifters similar to those used to sift
flour. not acceptable for the incorporation
of potent drugs into a diluent powder.
Types of Paper used
VEGETABLE PARCHMENT
 A thin, semi-opaque paper. With limited
moisture resistance.

TUMBLING
• Process of mixing powders in a large
container rotated by a motorized process

GLASSINE
 Glazed, transparent paper With limited
moisture resistance.

Powder Preparation – Packaging


 Depending on their intended use, powders
are packaged and dispensed by
pharmacists as bulk powders or divided
powders. PLAIN, WHITE BOND PAPER

Bulk Powders For powders containing neither:

 Oral powders are packed in glass, plastic, 1. volatile components


metal or other containers that have a wide 2. ingredients adversely affected by air or
mouth. Single unit dosage are packed in moisture
sachets or packets.
 For topical powders, they are packed in a
perforated, sifter top container, or powder
shaker. Aerosol container is used for
spraying on skin.

WAXED PAPER
1. Transparent, waterproof paper.
2. Used in “double-wrapping” hygroscopic or
deliquescent powders.
Preparation of Extemporaneous Divided Powders
•Individual weighing of doses
• Block and divide method
-Used for nonpotent drugs
Medicated Powders 3. Foradil Aerolizer (formoterol fumarate) 4.
Relenza (zanamivir)
• May be used internally or externally
• INTERNAL USE
-Oral administration after mixing with water
-Inhalation (local or systemic)
-Powder for reconstitution
- Oral, injection and vaginal douche
• May be used internally or externally

• EXTERNAL USE
 Dusted from a sifter-type container •Oral inhalation powders
or powder aerosol
1. Advair Diskus (fluticasone propionate +
 Label: EXTERNAL USE ONLY
salmeterol)
2. Flovent Rotadisk (fluticasone propionate)
3. Foradil Aerolizer (formoterol fumarate)
4. Relenza (zanamivir)

Aerosol Powders
 Oral inhalation
 Makes use of dry powder inhaler / metered
dose inhaler •Oral inhalation powders
-Delivers micronized particles of medication
1. Advair Diskus (fluticasone propionate +
in metered quantities
salmeterol)
 Makes use of insufflator / powder blower
2. Flovent Rotadisk (fluticasone propionate)
 Powder size: 1 to 6 𝜇m in diameter
3. Foradil Aerolizer (formoterol fumarate)
4. Relenza (zanamivir)

Bulk Powders
•Oral inhalation powders  Oral powders - Antacids and laxatives
 Douche powders (e.g., for vaginal use)
1. Advair Diskus (fluticasone propionate +
 Dusting powders - Medicated powders for
salmeterol)
external application (i.e., anti-infective,
2. Flovent Rotadisk (fluticasone propionate)
antifungal)
3. Foradil Aerolizer (formoterol fumarate)
• Brewer’s yeast powder
4. Relenza (zanamivir)

•Oral inhalation powders


• Oral powders - Antacids and laxatives
1. Advair Diskus (fluticasone propionate +
• Douche powders (e.g., for vaginal use)
salmeterol)
• Dusting powders - Medicated powders for
2. Flovent Rotadisk (fluticasone propionate)
external application (i.e., anti-infective,
antifungal)
• Brewer’s yeast powder

• Oral powders - Antacids and laxatives Divided Powders (Chartula or chartulae)


• Douche powders (e.g., for vaginal use) - “ After a powder has been properly
• Dusting powders - Medicated powders for blended, it may be divided into individual
external application (i.e., anti-infective, dosing units based on the amount to be
antifungal) taken or used at a single time.
• Brewer’s yeast powder 1. Prepared by pharmacist
2. Commercially available

1.
• Oral powders - Antacids and laxatives 1.
• Douche powders (e.g., for vaginal use) 1.
• Dusting powders - Medicated powders for 1.
external application (i.e., anti-infective, Prepared by pharmacist
antifungal) 2. Commercially available
• Brewer’s yeast powder

1. Prepared by pharmacist
2. Commercially available

• Oral powders - Antacids and laxatives


• Douche powders (e.g., for vaginal use)
• Dusting powders - Medicated powders for
external application (i.e., anti-infective,
antifungal)
• Brewer’s yeast powder 1. Prepared by pharmacist
2. Commercially
available

Granules
Granules (Dosage form)
• BC powders (for headache) \
• DENTRIFICES – generally containing a soap • A dosage form composed of dry aggregates
or detergent, mild abrasive, and of powder particles that may contain one or
anticariogenic agent more APIs, with or without other
ingredients.
• They may be swallowed as such, dispersed
in food, or dissolved in water.
• Granules are frequently compacted into
tablets or filled into capsules, with or
without additional ingredients.
Granule Characteristics • The resulting carbonated solution masks
undesirable taste of any medicinal agent
• Prepared agglomerates of smaller particles
of powder
• Irregularly shaped, but can be spherical
Preparation of Effervescent Granulated Salts
• Size: usually 4 to 12-sieve size range

•DRY OR FUSION METHOD


- The water of crystallization of citric acid
acts as the binding agent.
•WET FUSION METHOD
- The source of binding agent is not the
• Prepared by wet or dry granulation water of crystallization from citric acid but
methods water added to alcohol as the moistening
• Free-flowing, thus are used in tablet making agent. Forming the pliable mass for
• More stable to the effects of atmospheric granulation.
humidity
• Less likely to cake or harden upon standing Compressed effervescent granules
• More easily wetted • Zantac EFFERdose tablets
Applications of Using Granules (GlaxoSmithKline). Effervescent granules
and tablets are dissolved in water before us
1. Commercial antibiotic products that are
unstable in aqueous solution
2. Commercial probiotic product
3. Effervescent granulated salts
4. Compressed effervescent granules
Commercial antibiotic products that are unstable
in aqueous solution

Antibiotic granules

Commercial probiotic product


• Probiotic granules - Lactinex granules, a
mixed culture of Lactobacillus acidophilus
and Lactobacillus bulgaricus in 1-g packets
used in the treatment of uncomplicated
diarrhea and diarrhea due to antibiotic
therapy.

Effervescent Granulated Salts


• Are granules or coarse to very coarse
powders containing a soluble medicinal
agent in a dry mixture usually composed of
sodium bicarbonate, citric acid, and tartaric
acid.
• When mixed with water, acids
and base react to liberate
carbon dioxide resulting in
effervescence.

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