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Powders and
GranulesUy, Orlando Louis
Villanueva, Berle Joy
Villespin, Vanessa Jae
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Powder
A dry substance
composed of finely
divided particles
A type of
pharmaceutical
preparation A medicated powder
intended for internal
or external use.
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PARTICLE SIZE AND
ANALYSIS
The particles of powders and
granules may range from being
extremely COARSE, about 10mm
(1cm) in diameter, to EXTREMELYFINE, approaching colloidal
dimensions of 1mcg or less.
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Characterization of USP
of powders
Very coarse, moderately
coarse, fine and very fine
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DESCRIPTIVE TERMS
VERY COARSE (No. 8) All particles pass through (No. 8) sieve and not more than 20 % pass through a No.
6 sieve
COARSE (No. 20) All particles pass through (No. 20) sieve and not more than 40 % pass through a No.
60 sieve
MODERATELY COARSE (No. 40) All particles pass through (No. 40) sieve and not more than 40 % pass through a No.
80 sieve
FINE (No. 60) All particles pass through (No. 60) sieve and not more than 40 % pass through a No.
100 sieve
VERY FINE (No. 80) All particles pass through (No. 80) sieve. There is no limit to greater fineness.
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SIEVES
Made of wire
cloth woven
from brass,bronze and
other suitablewire. Not
coated or
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POWDERS OF VEGETABLE
AND ANIMAL ORIGIN
DRUGS Granules 4 to 12 sieve size.
12 20 sieve range are sometimes
used in tablet making
(REFER TO THE TABLE, page 185)
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PURPOSE OF PARTICLE
SIZE ANALYSIS
To obtain quantitative data onthe size, distribution, and
shapes of the drug and other
components to be used in
pharmaceutical formulations.
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PARTICLE SIZE
INFLUENCES ON VARIETY
OF FACTORS: Dissolution rate of particles intended to dissolve
(smaller: increases rate of distribution and itsbioavailability)
Suspendability intended to remain undissolvedbut uniformly dispersed in a liquid vehicle (finedispersions: .5-10mcg)
Uniform distribution of a drug substance in a
powder mixture or solid dosage form ensuresDOSE TO DOSE CONTENT UNIFORMITY
Penetrability (to be inhaled for deposition deep inthe respiratory tract
Lack of Grittness of solid particles in semi-solid
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METHODS TO DETERMINE
PARTICLE SIZE SIEVING
MICROSCOPY
SEDIMENTATION
RATE
LIGHT ENERGY
DIFFRACTION ORLIGHT SCATTERING
LASER
HOLOGRAPHY
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Why Micrometrics is
important It is important because the physical
state of particles can be altered byphysical manipulation and particle
characteristics can alter
THERAPEUTIC EFFECTIVENESS Particle any unit of matter having
defined physical dimensions
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Comminution
of Drugs
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SMALL SCALE Example: pharmacist
reduced the size of adrug by grinding with amortar and pestle
(porcelain is betterthan glass mortar dueto its ROUGHSURFACE)
TRITURATION ORCOMMINUTION grinding a drug in amortar to reduce its
particle size.
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LARGE SCALE: Mills and pulverizers are
used.
Example of machine:FITZMILL COMMINUTINGMACHINE WITH APRODUCT CONTAINMENTSYSTEM.
It is grinded rapidly into amoving blades in thecomminuting chamber,particles are reduced in size
and it is passed through a
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The collection and
containment systemsrole:
Protects the environmentfrom chemical dust
Reduces product loss
Prevents product
contamination
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LEVIGATION for small scale
preparation ofointments and
suspensions to reducethe particle size andgrittiness of the addedpowders
Mineral oil and glycerinare commonly used aslevigating agents
(added to the powder
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BLENDING
POWDERS
When two or more powderedsubstances are to be combined to
form a uniform mixture, it is best
to reduce the particle size of eachpowder individually before
weighing and blending.
METHODS
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METHODS
USED FOR
BLENDING
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Trituration glass mortar is usually preferred ifthere is no special need for
comminution.
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Geometric Dilution the blending of a
small amount of
potent substancewith a large
amount of diluent.
It ensures uniformdistribution of the
potent drug.
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Tumbling
tumbling the powder in a rotatingchamber. Thorough but time
consuming. This is widely
employed in the industry
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Segregation undesirable separation of thedifferent components of the blend.
It may occur through sifting or
percolation, air entrapment
(fluidization) and particle
entrapment (dusting).
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MEDICATED
POWDERS can be use internally or externally
Powders taken orally for systemicuse may be expected to result in
faster rates of dissolution andabsorption than solid dosage
forms, because there is an
immediate contact with the gastric
DISADVANTAGE OF
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DISADVANTAGE OF
MEDICATEDPOWER
Undesirable taste of the
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AEROSOL POWDERS
Administered by inhalation with the aid of
dry-powder inhalers, which deliver
micronized particles of medication in
metered quantities.
Prepared in 1 to 6mcg in diameter
Contain inert propellants and
pharmaceutical diluents such as
CRYSTALLINE ALPHA-LACTOSE
MONOHYDRATE to aid the formulations
flow properties and metering uniformity
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Powder Blowers
(Insufflators) may be used todeliver dry powders
to various parts of the
body. Examples:lung, nose, throat
and vagina
Depression of thedevices rubber
bulb causes
turbulence of the
powder in the vessel,
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BULK POWDERSLimited to non-potent substances
Examples:
ANTACIDS (NaHCO3)
LAXATIVES (Psyllium)
DOUCHE POWDERS (Massengill
powder)
Topical Anti- Infectives (Bacitracin zinc etc)
Anti-fungals (tolnaftate)
Nutritional supplements (brewers yeast
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DIVIDED POWDERS Division into individual dosing
units based on the amount to be
take or used at a single time POWDER paper latin word
chartula abbrev: chart
Placed on a small piece of paper
that is folded to enclose the
medication.
WAYS ON HOW
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WAYS ON HOW
PHARMACISTS DIVIDE
POWDERS: (depending on the potency of thedrug substance)
1. Block-and-divide method (for non-potent drug)
put in a porcelain or glass plate
spatula
2. Weigh each portion separately
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Papers used for Divided Powers
Simple bond paper Vegetable parchment
(semi-opaque with
limited moistureresistance
Glassine (glazed
transparent, limitedmoisture resistance)
Waxed paper
transparent waterproof
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Waxed Paper - If the powder is
hygrosgopic or deliquescent
Bond Paper - For aesthetic appeal
Vegetable parchment and glassine
limited barrier against moisture isnecessary
Glassine or waxed paper containing
volatile components White bond paper containing
neither volatile components or
moisture
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(STEPS ON HOW TO MAKE
PAPER TABS page 195)
It should fit snugly in the box,
have uniform folds and be
uniform in length and height. There should be NO powder in
the folds None should escape with
moderate agitation
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GRANULES prepared agglomerates
of similar particles of
powder
most of the time
irregularly shaped but
may be prepared to be
spherical
usually 4- to 12-mesh
sieve size range
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WET METHOD Moisten the powder of powder
mixture and then pass the
resulting paste through a screenof the mesh size to produce the
desired size of granules. The
granules are placed on dryingtrays and are dried by air or under
heat. It is periodically moved
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FLUID BED
PROCESSING -
particles are placedin a conical piece of
equipment and are
vigorouslydispersed and
suspended while a
liquid excipient is
sprayed on the
particles and the
product dried,
forming granules or
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DRY GRANULATION
METHODS Dry powder is passed
through a roll compactorand then through agranulating machine. The
roll compactor processes afine powder into densesheets or forms by forcing itthrough 2 mechanicallyrotating metal rolls running
counter to each other. Thesurface of the compactingrolls may be smooth or mayhave pocket indentations orcorrugations that allow
compaction of different
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SLUGGING - the
compression of a powder
mixture into large tablets
or slugs on a
compressing machine
under 8000 to 12000 lbs
of pressure.
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The dry process often
results in the production
of fines, that is, powder
that has not
agglomerated intogranules. These are
separated collected and GRANULES AND ITS
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GRANULES AND ITS
CHARACTERISTICS: More stable to the effects of atmospherichumidity(due to its less surface area
compared to a volume of powder) and areless likely to harden upon standing
More easily wetted by liquids than are
certain light and fluffy powders. (which
tend to float on the surface)
Often preferred for dry products intended
to be constituted into solutions or
sus ensions
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Example of a drug that is
made into granules:Antibiotic drugs
since these areunstable inaqueous solution
(constituted withpurified water justprior to
dispensing)
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EFFERVESCENT
GRANULATED SALTS Granules are coarse to very coarse powders containinga medicinal agent in a dry mixture usually composed of
NaHCO3, citric and tartaric acid.
When added to H20, the acids and base react toliberated CO2, resulting effervescence
Resulting carbonated solutions masks undesirable taste
of any medicinal agent.
Using granules or coarse particles decreases the rate ofsolution and prevents violent and uncontrollable
effervescence
Effervescence could overflow the glass and leave
residual carbonation in the solution
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TARTATIC ACID
alone granuleslose its firmness
and crumble
CITRIC ACID alone
results in a stickymixture difficult to
granulate
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PROCESSES
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DRY METHOD or
FUSION METHOD Citric acid crystals are powdered and then mixedwith the other powders of the same sieve size toensure uniformity of the mixture
Sieves and mixing equipment should be madeSTAINLESS STEEL or other material resistant tothe effect of the acids
The mixing is performed as rapidly as is practical
Preferably in a low environment humidity to avoidabsorption of moisture and a premature chemicalreaction
After mixing, it is placed in an oven and an acid-resistant spatula is used to turn the powder
As it became spongy after heating, it is now
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WET METHOD It differs from the fusion method in that the
source of binding agent is not the water ofcrystallization from the citric acid but the
water added to alcohol as the moisteningagent, forming the mass of granulation.
All of the powders may be ANHYDROUSEas long as water is added to the
moistening liquid.
Just enough liquid is added (in portions) toprepare a mass of proper consistency until