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PCT 221
3rd Semester
)
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IHS-Gaborone
Unit-1
Unit-2
Unit-3
Unit-4
Unit-5
Total Credit = 3
Assessment
= 2CAs(60%) + End of sem.
Exam
(40%)
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Recommended Books
1. Pharmaceutical dosage forms and drug delivery systems
Ansel H.C, Popovich
2. Pharmaceutics, The science of dosage form design, M.E
Aulton
3. Remington, The science and practice of Pharmacy Vol-1 & 2
4. Pharmaceutical Calculations by Stocklosa & Ansel
5. Any other handouts / Reference material given to the class
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Unit-1
Powders and Granules
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Unit contents
1. Powders and granules as dosage forms
2. Special problems in powdered dosage
forms
3. Factors affecting drug availability from
powdered dosage forms
4. Package and storage of powders
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TOCs
Basic definitions
Advantages and disadvantages
Powders and granules as dosage forms
(types / Differences)
IHS-Gaborone
Definitions
Micromeritics:
Science of small particles
Powders:
Is a mixture of finely divided drugs and /or Chemicals in a dry
form
According to B.P = subdivided solids containing constituent
particles which can range 1.25um 1.7mm in diameter
As DF = are formulations in which powdered drug has been
mixed with powdered excipients to produce final formulations
Eg. Oral powders, Dusting, dentifrices, bulk powders etc
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Granules
(Sieve size=4-12)
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Sieve Number
A number used to designate the size of the Sieve,
which corresponds to the no. of openings per linear
inch
E.g.. Sieve 20 will have 20 openings in 1 linear
inch
Sieve opening
Its an approximate size of aperture of a given sieve
as given in USP
E.g. sieve no 20 will have 20 opening per linear
inch and each opening will have an aperture size =
850m
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Sieve Number
Sieve opening
(m)
20
850
40
425
60
250
80
180
120
125
..
..
400
38
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Glidents
Excipients that increase flow properties of
given material By correcting surface
irregularity, reducing friction or by neutralizing
surface charges b/w particles
E.g.,
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Mag. Stearate,
Aerosil (colloidal silicon dioxide),
Starch,
Talc
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Geometric mixing/dilution
(doubling up method)
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Trituration
is the process for reducing the particle size of a substance
by grinding, eg grinding of powders in a mortar with a pestle
Sifting
relates to putting through a sieve or straining device to
separate fine particles from coarse ones
Tumbling
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Advantage of powders/granules
1. Stability
Solid are more stable than liquids
E.g. (Ampicillin)
Antibiotics powders dry form = 2-3 yrs shelf
life
While liquid of same antibiotics = 1-2 weeks
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Disadvantages
Inconvenient to carry / handle
(except when presented as divided DF)
Unpleasant Taste
Not very suitable DDS for potent drugs
Divided DF can be used however Tabs are
preferred
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Disadvantages. (Cont.)
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Powders VS Granules
Powders
Granules
Less likely
Good compressibility
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Preparation of Granules
Wet method
Moistening the desired powder
Passing paste like mass thru sieve no 4-14.
Tray dry / oven dry / vacuum dry
Packed and labeled
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Dry method
Powder material is passed through a roll
compactor
Granulating machine.
Densified sheets or flakes
The compacted powder is then granulated to
uniform particle size by passing through a
mechanical granulator.
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Therapeutic use:
As a true & proper
pharmaceutical
dosage form
Bulk/divided/
dusting/insu
fflations/DPI/
Reconstitutio
n
Non therapeutic
use:
for the preparation
of other dosage
forms
Tablets,
Capsules,
Suspensions,
Solutions etc
Powders /
Granules
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Bulk Powders
Mixed ingredients are packed suitable
containers like wide mouthed bottles or
glass jars
Constituents are non toxic / Less potent
Large doses can be dispensed
Usually supplied with a measuring spoon
Proper directions for use should be provided
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Divided powders
More potent ingredients are usually
packed individually/ separately wrapped.
List advantages / Disadvantages
E.g.
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Packaging
Ind. Wrapped paper, (How to wrap)
If material is volatile or moisture sensitive than
wax lined paper or grease proof paper
Air tight sealed sachets
Foiled laminate (replaced Paper)
Individual powder are than boxed. (easy
handling)
Storage
Cool and dry place, Avoid moisture (avoids
agglomerates formation)
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Dusting Powders.
Used externally for
Therapeutic ---- antifungal
Prophylaxis----- antifungal/antiseptic
Lubricating------ talc, Kaolin etc
Dusting powders for open wounds should be
sterile (chlorohexidine Dusting Powders), but lubricating
powders do not need to be sterilized, however
should be free from pathogens/Spores,
Dry heat for sterilization is usually used,,
for more than 60 minute)
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(1600C
Dusting Powders.(Cont)
Packaging,
Plastic, Glass or metal drum fitted with a perforated
lid.
Glidents are usually added to enhance the flow
(Talc, Sterillizable Maiz starch)
Storage:
Closed Lid, Dry place, Away from child..
Examples
Antifungal/ Antibacterial foot powders.
Zinc undecylinate, Chlorohexidine
Lubricating dusting powder,
Talc
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Insufflations
Are medicated powders intended to be blown into
regions such as ear, nose, and throat with the help of
an insufflators
Not very acceptable, In-elegent and less convenient
to use,
May show systemic effects (Rapid abosrption)
Some drugs are more rapidly absorbed from lungs
than oral use. E.g. Sodium Chromoglycolate
Traditional insufflator replaced by Advance devices,
Handihaler,
Accuhaler, Etc.
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Handihaler
Uses a capsule in device which is broken down as you
operate and than u inhale medicaments.
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(Insulin DPI)
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Video Demonstration
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E.g.
Augmenting PFI
Amphoteracin B, Ampicillin, Ceftriaxone PFI
Cephradine, and chloramphenical PFI
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Special problems in
Powdered DF / Solution
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Volatile substances
Such as
Camphor, menthol, essential oils
Evaporation loss.
Solution
Packed into heat sealed plastic bags,
Air tight containers
Proper storage instructions to the client
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Eutectic mixture
Some solids when mixed together form liquid.
E.e. Phenol, menthol, thymol, antipyrene,
phenacetin.
Solution.
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Liquids
Can be added in small amounts to
powders.
Some adsorbing materials should be added.
Lactose,
Mag.Carbonate, Starch.
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Efflorescent materials
Crystalline substances may liberate water
of crystallization due to trituration and
powder becomes wet.
Anhydrous salt form can be used.
Inert diluents can be added.
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Factors affecting
Drug availability
from Powdered DF
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Dissolution
Process by which a drug particle dissolves
Noyes Whiteny
Equation
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Surface area
Particle size is inversely related to S.A
Poorly or slowly soluble drugs when presented
in small particle size enhanced
dissolution enhanced bioavailability
E.g.
Theophyllin,
Griseofulvin
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Salt form
Drugs are either week acid or week basis.
Sodium and potassium salts of week organic acids
&
Hydrochloric salts of week organic basis
SHOW
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Sate of hydration
Anhydrous form of an organic molecule is
more soluble than its hydrated counter
part.
E.g.
Ampicillin Anhydrous is more soluble than its
tri-hydrate form
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Effect of pH
Unionized form of drug absorb more faster
than ionized form.
Week acidic drugs absorb well in acidic pH.
i.e Stomach
Basic drugs absorb well in intestine.
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2. Sieving
3. Sedimentation rate
5. Laser holography
3D picture by holography camera
6. Cascade impact
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Sieving technique
Sieve number ?
Sieve Opening ?
Principle
Particles passed by mechanical shaking through
a series of sieves of known sizes (which reduces
gradually from top to bottom),
Amount of powder retained / Passed through is
determined and manipulated
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Sieve No.
Sieve
Opening
(m)
20
850
40
425
60
250
80
180
120
125
..
400
38
67
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Type of powder
All particles
pass thru Sieve
No
Not more
than
Very coarse
20% thru 60
Coarse
20
40% thru 60
Moderately
coarse
40
40%thru 80
Fine
60
Very fine
100
No limit
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Powders calculations
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E.g.
Rx
Hyoscine HBr 300 mcg
mitte 4 powders
one to given 30minutes before journey
(Remember: minimum powder weight for divided powder = 120mg)
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Step-1
Hyoscine HBr =100mg
Diluent =900mg
Step-2
Triturate A =100mg
Diluent =900mg
Step-3
Triturate B =?
Diluent =?
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Example
Rx
Send 10 aspirin powders 200mg for a
child
of 3-years (14kg)
Is dilution required?
300 mg tabs are available in dispensary
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Example
Calculate quantities required to make 8
powders each containing 200mcg of digoxin
per 120 mg of powder.
Use lactose as a diluents
Min. weighable qty = 100mg (class B
balance)
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5mL contains
150mL contains
=250mg
=7500mg
7500mg /500mg/5mL
=75mL
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75mL-39mL
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